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([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCCN(C)CCOC23CC4(C)CC(C)(CC(Cn5ncc(-c6ccc(N7CCCc8c7nnc(Nc7nc9ccccc9s7)c8C)nc6C(=O)O)c5C)(C4)C2)C3)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
HCT 116
DC50
nM
0.286
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-USLYHX
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
1,703
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCCN(C)CCOC23CC4(C)CC(C)(CC(Cn5ncc(-c6ccc(N7CCCc8c7nnc(Nc7nc9ccccc9s7)c8C)nc6C(=O)O)c5C)(C4)C2)C3)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
NCI-H1650
DC50
nM
1
null
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-USLYHX
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
1,703
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
SW1573
DC50
nM
116
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-KR9P9M
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
1,704
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
SW1573
Dmax
%
75
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-KR9P9M
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
1,704
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
SW1573
DC50
nM
10,000
null
null
null
null
null
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-KR9P9M
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
1,704
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
SW1573
Dmax
%
17
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-KR9P9M
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
1,704
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCCNC(=O)c2nc(N3CCCc4c3nnc(Nc3nc5ccccc5s3)c4C)ccc2-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN3CCCC3)(C5)C4)c2C)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
HCT 116
DC50
nM
1.34
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-1TY9B7
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
1,705
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCCNC(=O)c2nc(N3CCCc4c3nnc(Nc3nc5ccccc5s3)c4C)ccc2-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN3CCCC3)(C5)C4)c2C)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
NCI-H1650
DC50
nM
1
null
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-1TY9B7
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
1,705
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCCNCCCCONC(=O)c2ccc(F)c(F)c2Nc2ccc(I)cc2F)C(C)(C)C)cc1
MEK1
MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKVGELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYLREKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHYSVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSYGMDSRPPMAIFELLDYIVNE...
VHL
HT-29
DC50
nM
18
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q02750
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0320
Homo sapiens
10.1021/acs.jmedchem.0c01609
Degradation of MEK1 in HT-29/SK-MEL-28 cells after 24 h treatment
PROTAC-DB
null
null
African=1.57%; Native American=1.05%; East Asian, North=3.24%; East Asian, South=0%; South Asian=4.8%; European, North=26.11%; European, South=63.24%. Hypertriploid karyotype. Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19). Indicated in PubMed=11921276 as originating from an adenocarcinoma o...
26
false
1,706
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCCNCCCCONC(=O)c2ccc(F)c(F)c2Nc2ccc(I)cc2F)C(C)(C)C)cc1
MEK1
MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKVGELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYLREKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHYSVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSYGMDSRPPMAIFELLDYIVNE...
VHL
SK-MEL-28
DC50
nM
10
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q02750
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0526
Homo sapiens
10.1021/acs.jmedchem.0c01609
Degradation of MEK1 in HT-29/SK-MEL-28 cells after 24 h treatment
PROTAC-DB
null
null
African=1.75%; Native American=0.56%; East Asian, North=3%; East Asian, South=1.38%; South Asian=8.29%; European, North=20.11%; European, South=64.91%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Lightly pigmented. A*11 A*11 A*11 Stable (...
26
false
1,706
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCCNCCCCONC(=O)c2ccc(F)c(F)c2Nc2ccc(I)cc2F)C(C)(C)C)cc1
MEK2
MLARRKPVLPALTINPTIAEGPSPTSEGASEANLVDLQKKLEELELDEQQKKRLEAFLTQKAKVGELKDDDFERISELGAGNGGVVTKVQHRPSGLIMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKEAKRIPEEILGKVSIAVLRGLAYLREKHQIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMAPERLQGTHYSVQSDIWSMGLSLVELAVGRYPIPPPDAKELEAIFGRPVVDGEEGEPHSISPRPRPPGRPVSGHGMDSRPAMAIFE...
VHL
HT-29
DC50
nM
9
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P36507
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0320
Homo sapiens
10.1021/acs.jmedchem.0c01609
Degradation of MEK2 in HT-29/SK-MEL-28 cells after 24 h treatment
PROTAC-DB
null
null
African=1.57%; Native American=1.05%; East Asian, North=3.24%; East Asian, South=0%; South Asian=4.8%; European, North=26.11%; European, South=63.24%. Hypertriploid karyotype. Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19). Indicated in PubMed=11921276 as originating from an adenocarcinoma o...
26
false
1,706
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCCNCCCCONC(=O)c2ccc(F)c(F)c2Nc2ccc(I)cc2F)C(C)(C)C)cc1
MEK2
MLARRKPVLPALTINPTIAEGPSPTSEGASEANLVDLQKKLEELELDEQQKKRLEAFLTQKAKVGELKDDDFERISELGAGNGGVVTKVQHRPSGLIMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKEAKRIPEEILGKVSIAVLRGLAYLREKHQIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMAPERLQGTHYSVQSDIWSMGLSLVELAVGRYPIPPPDAKELEAIFGRPVVDGEEGEPHSISPRPRPPGRPVSGHGMDSRPAMAIFE...
VHL
SK-MEL-28
DC50
nM
4
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P36507
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0526
Homo sapiens
10.1021/acs.jmedchem.0c01609
Degradation of MEK2 in HT-29/SK-MEL-28 cells after 24 h treatment
PROTAC-DB
null
null
African=1.75%; Native American=0.56%; East Asian, North=3%; East Asian, South=1.38%; South Asian=8.29%; European, North=20.11%; European, South=64.91%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Lightly pigmented. A*11 A*11 A*11 Stable (...
26
false
1,706
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCN(C)CCCONC(=O)c2ccc(F)c(F)c2Nc2ccc(I)cc2F)C(C)(C)C)cc1
MEK1
MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKVGELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYLREKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHYSVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSYGMDSRPPMAIFELLDYIVNE...
VHL
HT-29
DC50
nM
18
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q02750
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0320
Homo sapiens
10.1021/acs.jmedchem.0c01609
Degradation of MEK1 in HT-29/SK-MEL-28 cells after 24 h treatment
PROTAC-DB
null
null
African=1.57%; Native American=1.05%; East Asian, North=3.24%; East Asian, South=0%; South Asian=4.8%; European, North=26.11%; European, South=63.24%. Hypertriploid karyotype. Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19). Indicated in PubMed=11921276 as originating from an adenocarcinoma o...
26
false
1,707
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCN(C)CCCONC(=O)c2ccc(F)c(F)c2Nc2ccc(I)cc2F)C(C)(C)C)cc1
MEK1
MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKVGELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYLREKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHYSVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSYGMDSRPPMAIFELLDYIVNE...
VHL
SK-MEL-28
DC50
nM
16
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q02750
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0526
Homo sapiens
10.1021/acs.jmedchem.0c01609
Degradation of MEK1 in HT-29/SK-MEL-28 cells after 24 h treatment
PROTAC-DB
null
null
African=1.75%; Native American=0.56%; East Asian, North=3%; East Asian, South=1.38%; South Asian=8.29%; European, North=20.11%; European, South=64.91%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Lightly pigmented. A*11 A*11 A*11 Stable (...
26
false
1,707
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCN(C)CCCONC(=O)c2ccc(F)c(F)c2Nc2ccc(I)cc2F)C(C)(C)C)cc1
MEK2
MLARRKPVLPALTINPTIAEGPSPTSEGASEANLVDLQKKLEELELDEQQKKRLEAFLTQKAKVGELKDDDFERISELGAGNGGVVTKVQHRPSGLIMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKEAKRIPEEILGKVSIAVLRGLAYLREKHQIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMAPERLQGTHYSVQSDIWSMGLSLVELAVGRYPIPPPDAKELEAIFGRPVVDGEEGEPHSISPRPRPPGRPVSGHGMDSRPAMAIFE...
