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
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCCOc2ccc(CN3CCN(c4cc(-c5ccccc5O)nnc4N)CC3)cc2)c1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
A-549
Dmax
%
100
null
null
null
null
null
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
10.1021/acsmedchemlett.0c00347
Degradation of SMARCA4 in A549 cells
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
9
false
1,412
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCCc2ccc(CN3CCN(c4cc(-c5ccccc5O)nnc4N)CC3)cc2)c1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
A-549
DC50
nM
58
null
null
null
null
null
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
10.1021/acsmedchemlett.0c00347
Degradation of SMARCA2 in A549 cells
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
9
false
1,413
23
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCCc2ccc(CN3CCN(c4cc(-c5ccccc5O)nnc4N)CC3)cc2)c1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
A-549
Dmax
%
90
null
null
null
null
null
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
10.1021/acsmedchemlett.0c00347
Degradation of SMARCA2 in A549 cells
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
9
false
1,413
23
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCCc2ccc(CN3CCN(c4cc(-c5ccccc5O)nnc4N)CC3)cc2)c1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
A-549
DC50
nM
25
null
null
null
null
null
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
10.1021/acsmedchemlett.0c00347
Degradation of SMARCA4 in A549 cells
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
9
false
1,413
23
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCCc2ccc(CN3CCN(c4cc(-c5ccccc5O)nnc4N)CC3)cc2)c1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
A-549
Dmax
%
92
null
null
null
null
null
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
10.1021/acsmedchemlett.0c00347
Degradation of SMARCA4 in A549 cells
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
9
false
1,413
23
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCOCCOCCN2CCN(c3cc(-c4ccccc4O)nnc3N)CC2)c1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
MV4-11
DC50
nM
300
null
null
null
null
18
<
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0064
Homo sapiens
10.1038/s41589-019-0294-6; https://pubmed.ncbi.nlm.nih.gov/31178587/
Degradation of SMARCA2 in MV-4-11 cells after 18 h treatment; poor cellular permeability, ternary complex crystal structure: 6HAY (VCB:PROTAC 1:SMARCA2). DC50 is SMARCA2 300nM, SMARCA4 250nM. DCmax isSMARCA2 65%, SMARCA4 70%.
PROTAC-DB; PROTACpedia
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...
9
false
1,414
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCOCCOCCN2CCN(c3cc(-c4ccccc4O)nnc3N)CC2)c1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
MV4-11
Dmax
%
67.5
null
null
null
null
18
<
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0064
Homo sapiens
10.1038/s41589-019-0294-6; https://pubmed.ncbi.nlm.nih.gov/31178587/
Degradation of SMARCA2 in MV-4-11 cells after 18 h treatment; poor cellular permeability, ternary complex crystal structure: 6HAY (VCB:PROTAC 1:SMARCA2). DC50 is SMARCA2 300nM, SMARCA4 250nM. DCmax isSMARCA2 65%, SMARCA4 70%.
PROTAC-DB; PROTACpedia
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...
9
false
1,414
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCOCCOCCN2CCN(c3cc(-c4ccccc4O)nnc3N)CC2)c1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
MV4-11
DC50
nM
250
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0064
Homo sapiens
10.1038/s41589-019-0294-6
Degradation of SMARCA4 in MV-4-11 cells after 18 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...
9
false
1,414
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCOCCOCCN2CCN(c3cc(-c4ccccc4O)nnc3N)CC2)c1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
MV4-11
Dmax
%
70
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0064
Homo sapiens
10.1038/s41589-019-0294-6
Degradation of SMARCA4 in MV-4-11 cells after 18 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...
9
false
1,414
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCOc2ccc(CN3CCN(c4cc(-c5ccccc5O)nnc4N)CC3)cc2)c1
PBRM1
MGSKRRRATSPSSSVSGDFDDGHHSVSTPGPSRKRRRLSNLPTVDPIAVCHELYNTIRDYKDEQGRLLCELFIRAPKRRNQPDYYEVVSQPIDLMKIQQKLKMEEYDDVNLLTADFQLLFNNAKSYYKPDSPEYKAACKLWDLYLRTRNEFVQKGEADDEDDDEDGQDNQGTVTEGSSPAYLKEILEQLLEAIVVATNPSGRLISELFQKLPSKVQYPDYYAIIKEPIDLKTIAQRIQNGSYKSIHAMAKDIDLLAKNAKTYNEPGSQVFKDANSIKKIFYMKKAEIEHHEMAKSSLRMRTPSNLAAARLTGPSHSKGSL...
VHL
MV4-11
DC50
nM
32
null
null
null
null
18
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q86U86
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0064
Homo sapiens
10.1038/s41589-019-0294-6; https://pubmed.ncbi.nlm.nih.gov/31178587/
Degradation of PBRM1 in MV-4-11/NCI-H1568 cells after 18 h treatment; EC50 of PROTAC is 28nM in MV-4-11, 68nM in NCI-H1568. DC50 is (SMARCA2 6nM, SMARCA4 11nM, PBRM1 32nM in MV-4-11; SMARCA2 3.3nM, PBRM1 15.6nM in NCI-H1568)
PROTAC-DB; PROTACpedia
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...
-1
false
1,415
23
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCOc2ccc(CN3CCN(c4cc(-c5ccccc5O)nnc4N)CC3)cc2)c1
PBRM1
MGSKRRRATSPSSSVSGDFDDGHHSVSTPGPSRKRRRLSNLPTVDPIAVCHELYNTIRDYKDEQGRLLCELFIRAPKRRNQPDYYEVVSQPIDLMKIQQKLKMEEYDDVNLLTADFQLLFNNAKSYYKPDSPEYKAACKLWDLYLRTRNEFVQKGEADDEDDDEDGQDNQGTVTEGSSPAYLKEILEQLLEAIVVATNPSGRLISELFQKLPSKVQYPDYYAIIKEPIDLKTIAQRIQNGSYKSIHAMAKDIDLLAKNAKTYNEPGSQVFKDANSIKKIFYMKKAEIEHHEMAKSSLRMRTPSNLAAARLTGPSHSKGSL...
VHL
NCI-H1568
DC50
nM
15.6
null
null
null
null
18
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q86U86
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1476
Homo sapiens
10.1038/s41589-019-0294-6; https://pubmed.ncbi.nlm.nih.gov/31178587/
Degradation of PBRM1 in MV-4-11/NCI-H1568 cells after 18 h treatment; EC50 of PROTAC is 28nM in MV-4-11, 68nM in NCI-H1568. DC50 is (SMARCA2 6nM, SMARCA4 11nM, PBRM1 32nM in MV-4-11; SMARCA2 3.3nM, PBRM1 15.6nM in NCI-H1568)
PROTAC-DB; PROTACpedia
null
null
African=0.1%; Native American=0%; East Asian, North=2.23%; East Asian, South=0%; South Asian=2.88%; European, North=56.39%; European, South=38.41%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*03 Stable (MSS) (Sanger). Metastatic; Lymph node; Caucasian. Cancer cell line
-1
false
1,415
23
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCOc2ccc(CN3CCN(c4cc(-c5ccccc5O)nnc4N)CC3)cc2)c1
SMARCA2
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
MV4-11
DC50
nM
11
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0064
Homo sapiens
10.1038/s41589-019-0294-6
Degradation of SMARCA2 in MV-4-11 cells after 18 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...
9
false
1,415
23
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCOc2ccc(CN3CCN(c4cc(-c5ccccc5O)nnc4N)CC3)cc2)c1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
MV4-11
DC50
nM
6
null
null
null
null
18
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0064
Homo sapiens
10.1038/s41589-019-0294-6; https://pubmed.ncbi.nlm.nih.gov/31178587/
Degradation of SMARCA2 in MV-4-11/NCI-H1568 cells after 18 h treatment; EC50 of PROTAC is 28nM in MV-4-11, 68nM in NCI-H1568. DC50 is (SMARCA2 6nM, SMARCA4 11nM, PBRM1 32nM in MV-4-11; SMARCA2 3.3nM, PBRM1 15.6nM in NCI-H1568)
PROTAC-DB; PROTACpedia
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...
