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 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
COc1cc(N2CCC(N3CCN(C(=O)[C@H]4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | NCI-H1975 | DC50 | nM | 3.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1511 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day1, H1975 cells are seeded at 30000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, H1975 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 1000× ... | TPDdb | HTRF | TPD-H15E5M | African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Stable (MSS) (Sanger).
In situ; Lung;
Caucasian.
Cancer cell line | 23 | false | 826 | 64 |
COc1cc(N2CCC(N3CCN(C(=O)[C@H]4C[C@H](N(C)c5ccc(C6CCC(=O)NC6=O)cc5)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 15.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-2T8MZH | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(C(=O)[C@H]4C[C@H](N(C)c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 30 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-SAHHY2 | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 827 | 64 |
COc1cc(N2CCC(N3CCN(C4CC(c5ccc(NC6CCC(=O)NC6=O)cc5)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 73.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-GFED5P | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(C4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 5,112.5 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-V7P49G | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 828 | 64 |
COc1cc(N2CCC(N3CCN(C4CCN(c5cccc(C6CCC(=O)NC6=O)c5)CC4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 5,061.5 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-4S1E29 | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 829 | 64 |
COc1cc(N2CCC(N3CCN(CC4CCN(c5cc(F)c(C6CCC(=O)NC6=O)c(F)c5)CC4)CC3)CC2)c(C)cc1Nc1ncc(C)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 53.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-JR4HCK | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 830 | 64 |
COc1cc(N2CCC(N3CCN(CC4CCN(c5ccc(C6CCC(=O)NC6=O)cc5)CC4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | HCC827 | DC50 | nM | 8.2 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2063 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100... | TPDdb | HTRF | TPD-VWKEN4 | African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%.
Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566).
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*11 A*11
Stable (MSS) (Sanger).
In situ; Lung;
Caucasia... | 23 | false | 830 | 64 |
COc1cc(N2CCC(N3CCN(CC4CCN(c5ccc(C6CCC(=O)NC6=O)cc5)CC4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | NCI-H1975 | DC50 | nM | 10.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1511 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day1, H1975 cells are seeded at 30000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, H1975 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 1000× ... | TPDdb | HTRF | TPD-VWKEN4 | African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Stable (MSS) (Sanger).
In situ; Lung;
Caucasian.
Cancer cell line | 23 | false | 830 | 64 |
COc1cc(N2CCC(N3CCN(CC4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)CC3)CC2)c2cc1Nc1ncc(Br)c(n1)Nc1ccc(cc1N(C)S(C)(=O)=O)OCCCCOC2=O | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 55.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | MACROCYCLE FOR INHIBITING AND INDUCING EGFR DEGRADATION AND PREPARATION METHOD FOR AND USE OF MACROCYCLE (patent) | Test Example 2: Determination of Total EGFR Protein Degradation in BaF3/EGFR L858R-T790M-C797S Cells by Compounds of the Present Disclosure
2. Experimental Methods
2.1. Cell Plating (Day 1)
a. Observe the cells under a microscope.
b. Collect the cell suspension into a 15 mL centrifuge tube and centrifuge at 300 g for 4... | TPDdb | HTRF | TPD-Q48SVK | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 831 | 0 |
COc1cc(N2CCC(N3CCN(CC4CCN(c5ccc6c(c5)CN(C5CCC(=O)NC5=O)C6=O)CC4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 24 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-QX00KW | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 832 | 64 |
COc1cc(N2CCC(N3CCN(CC4CN(c5cc(F)c(C6CCC(=O)NC6=O)c(F)c5)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 30 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-5STO3T | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CC4CN(c5ccc(C6CCC(=O)NC6=O)c(F)c5)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 48 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-JV7M9F | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CC4CN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 22 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-966PLS | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 833 | 64 |
COc1cc(N2CCC(N3CCN(CC4CN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 15.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-W51BZP | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 834 | 64 |
COc1cc(N2CCC(N3CCN(CC4CN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)ccc1Nc1ncc(Cl)c(NC2=C3C(CC=C2)CCN3S(C)(=O)=O)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 14.6 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-IL0QO4 | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 835 | 134 |
COc1cc(N2CCC(N3CCN(CC4CN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)ccc1Nc1ncc(Cl)c(NC2=C3C(CC=C2)CCN3S(C)(=O)=O)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | HCC827 | DC50 | nM | 2.7 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2063 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100... | TPDdb | HTRF | TPD-IL0QO4 | African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%.
Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566).
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*11 A*11
Stable (MSS) (Sanger).
In situ; Lung;
Caucasia... | 23 | false | 835 | 134 |
COc1cc(N2CCC(N3CCN(CC4CN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)ccc1Nc1ncc(Cl)c(NC2=C3C(CC=C2)CCN3S(C)(=O)=O)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | NCI-H1975 | DC50 | nM | 1.8 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1511 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day1, H1975 cells are seeded at 30000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, H1975 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 1000× ... | TPDdb | HTRF | TPD-IL0QO4 | African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Stable (MSS) (Sanger).
In situ; Lung;
Caucasian.
Cancer cell line | 23 | false | 835 | 134 |
COc1cc(N2CCC(N3CCN(CC4CN(c5ccc6c(c5)CN(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 2.3 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-UN3Y75 | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 836 | 134 |
COc1cc(N2CCC(N3CCN(CC4CN(c5ccc6c(c5)CN(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | HCC827 | DC50 | nM | 2.9 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2063 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100... | TPDdb | HTRF | TPD-UN3Y75 | African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%.
Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566).
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*11 A*11
Stable (MSS) (Sanger).
In situ; Lung;
Caucasia... | 23 | false | 836 | 134 |
COc1cc(N2CCC(N3CCN(CC4CN(c5ccc6c(c5)CN(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | NCI-H1975 | DC50 | nM | 3 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1511 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day1, H1975 cells are seeded at 30000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, H1975 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 1000× ... | TPDdb | HTRF | TPD-UN3Y75 | African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Stable (MSS) (Sanger).
In situ; Lung;
Caucasian.
Cancer cell line | 23 | false | 836 | 134 |
COc1cc(N2CCC(N3CCN(CCC4CCN(c5cc(F)c(C6CCC(=O)NC6=O)c(F)c5)CC4)CC3=O)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 16.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-2SSAJQ | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CCC4CCN(c5ccc(C6CCC(=O)NC6=O)c(F)c5)CC4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | HCC827 | DC50 | nM | 40.2 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2063 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100... | TPDdb | HTRF | TPD-W6BECN | African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%.
Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566).
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*11 A*11
Stable (MSS) (Sanger).
In situ; Lung;
Caucasia... | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CCC4CCN(c5ccc(C6CCC(=O)NC6=O)c(F)c5)CC4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | NCI-H1975 | DC50 | nM | 96.4 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1511 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day1, H1975 cells are seeded at 30000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, H1975 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 1000× ... | TPDdb | HTRF | TPD-W6BECN | African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Stable (MSS) (Sanger).
In situ; Lung;
Caucasian.
Cancer cell line | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CCC4CCN(c5ccc(C6CCC(=O)NC6=O)c(F)c5)CC4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 34.45 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-QJ9AL4 | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CCC4CCN(c5ccc(C6CCC(=O)NC6=O)c(F)c5)CC4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | HCC827 | DC50 | nM | 8.6 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2063 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100... | TPDdb | HTRF | TPD-QJ9AL4 | African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%.
Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566).
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*11 A*11
Stable (MSS) (Sanger).
In situ; Lung;
Caucasia... | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CCC4CCN(c5ccc(C6CCC(=O)NC6=O)c(F)c5)CC4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | NCI-H1975 | DC50 | nM | 15.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1511 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day1, H1975 cells are seeded at 30000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, H1975 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 1000× ... | TPDdb | HTRF | TPD-QJ9AL4 | African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Stable (MSS) (Sanger).
In situ; Lung;
Caucasian.
Cancer cell line | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CCC4CCN(c5ccc(C6CCC(=O)NC6=O)cc5)CC4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | HCC827 | DC50 | nM | 16.7 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2063 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100... | TPDdb | HTRF | TPD-I5IVLV | African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%.
Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566).
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*11 A*11
Stable (MSS) (Sanger).
In situ; Lung;
Caucasia... | 23 | false | 543 | 64 |
COc1cc(N2CCC(N3CCN(CCC4CCN(c5ccc(C6CCC(=O)NC6=O)cc5)CC4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | NCI-H1975 | DC50 | nM | 20.7 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1511 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day1, H1975 cells are seeded at 30000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, H1975 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 1000× ... | TPDdb | HTRF | TPD-I5IVLV | African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Stable (MSS) (Sanger).
In situ; Lung;
Caucasian.
Cancer cell line | 23 | false | 543 | 64 |
COc1cc(N2CCC(N3CCN(CCC4CCN(c5ccc(C6CCC(=O)NC6=O)cc5)CC4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 125.45 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-RTDJH1 | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 543 | 66 |
COc1cc(N2CCC(N3CCN(CCC4CCN(c5ccc(C6CCC(=O)NC6=O)cc5)CC4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | HCC827 | DC50 | nM | 8.4 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2063 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100... | TPDdb | HTRF | TPD-RTDJH1 | African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%.
Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566).
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*11 A*11
Stable (MSS) (Sanger).
In situ; Lung;
Caucasia... | 23 | false | 543 | 66 |
COc1cc(N2CCC(N3CCN(CCC4CCN(c5ccc(C6CCC(=O)NC6=O)cc5)CC4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | NCI-H1975 | DC50 | nM | 7.2 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1511 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day1, H1975 cells are seeded at 30000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, H1975 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 1000× ... | TPDdb | HTRF | TPD-RTDJH1 | African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Stable (MSS) (Sanger).
In situ; Lung;
Caucasian.
Cancer cell line | 23 | false | 543 | 66 |
COc1cc(N2CCC(N3CCN(CCC4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 27.4 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-1TKYDB | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 837 | 56 |
COc1cc(N2CCC(N3CCN(CCC4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | HCC827 | DC50 | nM | 6.4 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2063 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100... | TPDdb | HTRF | TPD-1TKYDB | African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%.
Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566).
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*11 A*11
Stable (MSS) (Sanger).
In situ; Lung;
Caucasia... | 23 | false | 837 | 56 |
COc1cc(N2CCC(N3CCN(CCC4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | NCI-H1975 | DC50 | nM | 3.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1511 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day1, H1975 cells are seeded at 30000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, H1975 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 1000× ... | TPDdb | HTRF | TPD-1TKYDB | African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Stable (MSS) (Sanger).
In situ; Lung;
Caucasian.
Cancer cell line | 23 | false | 837 | 56 |
COc1cc(N2CCC(N3CCN(CCC4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 29.9 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-4L7B0V | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 837 | 56 |
COc1cc(N2CCC(N3CCN(CCC4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | HCC827 | DC50 | nM | 3.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2063 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100... | TPDdb | HTRF | TPD-4L7B0V | African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%.
Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566).
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*11 A*11
Stable (MSS) (Sanger).
In situ; Lung;
Caucasia... | 23 | false | 837 | 56 |
COc1cc(N2CCC(N3CCN(CCC4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | NCI-H1975 | DC50 | nM | 3.8 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1511 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day1, H1975 cells are seeded at 30000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, H1975 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 1000× ... | TPDdb | HTRF | TPD-4L7B0V | African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Stable (MSS) (Sanger).
In situ; Lung;
Caucasian.
Cancer cell line | 23 | false | 837 | 56 |
COc1cc(N2CCC(N3CCN(CCC4CN(c5ccc(C6CCC(=O)NC6=O)cc5)C4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | HCC827 | DC50 | nM | 1,977.2 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2063 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100... | TPDdb | HTRF | TPD-ZQ84H0 | African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%.
Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566).
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*11 A*11
Stable (MSS) (Sanger).
In situ; Lung;
Caucasia... | 23 | false | 838 | 134 |
COc1cc(N2CCC(N3CCN(CCC4CN(c5ccc(C6CCC(=O)NC6=O)cc5)C4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | NCI-H1975 | DC50 | nM | 10,000 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1511 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day1, H1975 cells are seeded at 30000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, H1975 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 1000× ... | TPDdb | HTRF | TPD-ZQ84H0 | African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Stable (MSS) (Sanger).
In situ; Lung;
Caucasian.
Cancer cell line | 23 | false | 838 | 134 |
COc1cc(N2CCC(N3CCN(CCCC4CN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | HCC827 | DC50 | nM | 4.6 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2063 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100... | TPDdb | HTRF | TPD-T5RDVF | African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%.
Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566).
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*11 A*11
Stable (MSS) (Sanger).
In situ; Lung;
Caucasia... | 23 | false | 839 | 64 |
COc1cc(N2CCC(N3CCN(CCCC4CN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | NCI-H1975 | DC50 | nM | 10.9 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1511 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day1, H1975 cells are seeded at 30000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, H1975 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 1000× ... | TPDdb | HTRF | TPD-T5RDVF | African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Stable (MSS) (Sanger).
In situ; Lung;
Caucasian.
Cancer cell line | 23 | false | 839 | 64 |
COc1cc(N2CCC(N3CCN(CCN4CCC(c5ccc(NC6CCC(=O)NC6=O)cc5)CC4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 348 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-IPY0KR | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CCNc4cccc5c4CN(C4CCC(=O)NC4=O)C5=O)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 21 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-0MFZVQ | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CCOc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)CC2)c(C)cc1NC1=NC=C(Br)C(Nc2cccc3c2N(S(C)(=O)=O)CC3)N1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 211 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-B41STF | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CCc4cc(Cl)c(C5CCC(=O)NC5=O)cc4F)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 49.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-TQ6KSJ | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CCc4cc(F)c(C5CCC(=O)NC5=O)c(F)c4)CC3)CC2)c(C)cc1Nc1nc(Nc2cccc3c2N(S(C)(=O)=O)CC3)c2cc[nH]c2n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 44.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-7YYEXI | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CCc4cc(F)c(C5CCC(=O)NC5=O)c(F)c4)CC3)CC2)c(C)cc1Nc1nc(Nc2cccc3c2N(S(C)(=O)=O)CC3)c2cc[nH]c2n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | HCC827 | DC50 | nM | 20 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2063 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100... | TPDdb | HTRF | TPD-7YYEXI | African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%.
Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566).
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*11 A*11
Stable (MSS) (Sanger).