VHL
HT-29
DC50
nM
8
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P36507
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0320
Homo sapiens
10.1021/acs.jmedchem.0c01609
Degradation of MEK2 in HT-29/SK-MEL-28 cells after 24 h treatment
PROTAC-DB
null
null
African=1.57%; Native American=1.05%; East Asian, North=3.24%; East Asian, South=0%; South Asian=4.8%; European, North=26.11%; European, South=63.24%. Hypertriploid karyotype. Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19). Indicated in PubMed=11921276 as originating from an adenocarcinoma o...
26
false
1,707
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCN(C)CCCONC(=O)c2ccc(F)c(F)c2Nc2ccc(I)cc2F)C(C)(C)C)cc1
MEK2
MLARRKPVLPALTINPTIAEGPSPTSEGASEANLVDLQKKLEELELDEQQKKRLEAFLTQKAKVGELKDDDFERISELGAGNGGVVTKVQHRPSGLIMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKEAKRIPEEILGKVSIAVLRGLAYLREKHQIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMAPERLQGTHYSVQSDIWSMGLSLVELAVGRYPIPPPDAKELEAIFGRPVVDGEEGEPHSISPRPRPPGRPVSGHGMDSRPAMAIFE...
VHL
SK-MEL-28
DC50
nM
6
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P36507
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0526
Homo sapiens
10.1021/acs.jmedchem.0c01609
Degradation of MEK2 in HT-29/SK-MEL-28 cells after 24 h treatment
PROTAC-DB
null
null
African=1.75%; Native American=0.56%; East Asian, North=3%; East Asian, South=1.38%; South Asian=8.29%; European, North=20.11%; European, South=64.91%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Lightly pigmented. A*11 A*11 A*11 Stable (...
26
false
1,707
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCN(C)CCOC23CC4(C)CC(C)(CC(Cn5ncc(-c6ccc(N7CCCc8c7nnc(Nc7nc9ccccc9s7)c8C)nc6C(=O)O)c5C)(C4)C2)C3)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
HCT 116
DC50
nM
0.978
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-K2HKNI
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
1,708
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCN(C)CCOC23CC4(C)CC(C)(CC(Cn5ncc(-c6ccc(N7CCCc8c7nnc(Nc7nc9ccccc9s7)c8C)nc6C(=O)O)c5C)(C4)C2)C3)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
NCI-H1650
DC50
nM
1
null
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-K2HKNI
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
1,708
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
SW1573
DC50
nM
139
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-KQH4VJ
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
1,709
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
SW1573
Dmax
%
78
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-KQH4VJ
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
1,709
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
SW1573
DC50
nM
10,000
null
null
null
null
null
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-KQH4VJ
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
1,709
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
SW1573
Dmax
%
1.2
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-KQH4VJ
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
1,709
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCNC(=O)c2nc(N3CCCc4c3nnc(Nc3nc5ccccc5s3)c4C)ccc2-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN3CCCC3)(C5)C4)c2C)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
HCT 116
DC50
nM
0.487
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-4A3RX9
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
1,710
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCNC(=O)c2nc(N3CCCc4c3nnc(Nc3nc5ccccc5s3)c4C)ccc2-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN3CCCC3)(C5)C4)c2C)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
NCI-H1650
DC50
nM
1
null
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-4A3RX9
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
1,710
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCNCCCONC(=O)c2ccc(F)c(F)c2Nc2ccc(I)cc2F)C(C)(C)C)cc1
MEK1
MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKVGELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYLREKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHYSVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSYGMDSRPPMAIFELLDYIVNE...
VHL
COLO 205
DC50
nM
18
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q02750
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0218
Homo sapiens
10.1021/acs.jmedchem.9b01528
Degradation of MEK1 in HT-29/SK-MEL-28/COLO 205 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=2.08%; East Asian, South=0%; South Asian=0%; European, North=61.39%; European, South=36.53%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*01,02; B*07,08; C*07 A*01 A*01 Stable (MSS). Metastatic; Ascites; Caucasian. Cancer cell l...
26
false
1,707
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCNCCCONC(=O)c2ccc(F)c(F)c2Nc2ccc(I)cc2F)C(C)(C)C)cc1
MEK1
MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKVGELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYLREKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHYSVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSYGMDSRPPMAIFELLDYIVNE...
VHL
HT-29
DC50
nM
31
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q02750
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0320
Homo sapiens
10.1021/acs.jmedchem.9b01528
Degradation of MEK1 in HT-29/SK-MEL-28/COLO 205 cells after 24 h treatment
PROTAC-DB
null
null
African=1.57%; Native American=1.05%; East Asian, North=3.24%; East Asian, South=0%; South Asian=4.8%; European, North=26.11%; European, South=63.24%. Hypertriploid karyotype. Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19). Indicated in PubMed=11921276 as originating from an adenocarcinoma o...
26
false
1,707
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCNCCCONC(=O)c2ccc(F)c(F)c2Nc2ccc(I)cc2F)C(C)(C)C)cc1
MEK1
MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKVGELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYLREKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHYSVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSYGMDSRPPMAIFELLDYIVNE...
VHL
SK-MEL-28
DC50
nM
31
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q02750
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0526
Homo sapiens
10.1021/acs.jmedchem.9b01528
Degradation of MEK1 in HT-29/SK-MEL-28/COLO 205 cells after 24 h treatment
PROTAC-DB
null
null
African=1.75%; Native American=0.56%; East Asian, North=3%; East Asian, South=1.38%; South Asian=8.29%; European, North=20.11%; European, South=64.91%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Lightly pigmented. A*11 A*11 A*11 Stable (...
26
false
1,707
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCNCCCONC(=O)c2ccc(F)c(F)c2Nc2ccc(I)cc2F)C(C)(C)C)cc1
MEK2
MLARRKPVLPALTINPTIAEGPSPTSEGASEANLVDLQKKLEELELDEQQKKRLEAFLTQKAKVGELKDDDFERISELGAGNGGVVTKVQHRPSGLIMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKEAKRIPEEILGKVSIAVLRGLAYLREKHQIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMAPERLQGTHYSVQSDIWSMGLSLVELAVGRYPIPPPDAKELEAIFGRPVVDGEEGEPHSISPRPRPPGRPVSGHGMDSRPAMAIFE...
VHL
COLO 205
DC50
nM
11
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P36507
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0218
Homo sapiens
10.1021/acs.jmedchem.9b01528
Degradation of MEK2 in HT-29/SK-MEL-28/COLO 205 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=2.08%; East Asian, South=0%; South Asian=0%; European, North=61.39%; European, South=36.53%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*01,02; B*07,08; C*07 A*01 A*01 Stable (MSS). Metastatic; Ascites; Caucasian. Cancer cell l...
26
false
1,707
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCNCCCONC(=O)c2ccc(F)c(F)c2Nc2ccc(I)cc2F)C(C)(C)C)cc1
MEK2
MLARRKPVLPALTINPTIAEGPSPTSEGASEANLVDLQKKLEELELDEQQKKRLEAFLTQKAKVGELKDDDFERISELGAGNGGVVTKVQHRPSGLIMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKEAKRIPEEILGKVSIAVLRGLAYLREKHQIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMAPERLQGTHYSVQSDIWSMGLSLVELAVGRYPIPPPDAKELEAIFGRPVVDGEEGEPHSISPRPRPPGRPVSGHGMDSRPAMAIFE...
