SMILES stringlengths 71 300 | POI_Name stringclasses 164
values | POI_Sequence stringclasses 133
values | Ligase_Name stringclasses 9
values | Cell_Line stringclasses 155
values | Value_Type stringclasses 2
values | Value_Unit stringclasses 2
values | Value float64 -53.5 100k | Value_Error float64 1 81.3 ⌀ | Value_Range_Min float64 0.1 1.49k ⌀ | Value_Range_Max float64 0.76 1.99k ⌀ | Value_Concentration float64 0.1 100 ⌀ | Assay_Time float64 2 96 ⌀ | Value_Operator stringclasses 5
values | Value_Category stringclasses 2
values | Value_Concentration_Unit stringclasses 2
values | Modality stringclasses 1
value | POI_UniProt stringclasses 131
values | Ligase_UniProt stringclasses 11
values | Ligase_Sequence stringclasses 11
values | Cell_Line_ID stringclasses 154
values | Cell_Line_Species stringclasses 4
values | Reference stringclasses 367
values | Description stringclasses 501
values | Database stringclasses 6
values | Assay stringclasses 21
values | TPD_ID stringlengths 10 10 ⌀ | Cell_Line_Description stringclasses 151
values | POI_Cluster int64 -1 37 | SMILES_Held_Out bool 2
classes | SMILES_Scaffold_Cluster int64 -1 2.35k | SMILES_Butina_Cluster int64 -1 278 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
COc1cc2nn(C3CC4(CCN(C(=O)C5CCN(c6cc7c(cc6F)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1cccc(N2CCOCC2)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 9.15 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-6S3MVO | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 951 | 34 |
COc1cc2nn(C3CC4(CCN(C(=O)C5CCN(c6cc7c(cc6F)C(=O)N([C@@H]6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 3.26 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-97J7SI | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 192 | 26 |
COc1cc2nn(C3CC4(CCN(C(=O)C5CCN(c6cc7c(cc6F)C(=O)N([C@H]6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 7.62 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-386PPX | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 192 | 26 |
COc1cc2nn(C3CC4(CCN(C(=O)C5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5(F)F)CC4)C3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 7.86 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-BLQMSV | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 192 | 26 |
COc1cc2nn(C3CC4(CCN(C(=O)C5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5(F)F)CC4)C3)cc2cc1NC(=O)c1cccc(N2CCOCC2)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 14.6 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-YM5BL6 | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 951 | 0 |
COc1cc2nn(C3CC4(CCN(C(=O)C5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 4.02 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-8G0NZN | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 192 | 26 |
COc1cc2nn(C3CC4(CCN(C(=O)C5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1cccc(C(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 1.2 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-988EH4 | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 192 | 26 |
COc1cc2nn(C3CC4(CCN(C(=O)C5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1cccc(C)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 2.61 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-SKPZF9 | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 192 | 26 |
COc1cc2nn(C3CC4(CCN(C(=O)C5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1cccc(N2CC3CC2CO3)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 3.9 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-9GXK66 | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 954 | 0 |
COc1cc2nn(C3CC4(CCN(C(=O)C5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1cccc(N2CCOCC2)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 4.42 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-4FGHOT | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 951 | 0 |
COc1cc2nn(C3CC4(CCN(C(=O)C5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1ccn(C(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 5.53 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-MKARL5 | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 955 | 0 |
COc1cc2nn(C3CC4(CCN(C(=O)C5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1cnn2ccc(N3CCN(C)CC3)nc12 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 9.79 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-V8J3RN | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 956 | 0 |
COc1cc2nn(C3CC4(CCN(C(=O)C5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1cnn2ccc(N3C[C@H]4C[C@@H]3CO4)nc12 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 1.16 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-GMEBA5 | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 957 | 0 |
COc1cc2nn(C3CC4(CCN(C(=O)C5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1coc(-c2ccnc(C)c2)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 1.16 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-1DIW1Y | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 958 | 0 |
COc1cc2nn(C3CC4(CCN(C(=O)C5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1coc(N2CCOCC2)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 6.2 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-A6D11Y | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 959 | 0 |
COc1cc2nn(C3CC4(CCN(C(=O)C5CCN(c6ccc7c(c6)C(=O)N([C@@H]6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 2.67 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-YDZ6E0 | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 192 | 26 |
COc1cc2nn(C3CC4(CCN(C(=O)C5CCN(c6ccc7c(c6)C(=O)N([C@H]6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 12.15 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-XIIHCV | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 192 | 26 |
COc1cc2nn(C3CC4(CCN(C(=O)C5CCN(c6ccc7c(c6)C(=O)N(c6ccc(=O)[nH]n6)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 1,000 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-AEWO72 | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 960 | 26 |
COc1cc2nn(C3CC4(CCN(C(=O)C5CCN(c6ccc7c(c6)CN(C6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 3.6 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-UWNFQ9 | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 961 | 26 |
COc1cc2nn(C3CC4(CCN(C(=O)C5CCN(c6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 1,000 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-QIHRYY | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 962 | 26 |
COc1cc2nn(C3CC4(CCN(C(=O)[C@H]5CC[C@H](C(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)N[C@@H](C)c6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)CC4)C3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 16.32 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-0RK4YX | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 963 | 0 |
COc1cc2nn(C3CC4(CCN(C(=O)[C@H]5CC[C@H](CNc6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 3.64 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-IIBCFL | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 964 | 26 |
COc1cc2nn(C3CC4(CCN(C(=O)[C@H]5CC[C@H](Nc6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 2.06 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-T2Z0GA | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 965 | 0 |
COc1cc2nn(C3CC4(CCN(C(=O)[C@H]5CC[C@H](Nc6ccc7c(c6)C(=O)N([C@@H]6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 2.75 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-NZXO2V | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 965 | 26 |
COc1cc2nn(C3CC4(CCN(C(=O)[C@H]5CC[C@H](Nc6ccc7c(c6)C(=O)N([C@H]6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 8.05 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-C838T7 | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 965 | 26 |
COc1cc2nn(C3CC4(CCN(C(=O)[C@H]5CC[C@H](Oc6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 47.28 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-O56OJB | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 966 | 26 |
COc1cc2nn(C3CC4(CCN(C5CC6(CCN(c7ccc8c(c7)C(=O)N(C7CCC(=O)NC7=O)C8=O)CC6)C5)CC4)C3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 15.3 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-907B5D | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 967 | 26 |
COc1cc2nn(C3CC4(CCN(C5CCN(C(=O)c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 148.9 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-8CI1PN | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 968 | 26 |
COc1cc2nn(C3CC4(CCN(CC(=O)N5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 4.41 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-ZSIOAF | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 969 | 26 |
COc1cc2nn(C3CC4(CCN(CC5CC(OCC#Cc6cccc7c6n(C)c(=O)n7C6CCC(=O)NC6=O)C5)CC4)C3)cc2cc1C(=O)Nc1cnc2cccnn12 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | SU-DHL-2 | DC50 | nM | 2.8 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_9550 | Homo sapiens | IRAK4 DEGRADER AND USE THEREOF (patent) | Degradation of IRAK4 by Compounds in SU-DHL-2 and OCI-LY3 Cells
(1) Experimental Purpose
Flow cytometry was used to detect the degradation level of IRAK4 protein in SU-DHL-2 cell lines.