9
false
1,415
23
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCOc2ccc(CN3CCN(c4cc(-c5ccccc5O)nnc4N)CC3)cc2)c1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
NCI-H1568
DC50
nM
3.3
null
null
null
null
18
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1476
Homo sapiens
10.1038/s41589-019-0294-6; https://pubmed.ncbi.nlm.nih.gov/31178587/
Degradation of SMARCA2 in MV-4-11/NCI-H1568 cells after 18 h treatment; EC50 of PROTAC is 28nM in MV-4-11, 68nM in NCI-H1568. DC50 is (SMARCA2 6nM, SMARCA4 11nM, PBRM1 32nM in MV-4-11; SMARCA2 3.3nM, PBRM1 15.6nM in NCI-H1568)
PROTAC-DB; PROTACpedia
null
null
African=0.1%; Native American=0%; East Asian, North=2.23%; East Asian, South=0%; South Asian=2.88%; European, North=56.39%; European, South=38.41%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*03 Stable (MSS) (Sanger). Metastatic; Lymph node; Caucasian. Cancer cell line
9
false
1,415
23
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCOc2ccc(CN3CCN(c4cc(-c5ccccc5O)nnc4N)CC3)cc2)c1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
MV4-11
DC50
nM
11
null
null
null
null
18
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0064
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31178587/
EC50 of PROTAC is 28nM in MV-4-11, 68nM in NCI-H1568. DC50 is (SMARCA2 6nM, SMARCA4 11nM, PBRM1 32nM in MV-4-11; SMARCA2 3.3nM, PBRM1 15.6nM in NCI-H1568)
PROTACpedia
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...
9
false
1,415
23
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCc2ccc(CN3CCN(c4cc(-c5ccccc5O)nnc4N)CC3)c(F)c2)c1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
A-549
DC50
nM
55
null
null
null
null
null
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
10.1021/acsmedchemlett.0c00347
Degradation of SMARCA2 in A549 cells
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
9
true
-1
-1
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCc2ccc(CN3CCN(c4cc(-c5ccccc5O)nnc4N)CC3)c(F)c2)c1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
A-549
Dmax
%
95
null
null
null
null
null
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
10.1021/acsmedchemlett.0c00347
Degradation of SMARCA2 in A549 cells
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
9
true
-1
-1
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCc2ccc(CN3CCN(c4cc(-c5ccccc5O)nnc4N)CC3)c(F)c2)c1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
A-549
DC50
nM
33
null
null
null
null
null
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
10.1021/acsmedchemlett.0c00347
Degradation of SMARCA4 in A549 cells
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
9
true
-1
-1
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCc2ccc(CN3CCN(c4cc(-c5ccccc5O)nnc4N)CC3)c(F)c2)c1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
A-549
Dmax
%
95
null
null
null
null
null
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
10.1021/acsmedchemlett.0c00347
Degradation of SMARCA4 in A549 cells
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
9
true
-1
-1
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCc2ccc(OCCN3CCN(c4cc(-c5ccccc5O)nnc4N)CC3)cc2)c1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
A-549
DC50
nM
41
null
null
null
null
null
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
10.1021/acsmedchemlett.0c00347
Degradation of SMARCA2 in A549 cells
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
9
false
1,416
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCc2ccc(OCCN3CCN(c4cc(-c5ccccc5O)nnc4N)CC3)cc2)c1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
A-549
Dmax
%
99
null
null
null
null
null
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
10.1021/acsmedchemlett.0c00347
Degradation of SMARCA2 in A549 cells
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
9
false
1,416
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCc2ccc(OCCN3CCN(c4cc(-c5ccccc5O)nnc4N)CC3)cc2)c1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
A-549
DC50
nM
26
null
null
null
null
null
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
10.1021/acsmedchemlett.0c00347
Degradation of SMARCA4 in A549 cells
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
9
false
1,416
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCc2ccc(OCCN3CCN(c4cc(-c5ccccc5O)nnc4N)CC3)cc2)c1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
A-549
Dmax
%
99
null
null
null
null
null
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
10.1021/acsmedchemlett.0c00347
Degradation of SMARCA4 in A549 cells
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
9
false
1,416
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)SCCCCCCCCCCCCCCN(C)CCOC23CC4(C)CC(C)(CC(Cn5ncc(-c6ccc(N7CCCc8c7nnc(Nc7nc9ccccc9s7)c8C)nc6C(=O)O)c5C)(C4)C2)C3)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
HCT 116
DC50
nM
3.57
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent)
HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2. Cells were seeded in 96 microwell plates, 24 h ...
TPDdb
Automated Capillary Electrophoresis Immunoassay
TPD-0TN5HA
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
5
false
1,417
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)SCCCCCCCCCCCCCCN(C)CCOC23CC4(C)CC(C)(CC(Cn5ncc(-c6ccc(N7CCCc8c7nnc(Nc7nc9ccccc9s7)c8C)nc6C(=O)O)c5C)(C4)C2)C3)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
NCI-H1650
DC50
nM
1,670
null
null
null
null
null
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1483
Homo sapiens
SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent)
The ability of the BCL-xL degrader low molecular weight compounds to inhibit cell proliferation and survival was assessed using the Promega CellTiter-Glo proliferation assay on the EBC-1 lung cancer cell line (RCB1965, obtained from RIKEN). The cells were cultured in media that is optimal for their growth at 5% CO2, 37...
TPDdb
HiBiT
TPD-0TN5HA
African=0.57%; Native American=0%; East Asian, North=3.27%; East Asian, South=0%; South Asian=0%; European, North=61.83%; European, South=34.34%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). Metastatic; Pleural effusion; Caucasian. Cancer cell line
5
false
1,417
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)SCCCCCCCCCCCCCN(C)CCOC23CC4(C)CC(C)(CC(Cn5ncc(-c6ccc(N7CCCc8c7nnc(Nc7nc9ccccc9s7)c8C)nc6C(=O)O)c5C)(C4)C2)C3)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
HCT 116
DC50
nM
316
null
null
null
null
null
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent)
HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2. Cells were seeded in 96 microwell plates, 24 h ...
TPDdb
Automated Capillary Electrophoresis Immunoassay
TPD-0IDNWT
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
5
false
1,418
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)SCCCCCCCCCCCCCN(C)CCOC23CC4(C)CC(C)(CC(Cn5ncc(-c6ccc(N7CCCc8c7nnc(Nc7nc9ccccc9s7)c8C)nc6C(=O)O)c5C)(C4)C2)C3)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
NCI-H1650
DC50
nM
1,670
null
null
null
null
null
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1483
Homo sapiens
SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent)
The ability of the BCL-xL degrader low molecular weight compounds to inhibit cell proliferation and survival was assessed using the Promega CellTiter-Glo proliferation assay on the EBC-1 lung cancer cell line (RCB1965, obtained from RIKEN). The cells were cultured in media that is optimal for their growth at 5% CO2, 37...
TPDdb
HiBiT
TPD-0IDNWT
African=0.57%; Native American=0%; East Asian, North=3.27%; East Asian, South=0%; South Asian=0%; European, North=61.83%; European, South=34.34%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). Metastatic; Pleural effusion; Caucasian. Cancer cell line
5
false
1,418
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)SCCCCCCCCCCCCN(C)CCOC23CC4(C)CC(C)(CC(Cn5ncc(-c6ccc(N7CCCc8c7nnc(Nc7nc9ccccc9s7)c8C)nc6C(=O)O)c5C)(C4)C2)C3)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
HCT 116
DC50
nM
0.399
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent)
HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2. Cells were seeded in 96 microwell plates, 24 h ...
TPDdb
Automated Capillary Electrophoresis Immunoassay
TPD-PPJWGG
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
5
false
1,419
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)SCCCCCCCCCCCCN(C)CCOC23CC4(C)CC(C)(CC(Cn5ncc(-c6ccc(N7CCCc8c7nnc(Nc7nc9ccccc9s7)c8C)nc6C(=O)O)c5C)(C4)C2)C3)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
NCI-H1650
DC50
nM
1,670
null
null
null
null
null
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1483
Homo sapiens
SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent)
The ability of the BCL-xL degrader low molecular weight compounds to inhibit cell proliferation and survival was assessed using the Promega CellTiter-Glo proliferation assay on the EBC-1 lung cancer cell line (RCB1965, obtained from RIKEN). The cells were cultured in media that is optimal for their growth at 5% CO2, 37...
TPDdb
HiBiT
TPD-PPJWGG
African=0.57%; Native American=0%; East Asian, North=3.27%; East Asian, South=0%; South Asian=0%; European, North=61.83%; European, South=34.34%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). Metastatic; Pleural effusion; Caucasian. Cancer cell line
5
false
1,419
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)SCCCCCCCCCCCN(C)CCOC23CC4(C)CC(C)(CC(Cn5ncc(-c6ccc(N7CCCc8c7nnc(Nc7nc9ccccc9s7)c8C)nc6C(=O)O)c5C)(C4)C2)C3)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
HCT 116
DC50
nM
1.17
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent)
HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2. Cells were seeded in 96 microwell plates, 24 h ...
