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
Cc1cccc(-c2cnc(Nc3cnn(C4CCN(CCNC(=O)COc5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)c3)c3nccn23)c1
IRAK3
MAGNCGARGALSAHTLLFDLPPALLGELCAVLDSCDGALGWRGLAERLSSSWLDVRHIEKYVDQGKSGTRELLWSWAQKNKTIGDLLQVLQEMGHRRAIHLITNYGAVLSPSEKSYQEGGFPNILFKETANVTVDNVLIPEHNEKGILLKSSISFQNIIEGTRNFHKDFLIGEGEIFEVYRVEIQNLTYAVKLFKQEKKMQCKKHWKRFLSELEVLLLFHHPNILELAAYFTETEKFCLIYPYMRNGTLFDRLQCVGDTAPLPWHIRIGILIGISKAIHYLHNVQPCSVICGSISSANILLDDQFQPKLTDFAMAHFRSH...
CRBN
HEK293T
Dmax
%
78
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q9Y616
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0063
Homo sapiens
SUBSTITUTED IMIDAZOPYRAZINE COMPOUNDS AS LIGAND DIRECTED DEGRADERS OF IRAK3 (patent)
IRAK3-ePL cellular dose response curve degradation assays were performed by the following protocol. Compounds to be tested were dispensed into a white 384-well tissue-culture treated plate using an acoustic liquid handler. Dilutions were prepared based on a 25 pL assay volume in duplicate 10 point 3 -fold serial diluti...
TPDdb
InCELL Hunter Test
TPD-JIJV4S
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
1,325
177
Cc1cccc(-c2cnc(Nc3cnn(C4CCN(CCNC(=O)COc5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)c3)c3nccn23)c1
IRAK3
MAGNCGARGALSAHTLLFDLPPALLGELCAVLDSCDGALGWRGLAERLSSSWLDVRHIEKYVDQGKSGTRELLWSWAQKNKTIGDLLQVLQEMGHRRAIHLITNYGAVLSPSEKSYQEGGFPNILFKETANVTVDNVLIPEHNEKGILLKSSISFQNIIEGTRNFHKDFLIGEGEIFEVYRVEIQNLTYAVKLFKQEKKMQCKKHWKRFLSELEVLLLFHHPNILELAAYFTETEKFCLIYPYMRNGTLFDRLQCVGDTAPLPWHIRIGILIGISKAIHYLHNVQPCSVICGSISSANILLDDQFQPKLTDFAMAHFRSH...
CRBN
null
DC50
nM
20
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q9Y616
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
null
Homo sapiens
SUBSTITUTED IMIDAZOPYRAZINE COMPOUNDS AS LIGAND DIRECTED DEGRADERS OF IRAK3 (patent)
Cells (~50k) were plated in Cisbio 96-well low volume white plates. Compounds were dissolved in DMSO and a 3-fold serial dilution was performed using a TECAN D300E. Cells were incubated with the compound overnight. Total-IRAK3 HTRF kit from Cisbio was used for degradation analysis. Cryptate and D2 antibodies were dilut...
TPDdb
HTRF
TPD-JIJV4S
null
25
false
1,325
177
Cc1cccc(N(CC(=O)OC(C)(C)C)C(=O)c2ccc(-c3nn4c(c3C(N)=O)Cc3ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)N(CC(=O)OC(C)(C)C)C8=O)cc7)CC6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
3.68
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-27TCG0
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
1,326
227
Cc1cccc(N(CC(=O)OCc2ccccc2)C(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)N(CC(=O)OCc9ccccc9)C8=O)cc7)CC6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
2,000
null
null
null
null
null
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-1BTTZP
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
1,327
0
Cc1cccc(N(COC(=O)C(C)(C)C)C(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)N(COC(=O)C(C)(C)C)C8=O)cc7)CC6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
2,000
null
null
null
null
null
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-AFZGWI
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
481
15
Cc1cccc(NC(=O)c2cc(F)c(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)NC8=O)cc7)CC6)CC5)cc3CC4)cc2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
11.55
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-TC6UBY
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
true
-1
-1
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(C(=O)C6CCN(c7ccc(N8CCC(=O)NC8=O)cc7)CC6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
2.18
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-1E53JD
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
1,328
15
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(C(=O)Cc6cccc(N7CCC(=O)NC7=O)c6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
30.06
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-G33PHC
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
true
-1
-1
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(C6CC(c7ccc(N8CCC(=O)NC8=O)cc7)C6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
1.7
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-SL9PU9
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
true
-1
-1
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(C6CC(c7ccc(N[C@@H]8CCC(=O)NC8=O)cc7)C6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
7.45
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-I9KTY1
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
1,329
15
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(C6CC(c7ccc(N[C@H]8CCC(=O)NC8=O)cc7)C6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
6.23
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-Z0G65I
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
1,329
15
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(C6CC(c7ccc([C@@H]8CCC(=O)NC8=O)cc7)C6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
1.35
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-F5AQKT
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
true
-1
-1
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(C6CC(c7ccc([C@H]8CCC(=O)NC8=O)cc7)C6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
1.78
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-IQJIY5
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
true
-1
-1
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(C6CN(C7CN(c8ccc(C9CCC(=O)NC9=O)cc8)C7)C6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
2.32
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-AZ96AL
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
1,330
15
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(C6CN(C7CN(c8ccc9c(c8)C(=O)N(C8CCC(=O)NC8=O)C9=O)C7)C6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
2.42
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-XT4S7I
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
1,331
15
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(C6CN(c7ccc(N8CCC(=O)NC8=O)cc7)C6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
4.85
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-SBJC3J
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
true
-1
-1
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7cc8c(cc7F)C(=O)N(C7CCC(=O)NC7=O)C8=O)CC6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
18.64
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-82L0V4
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
1,332
15
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7cc8c(cc7F)CN(C7CCC(=O)NC7=O)C8=O)CC6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
3.75
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-420W5X
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
1,333
15
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7ccc(CN8CCC(=O)NC8=O)cc7)CC6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
0.622
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-PQM8I7
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
1,334
15
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)N(CC(=O)OC(C)(C)C)C8=O)cc7)CC6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
2,000
null
null
null
null
null
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-92MVC8
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
481
15
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)N(CC(=O)OCc9ccccc9)C8=O)cc7)CC6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
2,000
null
null
null
null
null
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-25X57G
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
1,335
0
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)N(COC(=O)C(C)(C)C)C8=O)cc7)CC6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
6.27
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-7VRDJG
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
481
15
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)NC8=O)c(C)c7)CC6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
4.06
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-12FBZX
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
true
-1
-1
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)NC8=O)cc7)CC6)CC5)cc3CC4)c(Cl)c2)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
0.469
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-HKO21Q
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
481
15
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)NC8=O)cc7)CC6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
0.928
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-M0KVMJ
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
481
15
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)NC8=O)cc7)CC6)CC5)cc3CC4)cc2)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
0.284
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-VCSMGW
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
481
15
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)NC8=O)cc7)CC6)CC5)cc3CC4)cc2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
0.602
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-RPAIFS
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
481
15
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)NC8=O)cc7)CC6)CC5)cc3CC4)nc2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
47.24
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-W7JTC1
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
1,336
15
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7ccc8c(c7)CN(C7CCC(=O)NC7=O)C8=O)CC6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
4.31
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-Z6AZHG
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
1,337
15
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7cccc(CN8CCC(=O)NC8=O)c7)CC6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
2.56
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-FIWO8Y