VHL
HT-29
DC50
nM
17
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P36507
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0320
Homo sapiens
10.1021/acs.jmedchem.9b01528
Degradation of MEK2 in HT-29/SK-MEL-28/COLO 205 cells after 24 h treatment
PROTAC-DB
null
null
African=1.57%; Native American=1.05%; East Asian, North=3.24%; East Asian, South=0%; South Asian=4.8%; European, North=26.11%; European, South=63.24%. Hypertriploid karyotype. Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19). Indicated in PubMed=11921276 as originating from an adenocarcinoma o...
26
false
1,707
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCCNCCCONC(=O)c2ccc(F)c(F)c2Nc2ccc(I)cc2F)C(C)(C)C)cc1
MEK2
MLARRKPVLPALTINPTIAEGPSPTSEGASEANLVDLQKKLEELELDEQQKKRLEAFLTQKAKVGELKDDDFERISELGAGNGGVVTKVQHRPSGLIMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKEAKRIPEEILGKVSIAVLRGLAYLREKHQIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMAPERLQGTHYSVQSDIWSMGLSLVELAVGRYPIPPPDAKELEAIFGRPVVDGEEGEPHSISPRPRPPGRPVSGHGMDSRPAMAIFE...
VHL
SK-MEL-28
DC50
nM
9.3
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P36507
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0526
Homo sapiens
10.1021/acs.jmedchem.9b01528
Degradation of MEK2 in HT-29/SK-MEL-28/COLO 205 cells after 24 h treatment
PROTAC-DB
null
null
African=1.75%; Native American=0.56%; East Asian, North=3%; East Asian, South=1.38%; South Asian=8.29%; European, North=20.11%; European, South=64.91%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Lightly pigmented. A*11 A*11 A*11 Stable (...
26
false
1,707
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCN(C)CCOC23CC4(C)CC(C)(CC(Cn5ncc(-c6ccc(N7CCCc8c7nnc(Nc7nc9ccccc9s7)c8C)nc6C(=O)O)c5C)(C4)C2)C3)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-TFR030
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
1,711
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
A-549
DC50
nM
188
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-4879XC
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
1,712
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
A-549
Dmax
%
70
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-4879XC
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
1,712
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
SW1573
DC50
nM
24
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-4879XC
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
1,712
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
SW1573
Dmax
%
93
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-4879XC
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
1,712
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
SW1573
DC50
nM
10,000
null
null
null
null
null
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-4879XC
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
1,712
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
SW1573
Dmax
%
17
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-4879XC
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
1,712
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCN2CCN(CC#Cc3ccc(OCCCc4sc(N5CCCc6c5nnc(Nc5nc7ccccc7s5)c6C)nc4C(=O)O)c(F)c3)CC2)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
HCT 116
DC50
nM
0.564
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-1DTE58
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
1,713
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCN2CCN(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
null
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-1DTE58
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
1,713
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCN2CCc3cc(O)c(N4CC(=O)NS4(=O)=O)c(F)c3CC2)C(C)(C)C)cc1
PTPN1
MEMEKEFEQIDKSGSWAAIYQDIRHEASDFPCRVAKLPKNKNRNRYRDVSPFDHSRIKLHQEDNDYINASLIKMEEAQRSYILTQGPLPNTCGHFWEMVWEQKSRGVVMLNRVMEKGSLKCAQYWPQKEEKEMIFEDTNLKLTLISEDIKSYYTVRQLELENLTTQETREILHFHYTTWPDFGVPESPASFLNFLFKVRESGSLSPEHGPVVVHCSAGIGRSGTFCLADTCLLLMDKRKDPSSVDIKKVLLEMRKFRMGLIQTADQLRFSYLAVIEGAKFIMGDSSVQDQWKELSHEDLEPPPEHIPPPPRPPKRILEPH...
VHL
Jurkat
DC50
nM
547
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P18031
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0065
Homo sapiens
PROTEIN TYROSINE PHOSPHATASE DEGRADERS AND USES THEREOF (patent)
Parental Jurkat cells (ATCC, TIB-152) were grown in complete RPMI medium consisting of RPMI 1640 Medium (Gibco, 61870036) supplemented with 10% fetal bovine serum (Gibco, 10082147) and 1x Pen Strep (Gibco, 15140122). The sequence encoding the HiBiT tag (Promega) was integrated into the 5' end of the coding sequence on ...
TPDdb
HiBiT
TPD-M2F6CY
African=0.4%; Native American=0%; East Asian, North=0.13%; East Asian, South=1.21%; South Asian=1.08%; European, North=70.73%; European, South=26.45%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC M...
14
false
1,714
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCN2CCc3cc(O)c(N4CC(=O)NS4(=O)=O)c(F)c3CC2)C(C)(C)C)cc1
PTPN1
MEMEKEFEQIDKSGSWAAIYQDIRHEASDFPCRVAKLPKNKNRNRYRDVSPFDHSRIKLHQEDNDYINASLIKMEEAQRSYILTQGPLPNTCGHFWEMVWEQKSRGVVMLNRVMEKGSLKCAQYWPQKEEKEMIFEDTNLKLTLISEDIKSYYTVRQLELENLTTQETREILHFHYTTWPDFGVPESPASFLNFLFKVRESGSLSPEHGPVVVHCSAGIGRSGTFCLADTCLLLMDKRKDPSSVDIKKVLLEMRKFRMGLIQTADQLRFSYLAVIEGAKFIMGDSSVQDQWKELSHEDLEPPPEHIPPPPRPPKRILEPH...
VHL
Jurkat
Dmax
%
89
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P18031
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0065
Homo sapiens
PROTEIN TYROSINE PHOSPHATASE DEGRADERS AND USES THEREOF (patent)
Parental Jurkat cells (ATCC, TIB-152) were grown in complete RPMI medium consisting of RPMI 1640 Medium (Gibco, 61870036) supplemented with 10% fetal bovine serum (Gibco, 10082147) and 1x Pen Strep (Gibco, 15140122). The sequence encoding the HiBiT tag (Promega) was integrated into the 5' end of the coding sequence on ...
TPDdb
HiBiT
TPD-M2F6CY
African=0.4%; Native American=0%; East Asian, North=0.13%; East Asian, South=1.21%; South Asian=1.08%; European, North=70.73%; European, South=26.45%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC M...
14
false
1,714
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCN2CCc3cc(O)c(N4CC(=O)NS4(=O)=O)c(F)c3CC2)C(C)(C)C)cc1
PTPN2
MPTTIEREFEELDTQRRWQPLYLEIRNESHDYPHRVAKFPENRNRNRYRDVSPYDHSRVKLQNAENDYINASLVDIEEAQRSYILTQGPLPNTCCHFWLMVWQQKTKAVVMLNRIVEKESVKCAQYWPTDDQEMLFKETGFSVKLLSEDVKSYYTVHLLQLENINSGETRTISHFHYTTWPDFGVPESPASFLNFLFKVRESGSLNPDHGPAVIHCSAGIGRSGTFSLVDTCLVLMEKGDDINIKQVLLNMRKYRMGLIQTPDQLRFSYMAIIEGAKCIKGDSSIQKRWKELSKEDLSPAFDHSPNKIMTEKYNGNRIGL...
VHL
Jurkat
DC50
nM
124
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P17706
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0065
Homo sapiens
PROTEIN TYROSINE PHOSPHATASE DEGRADERS AND USES THEREOF (patent)
Parental Jurkat cells (ATCC, TIB-152) were grown in complete RPMI medium consisting of RPMI 1640 Medium (Gibco, 61870036) supplemented with 10% fetal bovine serum (Gibco, 10082147) and 1x Pen Strep (Gibco, 15140122). The sequence encoding the HiBiT tag (Promega) was integrated into the 5' end of the coding sequence on ...