Experimental Methods
Step 1: SU-DHL-2 cell lines were cultured in RPMI 1640 medium supplemented with 10% fetal bovine serum and 1% dou... | TPDdb | Flow Cytometry | TPD-3G0PPV | Mutation; HGNC; HGNC
In situ; Pleural effusion;
Caucasian.
Cancer cell line | 25 | false | 970 | 0 |
COc1cc2nn(C3CC4(CCN(CC5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)C3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 15.75 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-ND0W2P | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 971 | 26 |
COc1cc2nn(C3CC4(CCN(c5ccn(C6CCN(c7ccc8c(c7)C(=O)N(C7CCC(=O)NC7=O)C8=O)CC6)c5)CC4)C3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 33.8 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-3F386C | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 972 | 0 |
COc1cc2nn(C3CC4CCC(C3)N4CC(=O)N3CCN(c4ccc5c(c4)C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 478.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-44ZHUO | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 973 | 40 |
COc1cc2nn(C3CCC4(CC3)CCN(C(=O)C3CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC3)CC4)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 6.9 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-CX4IK8 | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 974 | 40 |
COc1cc2nn(C3CCC4(CC3)CCN(C3CC(OCC#Cc5cccc6c5n(C)c(=O)n6C5CCC(=O)NC5=O)C3)CC4)cc2cc1C(=O)Nc1cnc2cccnn12 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | SU-DHL-2 | DC50 | nM | 1 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_9550 | Homo sapiens | IRAK4 DEGRADER AND USE THEREOF (patent) | Degradation of IRAK4 by Compounds in SU-DHL-2 and OCI-LY3 Cells
(1) Experimental Purpose
Flow cytometry was used to detect the degradation level of IRAK4 protein in SU-DHL-2 cell lines.
Experimental Methods
Step 1: SU-DHL-2 cell lines were cultured in RPMI 1640 medium supplemented with 10% fetal bovine serum and 1% dou... | TPDdb | Flow Cytometry | TPD-F70OGS | Mutation; HGNC; HGNC
In situ; Pleural effusion;
Caucasian.
Cancer cell line | 25 | false | 975 | 0 |
COc1cc2nn(C3CCC4(CC3)CCN(CC3CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC3)CC4)cc2cc1C(=O)Nc1cnc2cccnn12 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | SU-DHL-2 | DC50 | nM | 0.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_9550 | Homo sapiens | IRAK4 DEGRADER AND USE THEREOF (patent) | Degradation of IRAK4 by Compounds in SU-DHL-2 and OCI-LY3 Cells
(1) Experimental Purpose
Flow cytometry was used to detect the degradation level of IRAK4 protein in SU-DHL-2 cell lines.
Experimental Methods
Step 1: SU-DHL-2 cell lines were cultured in RPMI 1640 medium supplemented with 10% fetal bovine serum and 1% dou... | TPDdb | Flow Cytometry | TPD-FW8ANC | Mutation; HGNC; HGNC
In situ; Pleural effusion;
Caucasian.
Cancer cell line | 25 | false | 976 | 111 |
COc1cc2nn(C3CCC4(CC3)CCN(CC3CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC3)CC4)cc2cc1NC(=O)c1cnc2cccnn12 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | SU-DHL-2 | DC50 | nM | 45 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_9550 | Homo sapiens | IRAK4 DEGRADER AND USE THEREOF (patent) | Degradation of IRAK4 by Compounds in SU-DHL-2 and OCI-LY3 Cells
(1) Experimental Purpose
Flow cytometry was used to detect the degradation level of IRAK4 protein in SU-DHL-2 cell lines.
Experimental Methods
Step 1: SU-DHL-2 cell lines were cultured in RPMI 1640 medium supplemented with 10% fetal bovine serum and 1% dou... | TPDdb | Flow Cytometry | TPD-9QFEDL | Mutation; HGNC; HGNC
In situ; Pleural effusion;
Caucasian.
Cancer cell line | 25 | false | 977 | 40 |
COc1cc2nn(C3CCC4(CC3)CCN(CC3CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC3)CC4)cc2cc1NC(=O)c1cnn2cccnc12 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | SU-DHL-2 | DC50 | nM | 1 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_9550 | Homo sapiens | IRAK4 DEGRADER AND USE THEREOF (patent) | Degradation of IRAK4 by Compounds in SU-DHL-2 and OCI-LY3 Cells
(1) Experimental Purpose
Flow cytometry was used to detect the degradation level of IRAK4 protein in SU-DHL-2 cell lines.
Experimental Methods
Step 1: SU-DHL-2 cell lines were cultured in RPMI 1640 medium supplemented with 10% fetal bovine serum and 1% dou... | TPDdb | Flow Cytometry | TPD-XFFQEA | Mutation; HGNC; HGNC
In situ; Pleural effusion;
Caucasian.
Cancer cell line | 25 | false | 978 | 40 |
COc1cc2nn(C3CCC4(CC3)CN(C(=O)C3CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC3)C4)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 1.78 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-ETKOOU | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 979 | 34 |
COc1cc2nn(C3CCN(C(=O)C4CCN(Cc5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)CC3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 32.92 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-RVJXY2 | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 980 | 0 |
COc1cc2nn(C3CCN(C(=O)CN4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)CC3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 12.4 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-4Q0OWR | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 981 | 40 |
COc1cc2nn(C3CCN(C(C)C(=O)N4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)CC3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 5.98 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-REXWOT | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 193 | 40 |
COc1cc2nn(C3CCN(C4CC5(CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)C4)CC3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 20.49 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-BD92SX | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 982 | 34 |
COc1cc2nn(C3CCN(C4CCN(C(=O)c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)CC3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 1,000 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-LOP1D3 | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 983 | 40 |
COc1cc2nn(C3CCN(CC(=O)N4CCN(c5cc6c(cc5F)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)CC3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 6.15 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-6MKE64 | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 193 | 34 |
COc1cc2nn(C3CCN(CC(=O)N4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)CC3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 4.33 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-IQMFBY | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 193 | 40 |
COc1cc2nn(C3CCN(CC(=O)N4CCN(c5ccc6c(c5)CN(C5CCC(=O)NC5=O)C6=O)CC4)CC3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 2.2 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-DECEQF | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 984 | 100 |
COc1cc2nn(C3CCN(CC(=O)N4CCN(c5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)CC3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 14.06 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-D4KEJO | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | false | 985 | 100 |
COc1cc2nn(C3CCN(CCOCCOc4ccc5c(c4)C(=O)N(C4CCC(=O)NC4=O)C5)CC3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | MCF-7 | DC50 | nM | 30 | null | null | null | null | null | < | null | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0031 | Homo sapiens | 10.1021/acsmedchemlett.9b00385 | Degradation of IRAK4 in MCF7 cells | PROTAC-DB | null | null | African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%.
Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu... | 25 | false | 986 | 110 |
COc1cc2nn(C3CCN(CCOCCOc4ccc5c(c4)C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | MCF-7 | DC50 | nM | 30 | null | null | null | null | null | < | null | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0031 | Homo sapiens | 10.1021/acsmedchemlett.9b00385 | Degradation of IRAK4 in MCF7 cells | PROTAC-DB | null | null | African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%.
Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu... | 25 | false | 987 | 110 |
COc1cc2nn([C@H]3C[C@@H]4CN(C(=O)C5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)C[C@@H]4C3)cc2cc1NC(=O)c1cccc(C(F)(F)F)n1 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | THP-1 | DC50 | nM | 8.3 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0006 | Homo sapiens | FIVE-MEMBERED RING-FUSED SIX-MEMBERED COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent) | PROTAC-induced IRAK4 protein degradation in THP-1 cells
Based on a Western blot assay, THP-1 cell samples were stained with specific antibodies after gel electrophoresis. The IRAK4 protein degradation activity of the compounds in THP-1 cells was determined by analyzing the location and depth of staining. Compound conc... | TPDdb | Western Blot | TPD-J8WPWV | African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%.
Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test.
Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
NRAS muta... | 25 | true | -1 | -1 |
COc1ccc(-c2cn(CCCN)c3ccc(CN4CCC(CN5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)cc23)c(F)c1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | Calu-1 | DC50 | nM | 6,500 | null | 3 | 10 | null | null | null | range | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0608 | Homo sapiens | COMPOUNDS FOR MUTANT KRAS PROTEIN DEGRADATION AND USES THEREOF (patent) | Western blot to evaluate the cellular potencies of RAS-PROTACs in KRAS protein degradation. For western blot experiments, BT-474 (KRASWT) and MIA PaCa-2 (KRASG12C) cells were cultured in DMEM medium with 10% FBS. BxPC3 (KRASWT) and KLM-1 (KRASG12D) cells were cultured in DMEM medium with 10% FBS. MDA-MB-231 (KRASG13D) ... | TPDdb | Western Blot | TPD-BV0MW8 | African=0%; Native American=0.74%; East Asian, North=0.11%; East Asian, South=0%; South Asian=9.94%; European, North=31.4%; European, South=57.8%.
Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*10,11; B*15,w35 (CLS=300141). A*26
Metastatic; Pleural effusion;
Caucasian.
Cancer cell line | -1 | true | -1 | -1 |
COc1ccc(-c2cn(CCCN)c3ccc(CN4CCC(CN5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)cc23)c(F)c1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | HCT 116 | DC50 | nM | 6,500 | null | 3 | 10 | null | null | null | range | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0291 | Homo sapiens | COMPOUNDS FOR MUTANT KRAS PROTEIN DEGRADATION AND USES THEREOF (patent) | Western blot to evaluate the cellular potencies of RAS-PROTACs in KRAS protein degradation. For western blot experiments, BT-474 (KRASWT) and MIA PaCa-2 (KRASG12C) cells were cultured in DMEM medium with 10% FBS. BxPC3 (KRASWT) and KLM-1 (KRASG12D) cells were cultured in DMEM medium with 10% FBS. MDA-MB-231 (KRASG13D) ... | TPDdb | Western Blot | TPD-BV0MW8 | African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut... | -1 | true | -1 | -1 |
COc1ccc(-c2cn(CCCN)c3ccc(CN4CCC(CN5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)cc23)c(F)c1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | KLM-1 | DC50 | nM | 6,500 | null | 3 | 10 | null | null | null | range | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_5146 | Homo sapiens | COMPOUNDS FOR MUTANT KRAS PROTEIN DEGRADATION AND USES THEREOF (patent) | Western blot to evaluate the cellular potencies of RAS-PROTACs in KRAS protein degradation. For western blot experiments, BT-474 (KRASWT) and MIA PaCa-2 (KRASG12C) cells were cultured in DMEM medium with 10% FBS. BxPC3 (KRASWT) and KLM-1 (KRASG12D) cells were cultured in DMEM medium with 10% FBS. MDA-MB-231 (KRASG13D) ... | TPDdb | Western Blot | TPD-BV0MW8 | African=0.52%; Native American=0%; East Asian, North=88.41%; East Asian, South=10.63%; South Asian=0.44%; European, North=0%; European, South=0%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established after 2 rounds of injection of cell suspensions of subcutaneous tumors arising from PK-1 in BALB/c nude mice.
A*24
CVCL_... | -1 | true | -1 | -1 |
COc1ccc(-c2cn(CCCN)c3ccc(CN4CCC(CN5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)cc23)c(F)c1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | NCI-H358 | DC50 | nM | 6,500 | null | 3 | 10 | null | null | null | range | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1559 | Homo sapiens | COMPOUNDS FOR MUTANT KRAS PROTEIN DEGRADATION AND USES THEREOF (patent) | Western blot to evaluate the cellular potencies of RAS-PROTACs in KRAS protein degradation. For western blot experiments, BT-474 (KRASWT) and MIA PaCa-2 (KRASG12C) cells were cultured in DMEM medium with 10% FBS. BxPC3 (KRASWT) and KLM-1 (KRASG12D) cells were cultured in DMEM medium with 10% FBS. MDA-MB-231 (KRASG13D) ... | TPDdb | Western Blot | TPD-BV0MW8 | African=3.45%; Native American=0%; East Asian, North=4.63%; East Asian, South=0%; South Asian=0%; European, North=56.1%; European, South=35.82%.
NCI-H358 and NCI-H358M (Cellosaurus=CVCL_JA53) could be identical.
Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*03
Stable (MSS) (Sanger).
In situ; Lun... | -1 | true | -1 | -1 |
COc1ccc(-c2cn(CCCN)c3ccc(CN4CCC(CN5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)cc23)c(F)c1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | NCI-H441 | DC50 | nM | 6,500 | null | 3 | 10 | null | null | null | range | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1561 | Homo sapiens | COMPOUNDS FOR MUTANT KRAS PROTEIN DEGRADATION AND USES THEREOF (patent) | Western blot to evaluate the cellular potencies of RAS-PROTACs in KRAS protein degradation. For western blot experiments, BT-474 (KRASWT) and MIA PaCa-2 (KRASG12C) cells were cultured in DMEM medium with 10% FBS. BxPC3 (KRASWT) and KLM-1 (KRASG12D) cells were cultured in DMEM medium with 10% FBS. MDA-MB-231 (KRASG13D) ... | TPDdb | Western Blot | TPD-BV0MW8 | African=0.09%; Native American=0%; East Asian, North=3.45%; East Asian, South=0%; South Asian=1.1%; European, North=61.67%; European, South=33.69%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02
Stable (MSS) (Sanger).
Metastatic; Pericardial effusion;
Caucasian.
Club cell; CL=CL_0000158.
Cancer cell line | -1 | true | -1 | -1 |
COc1ccc(-c2cn(CCCN)c3ccc(CN4CCC(CN5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)cc23)cn1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | Calu-1 | DC50 | nM | 10,000 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0608 | Homo sapiens | COMPOUNDS FOR MUTANT KRAS PROTEIN DEGRADATION AND USES THEREOF (patent) | Western blot to evaluate the cellular potencies of RAS-PROTACs in KRAS protein degradation. For western blot experiments, BT-474 (KRASWT) and MIA PaCa-2 (KRASG12C) cells were cultured in DMEM medium with 10% FBS. BxPC3 (KRASWT) and KLM-1 (KRASG12D) cells were cultured in DMEM medium with 10% FBS. MDA-MB-231 (KRASG13D) ... | TPDdb | Western Blot | TPD-28XF5J | African=0%; Native American=0.74%; East Asian, North=0.11%; East Asian, South=0%; South Asian=9.94%; European, North=31.4%; European, South=57.8%.
Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*10,11; B*15,w35 (CLS=300141). A*26
Metastatic; Pleural effusion;
Caucasian.
Cancer cell line | -1 | false | 988 | 114 |
COc1ccc(-c2cn(CCCN)c3ccc(CN4CCC(CN5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)cc23)cn1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | HCT 116 | DC50 | nM | 10,000 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0291 | Homo sapiens | COMPOUNDS FOR MUTANT KRAS PROTEIN DEGRADATION AND USES THEREOF (patent) | Western blot to evaluate the cellular potencies of RAS-PROTACs in KRAS protein degradation. For western blot experiments, BT-474 (KRASWT) and MIA PaCa-2 (KRASG12C) cells were cultured in DMEM medium with 10% FBS. BxPC3 (KRASWT) and KLM-1 (KRASG12D) cells were cultured in DMEM medium with 10% FBS. MDA-MB-231 (KRASG13D) ... | TPDdb | Western Blot | TPD-28XF5J | African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut... | -1 | false | 988 | 114 |
COc1ccc(-c2cn(CCCN)c3ccc(CN4CCC(CN5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)cc23)cn1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | KLM-1 | DC50 | nM | 10,000 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_5146 | Homo sapiens | COMPOUNDS FOR MUTANT KRAS PROTEIN DEGRADATION AND USES THEREOF (patent) | Western blot to evaluate the cellular potencies of RAS-PROTACs in KRAS protein degradation. For western blot experiments, BT-474 (KRASWT) and MIA PaCa-2 (KRASG12C) cells were cultured in DMEM medium with 10% FBS. BxPC3 (KRASWT) and KLM-1 (KRASG12D) cells were cultured in DMEM medium with 10% FBS. MDA-MB-231 (KRASG13D) ... | TPDdb | Western Blot | TPD-28XF5J | African=0.52%; Native American=0%; East Asian, North=88.41%; East Asian, South=10.63%; South Asian=0.44%; European, North=0%; European, South=0%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established after 2 rounds of injection of cell suspensions of subcutaneous tumors arising from PK-1 in BALB/c nude mice.
A*24
CVCL_... | -1 | false | 988 | 114 |
COc1ccc(-c2cn(CCCN)c3ccc(CN4CCC(CN5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)cc23)cn1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | MDA-MB-231 | DC50 | nM | 10,000 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0062 | Homo sapiens | COMPOUNDS FOR MUTANT KRAS PROTEIN DEGRADATION AND USES THEREOF (patent) | Western blot to evaluate the cellular potencies of RAS-PROTACs in KRAS protein degradation. For western blot experiments, BT-474 (KRASWT) and MIA PaCa-2 (KRASG12C) cells were cultured in DMEM medium with 10% FBS. BxPC3 (KRASWT) and KLM-1 (KRASG12D) cells were cultured in DMEM medium with 10% FBS. MDA-MB-231 (KRASG13D) ... | TPDdb | Western Blot | TPD-28XF5J | African=1.95%; Native American=0%; East Asian, North=2.44%; East Asian, South=0%; South Asian=7.42%; European, North=28.16%; European, South=60.03%.
Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02/28; B*07,08; C*w02,w06. A*02 A... | -1 | false | 988 | 114 |
COc1ccc(-c2cn(CCCN)c3ccc(CN4CCC(CN5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)cc23)cn1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | NCI-H441 | DC50 | nM | 10,000 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1561 | Homo sapiens | COMPOUNDS FOR MUTANT KRAS PROTEIN DEGRADATION AND USES THEREOF (patent) | Western blot to evaluate the cellular potencies of RAS-PROTACs in KRAS protein degradation. For western blot experiments, BT-474 (KRASWT) and MIA PaCa-2 (KRASG12C) cells were cultured in DMEM medium with 10% FBS. BxPC3 (KRASWT) and KLM-1 (KRASG12D) cells were cultured in DMEM medium with 10% FBS. MDA-MB-231 (KRASG13D) ... | TPDdb | Western Blot | TPD-28XF5J | African=0.09%; Native American=0%; East Asian, North=3.45%; East Asian, South=0%; South Asian=1.1%; European, North=61.67%; European, South=33.69%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02
Stable (MSS) (Sanger).
Metastatic; Pericardial effusion;
Caucasian.
Club cell; CL=CL_0000158.
Cancer cell line | -1 | false | 988 | 114 |
COc1ccc(-c2cn(CCCN)c3ccc(CN4CCN(CC5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)cc23)cc1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | Calu-1 | DC50 | nM | 6,500 | null | 3 | 10 | null | null | null | range | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0608 | Homo sapiens | COMPOUNDS FOR MUTANT KRAS PROTEIN DEGRADATION AND USES THEREOF (patent) | Western blot to evaluate the cellular potencies of RAS-PROTACs in KRAS protein degradation. For western blot experiments, BT-474 (KRASWT) and MIA PaCa-2 (KRASG12C) cells were cultured in DMEM medium with 10% FBS. BxPC3 (KRASWT) and KLM-1 (KRASG12D) cells were cultured in DMEM medium with 10% FBS. MDA-MB-231 (KRASG13D) ... | TPDdb | Western Blot | TPD-MPIBLG | African=0%; Native American=0.74%; East Asian, North=0.11%; East Asian, South=0%; South Asian=9.94%; European, North=31.4%; European, South=57.8%.
Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*10,11; B*15,w35 (CLS=300141). A*26
Metastatic; Pleural effusion;
Caucasian.
Cancer cell line | -1 | true | -1 | -1 |
COc1ccc(-c2cn(CCCN)c3ccc(CN4CCN(CC5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)cc23)cc1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | HCT 116 | DC50 | nM | 6,500 | null | 3 | 10 | null | null | null | range | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0291 | Homo sapiens | COMPOUNDS FOR MUTANT KRAS PROTEIN DEGRADATION AND USES THEREOF (patent) | Western blot to evaluate the cellular potencies of RAS-PROTACs in KRAS protein degradation. For western blot experiments, BT-474 (KRASWT) and MIA PaCa-2 (KRASG12C) cells were cultured in DMEM medium with 10% FBS. BxPC3 (KRASWT) and KLM-1 (KRASG12D) cells were cultured in DMEM medium with 10% FBS. MDA-MB-231 (KRASG13D) ... | TPDdb | Western Blot | TPD-MPIBLG | African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut... | -1 | true | -1 | -1 |
COc1ccc(-c2cn(CCCN)c3ccc(CN4CCN(CC5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)cc23)cc1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | KLM-1 | DC50 | nM | 6,500 | null | 3 | 10 | null | null | null | range | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_5146 | Homo sapiens | COMPOUNDS FOR MUTANT KRAS PROTEIN DEGRADATION AND USES THEREOF (patent) | Western blot to evaluate the cellular potencies of RAS-PROTACs in KRAS protein degradation. For western blot experiments, BT-474 (KRASWT) and MIA PaCa-2 (KRASG12C) cells were cultured in DMEM medium with 10% FBS. BxPC3 (KRASWT) and KLM-1 (KRASG12D) cells were cultured in DMEM medium with 10% FBS. MDA-MB-231 (KRASG13D) ... | TPDdb | Western Blot | TPD-MPIBLG | African=0.52%; Native American=0%; East Asian, North=88.41%; East Asian, South=10.63%; South Asian=0.44%; European, North=0%; European, South=0%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established after 2 rounds of injection of cell suspensions of subcutaneous tumors arising from PK-1 in BALB/c nude mice.