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
1,338
15
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CN(c7ccc(N8CCC(=O)NC8=O)cc7)C6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
0.526
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-WD0TNT
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
true
-1
-1
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CCc6cc(F)c(C7CCC(=O)NC7=O)c(F)c6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
4.97
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-P5OJ6K
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
true
-1
-1
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CCc6cc(F)c(C7CCC(=O)NC7=O)c(F)c6)CC5)cc3CC4)nc2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
15.24
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-BH2BH9
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
true
-1
-1
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CCc6cc(F)c([C@H]7CCC(=O)NC7=O)c(F)c6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
1.09
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-SBD5EF
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
true
-1
-1
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(C[C@H]6CCN(c7ccc(N8CCC(=O)NC8=O)cc7)C6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
7.15
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-EYNJXB
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
1,339
15
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(Cc6ccc7c(c6)C(C)(C)C(=O)N7C6CCC(=O)NC6=O)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
2.01
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-9YW6W8
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
true
-1
-1
Cc1cccc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(Cc6ccc7c(c6)oc(=O)n7C6CCC(=O)NC6=O)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
1.47
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-Y6HVAL
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
true
-1
-1
Cc1cccc(NC(=O)c2cnc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)NC8=O)cc7)CC6)CC5)cc3CC4)cc2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
57.8
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-FW64P4
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
1,336
15
Cc1cccc(NC(=O)c2cnc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CCc6cc(F)c(C7CCC(=O)NC7=O)c(F)c6)CC5)cc3CC4)cc2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
10.64
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-8C66Y6
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
true
-1
-1
Cc1cccc(NC(=O)c2ncc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(C6CC(c7ccc([C@@H]8CCC(=O)NC8=O)cc7)C6)CC5)cc3CC4)cc2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
17.64
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-6PYZZL
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
true
-1
-1
Cc1cccc(NC(=O)c2ncc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(C6CC(c7ccc([C@H]8CCC(=O)NC8=O)cc7)C6)CC5)cc3CC4)cc2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
8.86
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-WIYGP6
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
true
-1
-1
Cc1cccc(NC(=O)c2ncc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)NC8=O)cc7)CC6)CC5)cc3CC4)cc2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
2.53
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-MF2GJ9
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
1,340
15
Cc1cccc(NC(=O)c2ncc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CCc6cc(F)c(C7CCC(=O)NC7=O)c(F)c6)CC5)cc3CC4)cc2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
2,000
null
null
null
null
null
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-4VNR4X
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
1,341
237
Cc1ccccc1-c1cc(N2CC3(CCc4cc(N5CCC6(CC5)CC(C(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)N[C@@H](C)c5ccc(-c7scnc7C)cc5)C(C)(C)C)C6)ccc43)C2)c(N)nn1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
HT-1080
DC50
nM
5.65
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0317
Homo sapiens
SUBSTITUTED TRICYCLIC DERIVATIVE, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent)
1. On the first day, cells were plated, 10,000 HT-1080 (ATCC-CCL-121) cells were added to each well of a 384-well plate (Corning-3764), and cultured overnight at 37°C and 5% CO? (volume fraction, the rest was air). 2. On the second day, the compound was dissolved in DMSO with an initial concentration of 10 mM. The comp...
TPDdb
null
TPD-PKDTLN
African=0.86%; Native American=0.35%; East Asian, North=1.36%; East Asian, South=0.29%; South Asian=0%; European, North=68.21%; European, South=28.94%. This cell line is considered by some researchers to represent a dedifferentiated chondrosarcoma due to the presence of an IDH1 mutation. Gene deletion; HGNC; HGNC Mutat...
9
false
1,342
0
Cc1ccccc1-c1cc(N2CC3(CCc4cc(N5CCC6(CC5)CC(C(=O)N[C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)N[C@@H](C)c5ccc(-c7scnc7C)cc5)C(C)(C)C)C6)ccc43)C2)c(N)nn1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
HT-1080
DC50
nM
20.62
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0317
Homo sapiens
SUBSTITUTED TRICYCLIC DERIVATIVE, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent)
1. On the first day, cells were plated, 10,000 HT-1080 (ATCC-CCL-121) cells were added to each well of a 384-well plate (Corning-3764), and cultured overnight at 37°C and 5% CO? (volume fraction, the rest was air). 2. On the second day, the compound was dissolved in DMSO with an initial concentration of 10 mM. The comp...
TPDdb
null
TPD-PKDTLN
African=0.86%; Native American=0.35%; East Asian, North=1.36%; East Asian, South=0.29%; South Asian=0%; European, North=68.21%; European, South=28.94%. This cell line is considered by some researchers to represent a dedifferentiated chondrosarcoma due to the presence of an IDH1 mutation. Gene deletion; HGNC; HGNC Mutat...
9
false
1,342
0
Cc1ccnc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)NC8=O)cc7)CC6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
9.26
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-60X0NB
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
1,343
15
Cc1ccnc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)NC8=O)cc7)CC6)CC5)cc3CC4)cc2)c1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
4.69
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-M2H8YC
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
481
15
Cc1ccsc1C(=O)n1nc(Nc2ccc(S(=O)(=O)NCCOCc3cn(CCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)nn3)cc2)nc1N
CDK2
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
CRBN
DoHH2
DC50
nM
4
null
null
null
null
48
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P24941
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1179
Homo sapiens
10.1038/s41589-021-00742-5
Degradation of CDK2 in Pfeiffer/DOHH2/K562 cells after 48 h treatment
PROTAC-DB
null
null
African=0.28%; Native American=1.29%; East Asian, North=0%; East Asian, South=0%; South Asian=1.29%; European, North=69.22%; European, South=27.92%. A TP53 mutation is indicated as being at p.Ala138Pro (c.412G>C) in PubMed=17363600 but has not been confirmed by CCLE and Cosmic-CLP. A*01 A*01 A*01 Stable (MSS) (Sanger)....
37
false
1,344
0
Cc1ccsc1C(=O)n1nc(Nc2ccc(S(=O)(=O)NCCOCc3cn(CCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)nn3)cc2)nc1N
CDK2
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
CRBN
HBL-1 [Human AIDS-related non-Hodgkin lymphoma]
DC50
nM
33
null
null
null
null
48
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P24941
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_M572
Homo sapiens
10.1038/s41589-021-00742-5
Degradation of CDK2 in Z138/HBL-1/Mino cells after 48 h treatment
PROTAC-DB
null
null
Mutation; HGNC; HGNC In situ; Peripheral blood; B-cell; CL=CL_0000236. NCBI_TaxID; 10376; Epstein-Barr virus (EBV). Cancer cell line
37
false
1,344
0
Cc1ccsc1C(=O)n1nc(Nc2ccc(S(=O)(=O)NCCOCc3cn(CCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)nn3)cc2)nc1N
CDK2
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
CRBN
Jurkat
DC50
nM
38
null
null
null
null
48
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P24941
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0065
Homo sapiens
10.1038/s41589-021-00742-5
Degradation of CDK2 in Jurkat/MOLT-4/U937 cells after 48 h treatment
PROTAC-DB
null
null
African=0.4%; Native American=0%; East Asian, North=0.13%; East Asian, South=1.21%; South Asian=1.08%; European, North=70.73%; European, South=26.45%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC M...
37
false
1,344
0
Cc1ccsc1C(=O)n1nc(Nc2ccc(S(=O)(=O)NCCOCc3cn(CCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)nn3)cc2)nc1N
CDK2
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
CRBN
K-562
DC50
nM
9
null
null
null
null
48
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P24941
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0004
Homo sapiens
10.1038/s41589-021-00742-5
Degradation of CDK2 in Pfeiffer/DOHH2/K562 cells after 48 h treatment
PROTAC-DB
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
37
false
1,344
0
Cc1ccsc1C(=O)n1nc(Nc2ccc(S(=O)(=O)NCCOCc3cn(CCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)nn3)cc2)nc1N
CDK2
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
CRBN
Kasumi-1
DC50
nM
61
null
null
null
null
48
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P24941
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0589
Homo sapiens
10.1038/s41589-021-00742-5
Degradation of CDK2 in Kasumi-1/NB4/MV-4-11 cells after 48 h treatment
PROTAC-DB
null
null
African=1.19%; Native American=0%; East Asian, North=74.84%; East Asian, South=22.29%; South Asian=0%; European, North=0%; European, South=1.67%. Has lost chromosome Y. Some chromosome Y fragments are integrated into other chromosomes. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HG...