In situ; Lung;
Caucasia... | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CCc4cc(F)c(C5CCC(=O)NC5=O)c(F)c4)CC3)CC2)c(C)cc1Nc1nc(Nc2cccc3c2N(S(C)(=O)=O)CC3)c2cc[nH]c2n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | NCI-H1975 | DC50 | nM | 3 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1511 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day1, H1975 cells are seeded at 30000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, H1975 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 1000× ... | TPDdb | HTRF | TPD-7YYEXI | African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Stable (MSS) (Sanger).
In situ; Lung;
Caucasian.
Cancer cell line | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CCc4cc(F)c(C5CCC(=O)NC5=O)c(F)c4)CC3=O)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 11 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-GE17UA | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CCc4cc(F)c(C5CCC(=O)NC5=O)cc4F)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 37.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-ZZ6QFZ | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CCc4ccc(C5CCC(=O)NC5=O)c(F)c4)CC3)CC2)c(C)cc1Nc1nc(Nc2cccc3c2N(S(C)(=O)=O)CC3)c2cc[nH]c2n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 5,039 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-QLMCOB | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 840 | 219 |
COc1cc(N2CCC(N3CCN(CCc4ccc(C5CCC(=O)NC5=O)cc4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 95.45 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-O8SU5F | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CCc4ccc(C5CCC(=O)NC5=O)cc4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | HCC827 | DC50 | nM | 13.6 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2063 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100... | TPDdb | HTRF | TPD-O8SU5F | African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%.
Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566).
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*11 A*11
Stable (MSS) (Sanger).
In situ; Lung;
Caucasia... | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CCc4ccc(C5CCC(=O)NC5=O)cc4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | NCI-H1975 | DC50 | nM | 12.1 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1511 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day1, H1975 cells are seeded at 30000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, H1975 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 1000× ... | TPDdb | HTRF | TPD-O8SU5F | African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Stable (MSS) (Sanger).
In situ; Lung;
Caucasian.
Cancer cell line | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CCc4ccc(C5CCC(=O)NC5=O)cc4)CC3)CC2)ccc1Nc1nc(Nc2cccc3c2N(S(C)(=O)=O)CC3)c2cc[nH]c2n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | HCC827 | DC50 | nM | 113.3 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2063 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100... | TPDdb | HTRF | TPD-J3S4O5 | African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%.
Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566).
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*11 A*11
Stable (MSS) (Sanger).
In situ; Lung;
Caucasia... | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CCc4ccc(C5CCC(=O)NC5=O)cc4)CC3)CC2)ccc1Nc1nc(Nc2cccc3c2N(S(C)(=O)=O)CC3)c2cc[nH]c2n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | NCI-H1975 | DC50 | nM | 38.4 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1511 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day1, H1975 cells are seeded at 30000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, H1975 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 1000× ... | TPDdb | HTRF | TPD-J3S4O5 | African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Stable (MSS) (Sanger).
In situ; Lung;
Caucasian.
Cancer cell line | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CCc4ccc(C5CCC(=O)NC5=O)cc4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 157.15 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-P1HY8N | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CCc4ccc(C5CCC(=O)NC5=O)cc4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | HCC827 | DC50 | nM | 6.7 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2063 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100... | TPDdb | HTRF | TPD-P1HY8N | African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%.
Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566).
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*11 A*11
Stable (MSS) (Sanger).
In situ; Lung;
Caucasia... | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CCc4ccc(C5CCC(=O)NC5=O)cc4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | NCI-H1975 | DC50 | nM | 7 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1511 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day1, H1975 cells are seeded at 30000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, H1975 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 1000× ... | TPDdb | HTRF | TPD-P1HY8N | African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Stable (MSS) (Sanger).
In situ; Lung;
Caucasian.
Cancer cell line | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(CCc4ccc(NC5CCC(=O)NC5=O)cc4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 46.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-FECU4G | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(C[C@@H]4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 56 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-38OJUE | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 841 | 64 |
COc1cc(N2CCC(N3CCN(C[C@@H]4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)c2cc1Nc1ncc(Br)c(n1)Nc1ccc(cc1N(C)S(C)(=O)=O)OCCCCOC2=O | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 34.7 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | MACROCYCLE FOR INHIBITING AND INDUCING EGFR DEGRADATION AND PREPARATION METHOD FOR AND USE OF MACROCYCLE (patent) | Test Example 2: Determination of Total EGFR Protein Degradation in BaF3/EGFR L858R-T790M-C797S Cells by Compounds of the Present Disclosure
2. Experimental Methods
2.1. Cell Plating (Day 1)
a. Observe the cells under a microscope.
b. Collect the cell suspension into a 15 mL centrifuge tube and centrifuge at 300 g for 4... | TPDdb | HTRF | TPD-XZ03TH | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 842 | 0 |
COc1cc(N2CCC(N3CCN(C[C@@H]4CCN(c5ccc6c(c5)CN(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 12 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-2LTSQS | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 843 | 64 |
COc1cc(N2CCC(N3CCN(C[C@@H]4CCN(c5ccc6c(c5)CN(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | HCC827 | DC50 | nM | 6 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2063 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100... | TPDdb | HTRF | TPD-2LTSQS | African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%.
Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566).
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*11 A*11
Stable (MSS) (Sanger).
In situ; Lung;
Caucasia... | 23 | false | 843 | 64 |
COc1cc(N2CCC(N3CCN(C[C@@H]4CCN(c5ccc6c(c5)CN(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | NCI-H1975 | DC50 | nM | 16 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1511 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day1, H1975 cells are seeded at 30000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, H1975 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 1000× ... | TPDdb | HTRF | TPD-2LTSQS | African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Stable (MSS) (Sanger).
In situ; Lung;
Caucasian.
Cancer cell line | 23 | false | 843 | 64 |
COc1cc(N2CCC(N3CCN(C[C@H]4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 27 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-E4YFUE | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 841 | 0 |
COc1cc(N2CCC(N3CCN(C[C@H]4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)c2cc1Nc1ncc(Br)c(n1)Nc1ccc(cc1N(C)S(C)(=O)=O)OCCCCOC2=O | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 53.1 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | MACROCYCLE FOR INHIBITING AND INDUCING EGFR DEGRADATION AND PREPARATION METHOD FOR AND USE OF MACROCYCLE (patent) | Test Example 2: Determination of Total EGFR Protein Degradation in BaF3/EGFR L858R-T790M-C797S Cells by Compounds of the Present Disclosure
2. Experimental Methods
2.1. Cell Plating (Day 1)
a. Observe the cells under a microscope.
b. Collect the cell suspension into a 15 mL centrifuge tube and centrifuge at 300 g for 4... | TPDdb | HTRF | TPD-PNVAYV | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 842 | 0 |
COc1cc(N2CCC(N3CCN(C[C@H]4CCN(c5ccc6c(c5)CN(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 19.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-GUW7S4 | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 843 | 0 |
COc1cc(N2CCC(N3CCN(C[C@H]4CCN(c5ccc6c(c5)CN(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | HCC827 | DC50 | nM | 2 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2063 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100... | TPDdb | HTRF | TPD-GUW7S4 | African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%.
Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566).
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*11 A*11
Stable (MSS) (Sanger).
In situ; Lung;
Caucasia... | 23 | false | 843 | 0 |
COc1cc(N2CCC(N3CCN(C[C@H]4CCN(c5ccc6c(c5)CN(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | NCI-H1975 | DC50 | nM | 7 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1511 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day1, H1975 cells are seeded at 30000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, H1975 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 1000× ... | TPDdb | HTRF | TPD-GUW7S4 | African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Stable (MSS) (Sanger).
