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Assay Detail

CHEMBL1106536

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

Binding
Displacement of FITC-labeled Bak BH3 peptide from Bcl-XL after 30 mins by fluorescence polarization assay
ChEMBL ↗
7
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Bcl-2-like protein 1 (CHEMBL4625) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

BI-97C1, an optically pure Apogossypol derivative as pan-active inhibitor of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
Wei J, Stebbins JL, Kitada S, Dash R, Placzek W, Rega MF, Wu B, Cellitti J, Zhai D, Yang L, Dahl R, Fisher PB, Reed JC, Pellecchia M.
J Med Chem (2010) 53 : 4166 -4176
PubMed 20443627 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.32 6.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1094250 1,1',6,6',7,7'-HEXAHYDROXY-3,3'-DIMETHYL-N5-((R)-2-PHENYLPROPYL)-N5'-((R)-2-PHENYLPROPYL)-2,2'-BINAPHTHYL-5,5'-DICARBOXAMIDE (ATROPISOMERIC MIX) — 2 6.51
CHEMBL538616 — — 1 6.41
CHEMBL1094366 (S)-1',6,6',7,7'-HEXAHYDROXY-3,3'-DIMETHYL-N5-((S)-2-PHENYLPROPYL)-N5'-((S)-2-PHENYLPROPYL)-2,2'-BINAPHTHYL-5,5'-DICARBOXAMIDE (ATROPISOMERIC MIX) — 2 6.36
CHEMBL51483 GOSSYPOL 3.0 2 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1094250 1,1',6,6',7,7'-HEXAHYDROXY-3,3'-DIMETHYL-N5-((R)-2-PHENYLPROPYL)-N5'-((R)-2-PHENYLPROPYL)-2,2'-BINAPHTHYL-5,5'-DICARBOXAMIDE (ATROPISOMERIC MIX) IC50 = 310.0 nM 6.51
CHEMBL538616 — IC50 = 390.0 nM 6.41
CHEMBL1094366 (S)-1',6,6',7,7'-HEXAHYDROXY-3,3'-DIMETHYL-N5-((S)-2-PHENYLPROPYL)-N5'-((S)-2-PHENYLPROPYL)-2,2'-BINAPHTHYL-5,5'-DICARBOXAMIDE (ATROPISOMERIC MIX) IC50 = 440.0 nM 6.36
CHEMBL51483 GOSSYPOL IC50 = 480.0 nM 6.32
CHEMBL51483 GOSSYPOL IC50 = 540.0 nM 6.27
CHEMBL1094366 (S)-1',6,6',7,7'-HEXAHYDROXY-3,3'-DIMETHYL-N5-((S)-2-PHENYLPROPYL)-N5'-((S)-2-PHENYLPROPYL)-2,2'-BINAPHTHYL-5,5'-DICARBOXAMIDE (ATROPISOMERIC MIX) IC50 = 650.0 nM 6.19
CHEMBL1094250 1,1',6,6',7,7'-HEXAHYDROXY-3,3'-DIMETHYL-N5-((R)-2-PHENYLPROPYL)-N5'-((R)-2-PHENYLPROPYL)-2,2'-BINAPHTHYL-5,5'-DICARBOXAMIDE (ATROPISOMERIC MIX) IC50 = 680.0 nM 6.17