37
false
1,344
0
Cc1ccsc1C(=O)n1nc(Nc2ccc(S(=O)(=O)NCCOCc3cn(CCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)nn3)cc2)nc1N
CDK2
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
CRBN
MDA-MB-231
DC50
nM
8
null
null
null
null
48
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P24941
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0062
Homo sapiens
10.1038/s41589-021-00742-5
Degradation of CDK2 in MM.1S/MDA-MB-231 cells after 48 h treatment
PROTAC-DB
null
null
African=1.95%; Native American=0%; East Asian, North=2.44%; East Asian, South=0%; South Asian=7.42%; European, North=28.16%; European, South=60.03%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02/28; B*07,08; C*w02,w06. A*02 A...
37
false
1,344
0
Cc1ccsc1C(=O)n1nc(Nc2ccc(S(=O)(=O)NCCOCc3cn(CCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)nn3)cc2)nc1N
CDK2
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
CRBN
MM1.S
DC50
nM
22
null
null
null
null
48
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P24941
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_8792
Homo sapiens
10.1038/s41589-021-00742-5
Degradation of CDK2 in MM.1S/MDA-MB-231 cells after 48 h treatment
PROTAC-DB
null
null
African=88.68%; Native American=0%; East Asian, North=4.01%; East Asian, South=0%; South Asian=0.43%; European, North=0%; European, South=6.87%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Produces IgA lambda (ATCC=CRL-2974). Sensitive to dexamethasone. A*23,24; B*18,42; C*12,17. A*23 Instable (MSI-low) (Sanger). CVCL_58...
37
false
1,344
0
Cc1ccsc1C(=O)n1nc(Nc2ccc(S(=O)(=O)NCCOCc3cn(CCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)nn3)cc2)nc1N
CDK2
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
CRBN
MOLT-4
DC50
nM
53
null
null
null
null
48
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P24941
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0013
Homo sapiens
10.1038/s41589-021-00742-5
Degradation of CDK2 in Jurkat/MOLT-4/U937 cells after 48 h treatment
PROTAC-DB
null
null
African=0.38%; Native American=0%; East Asian, North=1.74%; East Asian, South=0%; South Asian=0.94%; European, North=68.08%; European, South=28.87%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*01 A*01 A*01 Instable (MSI-high). In situ; ...
37
false
1,344
0
Cc1ccsc1C(=O)n1nc(Nc2ccc(S(=O)(=O)NCCOCc3cn(CCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)nn3)cc2)nc1N
CDK2
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
CRBN
MV4-11
DC50
nM
1
null
null
null
null
48
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P24941
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0064
Homo sapiens
10.1038/s41589-021-00742-5
Degradation of CDK2 in Kasumi-1/NB4/MV-4-11 cells after 48 h treatment
PROTAC-DB
null
null
African=0.59%; Native American=0%; East Asian, North=0.34%; East Asian, South=0%; South Asian=2.57%; European, North=67.58%; European, South=28.91%. 48,XY,t(4;11)(q21;q23),+8,+19 (ATCC=CRL-9591). Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC CSF2 and IL3 dependent. A*03 A*03 Stable (MSS) (Sanger). In situ; Peripheral bl...
37
false
1,344
0
Cc1ccsc1C(=O)n1nc(Nc2ccc(S(=O)(=O)NCCOCc3cn(CCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)nn3)cc2)nc1N
CDK2
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
CRBN
Mino
DC50
nM
29
null
null
null
null
48
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P24941
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1872
Homo sapiens
10.1038/s41589-021-00742-5
Degradation of CDK2 in Z138/HBL-1/Mino cells after 48 h treatment
PROTAC-DB
null
null
African=0.85%; Native American=0%; East Asian, North=1.5%; East Asian, South=0%; South Asian=6.1%; European, North=39.56%; European, South=51.98%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11,68; B*35,39; C*04,12. A*11 In situ; Peripheral blood; Caucasian. Cancer cell line
37
false
1,344
0
Cc1ccsc1C(=O)n1nc(Nc2ccc(S(=O)(=O)NCCOCc3cn(CCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)nn3)cc2)nc1N
CDK2
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
CRBN
NB4
DC50
nM
12
null
null
null
null
48
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P24941
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0005
Homo sapiens
10.1038/s41589-021-00742-5
Degradation of CDK2 in Kasumi-1/NB4/MV-4-11 cells after 48 h treatment
PROTAC-DB
null
null
African=3.99%; Native American=0%; East Asian, North=4.75%; East Asian, South=0%; South Asian=0%; European, North=49.28%; European, South=41.98%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11 A*11 Stable (MSS) (Sanger). In situ; Bone marrow; Caucasian. Patented cell line. Cancer cell line
37
false
1,344
0
Cc1ccsc1C(=O)n1nc(Nc2ccc(S(=O)(=O)NCCOCc3cn(CCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)nn3)cc2)nc1N
CDK2
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
CRBN
OCI-AML-2
DC50
nM
56
null
null
null
null
48
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P24941
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1619
Homo sapiens
10.1038/s41589-021-00742-5
Degradation of CDK2 in OCI-AML2/OCI-AML3/Ramos cells after 48 h treatment
PROTAC-DB
null
null
African=1.2%; Native American=0%; East Asian, North=1.51%; East Asian, South=0%; South Asian=2.28%; European, North=62.12%; European, South=32.89%. Gene fusion; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ; Peripheral blood; Caucasian. Cancer cell line
37
false
1,344
0
Cc1ccsc1C(=O)n1nc(Nc2ccc(S(=O)(=O)NCCOCc3cn(CCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)nn3)cc2)nc1N
CDK2
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
CRBN
OCI-AML-3
DC50
nM
13
null
null
null
null
48
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P24941
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1844
Homo sapiens
10.1038/s41589-021-00742-5
Degradation of CDK2 in OCI-AML2/OCI-AML3/Ramos cells after 48 h treatment
PROTAC-DB
null
null
African=0%; Native American=1.44%; East Asian, North=2.86%; East Asian, South=0%; South Asian=0.99%; European, North=55.94%; European, South=38.78%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 A*02 Stable (MSS) (Sanger). In situ; Peripheral blood; Caucasian. Cancer cell line
37
false
1,344
0
Cc1ccsc1C(=O)n1nc(Nc2ccc(S(=O)(=O)NCCOCc3cn(CCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)nn3)cc2)nc1N
CDK2
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
CRBN
Pfeiffer
DC50
nM
160
null
null
null
null
48
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P24941
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_3326
Homo sapiens
10.1038/s41589-021-00742-5
Degradation of CDK2 in Pfeiffer/DOHH2/K562 cells after 48 h treatment
PROTAC-DB
null
null
African=1.72%; Native American=0.65%; East Asian, North=0%; East Asian, South=2.24%; South Asian=9.82%; European, North=22.11%; European, South=63.47%. Mutation; HGNC; HGNC Produces IgG kappa (ATCC=CRL-2632). A*01 In situ; Pleural effusion; Caucasian. B-cell; CL=CL_0000236. Cancer cell line
37
false
1,344
0
Cc1ccsc1C(=O)n1nc(Nc2ccc(S(=O)(=O)NCCOCc3cn(CCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)nn3)cc2)nc1N
CDK2
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
CRBN
Ramos
DC50
nM
18
null
null
null
null
48
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P24941
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0597
Homo sapiens
10.1038/s41589-021-00742-5
Degradation of CDK2 in OCI-AML2/OCI-AML3/Ramos cells after 48 h treatment
PROTAC-DB
null
null
EBV-negative. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*03 A*03 A*03 A*03 Stable (MSS). In situ; Ascites; Caucasian. B-cell; CL=CL_0000236. Cancer cell line
37
false
1,344
0
Cc1ccsc1C(=O)n1nc(Nc2ccc(S(=O)(=O)NCCOCc3cn(CCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)nn3)cc2)nc1N
CDK2
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
CRBN
U-937
DC50
nM
11
null
null
null
null
48
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P24941
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0007
Homo sapiens
10.1038/s41589-021-00742-5
Degradation of CDK2 in Jurkat/MOLT-4/U937 cells after 48 h treatment
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=2.39%; East Asian, South=0%; South Asian=0%; European, North=71.54%; European, South=26.06%. Has lost chromosome Y. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Can be induced to differentiate into macrophag...
