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Assay Detail

CHEMBL4182824

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of Bax-derived peptide from Bcl-2 (unknown origin) by fluorescence polarization assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design, synthesis and pharmacological evaluation of new acyl sulfonamides as potent and selective Bcl-2 inhibitors.
Liu X, Zhang Y, Huang W, Tan W, Zhang A.
Bioorg Med Chem (2018) 26 : 443 -454
PubMed 29229225 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.36 8.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3137309 VENETOCLAX 4.0 1 8.13
CHEMBL443684 NAVITOCLAX 3.0 1 7.99
CHEMBL4216466 1 7.90
CHEMBL4207006 1 7.84
CHEMBL4211198 1 7.76
CHEMBL4206829 1 7.68
CHEMBL4202464 1 7.46
CHEMBL4216380 1 7.42
CHEMBL4209752 1 7.39
CHEMBL4209621 1 7.34
CHEMBL4206007 1 7.33
CHEMBL4211496 1 7.24
CHEMBL4210809 1 7.19
CHEMBL4208633 1 7.17
CHEMBL4218253 1 7.17
CHEMBL4218405 1 6.97
CHEMBL4213316 1 6.78
CHEMBL4215940 1 6.71
CHEMBL4204650 1 6.30
CHEMBL4204583 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3137309 VENETOCLAX IC50 = 7.39 nM 8.13
CHEMBL443684 NAVITOCLAX IC50 = 10.3 nM 7.99
CHEMBL4216466 IC50 = 12.6 nM 7.90
CHEMBL4207006 IC50 = 14.5 nM 7.84
CHEMBL4211198 IC50 = 17.3 nM 7.76
CHEMBL4206829 IC50 = 20.7 nM 7.68
CHEMBL4202464 IC50 = 34.8 nM 7.46
CHEMBL4216380 IC50 = 38.1 nM 7.42
CHEMBL4209752 IC50 = 40.7 nM 7.39
CHEMBL4209621 IC50 = 46.0 nM 7.34
CHEMBL4206007 IC50 = 46.6 nM 7.33
CHEMBL4211496 IC50 = 57.9 nM 7.24
CHEMBL4210809 IC50 = 65.1 nM 7.19
CHEMBL4208633 IC50 = 68.2 nM 7.17
CHEMBL4218253 IC50 = 67.4 nM 7.17
CHEMBL4218405 IC50 = 108.0 nM 6.97
CHEMBL4213316 IC50 = 168.0 nM 6.78
CHEMBL4215940 IC50 = 193.0 nM 6.71
CHEMBL4204650 IC50 = 495.0 nM 6.30
CHEMBL4204583 IC50 > 1000.0 nM -