In situ; Lung;
Caucasian.
Cancer cell line | 23 | false | 843 | 0 |
COc1cc(N2CCC(N3CCN(C[C@H]4C[C@H](N(C)c5ccc(C6CCC(=O)NC6=O)cc5)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 79.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-AUPOO9 | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | true | -1 | -1 |
COc1cc(N2CCC(N3CCN(C[C@H]4C[C@H](N(C)c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 95.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-QXJ50R | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 844 | 64 |
COc1cc(N2CCC(N3CCN(C[C@H]4C[C@H](c5ccc6c(c5)CN(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 15 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS... | TPDdb | HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation) | TPD-WE1MG3 | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 845 | 64 |
COc1cc(N2CCC(N3CCN(C[C@H]4C[C@H](c5ccc6c(c5)CN(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | HCC827 | DC50 | nM | 2 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2063 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100... | TPDdb | HTRF | TPD-WE1MG3 | African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%.
Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566).
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*11 A*11
Stable (MSS) (Sanger).
In situ; Lung;
Caucasia... | 23 | false | 845 | 64 |
COc1cc(N2CCC(N3CCN(C[C@H]4C[C@H](c5ccc6c(c5)CN(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | NCI-H1975 | DC50 | nM | 3 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1511 | Homo sapiens | BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent) | Cell treatment
On day1, H1975 cells are seeded at 30000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, H1975 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 1000× ... | TPDdb | HTRF | TPD-WE1MG3 | African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Stable (MSS) (Sanger).
In situ; Lung;
Caucasian.
Cancer cell line | 23 | false | 845 | 64 |
COc1cc(N2CCC(NC(=O)CCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1 | ALK | MGAIGLLWLLPLLLSTAAVGSGMGTGQRAGSPAAGPPLQPREPLSYSRLQRKSLAVDFVVPSLFRVYARDLLLPPSSSELKAGRPEARGSLALDCAPLLRLLGPAPGVSWTAGSPAPAEARTLSRVLKGGSVRKLRRAKQLVLELGEEAILEGCVGPPGEAAVGLLQFNLSELFSWWIRQGEGRLRIRLMPEKKASEVGREGRLSAAIRASQPRLLFQIFGTGHSSLESPTNMPSPSPDYFTWNLTWIMKDSFPFLSHRSRYGLECSFDFPCELEYSPPLHDLRNQSWSWRRIPSEEASQMDLLDGPGAERSKEMPRGSF... | VHL | SR | DC50 | nM | 9.1 | null | null | null | null | 16 | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9UM73 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_1711 | Homo sapiens | 10.1016/j.ejmech.2020.112190; https://pubmed.ncbi.nlm.nih.gov/32179332/ | Degradation of ALK in SR cells after 16 h treatment; EC50 of ligand is 2.7 ± 0.4nM (SF cells), 58.2 ± 20.7 nM (H2228 cells). | PROTAC-DB; PROTACpedia | null | null | African=0%; Native American=0%; East Asian, North=3.12%; East Asian, South=0%; South Asian=0%; European, North=62.78%; European, South=34.1%.
Gene fusion; HGNC; HGNC
A*02,03; B*37 A*02 A*02
Stable (MSS) (Sanger).
In situ; Pleural effusion;
Caucasian.
Cancer cell line | -1 | false | 846 | 0 |
COc1cc(N2CCC(NC(=O)CCCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1 | ALK | MGAIGLLWLLPLLLSTAAVGSGMGTGQRAGSPAAGPPLQPREPLSYSRLQRKSLAVDFVVPSLFRVYARDLLLPPSSSELKAGRPEARGSLALDCAPLLRLLGPAPGVSWTAGSPAPAEARTLSRVLKGGSVRKLRRAKQLVLELGEEAILEGCVGPPGEAAVGLLQFNLSELFSWWIRQGEGRLRIRLMPEKKASEVGREGRLSAAIRASQPRLLFQIFGTGHSSLESPTNMPSPSPDYFTWNLTWIMKDSFPFLSHRSRYGLECSFDFPCELEYSPPLHDLRNQSWSWRRIPSEEASQMDLLDGPGAERSKEMPRGSF... | VHL | SR | DC50 | nM | 20.9 | null | null | null | null | 16 | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9UM73 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_1711 | Homo sapiens | 10.1016/j.ejmech.2020.112190; https://pubmed.ncbi.nlm.nih.gov/32179332/ | Degradation of ALK in SR cells after 16 h treatment; EC50 of ligand is 2.7 ± 0.4nM (SF cells), 58.2 ± 20.7 nM (H2228 cells). | PROTAC-DB; PROTACpedia | null | null | African=0%; Native American=0%; East Asian, North=3.12%; East Asian, South=0%; South Asian=0%; European, North=62.78%; European, South=34.1%.
Gene fusion; HGNC; HGNC
A*02,03; B*37 A*02 A*02
Stable (MSS) (Sanger).
In situ; Pleural effusion;
Caucasian.
Cancer cell line | -1 | false | 847 | 0 |
COc1cc(N2CCC(NC(=O)CCCCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1 | ALK | MGAIGLLWLLPLLLSTAAVGSGMGTGQRAGSPAAGPPLQPREPLSYSRLQRKSLAVDFVVPSLFRVYARDLLLPPSSSELKAGRPEARGSLALDCAPLLRLLGPAPGVSWTAGSPAPAEARTLSRVLKGGSVRKLRRAKQLVLELGEEAILEGCVGPPGEAAVGLLQFNLSELFSWWIRQGEGRLRIRLMPEKKASEVGREGRLSAAIRASQPRLLFQIFGTGHSSLESPTNMPSPSPDYFTWNLTWIMKDSFPFLSHRSRYGLECSFDFPCELEYSPPLHDLRNQSWSWRRIPSEEASQMDLLDGPGAERSKEMPRGSF... | VHL | SR | DC50 | nM | 7.2 | null | null | null | null | 16 | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9UM73 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_1711 | Homo sapiens | 10.1016/j.ejmech.2020.112190; https://pubmed.ncbi.nlm.nih.gov/32179332/ | Degradation of ALK in SR cells after 16 h treatment; EC50 of ligand is 2.7 ± 0.4nM (SF cells), 58.2 ± 20.7 nM (H2228 cells). | PROTAC-DB; PROTACpedia | null | null | African=0%; Native American=0%; East Asian, North=3.12%; East Asian, South=0%; South Asian=0%; European, North=62.78%; European, South=34.1%.
Gene fusion; HGNC; HGNC
A*02,03; B*37 A*02 A*02
Stable (MSS) (Sanger).
In situ; Pleural effusion;
Caucasian.