A*24
CVCL_... | -1 | true | -1 | -1 |
COc1ccc(-c2cn(CCCN)c3ccc(CN4CCN(CC5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)cc23)cc1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | MDA-MB-231 | DC50 | nM | 6,500 | null | 3 | 10 | null | null | null | range | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0062 | Homo sapiens | COMPOUNDS FOR MUTANT KRAS PROTEIN DEGRADATION AND USES THEREOF (patent) | Western blot to evaluate the cellular potencies of RAS-PROTACs in KRAS protein degradation. For western blot experiments, BT-474 (KRASWT) and MIA PaCa-2 (KRASG12C) cells were cultured in DMEM medium with 10% FBS. BxPC3 (KRASWT) and KLM-1 (KRASG12D) cells were cultured in DMEM medium with 10% FBS. MDA-MB-231 (KRASG13D) ... | TPDdb | Western Blot | TPD-MPIBLG | African=1.95%; Native American=0%; East Asian, North=2.44%; East Asian, South=0%; South Asian=7.42%; European, North=28.16%; European, South=60.03%.
Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02/28; B*07,08; C*w02,w06. A*02 A... | -1 | true | -1 | -1 |
COc1ccc(-c2cn(CCCN)c3ccc(CN4CCN(CC5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)cc23)cc1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | NCI-H358 | DC50 | nM | 6,500 | null | 3 | 10 | null | null | null | range | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1559 | Homo sapiens | COMPOUNDS FOR MUTANT KRAS PROTEIN DEGRADATION AND USES THEREOF (patent) | Western blot to evaluate the cellular potencies of RAS-PROTACs in KRAS protein degradation. For western blot experiments, BT-474 (KRASWT) and MIA PaCa-2 (KRASG12C) cells were cultured in DMEM medium with 10% FBS. BxPC3 (KRASWT) and KLM-1 (KRASG12D) cells were cultured in DMEM medium with 10% FBS. MDA-MB-231 (KRASG13D) ... | TPDdb | Western Blot | TPD-MPIBLG | African=3.45%; Native American=0%; East Asian, North=4.63%; East Asian, South=0%; South Asian=0%; European, North=56.1%; European, South=35.82%.
NCI-H358 and NCI-H358M (Cellosaurus=CVCL_JA53) could be identical.
Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*03
Stable (MSS) (Sanger).
In situ; Lun... | -1 | true | -1 | -1 |
COc1ccc(-c2cn(CCCN)c3ccc(CN4CCN(CC5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)cc23)cc1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | NCI-H441 | DC50 | nM | 6,500 | null | 3 | 10 | null | null | null | range | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1561 | Homo sapiens | COMPOUNDS FOR MUTANT KRAS PROTEIN DEGRADATION AND USES THEREOF (patent) | Western blot to evaluate the cellular potencies of RAS-PROTACs in KRAS protein degradation. For western blot experiments, BT-474 (KRASWT) and MIA PaCa-2 (KRASG12C) cells were cultured in DMEM medium with 10% FBS. BxPC3 (KRASWT) and KLM-1 (KRASG12D) cells were cultured in DMEM medium with 10% FBS. MDA-MB-231 (KRASG13D) ... | TPDdb | Western Blot | TPD-MPIBLG | African=0.09%; Native American=0%; East Asian, North=3.45%; East Asian, South=0%; South Asian=1.1%; European, North=61.67%; European, South=33.69%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02
Stable (MSS) (Sanger).
Metastatic; Pericardial effusion;
Caucasian.
Club cell; CL=CL_0000158.
Cancer cell line | -1 | true | -1 | -1 |
COc1ccc(C(=O)N2CCC(CN3CCC(Oc4ccc(-c5cc6c(-c7ccc(CNC(=O)c8nc(C(C)(C)C)no8)c(C)c7)ncnc6[nH]5)cc4)CC3)CC2)cc1N1CCC(=O)NC1=O | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | null | DC50 | nM | 1.9 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | null | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE (patent) | HTFR assay
After 6h treatment, add 10μl 4xlysis buffer to each well; seal the plate and incubate 30min at room temperature on a plate shaker; Once the cells are lysed, 16 μL of cell lysate are transferred to a PE 384-well HTRF detection plate; 4 μL of pre-mixed HTRF antibodies are added to each well; Cover the plate wi... | TPDdb | HTRF | TPD-VA1JHC | null | 31 | false | 989 | 0 |
COc1ccc(C(=O)N2CCC(N3CC(CN4CCN(c5c(C)cc(-c6cc7c(-c8cnn(C9CCN(C)CC9)c8)c[nH]c7nn6)cc5C)CC4)C3)CC2)cc1N1CCC(=O)NC1=O | MAP4K1 | MDVVDPDIFNRDPRDHYDLLQRLGGGTYGEVFKARDKVSGDLVALKMVKMEPDDDVSTLQKEILILKTCRHANIVAYHGSYLWLQKLWICMEFCGAGSLQDIYQVTGSLSELQISYVCREVLQGLAYLHSQKKIHRDIKGANILINDAGEVRLADFGISAQIGATLARRLSFIGTPYWMAPEVAAVALKGGYNELCDIWSLGITAIELAELQPPLFDVHPLRVLFLMTKSGYQPPRLKEKGKWSAAFHNFIKVTLTKSPKKRPSATKMLSHQLVSQPGLNRGLILDLLDKLKNPGKGPSIGDIEDEEPELPPAIPRRIRS... | CRBN | Ramos | DC50 | nM | 275 | null | 50 | 500 | null | null | null | range | null | PROteolysis-TArgeting Chimera (PROTAC) | Q92918 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0597 | Homo sapiens | PROTAC CHIMERIC COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF (patent) | HPK1 protein degradation detection
WB method was used to test HPK1 protein degradation and DC50/Dmax to evaluate the in vitro degradation ability of the compound.
RAMOS cell line was selected as the degradation cell line, and the culture conditions were RMPI 1640 medium with 10% FBS, 37°C, 5% CO2.
Experimental steps:
(... | TPDdb | Western Blot | TPD-TY5Z3G | EBV-negative.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC
A*03 A*03 A*03 A*03
Stable (MSS).
In situ; Ascites;
Caucasian.
B-cell; CL=CL_0000236.