TPDdb
HiBiT
TPD-M2F6CY
African=0.4%; Native American=0%; East Asian, North=0.13%; East Asian, South=1.21%; South Asian=1.08%; European, North=70.73%; European, South=26.45%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC M...
14
false
1,714
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCN2CCc3cc(O)c(N4CC(=O)NS4(=O)=O)c(F)c3CC2)C(C)(C)C)cc1
PTPN2
MPTTIEREFEELDTQRRWQPLYLEIRNESHDYPHRVAKFPENRNRNRYRDVSPYDHSRVKLQNAENDYINASLVDIEEAQRSYILTQGPLPNTCCHFWLMVWQQKTKAVVMLNRIVEKESVKCAQYWPTDDQEMLFKETGFSVKLLSEDVKSYYTVHLLQLENINSGETRTISHFHYTTWPDFGVPESPASFLNFLFKVRESGSLNPDHGPAVIHCSAGIGRSGTFSLVDTCLVLMEKGDDINIKQVLLNMRKYRMGLIQTPDQLRFSYMAIIEGAKCIKGDSSIQKRWKELSKEDLSPAFDHSPNKIMTEKYNGNRIGL...
VHL
Jurkat
Dmax
%
98
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P17706
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0065
Homo sapiens
PROTEIN TYROSINE PHOSPHATASE DEGRADERS AND USES THEREOF (patent)
Parental Jurkat cells (ATCC, TIB-152) were grown in complete RPMI medium consisting of RPMI 1640 Medium (Gibco, 61870036) supplemented with 10% fetal bovine serum (Gibco, 10082147) and 1x Pen Strep (Gibco, 15140122). The sequence encoding the HiBiT tag (Promega) was integrated into the 5' end of the coding sequence on ...
TPDdb
HiBiT
TPD-M2F6CY
African=0.4%; Native American=0%; East Asian, North=0.13%; East Asian, South=1.21%; South Asian=1.08%; European, North=70.73%; European, South=26.45%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC M...
14
false
1,714
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCNC(=O)C[C@@H]2CCN(CCc3cc(O)c(N4CC(=O)NS4(=O)=O)c(F)c3)C2)C(C)(C)C)cc1
PTPN1
MEMEKEFEQIDKSGSWAAIYQDIRHEASDFPCRVAKLPKNKNRNRYRDVSPFDHSRIKLHQEDNDYINASLIKMEEAQRSYILTQGPLPNTCGHFWEMVWEQKSRGVVMLNRVMEKGSLKCAQYWPQKEEKEMIFEDTNLKLTLISEDIKSYYTVRQLELENLTTQETREILHFHYTTWPDFGVPESPASFLNFLFKVRESGSLSPEHGPVVVHCSAGIGRSGTFCLADTCLLLMDKRKDPSSVDIKKVLLEMRKFRMGLIQTADQLRFSYLAVIEGAKFIMGDSSVQDQWKELSHEDLEPPPEHIPPPPRPPKRILEPH...
VHL
Jurkat
DC50
nM
2,380
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P18031
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0065
Homo sapiens
PROTEIN TYROSINE PHOSPHATASE DEGRADERS AND USES THEREOF (patent)
Parental Jurkat cells (ATCC, TIB-152) were grown in complete RPMI medium consisting of RPMI 1640 Medium (Gibco, 61870036) supplemented with 10% fetal bovine serum (Gibco, 10082147) and 1x Pen Strep (Gibco, 15140122). The sequence encoding the HiBiT tag (Promega) was integrated into the 5' end of the coding sequence on ...
TPDdb
HiBiT
TPD-EGVTJ9
African=0.4%; Native American=0%; East Asian, North=0.13%; East Asian, South=1.21%; South Asian=1.08%; European, North=70.73%; European, South=26.45%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC M...
14
false
1,715
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCNC(=O)C[C@@H]2CCN(CCc3cc(O)c(N4CC(=O)NS4(=O)=O)c(F)c3)C2)C(C)(C)C)cc1
PTPN1
MEMEKEFEQIDKSGSWAAIYQDIRHEASDFPCRVAKLPKNKNRNRYRDVSPFDHSRIKLHQEDNDYINASLIKMEEAQRSYILTQGPLPNTCGHFWEMVWEQKSRGVVMLNRVMEKGSLKCAQYWPQKEEKEMIFEDTNLKLTLISEDIKSYYTVRQLELENLTTQETREILHFHYTTWPDFGVPESPASFLNFLFKVRESGSLSPEHGPVVVHCSAGIGRSGTFCLADTCLLLMDKRKDPSSVDIKKVLLEMRKFRMGLIQTADQLRFSYLAVIEGAKFIMGDSSVQDQWKELSHEDLEPPPEHIPPPPRPPKRILEPH...
VHL
Jurkat
Dmax
%
73
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P18031
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0065
Homo sapiens
PROTEIN TYROSINE PHOSPHATASE DEGRADERS AND USES THEREOF (patent)
Parental Jurkat cells (ATCC, TIB-152) were grown in complete RPMI medium consisting of RPMI 1640 Medium (Gibco, 61870036) supplemented with 10% fetal bovine serum (Gibco, 10082147) and 1x Pen Strep (Gibco, 15140122). The sequence encoding the HiBiT tag (Promega) was integrated into the 5' end of the coding sequence on ...
TPDdb
HiBiT
TPD-EGVTJ9
African=0.4%; Native American=0%; East Asian, North=0.13%; East Asian, South=1.21%; South Asian=1.08%; European, North=70.73%; European, South=26.45%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC M...
14
false
1,715
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCNC(=O)C[C@@H]2CCN(CCc3cc(O)c(N4CC(=O)NS4(=O)=O)c(F)c3)C2)C(C)(C)C)cc1
PTPN2
MPTTIEREFEELDTQRRWQPLYLEIRNESHDYPHRVAKFPENRNRNRYRDVSPYDHSRVKLQNAENDYINASLVDIEEAQRSYILTQGPLPNTCCHFWLMVWQQKTKAVVMLNRIVEKESVKCAQYWPTDDQEMLFKETGFSVKLLSEDVKSYYTVHLLQLENINSGETRTISHFHYTTWPDFGVPESPASFLNFLFKVRESGSLNPDHGPAVIHCSAGIGRSGTFSLVDTCLVLMEKGDDINIKQVLLNMRKYRMGLIQTPDQLRFSYMAIIEGAKCIKGDSSIQKRWKELSKEDLSPAFDHSPNKIMTEKYNGNRIGL...
VHL
Jurkat
DC50
nM
219
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P17706
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0065
Homo sapiens
PROTEIN TYROSINE PHOSPHATASE DEGRADERS AND USES THEREOF (patent)
Parental Jurkat cells (ATCC, TIB-152) were grown in complete RPMI medium consisting of RPMI 1640 Medium (Gibco, 61870036) supplemented with 10% fetal bovine serum (Gibco, 10082147) and 1x Pen Strep (Gibco, 15140122). The sequence encoding the HiBiT tag (Promega) was integrated into the 5' end of the coding sequence on ...
TPDdb
HiBiT
TPD-EGVTJ9
African=0.4%; Native American=0%; East Asian, North=0.13%; East Asian, South=1.21%; South Asian=1.08%; European, North=70.73%; European, South=26.45%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC M...