Cancer cell line | -1 | false | 848 | 0 |
COc1cc(N2CCC(NC(=O)CCCCCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1 | ALK | MGAIGLLWLLPLLLSTAAVGSGMGTGQRAGSPAAGPPLQPREPLSYSRLQRKSLAVDFVVPSLFRVYARDLLLPPSSSELKAGRPEARGSLALDCAPLLRLLGPAPGVSWTAGSPAPAEARTLSRVLKGGSVRKLRRAKQLVLELGEEAILEGCVGPPGEAAVGLLQFNLSELFSWWIRQGEGRLRIRLMPEKKASEVGREGRLSAAIRASQPRLLFQIFGTGHSSLESPTNMPSPSPDYFTWNLTWIMKDSFPFLSHRSRYGLECSFDFPCELEYSPPLHDLRNQSWSWRRIPSEEASQMDLLDGPGAERSKEMPRGSF... | VHL | SR | DC50 | nM | 7 | null | null | null | null | 16 | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9UM73 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_1711 | Homo sapiens | 10.1016/j.ejmech.2020.112190; https://pubmed.ncbi.nlm.nih.gov/32179332/ | Degradation of ALK in SR cells after 16 h treatment; EC50 of ligand is 2.7 ± 0.4nM (SF cells), 58.2 ± 20.7 nM (H2228 cells). EC50 of PROTAC is 1.7 ± 1 nM (SF cells), 46nM ± 16 nM (H2228 cells). | PROTAC-DB; PROTACpedia | null | null | African=0%; Native American=0%; East Asian, North=3.12%; East Asian, South=0%; South Asian=0%; European, North=62.78%; European, South=34.1%.
Gene fusion; HGNC; HGNC
A*02,03; B*37 A*02 A*02
Stable (MSS) (Sanger).
In situ; Pleural effusion;
Caucasian.
Cancer cell line | -1 | false | 849 | 0 |
COc1cc(N2CCC(NC(=O)CCCCCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1 | ALK G1202R | MGAIGLLWLLPLLLSTAAVGSGMGTGQRAGSPAAGPPLQPREPLSYSRLQRKSLAVDFVVPSLFRVYARDLLLPPSSSELKAGRPEARGSLALDCAPLLRLLGPAPGVSWTAGSPAPAEARTLSRVLKGGSVRKLRRAKQLVLELGEEAILEGCVGPPGEAAVGLLQFNLSELFSWWIRQGEGRLRIRLMPEKKASEVGREGRLSAAIRASQPRLLFQIFGTGHSSLESPTNMPSPSPDYFTWNLTWIMKDSFPFLSHRSRYGLECSFDFPCELEYSPPLHDLRNQSWSWRRIPSEEASQMDLLDGPGAERSKEMPRGSF... | VHL | HEK293T | DC50 | nM | 200 | null | null | null | null | null | < | null | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9UM73 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_0063 | Homo sapiens | 10.1016/j.ejmech.2020.112190 | Degradation of G1202R ALK in 293T cells | PROTAC-DB | null | null | Highly susceptible to infection by Zika virus (ZIKV).
CVCL_0045 ! HEK293
In situ; Fetal kidney;
NCBI_TaxID; 28285; Human adenovirus C serotype 5. NCBI_TaxID; 1891767; Simian virus 40 (SV40) (Note=tsA).
Transformed cell line | -1 | false | 849 | 0 |
COc1cc(N2CCC(OCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)ccc1NC(=O)c1cccc(-c2ccn[nH]2)n1 | IRAK1 | MAGGPGPGEPAAPGAQHFLYEVPPWVMCRFYKVMDALEPADWCQFAALIVRDQTELRLCERSGQRTASVLWPWINRNARVADLVHILTHLQLLRARDIITAWHPPAPLPSPGTTAPRPSSIPAPAEAEAWSPRKLPSSASTFLSPAFPGSQTHSGPELGLVPSPASLWPPPPSPAPSSTKPGPESSVSLLQGARPFPFCWPLCEISRGTHNFSEELKIGEGGFGCVYRAVMRNTVYAVKRLKENADLEWTAVKQSFLTEVEQLSRFRHPNIVDFAGYCAQNGFYCLVYGFLPNGSLEDRLHCQTQACPPLSWPQRLDILL... | VHL | HEK293T | DC50 | nM | 16 | null | null | null | null | 24 | null | null | null | PROteolysis-TArgeting Chimera (PROTAC) | P51617 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_0063 | Homo sapiens | 10.1021/acsmedchemlett.1c00244 | Degradation of IRAK1 in HEK293T cells after 24 h treatment | PROTAC-DB | null | null | Highly susceptible to infection by Zika virus (ZIKV).
CVCL_0045 ! HEK293
In situ; Fetal kidney;
NCBI_TaxID; 28285; Human adenovirus C serotype 5. NCBI_TaxID; 1891767; Simian virus 40 (SV40) (Note=tsA).
Transformed cell line | 25 | false | 850 | 9 |
COc1cc(N2CCC(OCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)ccc1NC(=O)c1cccc(-c2ccn[nH]2)n1 | IRAK1 | MAGGPGPGEPAAPGAQHFLYEVPPWVMCRFYKVMDALEPADWCQFAALIVRDQTELRLCERSGQRTASVLWPWINRNARVADLVHILTHLQLLRARDIITAWHPPAPLPSPGTTAPRPSSIPAPAEAEAWSPRKLPSSASTFLSPAFPGSQTHSGPELGLVPSPASLWPPPPSPAPSSTKPGPESSVSLLQGARPFPFCWPLCEISRGTHNFSEELKIGEGGFGCVYRAVMRNTVYAVKRLKENADLEWTAVKQSFLTEVEQLSRFRHPNIVDFAGYCAQNGFYCLVYGFLPNGSLEDRLHCQTQACPPLSWPQRLDILL... | VHL | HEK293T | Dmax | % | 95 | null | null | null | null | 24 | null | null | null | PROteolysis-TArgeting Chimera (PROTAC) | P51617 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_0063 | Homo sapiens | 10.1021/acsmedchemlett.1c00244 | Degradation of IRAK1 in HEK293T cells after 24 h treatment | PROTAC-DB | null | null | Highly susceptible to infection by Zika virus (ZIKV).
CVCL_0045 ! HEK293
In situ; Fetal kidney;
NCBI_TaxID; 28285; Human adenovirus C serotype 5. NCBI_TaxID; 1891767; Simian virus 40 (SV40) (Note=tsA).
Transformed cell line | 25 | false | 850 | 9 |
COc1cc(N2CCC(OCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3F)C(C)(C)C)CC2)ccc1NC(=O)c1cccc(-c2ccn[nH]2)n1 | IRAK1 | MAGGPGPGEPAAPGAQHFLYEVPPWVMCRFYKVMDALEPADWCQFAALIVRDQTELRLCERSGQRTASVLWPWINRNARVADLVHILTHLQLLRARDIITAWHPPAPLPSPGTTAPRPSSIPAPAEAEAWSPRKLPSSASTFLSPAFPGSQTHSGPELGLVPSPASLWPPPPSPAPSSTKPGPESSVSLLQGARPFPFCWPLCEISRGTHNFSEELKIGEGGFGCVYRAVMRNTVYAVKRLKENADLEWTAVKQSFLTEVEQLSRFRHPNIVDFAGYCAQNGFYCLVYGFLPNGSLEDRLHCQTQACPPLSWPQRLDILL... | VHL | HEK293T | DC50 | nM | 13 | null | null | null | null | 24 | null | null | null | PROteolysis-TArgeting Chimera (PROTAC) | P51617 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_0063 | Homo sapiens | 10.1021/acsmedchemlett.1c00244 | Degradation of IRAK1 in HEK293T cells after 24 h treatment | PROTAC-DB | null | null | Highly susceptible to infection by Zika virus (ZIKV).