Cancer cell line | -1 | false | 990 | 93 |
COc1ccc(C(=O)N2CCC(N3CC(CN4CCN(c5c(C)cc(-c6cc7c(-c8cnn(C9CCN(C)CC9)c8)c[nH]c7nn6)cc5C)CC4)C3)CC2)cc1N1CCC(=O)NC1=O | MAP4K1 | MDVVDPDIFNRDPRDHYDLLQRLGGGTYGEVFKARDKVSGDLVALKMVKMEPDDDVSTLQKEILILKTCRHANIVAYHGSYLWLQKLWICMEFCGAGSLQDIYQVTGSLSELQISYVCREVLQGLAYLHSQKKIHRDIKGANILINDAGEVRLADFGISAQIGATLARRLSFIGTPYWMAPEVAAVALKGGYNELCDIWSLGITAIELAELQPPLFDVHPLRVLFLMTKSGYQPPRLKEKGKWSAAFHNFIKVTLTKSPKKRPSATKMLSHQLVSQPGLNRGLILDLLDKLKNPGKGPSIGDIEDEEPELPPAIPRRIRS... | CRBN | Ramos | Dmax | % | 50 | null | 40 | 60 | null | null | null | range | null | PROteolysis-TArgeting Chimera (PROTAC) | Q92918 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0597 | Homo sapiens | PROTAC CHIMERIC COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF (patent) | HPK1 protein degradation detection
WB method was used to test HPK1 protein degradation and DC50/Dmax to evaluate the in vitro degradation ability of the compound.
RAMOS cell line was selected as the degradation cell line, and the culture conditions were RMPI 1640 medium with 10% FBS, 37°C, 5% CO2.
Experimental steps:
(... | TPDdb | Western Blot | TPD-TY5Z3G | EBV-negative.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC
A*03 A*03 A*03 A*03
Stable (MSS).
In situ; Ascites;
Caucasian.
B-cell; CL=CL_0000236.
Cancer cell line | -1 | false | 990 | 93 |
COc1ccc(C(=O)N2CCC(c3ccc(-c4cc5c(-c6ccc(CNC(=O)c7nc(C(C)(C)C)no7)c(C)c6)ncnc5[nH]4)cc3)CC2)cc1N1CCC(=O)NC1=O | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | null | DC50 | nM | 2 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | null | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE (patent) | HTFR assay
After 6h treatment, add 10μl 4xlysis buffer to each well; seal the plate and incubate 30min at room temperature on a plate shaker; Once the cells are lysed, 16 μL of cell lysate are transferred to a PE 384-well HTRF detection plate; 4 μL of pre-mixed HTRF antibodies are added to each well; Cover the plate wi... | TPDdb | HTRF | TPD-PZD0O3 | null | 31 | true | -1 | -1 |
COc1ccc(C(=O)NCc2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)NC8=O)cc7)CC6)CC5)cc3CC4)cc2)c(OC)c1 | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 0.703 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_A442 | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent) | TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro... | TPDdb | HTRF | TPD-6DDGGQ | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 783 | 15 |
COc1ccc(C(F)(F)F)cc1C(=O)NCc1ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)c(F)c1 | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 1.79 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_A442 | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent) | TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro... | TPDdb | HTRF | TPD-1ZPNWU | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 783 | 15 |
COc1ccc(C(F)(F)F)cc1C(=O)NCc1ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)c(F)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 1.76 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_A442 | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent) | TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro... | TPDdb | HTRF | TPD-1QZGWG | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 783 | 15 |
COc1ccc(C(F)(F)F)cc1C(=O)NCc1ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)c(OC)c1 | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 0.956 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_A442 | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent) | TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro... | TPDdb | HTRF | TPD-E9ZMYM | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 783 | 15 |
COc1ccc(C(F)(F)F)cc1C(=O)NCc1ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)cc1 | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 0.282 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_A442 | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent) | TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro... | TPDdb | HTRF | TPD-LB31M6 | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 783 | 15 |
COc1ccc(C(F)(F)F)cc1C(=O)NCc1ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)cc1C | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 54.18 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_A442 | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent) | TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro... | TPDdb | HTRF | TPD-605JW7 | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 783 | 15 |
COc1ccc(C(F)(F)F)cc1C(=O)NCc1ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)cc1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 0.848 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_A442 | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent) | TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro... | TPDdb | HTRF | TPD-J6MU79 | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 783 | 15 |
COc1ccc(C)cc1C(=O)NCc1ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)cc1 | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 0.726 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_A442 | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent) | TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro... | TPDdb | HTRF | TPD-ZXDPCU | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 783 | 15 |
COc1ccc(C)cc1C(=O)NCc1ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)cc1C | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 10.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_A442 | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent) | TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro... | TPDdb | HTRF | TPD-5B8C72 | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 783 | 15 |
COc1ccc(C2CC2)cc1C(=O)NCc1ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)cc1 | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 2 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_A442 | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent) | TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro... | TPDdb | HTRF | TPD-OT4VE6 | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 991 | 15 |
COc1ccc(Cl)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CN(CCCCCCOCCCCCCOCC(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)NCc5ccc(-c6scnc6C)cc5)C(C)(C)C)CCO4)c4cn[nH]c4n3)cc2)c1 | SGK3 | MQRDHTMDYKESCPSVSIPSSDEHREKKKRFTVYKVLVSVGRSEWFVFRRYAEFDKLYNTLKKQFPAMALKIPAKRIFGDNFDPDFIKQRRAGLNEFIQNLVRYPELYNHPDVRAFLQMDSPKHQSDPSEDEDERSSQKLHSTSQNINLGPSGNPHAKPTDFDFLKVIGKGSFGKVLLAKRKLDGKFYAVKVLQKKIVLNRKEQKHIMAERNVLLKNVKHPFLVGLHYSFQTTEKLYFVLDFVNGGELFFHLQRERSFPEHRARFYAAEIASALGYLHSIKIVYRDLKPENILLDSVGHVVLTDFGLCKEGIAISDTTTT... | VHL | HEK293 | Dmax | % | 71 | null | null | null | null | 48 | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q96BR1 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_0045 | Homo sapiens | https://pubmed.ncbi.nlm.nih.gov/31461270/ | null | PROTACpedia | null | null | Used for the production of the Gamaleya SARS-CoV-2 (COVID-19) vaccine (Trade name
A*02 A*03
In situ; Fetal kidney;
Vaccine production cell line.
NCBI_TaxID; 28285; Human adenovirus C serotype 5.
Transformed cell line | 29 | false | 992 | 0 |
COc1ccc(Cl)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CN(CCCCCCOCCOCCOCCOCC(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)NCc5ccc(-c6scnc6C)cc5)C(C)(C)C)CCO4)c4c(C)n[nH]c4n3)cc2)c1 | SGK3 | MQRDHTMDYKESCPSVSIPSSDEHREKKKRFTVYKVLVSVGRSEWFVFRRYAEFDKLYNTLKKQFPAMALKIPAKRIFGDNFDPDFIKQRRAGLNEFIQNLVRYPELYNHPDVRAFLQMDSPKHQSDPSEDEDERSSQKLHSTSQNINLGPSGNPHAKPTDFDFLKVIGKGSFGKVLLAKRKLDGKFYAVKVLQKKIVLNRKEQKHIMAERNVLLKNVKHPFLVGLHYSFQTTEKLYFVLDFVNGGELFFHLQRERSFPEHRARFYAAEIASALGYLHSIKIVYRDLKPENILLDSVGHVVLTDFGLCKEGIAISDTTTT... | VHL | HEK293 | Dmax | % | 71 | null | null | null | null | 48 | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q96BR1 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_0045 | Homo sapiens | https://pubmed.ncbi.nlm.nih.gov/31461270/ | null | PROTACpedia | null | null | Used for the production of the Gamaleya SARS-CoV-2 (COVID-19) vaccine (Trade name
A*02 A*03
In situ; Fetal kidney;
Vaccine production cell line.
