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Assay Detail

CHEMBL937576

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Binding
Binding affinity to BCL2
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Apoptosis regulator Bcl-2 (CHEMBL4860)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis.
Nguyen M, Marcellus RC, Roulston A, Watson M, Serfass L, Murthy Madiraju SR, Goulet D, Viallet J, Bélec L, Billot X, Acoca S, Purisima E, Wiegmans A, Cluse L, Johnstone RW, Beauparlant P, Shore GC.
Proc Natl Acad Sci U S A (2007) 104 : 19512 -19517
PubMed 18040043 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.23 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL36327 EPICATECHIN GALLATE 1 6.64
CHEMBL297453 EPIGALOCATECHIN GALLATE 3.0 1 6.63
CHEMBL51483 GOSSYPOL 3.0 1 6.33
CHEMBL346119 THEAFLAVIN 1 6.16
CHEMBL436605 ANTIMYCIN A3 1 6.08
CHEMBL253536 1 5.91
CHEMBL255690 1 5.89
CHEMBL376408 ABT 737 1.0 1 -
CHEMBL206452 CATECHIN 1 -
CHEMBL47386 EPIGALLOCATECHIN 1 -
CHEMBL402609 THEAFLAVIN DIGALLTE 1 -
CHEMBL583912 (-)-EPICATECHIN 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL36327 EPICATECHIN GALLATE Ki = 229.09 nM 6.64
CHEMBL297453 EPIGALOCATECHIN GALLATE Ki = 234.42 nM 6.63
CHEMBL51483 GOSSYPOL Ki = 467.74 nM 6.33
CHEMBL346119 THEAFLAVIN Ki = 691.83 nM 6.16
CHEMBL436605 ANTIMYCIN A3 Ki = 831.76 nM 6.08
CHEMBL253536 Ki = 1230.27 nM 5.91
CHEMBL255690 Ki = 1288.25 nM 5.89
CHEMBL376408 ABT 737 Ki <= 1.0 nM -
CHEMBL206452 CATECHIN Ki > 100000.0 nM -
CHEMBL47386 EPIGALLOCATECHIN Ki > 100000.0 nM -
CHEMBL402609 THEAFLAVIN DIGALLTE Ki > 100000.0 nM -
CHEMBL583912 (-)-EPICATECHIN Ki > 100000.0 nM -