CVCL_0045 ! HEK293
In situ; Fetal kidney;
NCBI_TaxID; 28285; Human adenovirus C serotype 5. NCBI_TaxID; 1891767; Simian virus 40 (SV40) (Note=tsA).
Transformed cell line | 25 | false | 850 | 9 |
COc1cc(N2CCC(OCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3F)C(C)(C)C)CC2)ccc1NC(=O)c1cccc(-c2ccn[nH]2)n1 | IRAK1 | MAGGPGPGEPAAPGAQHFLYEVPPWVMCRFYKVMDALEPADWCQFAALIVRDQTELRLCERSGQRTASVLWPWINRNARVADLVHILTHLQLLRARDIITAWHPPAPLPSPGTTAPRPSSIPAPAEAEAWSPRKLPSSASTFLSPAFPGSQTHSGPELGLVPSPASLWPPPPSPAPSSTKPGPESSVSLLQGARPFPFCWPLCEISRGTHNFSEELKIGEGGFGCVYRAVMRNTVYAVKRLKENADLEWTAVKQSFLTEVEQLSRFRHPNIVDFAGYCAQNGFYCLVYGFLPNGSLEDRLHCQTQACPPLSWPQRLDILL... | VHL | HEK293T | Dmax | % | 96 | null | null | null | null | 24 | null | null | null | PROteolysis-TArgeting Chimera (PROTAC) | P51617 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_0063 | Homo sapiens | 10.1021/acsmedchemlett.1c00244 | Degradation of IRAK1 in HEK293T cells after 24 h treatment | PROTAC-DB | null | null | Highly susceptible to infection by Zika virus (ZIKV).
CVCL_0045 ! HEK293
In situ; Fetal kidney;
NCBI_TaxID; 28285; Human adenovirus C serotype 5. NCBI_TaxID; 1891767; Simian virus 40 (SV40) (Note=tsA).
Transformed cell line | 25 | false | 850 | 9 |
COc1cc(N2CCC(OCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)N[C@@H](C)c3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)ccc1NC(=O)c1cccc(-c2ccn[nH]2)n1 | IRAK1 | MAGGPGPGEPAAPGAQHFLYEVPPWVMCRFYKVMDALEPADWCQFAALIVRDQTELRLCERSGQRTASVLWPWINRNARVADLVHILTHLQLLRARDIITAWHPPAPLPSPGTTAPRPSSIPAPAEAEAWSPRKLPSSASTFLSPAFPGSQTHSGPELGLVPSPASLWPPPPSPAPSSTKPGPESSVSLLQGARPFPFCWPLCEISRGTHNFSEELKIGEGGFGCVYRAVMRNTVYAVKRLKENADLEWTAVKQSFLTEVEQLSRFRHPNIVDFAGYCAQNGFYCLVYGFLPNGSLEDRLHCQTQACPPLSWPQRLDILL... | VHL | HEK293T | DC50 | nM | 3 | null | null | null | null | 24 | null | null | null | PROteolysis-TArgeting Chimera (PROTAC) | P51617 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_0063 | Homo sapiens | 10.1021/acsmedchemlett.1c00244 | Degradation of IRAK1 in HEK293T cells after 24 h treatment | PROTAC-DB | null | null | Highly susceptible to infection by Zika virus (ZIKV).
CVCL_0045 ! HEK293
In situ; Fetal kidney;
NCBI_TaxID; 28285; Human adenovirus C serotype 5. NCBI_TaxID; 1891767; Simian virus 40 (SV40) (Note=tsA).
Transformed cell line | 25 | false | 850 | 9 |
COc1cc(N2CCC(OCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)N[C@@H](C)c3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)ccc1NC(=O)c1cccc(-c2ccn[nH]2)n1 | IRAK1 | MAGGPGPGEPAAPGAQHFLYEVPPWVMCRFYKVMDALEPADWCQFAALIVRDQTELRLCERSGQRTASVLWPWINRNARVADLVHILTHLQLLRARDIITAWHPPAPLPSPGTTAPRPSSIPAPAEAEAWSPRKLPSSASTFLSPAFPGSQTHSGPELGLVPSPASLWPPPPSPAPSSTKPGPESSVSLLQGARPFPFCWPLCEISRGTHNFSEELKIGEGGFGCVYRAVMRNTVYAVKRLKENADLEWTAVKQSFLTEVEQLSRFRHPNIVDFAGYCAQNGFYCLVYGFLPNGSLEDRLHCQTQACPPLSWPQRLDILL... | VHL | HEK293T | Dmax | % | 96 | null | null | null | null | 24 | null | null | null | PROteolysis-TArgeting Chimera (PROTAC) | P51617 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_0063 | Homo sapiens | 10.1021/acsmedchemlett.1c00244 | Degradation of IRAK1 in HEK293T cells after 24 h treatment | PROTAC-DB | null | null | Highly susceptible to infection by Zika virus (ZIKV).
CVCL_0045 ! HEK293
In situ; Fetal kidney;
NCBI_TaxID; 28285; Human adenovirus C serotype 5. NCBI_TaxID; 1891767; Simian virus 40 (SV40) (Note=tsA).
Transformed cell line | 25 | false | 850 | 9 |
COc1cc(N2CCC(c3ccc(OCCCCN4CCN(c5ccc6c(c5)CN(C5CCC(=O)NC5=O)C6=O)CC4)cc3)CC2)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP | DC50 | nM | 13.2 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0395 | Homo sapiens | COMPOUNDS AND THEIR USE IN TREATING CANCER (patent) | LNCaP Androgen Receptor Imaging Assay
This cell-based imaging assay uses immuno-fluorescence to measure both cell number and endogenous nuclear AR staining in the prostate cancer cell line LNCaP (expressing AR-full length). The purpose of the assay is to identify compounds that regulate AR protein level according to th... | TPDdb | Fluorescence Imaging Assay | TPD-XZ9D8U | Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Instable (MSI).
Metastatic; Left supraclavicular lymph node;
Caucasian.
Space-flown cell line (cellonaut).
Cancer cell line | 16 | false | 366 | 29 |
COc1cc(N2CCC(c3ccc(OCCCCN4CCN(c5ccc6c(c5)CN(C5CCC(=O)NC5=O)C6=O)CC4)cc3)CC2)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP | Dmax | % | 68 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0395 | Homo sapiens | COMPOUNDS AND THEIR USE IN TREATING CANCER (patent) | LNCaP Androgen Receptor Imaging Assay
This cell-based imaging assay uses immuno-fluorescence to measure both cell number and endogenous nuclear AR staining in the prostate cancer cell line LNCaP (expressing AR-full length). The purpose of the assay is to identify compounds that regulate AR protein level according to th... | TPDdb | Fluorescence Imaging Assay | TPD-XZ9D8U | Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Instable (MSI).
Metastatic; Left supraclavicular lymph node;
Caucasian.
Space-flown cell line (cellonaut).