NCBI_TaxID; 28285; Human adenovirus C serotype 5.
Transformed cell line | 29 | false | 993 | 0 |
COc1ccc(Cl)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CN(CCOCCOCCOCC(=O)NCCNc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CCO4)c4c(C)n[nH]c4n3)cc2)c1 | SGK3 | MQRDHTMDYKESCPSVSIPSSDEHREKKKRFTVYKVLVSVGRSEWFVFRRYAEFDKLYNTLKKQFPAMALKIPAKRIFGDNFDPDFIKQRRAGLNEFIQNLVRYPELYNHPDVRAFLQMDSPKHQSDPSEDEDERSSQKLHSTSQNINLGPSGNPHAKPTDFDFLKVIGKGSFGKVLLAKRKLDGKFYAVKVLQKKIVLNRKEQKHIMAERNVLLKNVKHPFLVGLHYSFQTTEKLYFVLDFVNGGELFFHLQRERSFPEHRARFYAAEIASALGYLHSIKIVYRDLKPENILLDSVGHVVLTDFGLCKEGIAISDTTTT... | CRBN | HEK293 | Dmax | % | 16 | null | null | null | null | 48 | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q96BR1 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0045 | Homo sapiens | https://pubmed.ncbi.nlm.nih.gov/31461270/ | null | PROTACpedia | null | null | Used for the production of the Gamaleya SARS-CoV-2 (COVID-19) vaccine (Trade name
A*02 A*03
In situ; Fetal kidney;
Vaccine production cell line.
NCBI_TaxID; 28285; Human adenovirus C serotype 5.
Transformed cell line | 29 | false | 994 | 0 |
COc1ccc(Cl)c(S(=O)(=O)Nc2ccc(-c3nc(OC[C@H]4CN(CCOCCOCCOCC(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)NCc5ccc(-c6scnc6C)cc5)C(C)(C)C)CCO4)c4c(C)n[nH]c4n3)cc2)c1 | SGK3 | MQRDHTMDYKESCPSVSIPSSDEHREKKKRFTVYKVLVSVGRSEWFVFRRYAEFDKLYNTLKKQFPAMALKIPAKRIFGDNFDPDFIKQRRAGLNEFIQNLVRYPELYNHPDVRAFLQMDSPKHQSDPSEDEDERSSQKLHSTSQNINLGPSGNPHAKPTDFDFLKVIGKGSFGKVLLAKRKLDGKFYAVKVLQKKIVLNRKEQKHIMAERNVLLKNVKHPFLVGLHYSFQTTEKLYFVLDFVNGGELFFHLQRERSFPEHRARFYAAEIASALGYLHSIKIVYRDLKPENILLDSVGHVVLTDFGLCKEGIAISDTTTT... | VHL | HEK293 | Dmax | % | 16 | null | null | null | null | 48 | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q96BR1 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_0045 | Homo sapiens | https://pubmed.ncbi.nlm.nih.gov/31461270/ | null | PROTACpedia | null | null | Used for the production of the Gamaleya SARS-CoV-2 (COVID-19) vaccine (Trade name
A*02 A*03
In situ; Fetal kidney;
Vaccine production cell line.
NCBI_TaxID; 28285; Human adenovirus C serotype 5.
Transformed cell line | 29 | false | 995 | 0 |
COc1ccc(Cl)cc1C(=O)NCc1ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)cc1C | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 10.1 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_A442 | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent) | TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro... | TPDdb | HTRF | TPD-QTKG7F | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 783 | 15 |
COc1ccc(F)c(F)c1C(=O)NCc1ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)cc1 | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 2.12 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_A442 | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent) | TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro... | TPDdb | HTRF | TPD-KV0GR5 | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 783 | 15 |
COc1ccc(F)cc1C(=O)NCc1ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)cc1C | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 29.43 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_A442 | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent) | TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro... | TPDdb | HTRF | TPD-7DC14I | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 783 | 15 |
COc1ccc2c(c1)c(=O)c(C(=O)Nc1ccc(Oc3ncnc4cc(OCCCCCC(=O)Nc5ccc6c(c5)CN(C5CCC(=O)NC5=O)C6=O)c(OC)cc34)c(F)c1)c(C)n2C | AXL | MAWRCPRMGRVPLAWCLALCGWACMAPRGTQAEESPFVGNPGNITGARGLTGTLRCQLQVQGEPPEVHWLRDGQILELADSTQTQVPLGEDEQDDWIVVSQLRITSLQLSDTGQYQCLVFLGHQTFVSQPGYVGLEGLPYFLEEPEDRTVAANTPFNLSCQAQGPPEPVDLLWLQDAVPLATAPGHGPQRSLHVPGLNKTSSFSCEAHNAKGVTTSRTATITVLPQQPRNLHLVSRQPTELEVAWTPGLSGIYPLTHCTLQAVLSDDGMGIQAGEPDPPEEPLTSQASVPPHQLRLGSLHPHTPYHIRVACTSSQGPSSW... | CRBN | MDA-MB-231 | DC50 | nM | 100 | null | null | null | null | null | < | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P30530 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0062 | Homo sapiens | PROTEIN KINASE DEGRADANT AND USE THEREOF (patent) | Effects of Compounds on AXL Expression in MDA-MB-231 Cells and FLT3 Expression in MV4-11 Cells
Methods: Cell lines: MDA-MB-231 and MV4-11 cell lines were purchased from the American Type Culture Collection (ATCC). Western blotting was performed as follows. MDA-MB-231 and MV4-11 cells were seeded in 12-well plates at d... | TPDdb | Western Blot | TPD-8YJPQG | African=1.95%; Native American=0%; East Asian, North=2.44%; East Asian, South=0%; South Asian=7.42%; European, North=28.16%; European, South=60.03%.
Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02/28; B*07,08; C*w02,w06. A*02 A... | -1 | false | 548 | 27 |
COc1ccc2c(c1)c(=O)c(C(=O)Nc1ccc(Oc3ncnc4cc(OCCCCCC(=O)Nc5ccc6c(c5)CN(C5CCC(=O)NC5=O)C6=O)c(OC)cc34)c(F)c1)c(C)n2C | FLT3 | MPALARDGGQLPLLVVFSAMIFGTITNQDLPVIKCVLINHKNNDSSVGKSSSYPMVSESPEDLGCALRPQSSGTVYEAAAVEVDVSASITLQVLVDAPGNISCLWVFKHSSLNCQPHFDLQNRGVVSMVILKMTETQAGEYLLFIQSEATNYTILFTVSIRNTLLYTLRRPYFRKMENQDALVCISESVPEPIVEWVLCDSQGESCKEESPAVVKKEEKVLHELFGTDIRCCARNELGRECTRLFTIDLNQTPQTTLPQLFLKVGEPLWIRCKAVHVNHGFGLTWELENKALEEGNYFEMSTYSTNRTMIRILFAFVSSV... | CRBN | MV4-11 | DC50 | nM | 100 | null | null | null | null | null | < | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P36888 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0064 | Homo sapiens | PROTEIN KINASE DEGRADANT AND USE THEREOF (patent) | Effects of Compounds on AXL Expression in MDA-MB-231 Cells and FLT3 Expression in MV4-11 Cells
Methods: Cell lines: MDA-MB-231 and MV4-11 cell lines were purchased from the American Type Culture Collection (ATCC). Western blotting was performed as follows. MDA-MB-231 and MV4-11 cells were seeded in 12-well plates at d... | TPDdb | Western Blot | TPD-8YJPQG | African=0.59%; Native American=0%; East Asian, North=0.34%; East Asian, South=0%; South Asian=2.57%; European, North=67.58%; European, South=28.91%.