TPDdb
Automated Capillary Electrophoresis Immunoassay
TPD-4WIWN8
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
5
false
1,420
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)SCCCCCCCCCCCN(C)CCOC23CC4(C)CC(C)(CC(Cn5ncc(-c6ccc(N7CCCc8c7nnc(Nc7nc9ccccc9s7)c8C)nc6C(=O)O)c5C)(C4)C2)C3)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
NCI-H1650
DC50
nM
1,670
null
null
null
null
null
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1483
Homo sapiens
SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent)
The ability of the BCL-xL degrader low molecular weight compounds to inhibit cell proliferation and survival was assessed using the Promega CellTiter-Glo proliferation assay on the EBC-1 lung cancer cell line (RCB1965, obtained from RIKEN). The cells were cultured in media that is optimal for their growth at 5% CO2, 37...
TPDdb
HiBiT
TPD-4WIWN8
African=0.57%; Native American=0%; East Asian, North=3.27%; East Asian, South=0%; South Asian=0%; European, North=61.83%; European, South=34.34%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). Metastatic; Pleural effusion; Caucasian. Cancer cell line
5
false
1,420
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)SCCCCCCCCCCN(C)CCOC23CC4(C)CC(C)(CC(Cn5ncc(-c6ccc(N7CCCc8c7nnc(Nc7nc9ccccc9s7)c8C)nc6C(=O)O)c5C)(C4)C2)C3)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
HCT 116
DC50
nM
1.06
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent)
HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2. Cells were seeded in 96 microwell plates, 24 h ...
TPDdb
Automated Capillary Electrophoresis Immunoassay
TPD-PZRY7E
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
5
false
1,421
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)SCCCCCCCCCCN(C)CCOC23CC4(C)CC(C)(CC(Cn5ncc(-c6ccc(N7CCCc8c7nnc(Nc7nc9ccccc9s7)c8C)nc6C(=O)O)c5C)(C4)C2)C3)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
NCI-H1650
DC50
nM
1,670
null
null
null
null
null
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1483
Homo sapiens
SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent)
The ability of the BCL-xL degrader low molecular weight compounds to inhibit cell proliferation and survival was assessed using the Promega CellTiter-Glo proliferation assay on the EBC-1 lung cancer cell line (RCB1965, obtained from RIKEN). The cells were cultured in media that is optimal for their growth at 5% CO2, 37...
TPDdb
HiBiT
TPD-PZRY7E
African=0.57%; Native American=0%; East Asian, North=3.27%; East Asian, South=0%; South Asian=0%; European, North=61.83%; European, South=34.34%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). Metastatic; Pleural effusion; Caucasian. Cancer cell line
5
false
1,421
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(O)CCN(c3ccc4c(c3)CCC43CCN(c4cc(-c5ccccc5O)nnc4N)CC3)CC2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
HT-1080
DC50
nM
17.21
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-8OYUNT
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
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(O)CCN(c3ccc4c(c3)CCC43CCN(c4cc(-c5ccccc5O)nnc4N)CC3)CC2)C(C)(C)C)cc1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
HT-1080
DC50
nM
231.4
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-8OYUNT
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
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2CC3(C2)CN(c2ccc4c(c2)CCC42CCN(c4cc(-c5ccccc5O)nnc4N)CC2)C3)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
HT-1080
DC50
nM
7.48
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-FXH2GZ
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
1,422
12
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2CC3(C2)CN(c2ccc4c(c2)CCC42CCN(c4cc(-c5ccccc5O)nnc4N)CC2)C3)C(C)(C)C)cc1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
HT-1080
DC50
nM
98.4
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-FXH2GZ
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
1,422
12
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2CCC(C3CCN(CC#Cc4ccc(OCCCc5sc(N6CCc7cccc(C(=O)Nc8nc9ccccc9s8)c7C6)nc5C(=O)O)cc4)CC3)CC2)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
DC50
nM
1.2
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
BCL-XL DEGRADING COMPOUNDS (patent)
BCL-XL Degradation Assay Cell Culture Human T lymphoblast MOLT-4 were cultured in RPMI 1640 media, supplemented with 10%FBS. All cell lines were maintained at 37 °C in an atmosphere of 5%CO2. Protein extraction and Western blotting Whole cell lysates were prepared using cell Lysis Buffer supplemented with Protease inhi...
TPDdb
Western Blot/CellTiterGlo
TPD-SJCZH2
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; ...
5
false
1,423
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2CCC(C3CCN(CC#Cc4ccc(OCCCc5sc(N6CCc7cccc(C(=O)Nc8nc9ccccc9s8)c7C6)nc5C(=O)O)cc4)CC3)CC2)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
Dmax
%
85
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
BCL-XL DEGRADING COMPOUNDS (patent)
BCL-XL Degradation Assay Cell Culture Human T lymphoblast MOLT-4 were cultured in RPMI 1640 media, supplemented with 10%FBS. All cell lines were maintained at 37 °C in an atmosphere of 5%CO2. Protein extraction and Western blotting Whole cell lysates were prepared using cell Lysis Buffer supplemented with Protease inhi...
TPDdb
Western Blot/CellTiterGlo
TPD-SJCZH2
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; ...
5
false
1,423
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2CCC(N3CCC(c4ccc5c(c4)CCC54CCN(c5cc(-c6ccccc6O)nnc5N)CC4)CC3)CC2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
HT-1080
DC50
nM
19.29
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-6YCESO
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
1,398
22
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2CCC(N3CCC(c4ccc5c(c4)CCC54CCN(c5cc(-c6ccccc6O)nnc5N)CC4)CC3)CC2)C(C)(C)C)cc1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
HT-1080
DC50
nM
1,373
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-6YCESO
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
1,398
22
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2CCC3(CC2)CCN(CC#Cc2ccc(OCCCc4sc(N5CCc6cccc(C(=O)Nc7nc8ccccc8s7)c6C5)nc4C(=O)O)cc2)CC3)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
DC50
nM
1.5
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
BCL-XL DEGRADING COMPOUNDS (patent)
BCL-XL Degradation Assay Cell Culture Human T lymphoblast MOLT-4 were cultured in RPMI 1640 media, supplemented with 10%FBS. All cell lines were maintained at 37 °C in an atmosphere of 5%CO2. Protein extraction and Western blotting Whole cell lysates were prepared using cell Lysis Buffer supplemented with Protease inhi...
TPDdb
Western Blot/CellTiterGlo
TPD-3XY5ST
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; ...
5
false
1,424
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2CCC3(CC2)CCN(CC#Cc2ccc(OCCCc4sc(N5CCc6cccc(C(=O)Nc7nc8ccccc8s7)c6C5)nc4C(=O)O)cc2)CC3)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
Dmax
%
96
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
BCL-XL DEGRADING COMPOUNDS (patent)
BCL-XL Degradation Assay Cell Culture Human T lymphoblast MOLT-4 were cultured in RPMI 1640 media, supplemented with 10%FBS. All cell lines were maintained at 37 °C in an atmosphere of 5%CO2. Protein extraction and Western blotting Whole cell lysates were prepared using cell Lysis Buffer supplemented with Protease inhi...
TPDdb
Western Blot/CellTiterGlo
TPD-3XY5ST
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; ...
5
false
1,424
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2CCN(c3ccc4c(c3)CCC43CN(c4cc(-c5ccccc5O)nnc4N)C3)CC2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
HT-1080
DC50
nM
0.99
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-D1Z2H8
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
1,425
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2CCN(c3ccc4c(c3)CCC43CN(c4cc(-c5ccccc5O)nnc4N)C3)CC2)C(C)(C)C)cc1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
HT-1080
DC50
nM
12.6
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-D1Z2H8
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
1,425
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2CN(c3ccc4c(c3)CCC43CCN(c4cc(-c5ccccc5O)nnc4N)CC3)C2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
HT-1080
DC50
nM
8.49
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-XJ5CAF
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
1,426
2
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2CN(c3ccc4c(c3)CCC43CCN(c4cc(-c5ccccc5O)nnc4N)CC3)C2)C(C)(C)C)cc1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
HT-1080
DC50
nM
152.68
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-XJ5CAF
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
1,426
2
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CC2CC(N3CC(C#Cc4ccc(OCCCc5sc(N6CCc7cccc(C(=O)Nc8nc9ccccc9s8)c7C6)nc5C(=O)O)cc4)C3)C2)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
DC50
nM
3.9
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
BCL-XL DEGRADING COMPOUNDS (patent)
BCL-XL Degradation Assay Cell Culture Human T lymphoblast MOLT-4 were cultured in RPMI 1640 media, supplemented with 10%FBS. All cell lines were maintained at 37 °C in an atmosphere of 5%CO2. Protein extraction and Western blotting Whole cell lysates were prepared using cell Lysis Buffer supplemented with Protease inhi...
