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Assay Detail

CHEMBL1106541

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

Functional
Cytotoxicity against human PC3 cells after 3 days by ATP-LITE assay
ChEMBL ↗
7
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type PC-3
Confidence 1 — Organism
Curated By Autocuration

Target

PC-3 (CHEMBL390) ↗
Type CELL-LINE
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
EC50 7 5.74 6.89

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 6.89
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 6.33
CHEMBL538616 — — 1 5.61
CHEMBL51483 GOSSYPOL 3.0 2 5.48

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) EC50 = 130.0 nM 6.89
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) EC50 = 470.0 nM 6.33
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) EC50 = 1610.0 nM 5.79
CHEMBL538616 — EC50 = 2450.0 nM 5.61
CHEMBL51483 GOSSYPOL EC50 = 3300.0 nM 5.48
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) EC50 = 4640.0 nM 5.33
CHEMBL51483 GOSSYPOL EC50 = 17800.0 nM 4.75