48,XY,t(4;11)(q21;q23),+8,+19 (ATCC=CRL-9591).
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC
CSF2 and IL3 dependent.
A*03 A*03
Stable (MSS) (Sanger).
In situ; Peripheral bl... | 33 | false | 548 | 27 |
COc1ccc2ccccc2c1C(=O)NCc1ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)cc1 | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 0.758 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_A442 | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent) | TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro... | TPDdb | HTRF | TPD-Z0LVI6 | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 996 | 15 |
COc1ccc2ccccc2c1C(=O)NCc1ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)cc1C | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 15.58 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_A442 | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent) | TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro... | TPDdb | HTRF | TPD-H9ZDEO | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 996 | 15 |
COc1ccc2ccccc2c1C(=O)NCc1ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)cc1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 3.4 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_A442 | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent) | TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro... | TPDdb | HTRF | TPD-1K3IAD | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 996 | 15 |
COc1ccc2ccccc2c1C(=O)N[C@H](C)c1ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)cc1 | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 3.82 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_A442 | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent) | TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro... | TPDdb | HTRF | TPD-73IENL | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 996 | 15 |
COc1cccc(C)c1C(=O)NCc1ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)cc1C | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 8.52 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_A442 | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent) | TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro... | TPDdb | HTRF | TPD-9L1GWD | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 783 | 15 |
COc1cccc(OC)c1C(=O)NCc1ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)cc1 | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 0.343 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_A442 | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent) | TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro... | TPDdb | HTRF | TPD-EXPH3C | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 783 | 15 |
COc1cccc(Oc2ccc(-c3nn(C4CC5CN(C6CN(C7CN(c8cc9c(cc8F)C(=O)N(C8CCC(=O)NC8=O)C9=O)C7)C6)CC5C4)c4ncnc(N)c34)cc2)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | HEK293 | DC50 | nM | 505 | null | 10 | 1,000 | null | null | null | range | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0045 | Homo sapiens | PROTAC COMPOUND, PHARMACEUTICAL COMPOSITION COMPRISING SAME, PREPARATION METHOD THEREFOR, AND USE THEREOF (patent) | Use Mino and HEK293 transfection BTK (C481S) cells to detect the degradation ability of the compound on BTK (WT) and BTK (C481S) protein. Mino human mantle cell lymphoma cell line was purchased from ATCC, cultured in RPMI-1640 medium with 15% FBS and 1% antibiotics. HEK293 OE BTK (C481S) human embryonic kidney cells 29... | TPDdb | Western Blot | TPD-P429Z8 | Used for the production of the Gamaleya SARS-CoV-2 (COVID-19) vaccine (Trade name
A*02 A*03
In situ; Fetal kidney;
Vaccine production cell line.
NCBI_TaxID; 28285; Human adenovirus C serotype 5.
Transformed cell line | 31 | false | 997 | 109 |
COc1cccc(Oc2ccc(-c3nn(C4CC5CN(C6CN(C7CN(c8cc9c(cc8F)C(=O)N(C8CCC(=O)NC8=O)C9=O)C7)C6)CC5C4)c4ncnc(N)c34)cc2)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | HEK293 | Dmax | % | 88.76 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0045 | Homo sapiens | PROTAC COMPOUND, PHARMACEUTICAL COMPOSITION COMPRISING SAME, PREPARATION METHOD THEREFOR, AND USE THEREOF (patent) | Use Mino and HEK293 transfection BTK (C481S) cells to detect the degradation ability of the compound on BTK (WT) and BTK (C481S) protein. Mino human mantle cell lymphoma cell line was purchased from ATCC, cultured in RPMI-1640 medium with 15% FBS and 1% antibiotics. HEK293 OE BTK (C481S) human embryonic kidney cells 29... | TPDdb | Western Blot | TPD-P429Z8 | Used for the production of the Gamaleya SARS-CoV-2 (COVID-19) vaccine (Trade name
A*02 A*03
In situ; Fetal kidney;
Vaccine production cell line.
NCBI_TaxID; 28285; Human adenovirus C serotype 5.
Transformed cell line | 31 | false | 997 | 109 |
COc1cccc(Oc2ccc(-c3nn(C4CC5CN(C6CN(C7CN(c8cc9c(cc8F)C(=O)N(C8CCC(=O)NC8=O)C9=O)C7)C6)CC5C4)c4ncnc(N)c34)cc2)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | Mino | DC50 | nM | 505 | null | 10 | 1,000 | null | null | null | range | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1872 | Homo sapiens | PROTAC COMPOUND, PHARMACEUTICAL COMPOSITION COMPRISING SAME, PREPARATION METHOD THEREFOR, AND USE THEREOF (patent) | Use Mino and HEK293 transfection BTK (C481S) cells to detect the degradation ability of the compound on BTK (WT) and BTK (C481S) protein. Mino human mantle cell lymphoma cell line was purchased from ATCC, cultured in RPMI-1640 medium with 15% FBS and 1% antibiotics. HEK293 OE BTK (C481S) human embryonic kidney cells 29... | TPDdb | Western Blot | TPD-P429Z8 | African=0.85%; Native American=0%; East Asian, North=1.5%; East Asian, South=0%; South Asian=6.1%; European, North=39.56%; European, South=51.98%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*11 A*11,68; B*35,39; C*04,12. A*11
In situ; Peripheral blood;
Caucasian.
Cancer cell line | 31 | false | 997 | 109 |
COc1cccc(Oc2ccc(-c3nn(C4CC5CN(C6CN(C7CN(c8cc9c(cc8F)C(=O)N(C8CCC(=O)NC8=O)C9=O)C7)C6)CC5C4)c4ncnc(N)c34)cc2)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | Mino | Dmax | % | 77.95 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1872 | Homo sapiens | PROTAC COMPOUND, PHARMACEUTICAL COMPOSITION COMPRISING SAME, PREPARATION METHOD THEREFOR, AND USE THEREOF (patent) | Use Mino and HEK293 transfection BTK (C481S) cells to detect the degradation ability of the compound on BTK (WT) and BTK (C481S) protein. Mino human mantle cell lymphoma cell line was purchased from ATCC, cultured in RPMI-1640 medium with 15% FBS and 1% antibiotics. HEK293 OE BTK (C481S) human embryonic kidney cells 29... | TPDdb | Western Blot | TPD-P429Z8 | African=0.85%; Native American=0%; East Asian, North=1.5%; East Asian, South=0%; South Asian=6.1%; European, North=39.56%; European, South=51.98%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*11 A*11,68; B*35,39; C*04,12. A*11
In situ; Peripheral blood;
Caucasian.
Cancer cell line | 31 | false | 997 | 109 |
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