14
false
1,715
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCNC(=O)C[C@@H]2CCN(CCc3cc(O)c(N4CC(=O)NS4(=O)=O)c(F)c3)C2)C(C)(C)C)cc1
PTPN2
MPTTIEREFEELDTQRRWQPLYLEIRNESHDYPHRVAKFPENRNRNRYRDVSPYDHSRVKLQNAENDYINASLVDIEEAQRSYILTQGPLPNTCCHFWLMVWQQKTKAVVMLNRIVEKESVKCAQYWPTDDQEMLFKETGFSVKLLSEDVKSYYTVHLLQLENINSGETRTISHFHYTTWPDFGVPESPASFLNFLFKVRESGSLNPDHGPAVIHCSAGIGRSGTFSLVDTCLVLMEKGDDINIKQVLLNMRKYRMGLIQTPDQLRFSYMAIIEGAKCIKGDSSIQKRWKELSKEDLSPAFDHSPNKIMTEKYNGNRIGL...
VHL
Jurkat
Dmax
%
96
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P17706
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0065
Homo sapiens
PROTEIN TYROSINE PHOSPHATASE DEGRADERS AND USES THEREOF (patent)
Parental Jurkat cells (ATCC, TIB-152) were grown in complete RPMI medium consisting of RPMI 1640 Medium (Gibco, 61870036) supplemented with 10% fetal bovine serum (Gibco, 10082147) and 1x Pen Strep (Gibco, 15140122). The sequence encoding the HiBiT tag (Promega) was integrated into the 5' end of the coding sequence on ...
TPDdb
HiBiT
TPD-EGVTJ9
African=0.4%; Native American=0%; East Asian, North=0.13%; East Asian, South=1.21%; South Asian=1.08%; European, North=70.73%; European, South=26.45%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC M...
14
false
1,715
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCNC(=O)c2nc(N3CCCc4c3nnc(Nc3nc5ccccc5s3)c4C)ccc2-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN3CCCC3)(C5)C4)c2C)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
HCT 116
DC50
nM
0.857
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-ZDMI29
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
1,716
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCCNC(=O)c2nc(N3CCCc4c3nnc(Nc3nc5ccccc5s3)c4C)ccc2-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN3CCCC3)(C5)C4)c2C)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
NCI-H1650
DC50
nM
1
null
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-ZDMI29
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
1,716
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
A-549
DC50
nM
182
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-JYK5KB
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
1,717
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
A-549
Dmax
%
61
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-JYK5KB
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
1,717
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
SW1573
DC50
nM
45
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-JYK5KB
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
1,717
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
SW1573
Dmax
%
86
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-JYK5KB
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
1,717
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
SW1573
DC50
nM
10,000
null
null
null
null
null
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-JYK5KB
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
1,717
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCN2CCN(C(=O)CCC(=O)Nc3cccc(Sc4ncc(N5CCC(C)(N)CC5)nc4N)c3Cl)CC2)C(C)(C)C)cc1
SHP2
MTSRRWFHPNITGVEAENLLLTRGVDGSFLARPSKSNPGDFTLSVRRNGAVTHIKIQNTGDYYDLYGGEKFATLAELVQYYMEHHGQLKEKNGDVIELKYPLNCADPTSERWFHGHLSGKEAEKLLTEKGKHGSFLVRESQSHPGDFVLSVRTGDDKGESNDGKSKVTHVMIRCQELKYDVGGGERFDSLTDLVEHYKKNPMVETLGTVLQLKQPLNTTRINAAEIESRVRELSKLAETTDKVKQGFWEEFETLQQQECKLLYSRKEGQRQENKNKNRYKNILPFDHTRVVLHDGDPNEPVSDYINANIIMPEFETKCNN...
VHL
KYSE-520
DC50
nM
6
null
null
null
null
12
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06124
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1355
Homo sapiens
10.1021/acs.jmedchem.0c00471
Degradation of SHP2 in KYSE520/MV4;11 cells after 12 h treatment
PROTAC-DB
null
null
African=1.52%; Native American=1.16%; East Asian, North=82.25%; East Asian, South=12.37%; South Asian=0%; European, North=0%; European, South=2.7%. Mutation; HGNC; HGNC A*24 Stable (MSS) (Sanger). In situ; Esophagus; Japanese. Cancer cell line
14
false
1,718
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCN2CCN(C(=O)CCC(=O)Nc3cccc(Sc4ncc(N5CCC(C)(N)CC5)nc4N)c3Cl)CC2)C(C)(C)C)cc1
SHP2
MTSRRWFHPNITGVEAENLLLTRGVDGSFLARPSKSNPGDFTLSVRRNGAVTHIKIQNTGDYYDLYGGEKFATLAELVQYYMEHHGQLKEKNGDVIELKYPLNCADPTSERWFHGHLSGKEAEKLLTEKGKHGSFLVRESQSHPGDFVLSVRTGDDKGESNDGKSKVTHVMIRCQELKYDVGGGERFDSLTDLVEHYKKNPMVETLGTVLQLKQPLNTTRINAAEIESRVRELSKLAETTDKVKQGFWEEFETLQQQECKLLYSRKEGQRQENKNKNRYKNILPFDHTRVVLHDGDPNEPVSDYINANIIMPEFETKCNN...
VHL
MV4-11
DC50
nM
2.6
null
null
null
null
12
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06124
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0064
Homo sapiens
10.1021/acs.jmedchem.0c00471
Degradation of SHP2 in KYSE520/MV4;11 cells after 12 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...
14
false
1,718
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCNC(=O)c2nc(N3CCCc4c3nnc(Nc3nc5ccccc5s3)c4C)ccc2-c2cnn(C[C@]34C[C@]5(C)C[C@](C)(C3)C[C@@](OCCN3CCCC3)(C5)C4)c2C)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
HCT 116
DC50
nM
1.01
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-MERMPE
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
1,719
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCCNC(=O)c2nc(N3CCCc4c3nnc(Nc3nc5ccccc5s3)c4C)ccc2-c2cnn(C[C@]34C[C@]5(C)C[C@](C)(C3)C[C@@](OCCN3CCCC3)(C5)C4)c2C)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
NCI-H1650
DC50
nM
1
null
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-MERMPE
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
1,719
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN(C)CCOC23CC4(C)CC(C)(CC(Cn5ncc(-c6ccc(N7CCCc8c7nnc(Nc7nc9ccccc9s7)c8C)nc6C(=O)O)c5C)(C4)C2)C3)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
HCT 116
DC50
nM
2.94
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-XBMLTT
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
1,720
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN(C)CCOC23CC4(C)CC(C)(CC(Cn5ncc(-c6ccc(N7CCCc8c7nnc(Nc7nc9ccccc9s7)c8C)nc6C(=O)O)c5C)(C4)C2)C3)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
NCI-H1650
DC50
nM
3
null
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-XBMLTT
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
1,720
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN(C)CCOc2ccc(C(=O)c3c(-c4ccc(O)cc4)sc4cc(O)ccc34)cc2)C(C)(C)C)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
73
null
null
null
null
4
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM 0 %).
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
464
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN(CCOc2ccc(C(=O)c3c(-c4ccc(O)cc4)sc4cc(O)ccc34)cc2)C(C)(C)C)C(C)(C)C)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
79
null
null
null
null
4
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM > 99 %).
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
464
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN(CCOc2ccc(C(=O)c3c(-c4ccc(O)cc4)sc4cc(O)ccc34)cc2)C(C)C)C(C)(C)C)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
72
null
null
null
null
4
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM > 99 %).
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
464
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN(CCOc2ccc(C(=O)c3c(-c4ccc(O)cc4)sc4cc(O)ccc34)cc2)C2CC2)C(C)(C)C)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
80
null
null
null
null
4
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM > 99 %).
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
1,721
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN(CCOc2ccc(C(=O)c3c(-c4ccc(O)cc4)sc4cc(O)ccc34)cc2)C2CCC2)C(C)(C)C)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
85
null
null
null
null
4
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM > 99 %).