37
false
1,344
0
Cc1ccsc1C(=O)n1nc(Nc2ccc(S(=O)(=O)NCCOCc3cn(CCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)nn3)cc2)nc1N
CDK2
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
CRBN
Z-138
DC50
nM
43
null
null
null
null
48
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P24941
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_B077
Homo sapiens
10.1038/s41589-021-00742-5
Degradation of CDK2 in Z138/HBL-1/Mino cells after 48 h treatment
PROTAC-DB
null
null
Mutation; HGNC; HGNC A*01 A*01,23; B*08,44; C*02,07. In situ; Bone marrow; Caucasian. Cancer cell line
37
false
1,344
0
Cc1cnc(Nc2ccc(OCCCOCCCCOCCCOCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)cc2)nc1NCCCN(C)C(=O)C1CCC1
TBK1
MQSTSNHLWLLSDILGQGATANVFRGRHKKTGDLFAIKVFNNISFLRPVDVQMREFEVLKKLNHKNIVKLFAIEEETTTRHKVLIMEFCPCGSLYTVLEEPSNAYGLPESEFLIVLRDVVGGMNHLRENGIVHRDIKPGNIMRVIGEDGQSVYKLTDFGAARELEDDEQFVSLYGTEEYLHPDMYERAVLRKDHQKKYGATVDLWSIGVTFYHAATGSLPFRPFEGPRRNKEVMYKIITGKPSGAISGVQKAENGPIDWSGDMPVSCSLSRGLQVLLTPVLANILEADQEKCWGFDQFFAETSDILHRMVIHVFSLQQMT...
VHL
Panc 02.13
DC50
nM
92
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q9UHD2
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1634
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/28692295/
null
PROTACpedia
null
null
African=2.03%; Native American=0.98%; East Asian, North=0.28%; East Asian, South=0%; South Asian=0.04%; European, North=63.98%; European, South=32.69%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC In situ; Pancreas; Caucasian. Cancer cell line
-1
false
95
0
Cc1cnc(Nc2ccc(OCCCOCCCCOCCCOCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)cc2)nc1NCCCN(C)C(=O)C1CCC1
TBK1
MQSTSNHLWLLSDILGQGATANVFRGRHKKTGDLFAIKVFNNISFLRPVDVQMREFEVLKKLNHKNIVKLFAIEEETTTRHKVLIMEFCPCGSLYTVLEEPSNAYGLPESEFLIVLRDVVGGMNHLRENGIVHRDIKPGNIMRVIGEDGQSVYKLTDFGAARELEDDEQFVSLYGTEEYLHPDMYERAVLRKDHQKKYGATVDLWSIGVTFYHAATGSLPFRPFEGPRRNKEVMYKIITGKPSGAISGVQKAENGPIDWSGDMPVSCSLSRGLQVLLTPVLANILEADQEKCWGFDQFFAETSDILHRMVIHVFSLQQMT...
VHL
Panc 02.13
Dmax
%
89
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q9UHD2
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1634
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/28692295/
null
PROTACpedia
null
null
African=2.03%; Native American=0.98%; East Asian, North=0.28%; East Asian, South=0%; South Asian=0.04%; European, North=63.98%; European, South=32.69%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC In situ; Pancreas; Caucasian. Cancer cell line
-1
false
95
0
Cc1cncc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)NC8=O)cc7)CC6)CC5)cc3CC4)c(F)c2C)n1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
4.89
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-M0VNUB
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
1,345
15
Cc1csc(Nc2ccc(CNC(=O)[C@@H]3C[C@@H](O)CN3C(=O)[C@@H](NC(=O)C3CCN(c4ccc5c(c4)CCC54CCN(c5cc(-c6ccccc6O)nnc5N)CC4)CC3)C(C)(C)C)cn2)n1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
HT-1080
DC50
nM
2.98
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0317
Homo sapiens
SUBSTITUTED TRICYCLIC DERIVATIVE, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent)
1. On the first day, cells were plated, 10,000 HT-1080 (ATCC-CCL-121) cells were added to each well of a 384-well plate (Corning-3764), and cultured overnight at 37°C and 5% CO? (volume fraction, the rest was air). 2. On the second day, the compound was dissolved in DMSO with an initial concentration of 10 mM. The comp...
TPDdb
null
TPD-60M6Z0
African=0.86%; Native American=0.35%; East Asian, North=1.36%; East Asian, South=0.29%; South Asian=0%; European, North=68.21%; European, South=28.94%. This cell line is considered by some researchers to represent a dedifferentiated chondrosarcoma due to the presence of an IDH1 mutation. Gene deletion; HGNC; HGNC Mutat...
9
true
-1
-1
Cc1csc(Nc2ccc(CNC(=O)[C@@H]3C[C@@H](O)CN3C(=O)[C@@H](NC(=O)C3CCN(c4ccc5c(c4)CCC54CCN(c5cc(-c6ccccc6O)nnc5N)CC4)CC3)C(C)(C)C)cn2)n1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
HT-1080
DC50
nM
86.58
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0317
Homo sapiens
SUBSTITUTED TRICYCLIC DERIVATIVE, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent)
1. On the first day, cells were plated, 10,000 HT-1080 (ATCC-CCL-121) cells were added to each well of a 384-well plate (Corning-3764), and cultured overnight at 37°C and 5% CO? (volume fraction, the rest was air). 2. On the second day, the compound was dissolved in DMSO with an initial concentration of 10 mM. The comp...
TPDdb
null
TPD-60M6Z0
African=0.86%; Native American=0.35%; East Asian, North=1.36%; East Asian, South=0.29%; South Asian=0%; European, North=68.21%; European, South=28.94%. This cell line is considered by some researchers to represent a dedifferentiated chondrosarcoma due to the presence of an IDH1 mutation. Gene deletion; HGNC; HGNC Mutat...
9
true
-1
-1
Cc1n[nH]c(C)c1-c1ccc([C@H](C)NC(=O)C2C[C@@H](O)CN2C(=O)C(c2cc(OCCN3CCC(O[C@H]4C[C@H](Oc5ccc6c(c5)C5(CC6)CCN(c6cc(-c7ccccc7O)nnc6N)CC5)C4)CC3)no2)C(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
HT-1080
DC50
nM
19.21
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0317
Homo sapiens
SUBSTITUTED TRICYCLIC DERIVATIVE, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent)
1. On the first day, cells were plated, 10,000 HT-1080 (ATCC-CCL-121) cells were added to each well of a 384-well plate (Corning-3764), and cultured overnight at 37°C and 5% CO? (volume fraction, the rest was air). 2. On the second day, the compound was dissolved in DMSO with an initial concentration of 10 mM. The comp...
