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Assay Detail

CHEMBL1106538

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

Binding
Displacement of FITC-labeled Bak BH3 peptide from Bfl-1 after 30 mins by fluorescence polarization assay
ChEMBL ↗
5
Total Activities
3
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-related protein A1 (CHEMBL6044) ↗
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 5 6.21 6.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL538616 — — 1 6.38
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 6.23
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 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL538616 — IC50 = 420.0 nM 6.38
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 = 590.0 nM 6.23
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 = 620.0 nM 6.21
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 = 750.0 nM 6.12
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 = 770.0 nM 6.11