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
1,722
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN(CCOc2ccc(C(=O)c3c(-c4ccc(O)cc4)sc4cc(O)ccc34)cc2)C2CCCC2)C(C)(C)C)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
25
null
null
null
null
4
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM > 99 %).
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
1,723
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN(CCOc2ccc(C(=O)c3c(-c4ccc(O)cc4)sc4cc(O)ccc34)cc2)C2CCCCC2)C(C)(C)C)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
32
null
null
null
null
4
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM > 99 %).
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
1,724
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN(CCOc2ccc(C(=O)c3c(-c4ccc(O)cc4)sc4cc(O)ccc34)cc2)CC2CCC2)C(C)(C)C)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
24
null
null
null
null
4
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM > 99 %).
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
1,725
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
A-549
DC50
nM
255
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-6OVBDR
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
1,726
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
A-549
Dmax
%
76
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-6OVBDR
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
1,726
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
SW1573
DC50
nM
44
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-6OVBDR
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
1,726
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
SW1573
Dmax
%
92
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-6OVBDR
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
1,726
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
SW1573
DC50
nM
10,000
null
null
null
null
null
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-6OVBDR
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
1,726
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCNC(=O)C[C@@H]2CCN(CCc3cc(O)c(N4CC(=O)NS4(=O)=O)c(F)c3)C2)C(C)(C)C)cc1
PTPN1
MEMEKEFEQIDKSGSWAAIYQDIRHEASDFPCRVAKLPKNKNRNRYRDVSPFDHSRIKLHQEDNDYINASLIKMEEAQRSYILTQGPLPNTCGHFWEMVWEQKSRGVVMLNRVMEKGSLKCAQYWPQKEEKEMIFEDTNLKLTLISEDIKSYYTVRQLELENLTTQETREILHFHYTTWPDFGVPESPASFLNFLFKVRESGSLSPEHGPVVVHCSAGIGRSGTFCLADTCLLLMDKRKDPSSVDIKKVLLEMRKFRMGLIQTADQLRFSYLAVIEGAKFIMGDSSVQDQWKELSHEDLEPPPEHIPPPPRPPKRILEPH...
VHL
Jurkat
DC50
nM
3,830
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P18031
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0065
Homo sapiens
PROTEIN TYROSINE PHOSPHATASE DEGRADERS AND USES THEREOF (patent)
Parental Jurkat cells (ATCC, TIB-152) were grown in complete RPMI medium consisting of RPMI 1640 Medium (Gibco, 61870036) supplemented with 10% fetal bovine serum (Gibco, 10082147) and 1x Pen Strep (Gibco, 15140122). The sequence encoding the HiBiT tag (Promega) was integrated into the 5' end of the coding sequence on ...
TPDdb
HiBiT
TPD-HO8YMZ
African=0.4%; Native American=0%; East Asian, North=0.13%; East Asian, South=1.21%; South Asian=1.08%; European, North=70.73%; European, South=26.45%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC M...
14
false
1,727
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCNC(=O)C[C@@H]2CCN(CCc3cc(O)c(N4CC(=O)NS4(=O)=O)c(F)c3)C2)C(C)(C)C)cc1
PTPN1
MEMEKEFEQIDKSGSWAAIYQDIRHEASDFPCRVAKLPKNKNRNRYRDVSPFDHSRIKLHQEDNDYINASLIKMEEAQRSYILTQGPLPNTCGHFWEMVWEQKSRGVVMLNRVMEKGSLKCAQYWPQKEEKEMIFEDTNLKLTLISEDIKSYYTVRQLELENLTTQETREILHFHYTTWPDFGVPESPASFLNFLFKVRESGSLSPEHGPVVVHCSAGIGRSGTFCLADTCLLLMDKRKDPSSVDIKKVLLEMRKFRMGLIQTADQLRFSYLAVIEGAKFIMGDSSVQDQWKELSHEDLEPPPEHIPPPPRPPKRILEPH...
VHL
Jurkat
Dmax
%
78
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P18031
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0065
Homo sapiens
PROTEIN TYROSINE PHOSPHATASE DEGRADERS AND USES THEREOF (patent)
Parental Jurkat cells (ATCC, TIB-152) were grown in complete RPMI medium consisting of RPMI 1640 Medium (Gibco, 61870036) supplemented with 10% fetal bovine serum (Gibco, 10082147) and 1x Pen Strep (Gibco, 15140122). The sequence encoding the HiBiT tag (Promega) was integrated into the 5' end of the coding sequence on ...
TPDdb
HiBiT
TPD-HO8YMZ
African=0.4%; Native American=0%; East Asian, North=0.13%; East Asian, South=1.21%; South Asian=1.08%; European, North=70.73%; European, South=26.45%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC M...
14
false
1,727
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCNC(=O)C[C@@H]2CCN(CCc3cc(O)c(N4CC(=O)NS4(=O)=O)c(F)c3)C2)C(C)(C)C)cc1
PTPN2
MPTTIEREFEELDTQRRWQPLYLEIRNESHDYPHRVAKFPENRNRNRYRDVSPYDHSRVKLQNAENDYINASLVDIEEAQRSYILTQGPLPNTCCHFWLMVWQQKTKAVVMLNRIVEKESVKCAQYWPTDDQEMLFKETGFSVKLLSEDVKSYYTVHLLQLENINSGETRTISHFHYTTWPDFGVPESPASFLNFLFKVRESGSLNPDHGPAVIHCSAGIGRSGTFSLVDTCLVLMEKGDDINIKQVLLNMRKYRMGLIQTPDQLRFSYMAIIEGAKCIKGDSSIQKRWKELSKEDLSPAFDHSPNKIMTEKYNGNRIGL...
VHL
Jurkat
DC50
nM
146
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P17706
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0065
Homo sapiens
PROTEIN TYROSINE PHOSPHATASE DEGRADERS AND USES THEREOF (patent)
Parental Jurkat cells (ATCC, TIB-152) were grown in complete RPMI medium consisting of RPMI 1640 Medium (Gibco, 61870036) supplemented with 10% fetal bovine serum (Gibco, 10082147) and 1x Pen Strep (Gibco, 15140122). The sequence encoding the HiBiT tag (Promega) was integrated into the 5' end of the coding sequence on ...
TPDdb
HiBiT
TPD-HO8YMZ
African=0.4%; Native American=0%; East Asian, North=0.13%; East Asian, South=1.21%; South Asian=1.08%; European, North=70.73%; European, South=26.45%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC M...
14
false
1,727
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCNC(=O)C[C@@H]2CCN(CCc3cc(O)c(N4CC(=O)NS4(=O)=O)c(F)c3)C2)C(C)(C)C)cc1
PTPN2
MPTTIEREFEELDTQRRWQPLYLEIRNESHDYPHRVAKFPENRNRNRYRDVSPYDHSRVKLQNAENDYINASLVDIEEAQRSYILTQGPLPNTCCHFWLMVWQQKTKAVVMLNRIVEKESVKCAQYWPTDDQEMLFKETGFSVKLLSEDVKSYYTVHLLQLENINSGETRTISHFHYTTWPDFGVPESPASFLNFLFKVRESGSLNPDHGPAVIHCSAGIGRSGTFSLVDTCLVLMEKGDDINIKQVLLNMRKYRMGLIQTPDQLRFSYMAIIEGAKCIKGDSSIQKRWKELSKEDLSPAFDHSPNKIMTEKYNGNRIGL...
VHL
Jurkat
Dmax
%
98
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P17706
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0065
Homo sapiens
PROTEIN TYROSINE PHOSPHATASE DEGRADERS AND USES THEREOF (patent)
Parental Jurkat cells (ATCC, TIB-152) were grown in complete RPMI medium consisting of RPMI 1640 Medium (Gibco, 61870036) supplemented with 10% fetal bovine serum (Gibco, 10082147) and 1x Pen Strep (Gibco, 15140122). The sequence encoding the HiBiT tag (Promega) was integrated into the 5' end of the coding sequence on ...