TPDdb
null
TPD-DKGORZ
African=0.86%; Native American=0.35%; East Asian, North=1.36%; East Asian, South=0.29%; South Asian=0%; European, North=68.21%; European, South=28.94%. This cell line is considered by some researchers to represent a dedifferentiated chondrosarcoma due to the presence of an IDH1 mutation. Gene deletion; HGNC; HGNC Mutat...
9
false
1,346
0
Cc1n[nH]c(C)c1-c1ccc([C@H](C)NC(=O)C2C[C@@H](O)CN2C(=O)C(c2cc(OCCN3CCC(O[C@H]4C[C@H](Oc5ccc6c(c5)C5(CC6)CCN(c6cc(-c7ccccc7O)nnc6N)CC5)C4)CC3)no2)C(C)C)cc1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
HT-1080
DC50
nM
283.86
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0317
Homo sapiens
SUBSTITUTED TRICYCLIC DERIVATIVE, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent)
1. On the first day, cells were plated, 10,000 HT-1080 (ATCC-CCL-121) cells were added to each well of a 384-well plate (Corning-3764), and cultured overnight at 37°C and 5% CO? (volume fraction, the rest was air). 2. On the second day, the compound was dissolved in DMSO with an initial concentration of 10 mM. The comp...
TPDdb
null
TPD-DKGORZ
African=0.86%; Native American=0.35%; East Asian, North=1.36%; East Asian, South=0.29%; South Asian=0%; European, North=68.21%; European, South=28.94%. This cell line is considered by some researchers to represent a dedifferentiated chondrosarcoma due to the presence of an IDH1 mutation. Gene deletion; HGNC; HGNC Mutat...
9
false
1,346
0
Cc1n[nH]c(Nc2ncnc3cc(OCCCN4CCN(C(=O)c5cnc(N6CCN(C[C@H]7CN[C@H](C)CN7CC(=O)N7CC(C)(C)c8c7cc(Cc7ccc(F)cc7)c(=O)n8C)[C@H](C)C6)nc5)CC4)c(S(=O)(=O)C(C)(C)C)cc23)c1C
RIPK2
MNGEAICSALPTIPYHKLADLRYLSRGASGTVSSARHADWRVQVAVKHLHIHTPLLDSERKDVLREAEILHKARFSYILPILGICNEPEFLGIVTEYMPNGSLNELLHRKTEYPDVAWPLRFRILHEIALGVNYLHNMTPPLLHHDLKTQNILLDNEFHVKIADFGLSKWRMMSLSQSRSSKSAPEGGTIIYMPPENYEPGQKSRASIKHDIYSYAVITWEVLSRKQPFEDVTNPLQIMYSVSQGHRPVINEESLPYDIPHRARMISLIESGWAQNPDERPSFLKCLIELEPVLRTFEEITFLEAVIQLKKTKLQSVSSA...
IAP
THP-1
DC50
nM
0.05
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O43353
P98170
MTFNSFEGSKTCVPADINKEEEFVEEFNRLKTFANFPSGSPVSASTLARAGFLYTGEGDTVRCFSCHAAVDRWQYGDSAVGRHRKVSPNCRFINGFYLENSATQSTNSGIQNGQYKVENYLGSRDHFALDRPSETHADYLLRTGQVVDISDTIYPRNPAMYSEEARLKSFQNWPDYAHLTPRELASAGLYYTGIGDQVQCFCCGGKLKNWEPCDRAWSEHRRHFPNCFFVLGRNLNIRSESDAVSSDRNFPNSTNLPRNPSMADYEARIFTFGTWIYSVNKEQLARAGFYALGEGDKVKCFHCGGGLTDWKPSEDPWEQH...
CVCL_0006
Homo sapiens
10.1021/acs.jmedchem.1c01118
Degradation of RIPK2 in THP1 cells after 18 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%. Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test. Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19). NRAS muta...
-1
false
1,347
0
Cc1n[nH]c(Nc2ncnc3cc(OCCCN4CCN(C(=O)c5cnc(N6CCN(C[C@H]7CN[C@H](C)CN7CC(=O)N7CC(C)(C)c8ncc(Cc9ccc(F)cc9)cc87)[C@H](C)C6)nc5)CC4)c(S(=O)(=O)C(C)(C)C)cc23)c1C
RIPK2
MNGEAICSALPTIPYHKLADLRYLSRGASGTVSSARHADWRVQVAVKHLHIHTPLLDSERKDVLREAEILHKARFSYILPILGICNEPEFLGIVTEYMPNGSLNELLHRKTEYPDVAWPLRFRILHEIALGVNYLHNMTPPLLHHDLKTQNILLDNEFHVKIADFGLSKWRMMSLSQSRSSKSAPEGGTIIYMPPENYEPGQKSRASIKHDIYSYAVITWEVLSRKQPFEDVTNPLQIMYSVSQGHRPVINEESLPYDIPHRARMISLIESGWAQNPDERPSFLKCLIELEPVLRTFEEITFLEAVIQLKKTKLQSVSSA...
IAP
THP-1
DC50
nM
0.16
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O43353
P98170
MTFNSFEGSKTCVPADINKEEEFVEEFNRLKTFANFPSGSPVSASTLARAGFLYTGEGDTVRCFSCHAAVDRWQYGDSAVGRHRKVSPNCRFINGFYLENSATQSTNSGIQNGQYKVENYLGSRDHFALDRPSETHADYLLRTGQVVDISDTIYPRNPAMYSEEARLKSFQNWPDYAHLTPRELASAGLYYTGIGDQVQCFCCGGKLKNWEPCDRAWSEHRRHFPNCFFVLGRNLNIRSESDAVSSDRNFPNSTNLPRNPSMADYEARIFTFGTWIYSVNKEQLARAGFYALGEGDKVKCFHCGGGLTDWKPSEDPWEQH...
CVCL_0006
Homo sapiens
10.1021/acs.jmedchem.1c01118
Degradation of RIPK2 in THP1 cells after 18 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.3%; East Asian, North=77.63%; East Asian, South=20.4%; South Asian=1.67%; European, North=0%; European, South=0%. Used in the human Cell Line Activation Test (h-CLAT), an in vitro skin sensitization test. Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19). NRAS muta...
-1
false
1,348
0
Cc1nc(CCC(=O)NCCCCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1-c1cnc(NCc2c(F)ccc3c2CCO3)n2cnnc12
EED
MSEREVSTAPAGTDMPAAKKQKLSSDENSNPDLSGDENDDAVSIESGTNTERPDTPTNTPNAPGRKSWGKGKWKSKKCKYSFKCVNSLKEDHNQPLFGVQFNWHSKEGDPLVFATVGSNRVTLYECHSQGEIRLLQSYVDADADENFYTCAWTYDSNTSHPLLAVAGSRGIIRIINPITMQCIKHYVGHGNAINELKFHPRDPNLLLSVSKDHALRLWNIQTDTLVAIFGGVEGHRDEVLSADYDLLGEKIMSCGMDHSLKLWRINSKRMMNAIKESYDYNPNKTNRPFISQKIHFPDFSTRDIHRNYVDCVRWLGDLIL...
VHL
Karpas-422
Dmax
%
100
null
null
null
null
24
~
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
O75530
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1325
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31786184/
null
PROTACpedia
null
null
African=0%; Native American=0.49%; East Asian, North=0%; East Asian, South=0%; South Asian=0.34%; European, North=71.53%; European, South=27.64%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Quite popular cell line because of its resistance to chemotherapy. B*56/73,56/39; DQA1*03 A*02 Stable (MSS) (Sanger). In situ; Pleur...
