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Assay Detail

CHEMBL4729292

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

Binding
Inhibition of N-terminal biotin-labeled BIM BH3 peptide (141 to 166 residues) binding to His-tagged Mcl-1 (171 to 327 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) cells incubated for >=30 mins by fluorescence polarization
13
Total Activities
13
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

Publication

Discovery of a Copper-Based Mcl-1 Inhibitor as an Effective Antitumor Agent.
Lu X,Liu YC,Orvig C,Liang H,Chen ZF
J Med Chem (2020) 63 : 9154 -9167
PubMed 32794745 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.81 8.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3417704 1 8.06
CHEMBL4778579 1 5.07
CHEMBL4796830 1 5.05
CHEMBL4757050 1 5.04
CHEMBL4578154 1 -
CHEMBL4744295 1 -
CHEMBL4758555 1 -
CHEMBL4743955 1 -
CHEMBL4777267 1 -
CHEMBL4760810 1 -
CHEMBL4794980 1 -
CHEMBL4748351 1 -
CHEMBL4792991 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3417704 IC50 = 8.8 nM 8.06
CHEMBL4778579 IC50 = 8523.9 nM 5.07
CHEMBL4796830 IC50 = 8812.3 nM 5.05
CHEMBL4757050 IC50 = 9082.3 nM 5.04
CHEMBL4578154 IC50 > 10000.0 nM -
CHEMBL4744295 IC50 > 10000.0 nM -
CHEMBL4758555 IC50 > 10000.0 nM -
CHEMBL4743955 IC50 > 10000.0 nM -
CHEMBL4777267 IC50 > 10000.0 nM -
CHEMBL4760810 IC50 > 10000.0 nM -
CHEMBL4794980 IC50 > 10000.0 nM -
CHEMBL4748351 IC50 > 10000.0 nM -
CHEMBL4792991 IC50 > 10000.0 nM -