TPDdb
HiBiT
TPD-HO8YMZ
African=0.4%; Native American=0%; East Asian, North=0.13%; East Asian, South=1.21%; South Asian=1.08%; European, North=70.73%; European, South=26.45%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC M...
14
false
1,727
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCNC(=O)c2nc(N3CCCc4c3nnc(Nc3nc5ccccc5s3)c4C)ccc2-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN3CCCC3)(C5)C4)c2C)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
HCT 116
DC50
nM
7.34
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-LLR5FR
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
1,728
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCNC(=O)c2nc(N3CCCc4c3nnc(Nc3nc5ccccc5s3)c4C)ccc2-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN3CCCC3)(C5)C4)c2C)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
NCI-H1650
DC50
nM
1
null
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-LLR5FR
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
1,728
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCc2ccc(-c3ccc(OCCCc4sc(N5CCc6cccc(C(=O)Nc7nc8ccccc8s7)c6C5)nc4C(=O)O)cc3)nc2)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
DC50
nM
3
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-DQ7X7T
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
1,729
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCc2cnc(-c3ccc(OCCCc4sc(N5CCc6cccc(C(=O)Nc7nc8ccccc8s7)c6C5)nc4C(=O)O)cc3)c(F)c2)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
DC50
nM
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-URJI7Z
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
1,729
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCN(C)CC[C@H](CSc2ccccc2)Nc2ccc(S(=O)(=O)NC(=O)c3ccc(N4CCN(CC5=C(c6ccc(Cl)cc6)CCC(C)(C)C5)CC4)cc3)cc2S(=O)(=O)C(F)(F)F)C(C)(C)C)cc1
BCL-XL
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
DC50
nM
71
null
null
null
null
16
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
10.1016/j.ejmech.2020.112186
Degradation of BCL-xL in MOLT-4 cells after 16 h treatment
PROTAC-DB
null
null
African=0.38%; Native American=0%; East Asian, North=1.74%; East Asian, South=0%; South Asian=0.94%; European, North=68.08%; European, South=28.87%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*01 A*01 A*01 Instable (MSI-high). In situ; ...
5
false
1,730
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCN(C)CC[C@H](CSc2ccccc2)Nc2ccc(S(=O)(=O)NC(=O)c3ccc(N4CCN(CC5=C(c6ccc(Cl)cc6)CCC(C)(C)C5)CC4)cc3)cc2S(=O)(=O)C(F)(F)F)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
DC50
nM
71
null
null
null
null
48
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/32145645/
IC50's are for cell viability assays
PROTACpedia
null
null
African=0.38%; Native American=0%; East Asian, North=1.74%; East Asian, South=0%; South Asian=0.94%; European, North=68.08%; European, South=28.87%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*01 A*01 A*01 Instable (MSI-high). In situ; ...
5
false
1,730
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
SW1573
DC50
nM
83
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-RG4ZJU
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
1,731
4
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
SW1573
Dmax
%
90
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-RG4ZJU
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
1,731
4
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
SW1573
DC50
nM
10,000
null
null
null
null
null
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-RG4ZJU
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
1,731
4
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCNC(=O)c2nc(N3CCCc4c3nnc(Nc3nc5ccccc5s3)c4C)ccc2-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN3CCCC3)(C5)C4)c2C)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
HCT 116
DC50
nM
1.68
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-C7BL6K
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
1,732
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCNC(=O)c2nc(N3CCCc4c3nnc(Nc3nc5ccccc5s3)c4C)ccc2-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN3CCCC3)(C5)C4)c2C)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
NCI-H1650
DC50
nM
1
null
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-C7BL6K
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
1,732
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
SW1573
DC50
nM
79
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-TY5RTH
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
747
4
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
SW1573
Dmax
%
94
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-TY5RTH
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
747
4
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
SW1573
DC50
nM
10,000
null
null
null
null
null
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-TY5RTH
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
747
4
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCN2CCC(n3nc(N)c4nnc(-c5ccccc5O)cc43)CC2)C(C)(C)C)cc1
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
SW1573
Dmax
%
12
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-TY5RTH
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
9
false
747
4
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCN2CCN(CC[C@H](CSc3ccccc3)Nc3ccc(S(=O)(=O)NC(=O)c4ccc(N5CCN(CC6=C(c7ccc(Cl)cc7)CCC(C)(C)C6)CC5)cc4)cc3S(=O)(=O)C(F)(F)F)CC2)C(C)(C)C)cc1
BCL-XL
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
DC50
nM
93
null
null
null
null
16
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
10.1016/j.ejmech.2020.112186
Degradation of BCL-xL in MOLT-4 cells after 16 h treatment
PROTAC-DB
null
null
African=0.38%; Native American=0%; East Asian, North=1.74%; East Asian, South=0%; South Asian=0.94%; European, North=68.08%; European, South=28.87%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*01 A*01 A*01 Instable (MSI-high). In situ; ...
5
false
1,733
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCN2CCN(CC[C@H](CSc3ccccc3)Nc3ccc(S(=O)(=O)NC(=O)c4ccc(N5CCN(CC6=C(c7ccc(Cl)cc7)CCC(C)(C)C6)CC5)cc4)cc3S(=O)(=O)C(F)(F)F)CC2)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
DC50
nM
93
null
null
null
null
48
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/32145645/
IC50's are for cell viability assays
PROTACpedia
null
null
African=0.38%; Native American=0%; East Asian, North=1.74%; East Asian, South=0%; South Asian=0.94%; European, North=68.08%; European, South=28.87%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*01 A*01 A*01 Instable (MSI-high). In situ; ...
5
false
1,733
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCN2CCN(CC[C@H](CSc3ccccc3)Nc3ccc(S(=O)(=O)NC(=O)c4ccc(N5CCN(CC6=C(c7ccc(Cl)cc7)CCC(C)(C)C6)CC5)cc4)cc3S(=O)(=O)C(F)(F)F)CC2)C(C)(C)C)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MOLT-4
Dmax
%
90
null
null
null
null
48
~
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0013
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/32145645/
IC50's are for cell viability assays
PROTACpedia
null
null
African=0.38%; Native American=0%; East Asian, North=1.74%; East Asian, South=0%; South Asian=0.94%; European, North=68.08%; European, South=28.87%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*01 A*01 A*01 Instable (MSI-high). In situ; ...
5
false
1,733
0
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCN2CCc3cc(O)c(N4CC(=O)NS4(=O)=O)c(F)c3CC2)C(C)(C)C)cc1
PTPN1
MEMEKEFEQIDKSGSWAAIYQDIRHEASDFPCRVAKLPKNKNRNRYRDVSPFDHSRIKLHQEDNDYINASLIKMEEAQRSYILTQGPLPNTCGHFWEMVWEQKSRGVVMLNRVMEKGSLKCAQYWPQKEEKEMIFEDTNLKLTLISEDIKSYYTVRQLELENLTTQETREILHFHYTTWPDFGVPESPASFLNFLFKVRESGSLSPEHGPVVVHCSAGIGRSGTFCLADTCLLLMDKRKDPSSVDIKKVLLEMRKFRMGLIQTADQLRFSYLAVIEGAKFIMGDSSVQDQWKELSHEDLEPPPEHIPPPPRPPKRILEPH...