11
false
1,349
1
Cc1nc(CCC(=O)NCCOc2ccc(OCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)cc2)ccc1-c1cnc(NCc2c(F)ccc3c2CCO3)n2cnnc12
EED
MSEREVSTAPAGTDMPAAKKQKLSSDENSNPDLSGDENDDAVSIESGTNTERPDTPTNTPNAPGRKSWGKGKWKSKKCKYSFKCVNSLKEDHNQPLFGVQFNWHSKEGDPLVFATVGSNRVTLYECHSQGEIRLLQSYVDADADENFYTCAWTYDSNTSHPLLAVAGSRGIIRIINPITMQCIKHYVGHGNAINELKFHPRDPNLLLSVSKDHALRLWNIQTDTLVAIFGGVEGHRDEVLSADYDLLGEKIMSCGMDHSLKLWRINSKRMMNAIKESYDYNPNKTNRPFISQKIHFPDFSTRDIHRNYVDCVRWLGDLIL...
VHL
Karpas-422
Dmax
%
100
null
null
null
null
24
~
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
O75530
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1325
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31786184/
null
PROTACpedia
null
null
African=0%; Native American=0.49%; East Asian, North=0%; East Asian, South=0%; South Asian=0.34%; European, North=71.53%; European, South=27.64%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Quite popular cell line because of its resistance to chemotherapy. B*56/73,56/39; DQA1*03 A*02 Stable (MSS) (Sanger). In situ; Pleur...
11
false
1,350
0
Cc1nc(N2CCC(c3ccc(OCCCCN4CCN(c5ccc6c(c5)CN(C5CCC(=O)NC5=O)C6=O)CC4)cc3)CC2)ccc1C#N
AR
MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL...
CRBN
LNCaP
DC50
nM
30.9
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-MDNC7S
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
1,351
29
Cc1nc(N2CCC(c3ccc(OCCCCN4CCN(c5ccc6c(c5)CN(C5CCC(=O)NC5=O)C6=O)CC4)cc3)CC2)ccc1C#N
AR
MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL...
CRBN
LNCaP
Dmax
%
64
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-MDNC7S
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
1,351
29
Cc1nc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)NC8=O)cc7)CC6)CC5)cc3CC4)c(F)c2C)ccc1Cl
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
2.16
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-7J392T
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
481
15
Cc1nc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)NC8=O)cc7)CC6)CC5)cc3CC4)c(F)c2C)ccc1F
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
3.67
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-4YOC6F
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
481
15
Cc1nc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CN(c7ccc(N8CCC(=O)NC8=O)cc7)C6)CC5)cc3CC4)c(F)c2C)ccc1Cl
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
7.39
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-TTSDSU
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
true
-1
-1
Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1
ABL1
MLEICLKLVGCKSKKGLSSSSSCYLEEALQRPVASDFEPQGLSEAARWNSKENLLAGPSENDPNLFVALYDFVASGDNTLSITKGEKLRVLGYNHNGEWCEAQTKNGQGWVPSNYITPVNSLEKHSWYHGPVSRNAAEYLLSSGINGSFLVRESESSPGQRSISLRYEGRVYHYRINTASDGKLYVSSESRFNTLAELVHHHSTVADGLITTLHYPAPKRNKPTVYGVSPNYDKWEMERTDITMKHKLGGGQYGEVYEGVWKKYSLTVAVKTLKEDTMEVEEFLKEAAVMKEIKHPNLVQLLGVCTREPPFYIITEFMTY...
VHL
K-562
DC50
nM
611
null
null
null
null
24
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00519
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0004
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31539241/
null
PROTACpedia
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
27
false
1,352
2
Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1
BCR-ABL
MVDPVGFAEAWKAQFPDSEPPRMELRSVGDIEQELERCKASIRRLEQEVNQERFRMIYLQTLLAKEKKSYDRQRWGFRRAAQAPDGASEPRASASRPQPAPADGADPPPAEEPEARPDGEGSPGKARPGTARRPGAAASGERDDRGPPASVAALRSNFERIRKGHGQPGADAEKPFYVNVEFHHERGLVKVNDKEVSDRISSLGSQAMQMERKKSQHGAGSSVGDASRPPYRGRSSESSCGVDGDYEDAELNPRFLKDNLIDANGGSRPPWPPLEYQPYQSIYVGGMMEGEGKGPLLRSQSTSEQEKRLTWPRRSYSPRS...
VHL
K-562
DC50
nM
611.4
null
null
null
null
16
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
A9UF07
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0004
Homo sapiens
10.1021/acs.jmedchem.9b01264
Degradation of BCR-ABL in K562 cells after 16 h treatment
PROTAC-DB
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
27
false
1,352
2
Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1
ABL1
MLEICLKLVGCKSKKGLSSSSSCYLEEALQRPVASDFEPQGLSEAARWNSKENLLAGPSENDPNLFVALYDFVASGDNTLSITKGEKLRVLGYNHNGEWCEAQTKNGQGWVPSNYITPVNSLEKHSWYHGPVSRNAAEYLLSSGINGSFLVRESESSPGQRSISLRYEGRVYHYRINTASDGKLYVSSESRFNTLAELVHHHSTVADGLITTLHYPAPKRNKPTVYGVSPNYDKWEMERTDITMKHKLGGGQYGEVYEGVWKKYSLTVAVKTLKEDTMEVEEFLKEAAVMKEIKHPNLVQLLGVCTREPPFYIITEFMTY...
VHL
K-562
DC50
nM
40.2
null
null
null
null
24
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00519
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0004
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31539241/
null
PROTACpedia
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
27
false
1,353
2
Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1
BCR-ABL
MVDPVGFAEAWKAQFPDSEPPRMELRSVGDIEQELERCKASIRRLEQEVNQERFRMIYLQTLLAKEKKSYDRQRWGFRRAAQAPDGASEPRASASRPQPAPADGADPPPAEEPEARPDGEGSPGKARPGTARRPGAAASGERDDRGPPASVAALRSNFERIRKGHGQPGADAEKPFYVNVEFHHERGLVKVNDKEVSDRISSLGSQAMQMERKKSQHGAGSSVGDASRPPYRGRSSESSCGVDGDYEDAELNPRFLKDNLIDANGGSRPPWPPLEYQPYQSIYVGGMMEGEGKGPLLRSQSTSEQEKRLTWPRRSYSPRS...
VHL
K-562
DC50
nM
40.2
null
null
null
null
16
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
A9UF07
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0004
Homo sapiens
10.1021/acs.jmedchem.9b01264
Degradation of BCR-ABL in K562 cells after 16 h treatment
PROTAC-DB
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
27
false
1,353
2
Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCCC(=O)Nc3cccc4c3CN(C3CCC(=O)NC3=O)C4=O)CC2)n1
BCR-ABL
MVDPVGFAEAWKAQFPDSEPPRMELRSVGDIEQELERCKASIRRLEQEVNQERFRMIYLQTLLAKEKKSYDRQRWGFRRAAQAPDGASEPRASASRPQPAPADGADPPPAEEPEARPDGEGSPGKARPGTARRPGAAASGERDDRGPPASVAALRSNFERIRKGHGQPGADAEKPFYVNVEFHHERGLVKVNDKEVSDRISSLGSQAMQMERKKSQHGAGSSVGDASRPPYRGRSSESSCGVDGDYEDAELNPRFLKDNLIDANGGSRPPWPPLEYQPYQSIYVGGMMEGEGKGPLLRSQSTSEQEKRLTWPRRSYSPRS...