Cancer cell line | 16 | false | 366 | 29 |
COc1cc(N2CCN(C(=O)CCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1 | ALK | MGAIGLLWLLPLLLSTAAVGSGMGTGQRAGSPAAGPPLQPREPLSYSRLQRKSLAVDFVVPSLFRVYARDLLLPPSSSELKAGRPEARGSLALDCAPLLRLLGPAPGVSWTAGSPAPAEARTLSRVLKGGSVRKLRRAKQLVLELGEEAILEGCVGPPGEAAVGLLQFNLSELFSWWIRQGEGRLRIRLMPEKKASEVGREGRLSAAIRASQPRLLFQIFGTGHSSLESPTNMPSPSPDYFTWNLTWIMKDSFPFLSHRSRYGLECSFDFPCELEYSPPLHDLRNQSWSWRRIPSEEASQMDLLDGPGAERSKEMPRGSF... | VHL | SR | DC50 | nM | 25,025 | null | null | null | null | 16 | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9UM73 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_1711 | Homo sapiens | 10.1016/j.ejmech.2020.112190; https://pubmed.ncbi.nlm.nih.gov/32179332/ | Degradation of ALK in SR cells after 16 h treatment; EC50 of ligand is 2.7 ± 0.4nM (SF cells), 58.2 ± 20.7 nM (H2228 cells). | PROTAC-DB; PROTACpedia | null | null | African=0%; Native American=0%; East Asian, North=3.12%; East Asian, South=0%; South Asian=0%; European, North=62.78%; European, South=34.1%.
Gene fusion; HGNC; HGNC
A*02,03; B*37 A*02 A*02
Stable (MSS) (Sanger).
In situ; Pleural effusion;
Caucasian.
Cancer cell line | -1 | false | 851 | 0 |
COc1cc(N2CCN(C(=O)CCCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1 | ALK | MGAIGLLWLLPLLLSTAAVGSGMGTGQRAGSPAAGPPLQPREPLSYSRLQRKSLAVDFVVPSLFRVYARDLLLPPSSSELKAGRPEARGSLALDCAPLLRLLGPAPGVSWTAGSPAPAEARTLSRVLKGGSVRKLRRAKQLVLELGEEAILEGCVGPPGEAAVGLLQFNLSELFSWWIRQGEGRLRIRLMPEKKASEVGREGRLSAAIRASQPRLLFQIFGTGHSSLESPTNMPSPSPDYFTWNLTWIMKDSFPFLSHRSRYGLECSFDFPCELEYSPPLHDLRNQSWSWRRIPSEEASQMDLLDGPGAERSKEMPRGSF... | VHL | SR | DC50 | nM | 15 | null | null | null | null | 16 | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9UM73 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_1711 | Homo sapiens | 10.1016/j.ejmech.2020.112190; https://pubmed.ncbi.nlm.nih.gov/32179332/ | Degradation of ALK in SR cells after 16 h treatment; EC50 of ligand is 2.7 ± 0.4nM (SF cells), 58.2 ± 20.7 nM (H2228 cells). | PROTAC-DB; PROTACpedia | null | null | African=0%; Native American=0%; East Asian, North=3.12%; East Asian, South=0%; South Asian=0%; European, North=62.78%; European, South=34.1%.
Gene fusion; HGNC; HGNC
A*02,03; B*37 A*02 A*02
Stable (MSS) (Sanger).
In situ; Pleural effusion;
Caucasian.
Cancer cell line | -1 | false | 852 | 0 |
COc1cc(N2CCN(C(=O)CCCCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1 | ALK | MGAIGLLWLLPLLLSTAAVGSGMGTGQRAGSPAAGPPLQPREPLSYSRLQRKSLAVDFVVPSLFRVYARDLLLPPSSSELKAGRPEARGSLALDCAPLLRLLGPAPGVSWTAGSPAPAEARTLSRVLKGGSVRKLRRAKQLVLELGEEAILEGCVGPPGEAAVGLLQFNLSELFSWWIRQGEGRLRIRLMPEKKASEVGREGRLSAAIRASQPRLLFQIFGTGHSSLESPTNMPSPSPDYFTWNLTWIMKDSFPFLSHRSRYGLECSFDFPCELEYSPPLHDLRNQSWSWRRIPSEEASQMDLLDGPGAERSKEMPRGSF... | VHL | SR | DC50 | nM | 25,025 | null | null | null | null | 16 | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9UM73 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_1711 | Homo sapiens | 10.1016/j.ejmech.2020.112190; https://pubmed.ncbi.nlm.nih.gov/32179332/ | Degradation of ALK in SR cells after 16 h treatment; EC50 of ligand is 2.7 ± 0.4nM (SF cells), 58.2 ± 20.7 nM (H2228 cells). | PROTAC-DB; PROTACpedia | null | null | African=0%; Native American=0%; East Asian, North=3.12%; East Asian, South=0%; South Asian=0%; European, North=62.78%; European, South=34.1%.
Gene fusion; HGNC; HGNC
A*02,03; B*37 A*02 A*02
Stable (MSS) (Sanger).
In situ; Pleural effusion;
Caucasian.
Cancer cell line | -1 | false | 853 | 0 |
COc1cc(N2CCN(C(=O)CN3CCC(c4ccc(NC5CCC(=O)NC5=O)cc4)CC3)CC2)c2cc1Nc1ncc(Br)c(n1)Nc1ccc(cc1N(C)S(C)(=O)=O)OCCCCC2 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 60.3 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | MACROCYCLE FOR INHIBITING AND INDUCING EGFR DEGRADATION AND PREPARATION METHOD FOR AND USE OF MACROCYCLE (patent) | Test Example 2: Determination of Total EGFR Protein Degradation in BaF3/EGFR L858R-T790M-C797S Cells by Compounds of the Present Disclosure
2. Experimental Methods
2.1. Cell Plating (Day 1)
a. Observe the cells under a microscope.
b. Collect the cell suspension into a 15 mL centrifuge tube and centrifuge at 300 g for 4... | TPDdb | HTRF | TPD-QZRL3Y | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 854 | 0 |
COc1cc(N2CCN(C(=O)CN3CCC(c4ccc(NC5CCC(=O)NC5=O)cc4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2C(C)=O)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | HCC827 | DC50 | nM | 15.56 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2063 | Homo sapiens | COMPOUND FOR DEGRADING EGFR PROTEIN AND USE THEREOF (patent) | As shown in Table 4, for DC50, AA ≤ 10 nM; 10 nM < A ≤ 100 nM; 100 nM < B < 1000 nM; C ≥ 1000 nM; for Dmax, 70% ≤ A ≤ 100%; 50% ≤ B < 70%; C < 50%; NA indicates not tested.
EGFR PROTAC In-cell Western Blot Assay
1. Experimental Materials
HCC827 cell culture medium was purchased from Corning. The HCC827 cell line was p... | TPDdb | In-Cell Western | TPD-SBDLGP | African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%.
Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566).
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*11 A*11
Stable (MSS) (Sanger).
In situ; Lung;
Caucasia... | 23 | false | 692 | 242 |
COc1cc(N2CCN(C(=O)CN3CCC(c4ccc(NC5CCC(=O)NC5=O)cc4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2C(C)=O)n1 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | HCC827 | Dmax | % | 70.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P00533 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2063 | Homo sapiens | COMPOUND FOR DEGRADING EGFR PROTEIN AND USE THEREOF (patent) | As shown in Table 4, for DC50, AA ≤ 10 nM; 10 nM < A ≤ 100 nM; 100 nM < B < 1000 nM; C ≥ 1000 nM; for Dmax, 70% ≤ A ≤ 100%; 50% ≤ B < 70%; C < 50%; NA indicates not tested.