TPDdb
Western Blot/CellTiterGlo
TPD-W52F4J
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; ...
5
false
1,427
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CC2CC(N3CC(C#Cc4ccc(OCCCc5sc(N6CCc7cccc(C(=O)Nc8nc9ccccc9s8)c7C6)nc5C(=O)O)cc4)C3)C2)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
Dmax
%
78
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
BCL-XL DEGRADING COMPOUNDS (patent)
BCL-XL Degradation Assay Cell Culture Human T lymphoblast MOLT-4 were cultured in RPMI 1640 media, supplemented with 10%FBS. All cell lines were maintained at 37 °C in an atmosphere of 5%CO2. Protein extraction and Western blotting Whole cell lysates were prepared using cell Lysis Buffer supplemented with Protease inhi...
TPDdb
Western Blot/CellTiterGlo
TPD-W52F4J
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; ...
5
false
1,427
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CC2CC3(CCN(CC#Cc4ccc(OCCCc5sc(N6CCc7cccc(C(=O)Nc8nc9ccccc9s8)c7C6)nc5C(=O)O)cc4)CC3)C2)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
DC50
nM
1.9
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
BCL-XL DEGRADING COMPOUNDS (patent)
BCL-XL Degradation Assay Cell Culture Human T lymphoblast MOLT-4 were cultured in RPMI 1640 media, supplemented with 10%FBS. All cell lines were maintained at 37 °C in an atmosphere of 5%CO2. Protein extraction and Western blotting Whole cell lysates were prepared using cell Lysis Buffer supplemented with Protease inhi...
TPDdb
Western Blot/CellTiterGlo
TPD-2ABPE8
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; ...
5
false
1,428
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CC2CC3(CCN(CC#Cc4ccc(OCCCc5sc(N6CCc7cccc(C(=O)Nc8nc9ccccc9s8)c7C6)nc5C(=O)O)cc4)CC3)C2)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
Dmax
%
97
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
BCL-XL DEGRADING COMPOUNDS (patent)
BCL-XL Degradation Assay Cell Culture Human T lymphoblast MOLT-4 were cultured in RPMI 1640 media, supplemented with 10%FBS. All cell lines were maintained at 37 °C in an atmosphere of 5%CO2. Protein extraction and Western blotting Whole cell lysates were prepared using cell Lysis Buffer supplemented with Protease inhi...
TPDdb
Western Blot/CellTiterGlo
TPD-2ABPE8
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; ...
5
false
1,428
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CC2CCC3(CC2)CCN(CC#Cc2ccc(OCCCc4sc(N5CCc6cccc(C(=O)Nc7nc8ccccc8s7)c6C5)nc4C(=O)O)c(F)c2)CC3)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
DC50
nM
0.8
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
BCL-XL DEGRADING COMPOUNDS (patent)
BCL-XL Degradation Assay Cell Culture Human T lymphoblast MOLT-4 were cultured in RPMI 1640 media, supplemented with 10%FBS. All cell lines were maintained at 37 °C in an atmosphere of 5%CO2. Protein extraction and Western blotting Whole cell lysates were prepared using cell Lysis Buffer supplemented with Protease inhi...
TPDdb
Western Blot/CellTiterGlo
TPD-4O9H1N
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; ...
5
false
1,429
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CC2CCC3(CC2)CCN(CC#Cc2ccc(OCCCc4sc(N5CCc6cccc(C(=O)Nc7nc8ccccc8s7)c6C5)nc4C(=O)O)cc2)CC3)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
DC50
nM
2.6
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
BCL-XL DEGRADING COMPOUNDS (patent)
BCL-XL Degradation Assay Cell Culture Human T lymphoblast MOLT-4 were cultured in RPMI 1640 media, supplemented with 10%FBS. All cell lines were maintained at 37 °C in an atmosphere of 5%CO2. Protein extraction and Western blotting Whole cell lysates were prepared using cell Lysis Buffer supplemented with Protease inhi...
TPDdb
Western Blot/CellTiterGlo
TPD-IBZNF1
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; ...
5
false
1,429
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CC2CCC3(CC2)CCN(CC#Cc2ccc(OCCCc4sc(N5CCc6cccc(C(=O)Nc7nc8ccccc8s7)c6C5)nc4C(=O)O)cc2)CC3)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
Dmax
%
87
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
BCL-XL DEGRADING COMPOUNDS (patent)
BCL-XL Degradation Assay Cell Culture Human T lymphoblast MOLT-4 were cultured in RPMI 1640 media, supplemented with 10%FBS. All cell lines were maintained at 37 °C in an atmosphere of 5%CO2. Protein extraction and Western blotting Whole cell lysates were prepared using cell Lysis Buffer supplemented with Protease inhi...
TPDdb
Western Blot/CellTiterGlo
TPD-IBZNF1
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; ...
5
false
1,429
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CC2CCC3(CC2)CN(CC#Cc2ccc(OCCCc4sc(N5CCc6cccc(C(=O)Nc7nc8ccccc8s7)c6C5)nc4C(=O)O)cc2)C3)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
DC50
nM
4.1
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
BCL-XL DEGRADING COMPOUNDS (patent)
BCL-XL Degradation Assay Cell Culture Human T lymphoblast MOLT-4 were cultured in RPMI 1640 media, supplemented with 10%FBS. All cell lines were maintained at 37 °C in an atmosphere of 5%CO2. Protein extraction and Western blotting Whole cell lysates were prepared using cell Lysis Buffer supplemented with Protease inhi...
TPDdb
Western Blot/CellTiterGlo
TPD-PZ083E
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; ...
5
false
1,430
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CC2CCC3(CC2)CN(CC#Cc2ccc(OCCCc4sc(N5CCc6cccc(C(=O)Nc7nc8ccccc8s7)c6C5)nc4C(=O)O)cc2)C3)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
Dmax
%
84
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
BCL-XL DEGRADING COMPOUNDS (patent)
BCL-XL Degradation Assay Cell Culture Human T lymphoblast MOLT-4 were cultured in RPMI 1640 media, supplemented with 10%FBS. All cell lines were maintained at 37 °C in an atmosphere of 5%CO2. Protein extraction and Western blotting Whole cell lysates were prepared using cell Lysis Buffer supplemented with Protease inhi...
TPDdb
Western Blot/CellTiterGlo
TPD-PZ083E
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; ...
5
false
1,430
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCC(=O)N2CCN(CC#Cc3ccc(OCCCc4sc(N5CCCc6c5nnc(Nc5nc7ccccc7s5)c6C)nc4C(=O)O)c(F)c3)CC2)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
NCI-H1650
DC50
nM
1,670
null
null
null
null
null
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1483
Homo sapiens
SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent)
The ability of the BCL-xL degrader low molecular weight compounds to inhibit cell proliferation and survival was assessed using the Promega CellTiter-Glo proliferation assay on the EBC-1 lung cancer cell line (RCB1965, obtained from RIKEN). The cells were cultured in media that is optimal for their growth at 5% CO2, 37...
TPDdb
HiBiT
TPD-3ZUES5
African=0.57%; Native American=0%; East Asian, North=3.27%; East Asian, South=0%; South Asian=0%; European, North=61.83%; European, South=34.34%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). Metastatic; Pleural effusion; Caucasian. Cancer cell line
5
false
1,431
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C(C)(C)C)cc1
CRBN
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
VHL
HEK293T
DC50
nM
2,546.1
null
null
null
null
24
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q96SW2
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0063
Homo sapiens
10.1038/s41598-019-56177-5; https://pubmed.ncbi.nlm.nih.gov/31873151/
Degradation of CRBN in HEK293T cells after 24h treatment
PROTAC-DB; PROTACpedia
null
null
Highly susceptible to infection by Zika virus (ZIKV). CVCL_0045 ! HEK293 In situ; Fetal kidney; NCBI_TaxID; 28285; Human adenovirus C serotype 5. NCBI_TaxID; 1891767; Simian virus 40 (SV40) (Note=tsA). Transformed cell line
-1
false
1,432
2
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C(C)(C)C)cc1
CRBN
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
VHL
HEK293T
Dmax
%
77.9
null
null
null
null
24
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q96SW2
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0063
Homo sapiens
10.1038/s41598-019-56177-5; https://pubmed.ncbi.nlm.nih.gov/31873151/
Degradation of CRBN in HEK293T cells after 24h treatment
PROTAC-DB; PROTACpedia
null
null
Highly susceptible to infection by Zika virus (ZIKV). CVCL_0045 ! HEK293 In situ; Fetal kidney; NCBI_TaxID; 28285; Human adenovirus C serotype 5. NCBI_TaxID; 1891767; Simian virus 40 (SV40) (Note=tsA). Transformed cell line
-1
false
1,432
2
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCC#Cc2ccc(OCCCc3sc(N4CCc5cccc(C(=O)Nc6nc7ccccc7s6)c5C4)nc3C(=O)O)cc2)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
DC50
nM
4.6
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
BCL-XL DEGRADING COMPOUNDS (patent)
BCL-XL Degradation Assay Cell Culture Human T lymphoblast MOLT-4 were cultured in RPMI 1640 media, supplemented with 10%FBS. All cell lines were maintained at 37 °C in an atmosphere of 5%CO2. Protein extraction and Western blotting Whole cell lysates were prepared using cell Lysis Buffer supplemented with Protease inhi...