CRBN
K-562
DC50
nM
125
null
null
null
null
16
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
A9UF07
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0004
Homo sapiens
10.1016/j.ejmech.2021.113645
Degradation of BCR-ABL in K562 cells after 16 h treatment
PROTAC-DB
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
27
false
1,354
77
Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1
ABL1
MLEICLKLVGCKSKKGLSSSSSCYLEEALQRPVASDFEPQGLSEAARWNSKENLLAGPSENDPNLFVALYDFVASGDNTLSITKGEKLRVLGYNHNGEWCEAQTKNGQGWVPSNYITPVNSLEKHSWYHGPVSRNAAEYLLSSGINGSFLVRESESSPGQRSISLRYEGRVYHYRINTASDGKLYVSSESRFNTLAELVHHHSTVADGLITTLHYPAPKRNKPTVYGVSPNYDKWEMERTDITMKHKLGGGQYGEVYEGVWKKYSLTVAVKTLKEDTMEVEEFLKEAAVMKEIKHPNLVQLLGVCTREPPFYIITEFMTY...
VHL
K-562
DC50
nM
34.7
null
null
null
null
24
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00519
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0004
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31539241/
null
PROTACpedia
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
27
false
1,355
0
Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1
BCR-ABL
MVDPVGFAEAWKAQFPDSEPPRMELRSVGDIEQELERCKASIRRLEQEVNQERFRMIYLQTLLAKEKKSYDRQRWGFRRAAQAPDGASEPRASASRPQPAPADGADPPPAEEPEARPDGEGSPGKARPGTARRPGAAASGERDDRGPPASVAALRSNFERIRKGHGQPGADAEKPFYVNVEFHHERGLVKVNDKEVSDRISSLGSQAMQMERKKSQHGAGSSVGDASRPPYRGRSSESSCGVDGDYEDAELNPRFLKDNLIDANGGSRPPWPPLEYQPYQSIYVGGMMEGEGKGPLLRSQSTSEQEKRLTWPRRSYSPRS...
VHL
K-562
DC50
nM
34.7
null
null
null
null
16
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
A9UF07
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0004
Homo sapiens
10.1021/acs.jmedchem.9b01264
Degradation of BCR-ABL in K562 cells after 16 h treatment
PROTAC-DB
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
27
false
1,355
0
Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1
ABL1
MLEICLKLVGCKSKKGLSSSSSCYLEEALQRPVASDFEPQGLSEAARWNSKENLLAGPSENDPNLFVALYDFVASGDNTLSITKGEKLRVLGYNHNGEWCEAQTKNGQGWVPSNYITPVNSLEKHSWYHGPVSRNAAEYLLSSGINGSFLVRESESSPGQRSISLRYEGRVYHYRINTASDGKLYVSSESRFNTLAELVHHHSTVADGLITTLHYPAPKRNKPTVYGVSPNYDKWEMERTDITMKHKLGGGQYGEVYEGVWKKYSLTVAVKTLKEDTMEVEEFLKEAAVMKEIKHPNLVQLLGVCTREPPFYIITEFMTY...
VHL
K-562
DC50
nM
17.9
null
null
null
null
24
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00519
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0004
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31539241/
null
PROTACpedia
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
27
false
1,356
0
Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)n1
BCR-ABL
MVDPVGFAEAWKAQFPDSEPPRMELRSVGDIEQELERCKASIRRLEQEVNQERFRMIYLQTLLAKEKKSYDRQRWGFRRAAQAPDGASEPRASASRPQPAPADGADPPPAEEPEARPDGEGSPGKARPGTARRPGAAASGERDDRGPPASVAALRSNFERIRKGHGQPGADAEKPFYVNVEFHHERGLVKVNDKEVSDRISSLGSQAMQMERKKSQHGAGSSVGDASRPPYRGRSSESSCGVDGDYEDAELNPRFLKDNLIDANGGSRPPWPPLEYQPYQSIYVGGMMEGEGKGPLLRSQSTSEQEKRLTWPRRSYSPRS...
VHL
K-562
DC50
nM
17.9
null
null
null
null
16
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
A9UF07
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0004
Homo sapiens
10.1021/acs.jmedchem.9b01264
Degradation of BCR-ABL in K562 cells after 16 h treatment
PROTAC-DB
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
27
false
1,356
0
Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(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)n1
ABL1
MLEICLKLVGCKSKKGLSSSSSCYLEEALQRPVASDFEPQGLSEAARWNSKENLLAGPSENDPNLFVALYDFVASGDNTLSITKGEKLRVLGYNHNGEWCEAQTKNGQGWVPSNYITPVNSLEKHSWYHGPVSRNAAEYLLSSGINGSFLVRESESSPGQRSISLRYEGRVYHYRINTASDGKLYVSSESRFNTLAELVHHHSTVADGLITTLHYPAPKRNKPTVYGVSPNYDKWEMERTDITMKHKLGGGQYGEVYEGVWKKYSLTVAVKTLKEDTMEVEEFLKEAAVMKEIKHPNLVQLLGVCTREPPFYIITEFMTY...
VHL
K-562
DC50
nM
8.5
null
null
null
null
24
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00519
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0004
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31539241/
null
PROTACpedia
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
27
false
1,357
0
Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(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)n1
BCR-ABL
MVDPVGFAEAWKAQFPDSEPPRMELRSVGDIEQELERCKASIRRLEQEVNQERFRMIYLQTLLAKEKKSYDRQRWGFRRAAQAPDGASEPRASASRPQPAPADGADPPPAEEPEARPDGEGSPGKARPGTARRPGAAASGERDDRGPPASVAALRSNFERIRKGHGQPGADAEKPFYVNVEFHHERGLVKVNDKEVSDRISSLGSQAMQMERKKSQHGAGSSVGDASRPPYRGRSSESSCGVDGDYEDAELNPRFLKDNLIDANGGSRPPWPPLEYQPYQSIYVGGMMEGEGKGPLLRSQSTSEQEKRLTWPRRSYSPRS...
VHL
K-562
DC50
nM
8.5
null
null
null
null
16
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
A9UF07
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0004
Homo sapiens
10.1021/acs.jmedchem.9b01264
Degradation of BCR-ABL in K562 cells after 16 h treatment
PROTAC-DB
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
27
false
1,357
0
Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(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)n1
ABL1
MLEICLKLVGCKSKKGLSSSSSCYLEEALQRPVASDFEPQGLSEAARWNSKENLLAGPSENDPNLFVALYDFVASGDNTLSITKGEKLRVLGYNHNGEWCEAQTKNGQGWVPSNYITPVNSLEKHSWYHGPVSRNAAEYLLSSGINGSFLVRESESSPGQRSISLRYEGRVYHYRINTASDGKLYVSSESRFNTLAELVHHHSTVADGLITTLHYPAPKRNKPTVYGVSPNYDKWEMERTDITMKHKLGGGQYGEVYEGVWKKYSLTVAVKTLKEDTMEVEEFLKEAAVMKEIKHPNLVQLLGVCTREPPFYIITEFMTY...
VHL
K-562
DC50
nM
37.9
null
null
null
null
24
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00519
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0004
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31539241/
null
PROTACpedia
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
27
false
1,358
0
Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(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)n1
BCR-ABL
MVDPVGFAEAWKAQFPDSEPPRMELRSVGDIEQELERCKASIRRLEQEVNQERFRMIYLQTLLAKEKKSYDRQRWGFRRAAQAPDGASEPRASASRPQPAPADGADPPPAEEPEARPDGEGSPGKARPGTARRPGAAASGERDDRGPPASVAALRSNFERIRKGHGQPGADAEKPFYVNVEFHHERGLVKVNDKEVSDRISSLGSQAMQMERKKSQHGAGSSVGDASRPPYRGRSSESSCGVDGDYEDAELNPRFLKDNLIDANGGSRPPWPPLEYQPYQSIYVGGMMEGEGKGPLLRSQSTSEQEKRLTWPRRSYSPRS...