EGFR PROTAC In-cell Western Blot Assay
1. Experimental Materials
HCC827 cell culture medium was purchased from Corning. The HCC827 cell line was p... | TPDdb | In-Cell Western | TPD-SBDLGP | African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%.
Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566).
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*11 A*11
Stable (MSS) (Sanger).
In situ; Lung;
Caucasia... | 23 | false | 692 | 242 |
COc1cc(N2CCN(C(=O)CN3CCC(c4ccc5c(N6CCC(=O)NC6=O)nn(C)c5c4)C(F)(F)C3)CC2)c2cc1Nc1ncc(Br)c(n1)Nc1ccc(cc1N(C)S(C)(=O)=O)OCCCCC2 | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 64.3 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | MACROCYCLE FOR INHIBITING AND INDUCING EGFR DEGRADATION AND PREPARATION METHOD FOR AND USE OF MACROCYCLE (patent) | Test Example 2: Determination of Total EGFR Protein Degradation in BaF3/EGFR L858R-T790M-C797S Cells by Compounds of the Present Disclosure
2. Experimental Methods
2.1. Cell Plating (Day 1)
a. Observe the cells under a microscope.
b. Collect the cell suspension into a 15 mL centrifuge tube and centrifuge at 300 g for 4... | TPDdb | HTRF | TPD-0WT7WY | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 619 | 112 |
COc1cc(N2CCN(C(=O)CN3CCC(c4ccc5c(N6CCC(=O)NC6=O)nn(C)c5c4)C(F)(F)C3)CC2)c2cc1Nc1ncc(Br)c(n1)Nc1ccc(cc1N(C)S(C)(=O)=O)OCCCCOC2=O | EGFR | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE... | CRBN | Ba/F3 | DC50 | nM | 24.2 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q01279 | Q8C7D2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0161 | Mus musculus | MACROCYCLE FOR INHIBITING AND INDUCING EGFR DEGRADATION AND PREPARATION METHOD FOR AND USE OF MACROCYCLE (patent) | Test Example 2: Determination of Total EGFR Protein Degradation in BaF3/EGFR L858R-T790M-C797S Cells by Compounds of the Present Disclosure
2. Experimental Methods
2.1. Cell Plating (Day 1)
a. Observe the cells under a microscope.
b. Collect the cell suspension into a 15 mL centrifuge tube and centrifuge at 300 g for 4... | TPDdb | HTRF | TPD-E67QCO | Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse.
IL3 dependent.
C3H.
In situ; Bone marrow;
Pro-B cell; CL=CL_0000826.
Factor-dependent cell line | 23 | false | 855 | 112 |
COc1cc(N2CCN(C(=O)OCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)ccc1NC(=O)c1cccc(-c2ccn[nH]2)n1 | IRAK1 | MAGGPGPGEPAAPGAQHFLYEVPPWVMCRFYKVMDALEPADWCQFAALIVRDQTELRLCERSGQRTASVLWPWINRNARVADLVHILTHLQLLRARDIITAWHPPAPLPSPGTTAPRPSSIPAPAEAEAWSPRKLPSSASTFLSPAFPGSQTHSGPELGLVPSPASLWPPPPSPAPSSTKPGPESSVSLLQGARPFPFCWPLCEISRGTHNFSEELKIGEGGFGCVYRAVMRNTVYAVKRLKENADLEWTAVKQSFLTEVEQLSRFRHPNIVDFAGYCAQNGFYCLVYGFLPNGSLEDRLHCQTQACPPLSWPQRLDILL... | VHL | HEK293T | DC50 | nM | 16 | null | null | null | null | 24 | null | null | null | PROteolysis-TArgeting Chimera (PROTAC) | P51617 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_0063 | Homo sapiens | 10.1021/acsmedchemlett.1c00244 | Degradation of IRAK1 in HEK293T cells after 24 h treatment | PROTAC-DB | null | null | Highly susceptible to infection by Zika virus (ZIKV).
CVCL_0045 ! HEK293
In situ; Fetal kidney;
NCBI_TaxID; 28285; Human adenovirus C serotype 5. NCBI_TaxID; 1891767; Simian virus 40 (SV40) (Note=tsA).
Transformed cell line | 25 | false | 856 | 0 |
COc1cc(N2CCN(C(=O)OCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)ccc1NC(=O)c1cccc(-c2ccn[nH]2)n1 | IRAK1 | MAGGPGPGEPAAPGAQHFLYEVPPWVMCRFYKVMDALEPADWCQFAALIVRDQTELRLCERSGQRTASVLWPWINRNARVADLVHILTHLQLLRARDIITAWHPPAPLPSPGTTAPRPSSIPAPAEAEAWSPRKLPSSASTFLSPAFPGSQTHSGPELGLVPSPASLWPPPPSPAPSSTKPGPESSVSLLQGARPFPFCWPLCEISRGTHNFSEELKIGEGGFGCVYRAVMRNTVYAVKRLKENADLEWTAVKQSFLTEVEQLSRFRHPNIVDFAGYCAQNGFYCLVYGFLPNGSLEDRLHCQTQACPPLSWPQRLDILL... | VHL | HEK293T | Dmax | % | 97 | null | null | null | null | 24 | null | null | null | PROteolysis-TArgeting Chimera (PROTAC) | P51617 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_0063 | Homo sapiens | 10.1021/acsmedchemlett.1c00244 | Degradation of IRAK1 in HEK293T cells after 24 h treatment | PROTAC-DB | null | null | Highly susceptible to infection by Zika virus (ZIKV).
CVCL_0045 ! HEK293
In situ; Fetal kidney;
NCBI_TaxID; 28285; Human adenovirus C serotype 5. NCBI_TaxID; 1891767; Simian virus 40 (SV40) (Note=tsA).
Transformed cell line | 25 | false | 856 | 0 |
COc1cc(N2CCN(C(=O)OCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)N[C@@H](C)c3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)ccc1NC(=O)c1cccc(-c2ccn[nH]2)n1 | IRAK1 | MAGGPGPGEPAAPGAQHFLYEVPPWVMCRFYKVMDALEPADWCQFAALIVRDQTELRLCERSGQRTASVLWPWINRNARVADLVHILTHLQLLRARDIITAWHPPAPLPSPGTTAPRPSSIPAPAEAEAWSPRKLPSSASTFLSPAFPGSQTHSGPELGLVPSPASLWPPPPSPAPSSTKPGPESSVSLLQGARPFPFCWPLCEISRGTHNFSEELKIGEGGFGCVYRAVMRNTVYAVKRLKENADLEWTAVKQSFLTEVEQLSRFRHPNIVDFAGYCAQNGFYCLVYGFLPNGSLEDRLHCQTQACPPLSWPQRLDILL... | VHL | HEK293T | DC50 | nM | 9 | null | null | null | null | 24 | null | null | null | PROteolysis-TArgeting Chimera (PROTAC) | P51617 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_0063 | Homo sapiens | 10.1021/acsmedchemlett.1c00244 | Degradation of IRAK1 in HEK293T cells after 24 h treatment | PROTAC-DB | null | null | Highly susceptible to infection by Zika virus (ZIKV).
CVCL_0045 ! HEK293
In situ; Fetal kidney;
NCBI_TaxID; 28285; Human adenovirus C serotype 5. NCBI_TaxID; 1891767; Simian virus 40 (SV40) (Note=tsA).
Transformed cell line | 25 | false | 856 | 4 |
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