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Assay Detail

CHEMBL4015012

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

Binding
Inhibition of 6-carboxyfluorescein succinimidyl ester fluorescence tagged-Bid BH3 peptide (79 to 99 residues) binding to Bcl-2 (unknown origin) after 30 mins by fluorescence polarization assay
16
Total Activities
16
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

Apoptosis regulator Bcl-2 (CHEMBL4860)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and structure-activity relationship studies of N-substituted indole derivatives as novel Mcl-1 inhibitors.
Luan S, Ge Q, Chen Y, Dai M, Yang J, Li K, Liu D, Zhao L.
Bioorg Med Chem Lett (2017) 27 : 1943 -1948
PubMed 28343875 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.30 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4082302 1 6.85
CHEMBL4098261 1 6.82
CHEMBL4081347 1 6.77
CHEMBL4062127 1 6.64
CHEMBL4071224 1 6.57
CHEMBL4097869 1 6.39
CHEMBL51483 GOSSYPOL 3.0 1 6.38
CHEMBL4070752 1 6.33
CHEMBL4067010 1 6.14
CHEMBL4105602 1 6.12
CHEMBL4094488 1 6.09
CHEMBL4100319 1 6.07
CHEMBL4088240 1 5.98
CHEMBL4094073 1 5.92
CHEMBL4073436 1 5.91
CHEMBL4090152 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4082302 Ki = 140.0 nM 6.85
CHEMBL4098261 Ki = 150.0 nM 6.82
CHEMBL4081347 Ki = 170.0 nM 6.77
CHEMBL4062127 Ki = 230.0 nM 6.64
CHEMBL4071224 Ki = 270.0 nM 6.57
CHEMBL4097869 Ki = 410.0 nM 6.39
CHEMBL51483 GOSSYPOL Ki = 420.0 nM 6.38
CHEMBL4070752 Ki = 470.0 nM 6.33
CHEMBL4067010 Ki = 730.0 nM 6.14
CHEMBL4105602 Ki = 760.0 nM 6.12
CHEMBL4094488 Ki = 810.0 nM 6.09
CHEMBL4100319 Ki = 850.0 nM 6.07
CHEMBL4088240 Ki = 1050.0 nM 5.98
CHEMBL4094073 Ki = 1190.0 nM 5.92
CHEMBL4073436 Ki = 1240.0 nM 5.91
CHEMBL4090152 Ki = 1410.0 nM 5.85