VHL
Jurkat
DC50
nM
1,640
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P18031
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0065
Homo sapiens
PROTEIN TYROSINE PHOSPHATASE DEGRADERS AND USES THEREOF (patent)
Parental Jurkat cells (ATCC, TIB-152) were grown in complete RPMI medium consisting of RPMI 1640 Medium (Gibco, 61870036) supplemented with 10% fetal bovine serum (Gibco, 10082147) and 1x Pen Strep (Gibco, 15140122). The sequence encoding the HiBiT tag (Promega) was integrated into the 5' end of the coding sequence on ...
TPDdb
HiBiT
TPD-VAOOU0
African=0.4%; Native American=0%; East Asian, North=0.13%; East Asian, South=1.21%; South Asian=1.08%; European, North=70.73%; European, South=26.45%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC M...
14
false
1,734
4
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCN2CCc3cc(O)c(N4CC(=O)NS4(=O)=O)c(F)c3CC2)C(C)(C)C)cc1
PTPN1
MEMEKEFEQIDKSGSWAAIYQDIRHEASDFPCRVAKLPKNKNRNRYRDVSPFDHSRIKLHQEDNDYINASLIKMEEAQRSYILTQGPLPNTCGHFWEMVWEQKSRGVVMLNRVMEKGSLKCAQYWPQKEEKEMIFEDTNLKLTLISEDIKSYYTVRQLELENLTTQETREILHFHYTTWPDFGVPESPASFLNFLFKVRESGSLSPEHGPVVVHCSAGIGRSGTFCLADTCLLLMDKRKDPSSVDIKKVLLEMRKFRMGLIQTADQLRFSYLAVIEGAKFIMGDSSVQDQWKELSHEDLEPPPEHIPPPPRPPKRILEPH...
VHL
Jurkat
Dmax
%
68
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P18031
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0065
Homo sapiens
PROTEIN TYROSINE PHOSPHATASE DEGRADERS AND USES THEREOF (patent)
Parental Jurkat cells (ATCC, TIB-152) were grown in complete RPMI medium consisting of RPMI 1640 Medium (Gibco, 61870036) supplemented with 10% fetal bovine serum (Gibco, 10082147) and 1x Pen Strep (Gibco, 15140122). The sequence encoding the HiBiT tag (Promega) was integrated into the 5' end of the coding sequence on ...
TPDdb
HiBiT
TPD-VAOOU0
African=0.4%; Native American=0%; East Asian, North=0.13%; East Asian, South=1.21%; South Asian=1.08%; European, North=70.73%; European, South=26.45%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC M...
14
false
1,734
4
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCN2CCc3cc(O)c(N4CC(=O)NS4(=O)=O)c(F)c3CC2)C(C)(C)C)cc1
PTPN2
MPTTIEREFEELDTQRRWQPLYLEIRNESHDYPHRVAKFPENRNRNRYRDVSPYDHSRVKLQNAENDYINASLVDIEEAQRSYILTQGPLPNTCCHFWLMVWQQKTKAVVMLNRIVEKESVKCAQYWPTDDQEMLFKETGFSVKLLSEDVKSYYTVHLLQLENINSGETRTISHFHYTTWPDFGVPESPASFLNFLFKVRESGSLNPDHGPAVIHCSAGIGRSGTFSLVDTCLVLMEKGDDINIKQVLLNMRKYRMGLIQTPDQLRFSYMAIIEGAKCIKGDSSIQKRWKELSKEDLSPAFDHSPNKIMTEKYNGNRIGL...
VHL
Jurkat
DC50
nM
1,150
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P17706
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0065
Homo sapiens
PROTEIN TYROSINE PHOSPHATASE DEGRADERS AND USES THEREOF (patent)
Parental Jurkat cells (ATCC, TIB-152) were grown in complete RPMI medium consisting of RPMI 1640 Medium (Gibco, 61870036) supplemented with 10% fetal bovine serum (Gibco, 10082147) and 1x Pen Strep (Gibco, 15140122). The sequence encoding the HiBiT tag (Promega) was integrated into the 5' end of the coding sequence on ...
TPDdb
HiBiT
TPD-VAOOU0
African=0.4%; Native American=0%; East Asian, North=0.13%; East Asian, South=1.21%; South Asian=1.08%; European, North=70.73%; European, South=26.45%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC M...
14
false
1,734
4
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCN2CCc3cc(O)c(N4CC(=O)NS4(=O)=O)c(F)c3CC2)C(C)(C)C)cc1
PTPN2
MPTTIEREFEELDTQRRWQPLYLEIRNESHDYPHRVAKFPENRNRNRYRDVSPYDHSRVKLQNAENDYINASLVDIEEAQRSYILTQGPLPNTCCHFWLMVWQQKTKAVVMLNRIVEKESVKCAQYWPTDDQEMLFKETGFSVKLLSEDVKSYYTVHLLQLENINSGETRTISHFHYTTWPDFGVPESPASFLNFLFKVRESGSLNPDHGPAVIHCSAGIGRSGTFSLVDTCLVLMEKGDDINIKQVLLNMRKYRMGLIQTPDQLRFSYMAIIEGAKCIKGDSSIQKRWKELSKEDLSPAFDHSPNKIMTEKYNGNRIGL...
VHL
Jurkat
Dmax
%
83
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P17706
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0065
Homo sapiens
PROTEIN TYROSINE PHOSPHATASE DEGRADERS AND USES THEREOF (patent)
Parental Jurkat cells (ATCC, TIB-152) were grown in complete RPMI medium consisting of RPMI 1640 Medium (Gibco, 61870036) supplemented with 10% fetal bovine serum (Gibco, 10082147) and 1x Pen Strep (Gibco, 15140122). The sequence encoding the HiBiT tag (Promega) was integrated into the 5' end of the coding sequence on ...
TPDdb
HiBiT
TPD-VAOOU0
African=0.4%; Native American=0%; East Asian, North=0.13%; East Asian, South=1.21%; South Asian=1.08%; European, North=70.73%; European, South=26.45%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC M...
14
false
1,734
4
Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCNC(=O)C[C@@H]2CCN(CCc3cc(O)c(N4CC(=O)NS4(=O)=O)c(F)c3)C2)C(C)(C)C)cc1
PTPN1
MEMEKEFEQIDKSGSWAAIYQDIRHEASDFPCRVAKLPKNKNRNRYRDVSPFDHSRIKLHQEDNDYINASLIKMEEAQRSYILTQGPLPNTCGHFWEMVWEQKSRGVVMLNRVMEKGSLKCAQYWPQKEEKEMIFEDTNLKLTLISEDIKSYYTVRQLELENLTTQETREILHFHYTTWPDFGVPESPASFLNFLFKVRESGSLSPEHGPVVVHCSAGIGRSGTFCLADTCLLLMDKRKDPSSVDIKKVLLEMRKFRMGLIQTADQLRFSYLAVIEGAKFIMGDSSVQDQWKELSHEDLEPPPEHIPPPPRPPKRILEPH...
VHL
Jurkat
DC50
nM
7,610
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P18031
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0065
Homo sapiens
PROTEIN TYROSINE PHOSPHATASE DEGRADERS AND USES THEREOF (patent)
Parental Jurkat cells (ATCC, TIB-152) were grown in complete RPMI medium consisting of RPMI 1640 Medium (Gibco, 61870036) supplemented with 10% fetal bovine serum (Gibco, 10082147) and 1x Pen Strep (Gibco, 15140122). The sequence encoding the HiBiT tag (Promega) was integrated into the 5' end of the coding sequence on ...
TPDdb
HiBiT
TPD-WWLSI9
African=0.4%; Native American=0%; East Asian, North=0.13%; East Asian, South=1.21%; South Asian=1.08%; European, North=70.73%; European, South=26.45%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC M...
14
false
1,735
0