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Assay Detail

CHEMBL4813625

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

Binding
Binding affinity to Bcl-2 (unknown origin) by fluorescence polarization competition assay
24
Total Activities
24
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

Bcl2-associated agonist of cell death (CHEMBL3817)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of dual Bcl-2/Mcl-1 inhibitors bearing 2-(1H-indol-4-yl)benzoic acid scaffold.
Niu Q, Deng H, Zhang Z, Xu Q, Luan S, Huang M, Liu D, Zhao L.
Bioorg Med Chem Lett (2021) 47 : 128215 -128215
PubMed 34153472 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 6.06 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4872320 1 7.00
CHEMBL4872671 1 6.60
CHEMBL4864929 1 6.60
CHEMBL4855114 1 6.52
CHEMBL4870608 1 6.44
CHEMBL51483 GOSSYPOL 3.0 1 6.34
CHEMBL4860820 1 6.31
CHEMBL4852823 1 6.28
CHEMBL4864735 1 6.25
CHEMBL4870458 1 6.18
CHEMBL4846508 1 6.10
CHEMBL4856143 1 6.09
CHEMBL4870837 1 6.09
CHEMBL4876348 1 6.06
CHEMBL4876147 1 5.97
CHEMBL4859740 1 5.89
CHEMBL4872495 1 5.89
CHEMBL4875429 1 5.76
CHEMBL4865871 1 5.75
CHEMBL4878113 1 5.59
CHEMBL4868913 1 5.49
CHEMBL4860027 1 5.34
CHEMBL3137309 VENETOCLAX 4.0 1 4.80
CHEMBL4851522 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4872320 Ki = 100.0 nM 7.00
CHEMBL4872671 Ki = 250.0 nM 6.60
CHEMBL4864929 Ki = 250.0 nM 6.60
CHEMBL4855114 Ki = 300.0 nM 6.52
CHEMBL4870608 Ki = 360.0 nM 6.44
CHEMBL51483 GOSSYPOL Ki = 460.0 nM 6.34
CHEMBL4860820 Ki = 490.0 nM 6.31
CHEMBL4852823 Ki = 530.0 nM 6.28
CHEMBL4864735 Ki = 560.0 nM 6.25
CHEMBL4870458 Ki = 660.0 nM 6.18
CHEMBL4846508 Ki = 800.0 nM 6.10
CHEMBL4856143 Ki = 820.0 nM 6.09
CHEMBL4870837 Ki = 820.0 nM 6.09
CHEMBL4876348 Ki = 870.0 nM 6.06
CHEMBL4876147 Ki = 1080.0 nM 5.97
CHEMBL4859740 Ki = 1300.0 nM 5.89
CHEMBL4872495 Ki = 1280.0 nM 5.89
CHEMBL4875429 Ki = 1740.0 nM 5.76
CHEMBL4865871 Ki = 1800.0 nM 5.75
CHEMBL4878113 Ki = 2550.0 nM 5.59
CHEMBL4868913 Ki = 3210.0 nM 5.49
CHEMBL4860027 Ki = 4530.0 nM 5.34
CHEMBL3137309 VENETOCLAX Ki = 16000.0 nM 4.80
CHEMBL4851522 Ki - -