TPDdb
Western Blot/CellTiterGlo
TPD-ICHLEB
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; ...
5
false
1,433
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCC#Cc2ccc(OCCCc3sc(N4CCc5cccc(C(=O)Nc6nc7ccccc7s6)c5C4)nc3C(=O)O)cc2)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
Dmax
%
96
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
BCL-XL DEGRADING COMPOUNDS (patent)
BCL-XL Degradation Assay Cell Culture Human T lymphoblast MOLT-4 were cultured in RPMI 1640 media, supplemented with 10%FBS. All cell lines were maintained at 37 °C in an atmosphere of 5%CO2. Protein extraction and Western blotting Whole cell lysates were prepared using cell Lysis Buffer supplemented with Protease inhi...
TPDdb
Western Blot/CellTiterGlo
TPD-ICHLEB
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; ...
5
false
1,433
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCC#Cc2ccc(OCCCc3sc(N4CCc5cccc(C(=O)Nc6nc7ccccc7s6)c5C4)nc3C(=O)O)cc2)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
DC50
nM
1.8
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
BCL-XL DEGRADING COMPOUNDS (patent)
BCL-XL Degradation Assay Cell Culture Human T lymphoblast MOLT-4 were cultured in RPMI 1640 media, supplemented with 10%FBS. All cell lines were maintained at 37 °C in an atmosphere of 5%CO2. Protein extraction and Western blotting Whole cell lysates were prepared using cell Lysis Buffer supplemented with Protease inhi...
TPDdb
Western Blot/CellTiterGlo
TPD-EFN6AM
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; ...
5
false
1,434
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCC#Cc2ccc(OCCCc3sc(N4CCc5cccc(C(=O)Nc6nc7ccccc7s6)c5C4)nc3C(=O)O)cc2)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
Dmax
%
91
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
BCL-XL DEGRADING COMPOUNDS (patent)
BCL-XL Degradation Assay Cell Culture Human T lymphoblast MOLT-4 were cultured in RPMI 1640 media, supplemented with 10%FBS. All cell lines were maintained at 37 °C in an atmosphere of 5%CO2. Protein extraction and Western blotting Whole cell lysates were prepared using cell Lysis Buffer supplemented with Protease inhi...
TPDdb
Western Blot/CellTiterGlo
TPD-EFN6AM
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; ...
5
false
1,434
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCC(=O)Nc2ccc(C(=O)Nc3cc(-c4cccs4)ccc3N)cc2)C(C)(C)C)cc1
HDAC1
MAQTQGTRRKVCYYYDGDVGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKANAEEMTKYHSDDYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVASAVKLNKQQTDIAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHHGDGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNYPLRDGIDDESYEAIFKPVMSKVMEMFQPSAVVLQCGSDSLSGDRLGCFNLTIKGHAKCVEFVKSFNLPMLMLGGGGYTIRNVARCWTYETAVAL...
VHL
HCT 116
Dmax
%
6
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q13547
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC1 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
17
false
1,435
1
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCC(=O)Nc2ccc(C(=O)Nc3cc(-c4cccs4)ccc3N)cc2)C(C)(C)C)cc1
HDAC2
MAYSQGGGKKKVCYYYDGDIGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKATAEEMTKYHSDEYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVAGAVKLNRQQTDMAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHHGDGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNFPMRDGIDDESYGQIFKPIISKVMEMYQPSAVVLQCGADSLSGDRLGCFNLTVKGHAKCVEVVKTFNLPLLMLGGGGYTIRNVARCWTYETAVA...
VHL
HCT 116
Dmax
%
6
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q92769
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC2 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
18
false
1,435
1
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCC(=O)Nc2ccc(C(=O)Nc3cc(-c4cccs4)ccc3N)cc2)C(C)(C)C)cc1
HDAC3
MAKTVAYFYDPDVGNFHYGAGHPMKPHRLALTHSLVLHYGLYKKMIVFKPYQASQHDMCRFHSEDYIDFLQRVSPTNMQGFTKSLNAFNVGDDCPVFPGLFEFCSRYTGASLQGATQLNNKICDIAINWAGGLHHAKKFEASGFCYVNDIVIGILELLKYHPRVLYIDIDIHHGDGVQEAFYLTDRVMTVSFHKYGNYFFPGTGDMYEVGAESGRYYCLNVPLRDGIDDQSYKHLFQPVINQVVDFYQPTCIVLQCGADSLGCDRLGCFNLSIRGHGECVEYVKSFNIPLLVLGGGGYTVRNVARCWTYETSLLVEEAIS...
VHL
HCT 116
Dmax
%
3
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O15379
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC3 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
13
false
1,435
1
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCC(=O)Nc2ccc(C(=O)Nc3ccc(F)cc3N)cc2)C(C)(C)C)cc1
HDAC1
MAQTQGTRRKVCYYYDGDVGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKANAEEMTKYHSDDYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVASAVKLNKQQTDIAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHHGDGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNYPLRDGIDDESYEAIFKPVMSKVMEMFQPSAVVLQCGSDSLSGDRLGCFNLTIKGHAKCVEFVKSFNLPMLMLGGGGYTIRNVARCWTYETAVAL...
VHL
HCT 116
Dmax
%
41
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q13547
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC1 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
17
false
1,436
1
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCC(=O)Nc2ccc(C(=O)Nc3ccc(F)cc3N)cc2)C(C)(C)C)cc1
HDAC2
MAYSQGGGKKKVCYYYDGDIGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKATAEEMTKYHSDEYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVAGAVKLNRQQTDMAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHHGDGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNFPMRDGIDDESYGQIFKPIISKVMEMYQPSAVVLQCGADSLSGDRLGCFNLTVKGHAKCVEVVKTFNLPLLMLGGGGYTIRNVARCWTYETAVA...
VHL
HCT 116
Dmax
%
13
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q92769
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC2 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
18
false
1,436
1
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCC(=O)Nc2ccc(C(=O)Nc3ccc(F)cc3N)cc2)C(C)(C)C)cc1
HDAC3
MAKTVAYFYDPDVGNFHYGAGHPMKPHRLALTHSLVLHYGLYKKMIVFKPYQASQHDMCRFHSEDYIDFLQRVSPTNMQGFTKSLNAFNVGDDCPVFPGLFEFCSRYTGASLQGATQLNNKICDIAINWAGGLHHAKKFEASGFCYVNDIVIGILELLKYHPRVLYIDIDIHHGDGVQEAFYLTDRVMTVSFHKYGNYFFPGTGDMYEVGAESGRYYCLNVPLRDGIDDQSYKHLFQPVINQVVDFYQPTCIVLQCGADSLGCDRLGCFNLSIRGHGECVEYVKSFNIPLLVLGGGGYTVRNVARCWTYETSLLVEEAIS...
VHL
HCT 116
Dmax
%
39
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O15379
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC3 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
13
false
1,436
1
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCC(=O)Nc2ccc(C(=O)Nc3ccccc3N)cc2)C(C)(C)C)cc1
HDAC1
MAQTQGTRRKVCYYYDGDVGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKANAEEMTKYHSDDYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVASAVKLNKQQTDIAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHHGDGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNYPLRDGIDDESYEAIFKPVMSKVMEMFQPSAVVLQCGSDSLSGDRLGCFNLTIKGHAKCVEFVKSFNLPMLMLGGGGYTIRNVARCWTYETAVAL...
VHL
HCT 116
Dmax
%
41
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q13547
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC1 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
17
false
1,436
1
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCC(=O)Nc2ccc(C(=O)Nc3ccccc3N)cc2)C(C)(C)C)cc1
HDAC2
MAYSQGGGKKKVCYYYDGDIGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKATAEEMTKYHSDEYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVAGAVKLNRQQTDMAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHHGDGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNFPMRDGIDDESYGQIFKPIISKVMEMYQPSAVVLQCGADSLSGDRLGCFNLTVKGHAKCVEVVKTFNLPLLMLGGGGYTIRNVARCWTYETAVA...