VHL
K-562
DC50
nM
37.9
null
null
null
null
16
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
A9UF07
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0004
Homo sapiens
10.1021/acs.jmedchem.9b01264
Degradation of BCR-ABL in K562 cells after 16 h treatment
PROTAC-DB
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
27
false
1,358
0
Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(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)n1
ABL1
MLEICLKLVGCKSKKGLSSSSSCYLEEALQRPVASDFEPQGLSEAARWNSKENLLAGPSENDPNLFVALYDFVASGDNTLSITKGEKLRVLGYNHNGEWCEAQTKNGQGWVPSNYITPVNSLEKHSWYHGPVSRNAAEYLLSSGINGSFLVRESESSPGQRSISLRYEGRVYHYRINTASDGKLYVSSESRFNTLAELVHHHSTVADGLITTLHYPAPKRNKPTVYGVSPNYDKWEMERTDITMKHKLGGGQYGEVYEGVWKKYSLTVAVKTLKEDTMEVEEFLKEAAVMKEIKHPNLVQLLGVCTREPPFYIITEFMTY...
VHL
K-562
DC50
nM
10.1
null
null
null
null
24
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00519
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0004
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31539241/
null
PROTACpedia
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
27
false
1,359
0
Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(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)n1
BCR-ABL
MVDPVGFAEAWKAQFPDSEPPRMELRSVGDIEQELERCKASIRRLEQEVNQERFRMIYLQTLLAKEKKSYDRQRWGFRRAAQAPDGASEPRASASRPQPAPADGADPPPAEEPEARPDGEGSPGKARPGTARRPGAAASGERDDRGPPASVAALRSNFERIRKGHGQPGADAEKPFYVNVEFHHERGLVKVNDKEVSDRISSLGSQAMQMERKKSQHGAGSSVGDASRPPYRGRSSESSCGVDGDYEDAELNPRFLKDNLIDANGGSRPPWPPLEYQPYQSIYVGGMMEGEGKGPLLRSQSTSEQEKRLTWPRRSYSPRS...
VHL
K-562
DC50
nM
10.1
null
null
null
null
16
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
A9UF07
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0004
Homo sapiens
10.1021/acs.jmedchem.9b01264
Degradation of BCR-ABL in K562 cells after 16 h treatment
PROTAC-DB
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
27
false
1,359
0
Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCCCCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)CC2)n1
BCR-ABL
MVDPVGFAEAWKAQFPDSEPPRMELRSVGDIEQELERCKASIRRLEQEVNQERFRMIYLQTLLAKEKKSYDRQRWGFRRAAQAPDGASEPRASASRPQPAPADGADPPPAEEPEARPDGEGSPGKARPGTARRPGAAASGERDDRGPPASVAALRSNFERIRKGHGQPGADAEKPFYVNVEFHHERGLVKVNDKEVSDRISSLGSQAMQMERKKSQHGAGSSVGDASRPPYRGRSSESSCGVDGDYEDAELNPRFLKDNLIDANGGSRPPWPPLEYQPYQSIYVGGMMEGEGKGPLLRSQSTSEQEKRLTWPRRSYSPRS...
CRBN
K-562
DC50
nM
9
null
null
null
null
16
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
A9UF07
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0004
Homo sapiens
10.1016/j.ejmech.2021.113645
Degradation of BCR-ABL in K562 cells after 16 h treatment
PROTAC-DB
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
27
false
1,360
2
Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)CC2)n1
BCR-ABL
MVDPVGFAEAWKAQFPDSEPPRMELRSVGDIEQELERCKASIRRLEQEVNQERFRMIYLQTLLAKEKKSYDRQRWGFRRAAQAPDGASEPRASASRPQPAPADGADPPPAEEPEARPDGEGSPGKARPGTARRPGAAASGERDDRGPPASVAALRSNFERIRKGHGQPGADAEKPFYVNVEFHHERGLVKVNDKEVSDRISSLGSQAMQMERKKSQHGAGSSVGDASRPPYRGRSSESSCGVDGDYEDAELNPRFLKDNLIDANGGSRPPWPPLEYQPYQSIYVGGMMEGEGKGPLLRSQSTSEQEKRLTWPRRSYSPRS...
CRBN
K-562
DC50
nM
11
null
null
null
null
16
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
A9UF07
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0004
Homo sapiens
10.1016/j.ejmech.2021.113645
Degradation of BCR-ABL in K562 cells after 16 h treatment
PROTAC-DB
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
27
false
1,361
2
Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCCCNc3cccc4c3CN(C3CCC(=O)NC3=O)C4=O)CC2)n1
BCR-ABL
MVDPVGFAEAWKAQFPDSEPPRMELRSVGDIEQELERCKASIRRLEQEVNQERFRMIYLQTLLAKEKKSYDRQRWGFRRAAQAPDGASEPRASASRPQPAPADGADPPPAEEPEARPDGEGSPGKARPGTARRPGAAASGERDDRGPPASVAALRSNFERIRKGHGQPGADAEKPFYVNVEFHHERGLVKVNDKEVSDRISSLGSQAMQMERKKSQHGAGSSVGDASRPPYRGRSSESSCGVDGDYEDAELNPRFLKDNLIDANGGSRPPWPPLEYQPYQSIYVGGMMEGEGKGPLLRSQSTSEQEKRLTWPRRSYSPRS...
CRBN
K-562
DC50
nM
11.1
null
null
null
null
16
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
A9UF07
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0004
Homo sapiens
10.1016/j.ejmech.2021.113645
Degradation of BCR-ABL in K562 cells after 16 h treatment
PROTAC-DB
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
27
true
-1
-1
Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)CC2)n1
BCR-ABL
MVDPVGFAEAWKAQFPDSEPPRMELRSVGDIEQELERCKASIRRLEQEVNQERFRMIYLQTLLAKEKKSYDRQRWGFRRAAQAPDGASEPRASASRPQPAPADGADPPPAEEPEARPDGEGSPGKARPGTARRPGAAASGERDDRGPPASVAALRSNFERIRKGHGQPGADAEKPFYVNVEFHHERGLVKVNDKEVSDRISSLGSQAMQMERKKSQHGAGSSVGDASRPPYRGRSSESSCGVDGDYEDAELNPRFLKDNLIDANGGSRPPWPPLEYQPYQSIYVGGMMEGEGKGPLLRSQSTSEQEKRLTWPRRSYSPRS...
CRBN
K-562
DC50
nM
7.8
null
null
null
null
16
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
A9UF07
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0004
Homo sapiens
10.1016/j.ejmech.2021.113645
Degradation of BCR-ABL in K562 cells after 16 h treatment
PROTAC-DB
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
27
false
1,362
2
Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(C(=O)CCCc3cn(CCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)nn3)CC2)n1
ABL1
MLEICLKLVGCKSKKGLSSSSSCYLEEALQRPVASDFEPQGLSEAARWNSKENLLAGPSENDPNLFVALYDFVASGDNTLSITKGEKLRVLGYNHNGEWCEAQTKNGQGWVPSNYITPVNSLEKHSWYHGPVSRNAAEYLLSSGINGSFLVRESESSPGQRSISLRYEGRVYHYRINTASDGKLYVSSESRFNTLAELVHHHSTVADGLITTLHYPAPKRNKPTVYGVSPNYDKWEMERTDITMKHKLGGGQYGEVYEGVWKKYSLTVAVKTLKEDTMEVEEFLKEAAVMKEIKHPNLVQLLGVCTREPPFYIITEFMTY...
CRBN
K-562
DC50
nM
56
null
null
null
null
32
~
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00519
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0004
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/32657579/
null
PROTACpedia
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
27
false
1,363
0