VHL
HCT 116
Dmax
%
32
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q92769
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC2 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
18
false
1,436
1
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCC(=O)Nc2ccc(C(=O)Nc3ccccc3N)cc2)C(C)(C)C)cc1
HDAC3
MAKTVAYFYDPDVGNFHYGAGHPMKPHRLALTHSLVLHYGLYKKMIVFKPYQASQHDMCRFHSEDYIDFLQRVSPTNMQGFTKSLNAFNVGDDCPVFPGLFEFCSRYTGASLQGATQLNNKICDIAINWAGGLHHAKKFEASGFCYVNDIVIGILELLKYHPRVLYIDIDIHHGDGVQEAFYLTDRVMTVSFHKYGNYFFPGTGDMYEVGAESGRYYCLNVPLRDGIDDQSYKHLFQPVINQVVDFYQPTCIVLQCGADSLGCDRLGCFNLSIRGHGECVEYVKSFNIPLLVLGGGGYTVRNVARCWTYETSLLVEEAIS...
VHL
HCT 116
Dmax
%
3
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O15379
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC3 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
13
false
1,436
1
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCC#Cc2ccc(OCCCc3sc(N4CCc5cccc(C(=O)Nc6nc7ccccc7s6)c5C4)nc3C(=O)O)cc2)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
DC50
nM
2.2
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
BCL-XL DEGRADING COMPOUNDS (patent)
BCL-XL Degradation Assay Cell Culture Human T lymphoblast MOLT-4 were cultured in RPMI 1640 media, supplemented with 10%FBS. All cell lines were maintained at 37 °C in an atmosphere of 5%CO2. Protein extraction and Western blotting Whole cell lysates were prepared using cell Lysis Buffer supplemented with Protease inhi...
TPDdb
Western Blot/CellTiterGlo
TPD-SGQDH1
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; ...
5
false
1,437
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCC#Cc2ccc(OCCCc3sc(N4CCc5cccc(C(=O)Nc6nc7ccccc7s6)c5C4)nc3C(=O)O)cc2)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
Dmax
%
97
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
BCL-XL DEGRADING COMPOUNDS (patent)
BCL-XL Degradation Assay Cell Culture Human T lymphoblast MOLT-4 were cultured in RPMI 1640 media, supplemented with 10%FBS. All cell lines were maintained at 37 °C in an atmosphere of 5%CO2. Protein extraction and Western blotting Whole cell lysates were prepared using cell Lysis Buffer supplemented with Protease inhi...
TPDdb
Western Blot/CellTiterGlo
TPD-SGQDH1
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; ...
5
false
1,437
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCC(=O)Nc2ccc(C(=O)Nc3ccccc3N)cc2)C(C)(C)C)cc1
HDAC1
MAQTQGTRRKVCYYYDGDVGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKANAEEMTKYHSDDYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVASAVKLNKQQTDIAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHHGDGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNYPLRDGIDDESYEAIFKPVMSKVMEMFQPSAVVLQCGSDSLSGDRLGCFNLTIKGHAKCVEFVKSFNLPMLMLGGGGYTIRNVARCWTYETAVAL...
VHL
HCT 116
Dmax
%
54
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q13547
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC1 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
17
false
1,438
1
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCC(=O)Nc2ccc(C(=O)Nc3ccccc3N)cc2)C(C)(C)C)cc1
HDAC2
MAYSQGGGKKKVCYYYDGDIGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKATAEEMTKYHSDEYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVAGAVKLNRQQTDMAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHHGDGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNFPMRDGIDDESYGQIFKPIISKVMEMYQPSAVVLQCGADSLSGDRLGCFNLTVKGHAKCVEVVKTFNLPLLMLGGGGYTIRNVARCWTYETAVA...
VHL
HCT 116
Dmax
%
37
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q92769
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC2 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
18
false
1,438
1
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCC(=O)Nc2ccc(C(=O)Nc3ccccc3N)cc2)C(C)(C)C)cc1
HDAC3
MAKTVAYFYDPDVGNFHYGAGHPMKPHRLALTHSLVLHYGLYKKMIVFKPYQASQHDMCRFHSEDYIDFLQRVSPTNMQGFTKSLNAFNVGDDCPVFPGLFEFCSRYTGASLQGATQLNNKICDIAINWAGGLHHAKKFEASGFCYVNDIVIGILELLKYHPRVLYIDIDIHHGDGVQEAFYLTDRVMTVSFHKYGNYFFPGTGDMYEVGAESGRYYCLNVPLRDGIDDQSYKHLFQPVINQVVDFYQPTCIVLQCGADSLGCDRLGCFNLSIRGHGECVEYVKSFNIPLLVLGGGGYTVRNVARCWTYETSLLVEEAIS...
VHL
HCT 116
Dmax
%
23
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O15379
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC3 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
13
false
1,438
1
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCC(=O)NCCN2CCN(Cc3cccc(-c4ccc(N5CCN(C)CC5)c(NC(=O)c5c[nH]c(=O)cc5C(F)(F)F)c4)c3)CC2)C(C)(C)C)cc1
WDR5
MATEEKKPETEAARAQPTPSSSATQSKPTPVKPNYALKFTLAGHTKAVSSVKFSPNGEWLASSSADKLIKIWGAYDGKFEKTISGHKLGISDVAWSSDSNLLVSASDDKTLKIWDVSSGKCLKTLKGHSNYVFCCNFNPQSNLIVSGSFDESVRIWDVKTGKCLKTLPAHSDPVSAVHFNRDGSLIVSSSYDGLCRIWDTASGQCLKTLIDDDNPPVSFVKFSPNGKYILAATLDNTLKLWDYSKGKCLKTYTGHKNEKYCIFANFSVTGGKWIVSGSEDNLVYIWNLQTKEIVQKLQGHTDVVISTACHPTENIIASAA...
VHL
MV4-11
DC50
nM
260
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P61964
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0064
Homo sapiens
10.1126/scitranslmed.abj1578
Degradation of WDR5 in MV4;11 cells after 18 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...
11
false
1,439
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCC(=O)NCCN2CCN(Cc3cccc(-c4ccc(N5CCN(C)CC5)c(NC(=O)c5c[nH]c(=O)cc5C(F)(F)F)c4)c3)CC2)C(C)(C)C)cc1
WDR5
MATEEKKPETEAARAQPTPSSSATQSKPTPVKPNYALKFTLAGHTKAVSSVKFSPNGEWLASSSADKLIKIWGAYDGKFEKTISGHKLGISDVAWSSDSNLLVSASDDKTLKIWDVSSGKCLKTLKGHSNYVFCCNFNPQSNLIVSGSFDESVRIWDVKTGKCLKTLPAHSDPVSAVHFNRDGSLIVSSSYDGLCRIWDTASGQCLKTLIDDDNPPVSFVKFSPNGKYILAATLDNTLKLWDYSKGKCLKTYTGHKNEKYCIFANFSVTGGKWIVSGSEDNLVYIWNLQTKEIVQKLQGHTDVVISTACHPTENIIASAA...
VHL
MV4-11
Dmax
%
71
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P61964
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0064
Homo sapiens
10.1126/scitranslmed.abj1578
Degradation of WDR5 in MV4;11 cells after 18 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...
11
false
1,439
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCC(=O)Nc2ccc(C(=O)Nc3ccccc3N)cc2)C(C)(C)C)cc1
HDAC1
MAQTQGTRRKVCYYYDGDVGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKANAEEMTKYHSDDYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVASAVKLNKQQTDIAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHHGDGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNYPLRDGIDDESYEAIFKPVMSKVMEMFQPSAVVLQCGSDSLSGDRLGCFNLTIKGHAKCVEFVKSFNLPMLMLGGGGYTIRNVARCWTYETAVAL...
VHL
HCT 116
Dmax
%
67
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q13547
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC1 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
17
false
1,440
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCC(=O)Nc2ccc(C(=O)Nc3ccccc3N)cc2)C(C)(C)C)cc1
HDAC2
MAYSQGGGKKKVCYYYDGDIGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKATAEEMTKYHSDEYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVAGAVKLNRQQTDMAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHHGDGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNFPMRDGIDDESYGQIFKPIISKVMEMYQPSAVVLQCGADSLSGDRLGCFNLTVKGHAKCVEVVKTFNLPLLMLGGGGYTIRNVARCWTYETAVA...
VHL
HCT 116
Dmax
%
43
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q92769
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC2 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
18
false
1,440
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCC(=O)Nc2ccc(C(=O)Nc3ccccc3N)cc2)C(C)(C)C)cc1
HDAC3
MAKTVAYFYDPDVGNFHYGAGHPMKPHRLALTHSLVLHYGLYKKMIVFKPYQASQHDMCRFHSEDYIDFLQRVSPTNMQGFTKSLNAFNVGDDCPVFPGLFEFCSRYTGASLQGATQLNNKICDIAINWAGGLHHAKKFEASGFCYVNDIVIGILELLKYHPRVLYIDIDIHHGDGVQEAFYLTDRVMTVSFHKYGNYFFPGTGDMYEVGAESGRYYCLNVPLRDGIDDQSYKHLFQPVINQVVDFYQPTCIVLQCGADSLGCDRLGCFNLSIRGHGECVEYVKSFNIPLLVLGGGGYTVRNVARCWTYETSLLVEEAIS...
VHL
HCT 116
Dmax
%
33
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O15379
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC3 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
13
false
1,440
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCC(=O)Nc2ccc(C(=O)Nc3cc(-c4cccs4)ccc3N)cc2)C(C)(C)C)cc1
HDAC1
MAQTQGTRRKVCYYYDGDVGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKANAEEMTKYHSDDYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVASAVKLNKQQTDIAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHHGDGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNYPLRDGIDDESYEAIFKPVMSKVMEMFQPSAVVLQCGSDSLSGDRLGCFNLTIKGHAKCVEFVKSFNLPMLMLGGGGYTIRNVARCWTYETAVAL...
VHL
HCT 116
Dmax
%
26
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q13547
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC1 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
17
false
1,441
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCC(=O)Nc2ccc(C(=O)Nc3cc(-c4cccs4)ccc3N)cc2)C(C)(C)C)cc1
HDAC2
MAYSQGGGKKKVCYYYDGDIGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKATAEEMTKYHSDEYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVAGAVKLNRQQTDMAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHHGDGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNFPMRDGIDDESYGQIFKPIISKVMEMYQPSAVVLQCGADSLSGDRLGCFNLTVKGHAKCVEVVKTFNLPLLMLGGGGYTIRNVARCWTYETAVA...
VHL
HCT 116
Dmax
%
15
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q92769
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC2 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
18
false
1,441
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCC(=O)Nc2ccc(C(=O)Nc3cc(-c4cccs4)ccc3N)cc2)C(C)(C)C)cc1
HDAC3
MAKTVAYFYDPDVGNFHYGAGHPMKPHRLALTHSLVLHYGLYKKMIVFKPYQASQHDMCRFHSEDYIDFLQRVSPTNMQGFTKSLNAFNVGDDCPVFPGLFEFCSRYTGASLQGATQLNNKICDIAINWAGGLHHAKKFEASGFCYVNDIVIGILELLKYHPRVLYIDIDIHHGDGVQEAFYLTDRVMTVSFHKYGNYFFPGTGDMYEVGAESGRYYCLNVPLRDGIDDQSYKHLFQPVINQVVDFYQPTCIVLQCGADSLGCDRLGCFNLSIRGHGECVEYVKSFNIPLLVLGGGGYTVRNVARCWTYETSLLVEEAIS...
VHL
HCT 116
Dmax
%
10
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O15379
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC3 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
13
false
1,441
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCC(=O)Nc2ccc(C(=O)Nc3ccc(F)cc3N)cc2)C(C)(C)C)cc1
HDAC1
MAQTQGTRRKVCYYYDGDVGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKANAEEMTKYHSDDYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVASAVKLNKQQTDIAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHHGDGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNYPLRDGIDDESYEAIFKPVMSKVMEMFQPSAVVLQCGSDSLSGDRLGCFNLTIKGHAKCVEFVKSFNLPMLMLGGGGYTIRNVARCWTYETAVAL...
VHL
HCT 116
Dmax
%
61
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q13547
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC1 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
17
false
1,442
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCC(=O)Nc2ccc(C(=O)Nc3ccc(F)cc3N)cc2)C(C)(C)C)cc1
HDAC2
MAYSQGGGKKKVCYYYDGDIGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKATAEEMTKYHSDEYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVAGAVKLNRQQTDMAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHHGDGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNFPMRDGIDDESYGQIFKPIISKVMEMYQPSAVVLQCGADSLSGDRLGCFNLTVKGHAKCVEVVKTFNLPLLMLGGGGYTIRNVARCWTYETAVA...
VHL
HCT 116
Dmax
%
26
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q92769
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC2 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
18
false
1,442
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCC(=O)Nc2ccc(C(=O)Nc3ccc(F)cc3N)cc2)C(C)(C)C)cc1
HDAC3
MAKTVAYFYDPDVGNFHYGAGHPMKPHRLALTHSLVLHYGLYKKMIVFKPYQASQHDMCRFHSEDYIDFLQRVSPTNMQGFTKSLNAFNVGDDCPVFPGLFEFCSRYTGASLQGATQLNNKICDIAINWAGGLHHAKKFEASGFCYVNDIVIGILELLKYHPRVLYIDIDIHHGDGVQEAFYLTDRVMTVSFHKYGNYFFPGTGDMYEVGAESGRYYCLNVPLRDGIDDQSYKHLFQPVINQVVDFYQPTCIVLQCGADSLGCDRLGCFNLSIRGHGECVEYVKSFNIPLLVLGGGGYTVRNVARCWTYETSLLVEEAIS...
VHL
HCT 116
Dmax
%
51
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O15379
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC3 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
13
false
1,442
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCC(=O)Nc2ccc(C(=O)Nc3ccccc3N)cc2)C(C)(C)C)cc1
HDAC1
MAQTQGTKRKVCYYYDGDVGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKANAEEMTKYHSDDYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVASAVKLNKQQTDIAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHHGDGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNYPLRDGIDDESYEAIFKPVMSKVMEMFQPSAVVLQCGSDSLSGDRLGCFNLTIKGHAKCVEFVKSFNLPMLMLGGGGYTIRNVARCWTYETAVAL...
VHL
ES-E14TG2a
Dmax
%
85
null
null
null
null
24
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
O09106
P40338
MPRKAASPEEAAGEPGPEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPLWLNFDGEPQPYPILPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDYPSVRKDIQRLSQEHLESQHLEEEP
CVCL_9108
Mus musculus
https://pubmed.ncbi.nlm.nih.gov/32201871/
For HDAC1/HDAC2/HDAC3, the Dmax of this PROTAC is: >85%, >76%, >63%, respectively.
PROTACpedia
null
null
CVCL_C320 ! ES-E14 129P2/Ola. In situ; Blastocyst; Embryonic stem cell; CL=CL_0002322. ChEBI; CHEBI_9555; Tioguanine (6-thioguanine; 6-TG). Embryonic stem cell
17
false
1,442
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCC(=O)Nc2ccc(C(=O)Nc3ccccc3N)cc2)C(C)(C)C)cc1
HDAC2
MAYSQGGGKKKVCYYYDGDIGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKATAEEMTKYHSDEYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVAGAVKLNRQQTDMAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHHGDGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNFPMRDGIDDESYGQIFKPIISKVMEMYQPSAVVLQCGADSLSGDRLGCFNLTVKGHAKCVEVAKTFNLPLLMLGGGGYTIRNVARCWTYETAVA...
VHL
ES-E14TG2a
Dmax
%
76
null
null
null
null
24
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P70288
P40338
MPRKAASPEEAAGEPGPEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPLWLNFDGEPQPYPILPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDYPSVRKDIQRLSQEHLESQHLEEEP
CVCL_9108
Mus musculus
https://pubmed.ncbi.nlm.nih.gov/32201871/
For HDAC1/HDAC2/HDAC3, the Dmax of this PROTAC is: >85%, >76%, >63%, respectively.
PROTACpedia
null
null
CVCL_C320 ! ES-E14 129P2/Ola. In situ; Blastocyst; Embryonic stem cell; CL=CL_0002322. ChEBI; CHEBI_9555; Tioguanine (6-thioguanine; 6-TG). Embryonic stem cell
18
false
1,442
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCC(=O)Nc2ccc(C(=O)Nc3ccccc3N)cc2)C(C)(C)C)cc1
HDAC3
MAKTVAYFYDPDVGNFHYGAGHPMKPHRLALTHSLVLHYGLYKKMIVFKPYQASQHDMCRFHSEDYIDFLQRVSPTNMQGFTKSLNAFNVGDDCPVFPGLFEFCSRYTGASLQGATQLNNKICDIAINWAGGLHHAKKFEASGFCYVNDIVIGILELLKYHPRVLYIDIDIHHGDGVQEAFYLTDRVMTVSFHKYGNYFFPGTGDMYEVGAESGRYYCLNVPLRDGIDDQSYKHLFQPVISQVVDFYQPTCIVLQCGADSLGCDRLGCFNLSIRGHGECVEYVKSFNIPLLVLGGGGYTVRNVARCWTYETSLLVEEAIS...
VHL
ES-E14TG2a
Dmax
%
63
null
null
null
null
24
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
O88895
P40338
MPRKAASPEEAAGEPGPEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPLWLNFDGEPQPYPILPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDYPSVRKDIQRLSQEHLESQHLEEEP
CVCL_9108
Mus musculus
https://pubmed.ncbi.nlm.nih.gov/32201871/
For HDAC1/HDAC2/HDAC3, the Dmax of this PROTAC is: >85%, >76%, >63%, respectively.
PROTACpedia
null
null
CVCL_C320 ! ES-E14 129P2/Ola. In situ; Blastocyst; Embryonic stem cell; CL=CL_0002322. ChEBI; CHEBI_9555; Tioguanine (6-thioguanine; 6-TG). Embryonic stem cell
13
false
1,442
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCC(=O)Nc2ccc(C(=O)Nc3ccccc3N)cc2)C(C)(C)C)cc1
Scn11a
MEERYYPVIFPDERNFRPFTFDSLAAIEKRITIQKEKKKSKDKAATEPQPRPQLDLKASRKLPKLYGDVPPDLIAKPLEDLDPFYKDHKTFMVLNKKRTIYRFSAKRALFILGPFNPIRSFMIRISVHSVFSMFIICTVIINCMFMANNSSVDSRPSSNIPEYVFIGIYVLEAVIKILARGFIVDEFSYLRDPWNWLDFIVIGTAIAPCFLGNKVNNLSTLRTFRVLRALKAISVISGLKVIVGALLRSVKKLVDVMVLTLFCLSIFALVGQQLFMGILSQKCIKDDCGPNAFSNKDCFVKENDSEDFIMCGNWLGRRSC...
VHL
ES-E14TG2a
DC50
nM
1,000
null
null
null
null
24
~
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q9R053
P40338
MPRKAASPEEAAGEPGPEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPLWLNFDGEPQPYPILPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDYPSVRKDIQRLSQEHLESQHLEEEP
CVCL_9108
Mus musculus
https://pubmed.ncbi.nlm.nih.gov/32201871/
For HDAC1/HDAC2/HDAC3, the Dmax of this PROTAC is: >85%, >76%, >63%, respectively.
PROTACpedia
null
null
CVCL_C320 ! ES-E14 129P2/Ola. In situ; Blastocyst; Embryonic stem cell; CL=CL_0002322. ChEBI; CHEBI_9555; Tioguanine (6-thioguanine; 6-TG). Embryonic stem cell
0
false
1,442
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCCCC(=O)Nc2ccc(C(=O)Nc3ccccc3N)cc2)C(C)(C)C)cc1
HDAC1
MAQTQGTRRKVCYYYDGDVGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKANAEEMTKYHSDDYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVASAVKLNKQQTDIAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHHGDGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNYPLRDGIDDESYEAIFKPVMSKVMEMFQPSAVVLQCGSDSLSGDRLGCFNLTIKGHAKCVEFVKSFNLPMLMLGGGGYTIRNVARCWTYETAVAL...
VHL
HCT 116
Dmax
%
63
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q13547
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC1 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
17
false
1,443
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCCCC(=O)Nc2ccc(C(=O)Nc3ccccc3N)cc2)C(C)(C)C)cc1
HDAC2
MAYSQGGGKKKVCYYYDGDIGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKATAEEMTKYHSDEYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVAGAVKLNRQQTDMAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHHGDGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNFPMRDGIDDESYGQIFKPIISKVMEMYQPSAVVLQCGADSLSGDRLGCFNLTVKGHAKCVEVVKTFNLPLLMLGGGGYTIRNVARCWTYETAVA...
VHL
HCT 116
Dmax
%
44
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q92769
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC2 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
18
false
1,443
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCCCC(=O)Nc2ccc(C(=O)Nc3ccccc3N)cc2)C(C)(C)C)cc1
HDAC3
MAKTVAYFYDPDVGNFHYGAGHPMKPHRLALTHSLVLHYGLYKKMIVFKPYQASQHDMCRFHSEDYIDFLQRVSPTNMQGFTKSLNAFNVGDDCPVFPGLFEFCSRYTGASLQGATQLNNKICDIAINWAGGLHHAKKFEASGFCYVNDIVIGILELLKYHPRVLYIDIDIHHGDGVQEAFYLTDRVMTVSFHKYGNYFFPGTGDMYEVGAESGRYYCLNVPLRDGIDDQSYKHLFQPVINQVVDFYQPTCIVLQCGADSLGCDRLGCFNLSIRGHGECVEYVKSFNIPLLVLGGGGYTVRNVARCWTYETSLLVEEAIS...
VHL
HCT 116
Dmax
%
44
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O15379
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0291
Homo sapiens
10.1021/acs.jmedchem.1c02179
Degradation of HDAC3 in HCT116 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
13
false
1,443
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCCNC(=O)c2ccc(N3C(=S)N(c4ccc(C#N)c(C(F)(F)F)c4)C(=O)C3(C)C)cc2F)C(C)(C)C)cc1
AR
MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL...
VHL
LNCaP
Dmax
%
75
null
null
null
null
6
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P10275
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0395
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30629437/
EC50 of ligand is LNCaP 25 nM, VCaP 87.4 nM, 22RV1 > 10 uM
PROTACpedia
null
null
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
1,444
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCNC(=O)CNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C(C)(C)C)cc1
CRBN
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
VHL
HEK293T
DC50
nM
28.8
null
null
null
null
24
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q96SW2
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0063
Homo sapiens
10.1038/s41598-019-56177-5; https://pubmed.ncbi.nlm.nih.gov/31873151/
Degradation of CRBN in HEK293T cells after 24h treatment
PROTAC-DB; PROTACpedia
null
null
Highly susceptible to infection by Zika virus (ZIKV). CVCL_0045 ! HEK293 In situ; Fetal kidney; NCBI_TaxID; 28285; Human adenovirus C serotype 5. NCBI_TaxID; 1891767; Simian virus 40 (SV40) (Note=tsA). Transformed cell line
-1
false
1,445
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCNC(=O)CNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C(C)(C)C)cc1
CRBN
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
VHL
HEK293T
Dmax
%
98.4
null
null
null
null
24
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q96SW2
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0063
Homo sapiens
10.1038/s41598-019-56177-5; https://pubmed.ncbi.nlm.nih.gov/31873151/
Degradation of CRBN in HEK293T cells after 24h treatment
PROTAC-DB; PROTACpedia
null
null
Highly susceptible to infection by Zika virus (ZIKV). CVCL_0045 ! HEK293 In situ; Fetal kidney; NCBI_TaxID; 28285; Human adenovirus C serotype 5. NCBI_TaxID; 1891767; Simian virus 40 (SV40) (Note=tsA). Transformed cell line
-1
false
1,445
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCNC(=O)COc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C(C)(C)C)cc1
CRBN
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
VHL
HEK293T
DC50
nM
367.7
null
null
null
null
24
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q96SW2
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0063
Homo sapiens
10.1038/s41598-019-56177-5; https://pubmed.ncbi.nlm.nih.gov/31873151/
Degradation of CRBN in HEK293T cells after 24h treatment
PROTAC-DB; PROTACpedia
null
null
Highly susceptible to infection by Zika virus (ZIKV). CVCL_0045 ! HEK293 In situ; Fetal kidney; NCBI_TaxID; 28285; Human adenovirus C serotype 5. NCBI_TaxID; 1891767; Simian virus 40 (SV40) (Note=tsA). Transformed cell line
-1
false
1,446
0
Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCNC(=O)COc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)C(C)(C)C)cc1
CRBN
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
VHL
HEK293T
Dmax
%
82
null
null
null
null
24
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q96SW2
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0063
Homo sapiens
10.1038/s41598-019-56177-5; https://pubmed.ncbi.nlm.nih.gov/31873151/
Degradation of CRBN in HEK293T cells after 24h treatment
PROTAC-DB; PROTACpedia
null
null
Highly susceptible to infection by Zika virus (ZIKV). CVCL_0045 ! HEK293 In situ; Fetal kidney; NCBI_TaxID; 28285; Human adenovirus C serotype 5. NCBI_TaxID; 1891767; Simian virus 40 (SV40) (Note=tsA). Transformed cell line
-1
false
1,446
0