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Assay Detail

CHEMBL3266883

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

Binding
Displacement of Flu-BID/FAM-BID from His-tagged A1-BFL-1 (1 to 151) (unknown origin) expressed in Escherichia coli BL21(DE3) after 3 hrs by fluorescence polarization assay
7
Total Activities
7
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

Bcl-2-related protein A1 (CHEMBL6044)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

3-Substituted-N-(4-hydroxynaphthalen-1-yl)arylsulfonamides as a novel class of selective Mcl-1 inhibitors: structure-based design, synthesis, SAR, and biological evaluation.
Abulwerdi FA, Liao C, Mady AS, Gavin J, Shen C, Cierpicki T, Stuckey JA, Showalter HD, Nikolovska-Coleska Z.
J Med Chem (2014) 57 : 4111 -4133
PubMed 24749893 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 5.40 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3265297 1 5.96
CHEMBL3265294 1 5.63
CHEMBL3265295 1 5.50
CHEMBL3265299 1 5.47
CHEMBL1331211 1 5.27
CHEMBL2030270 1 5.21
CHEMBL3265296 1 4.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3265297 Ki = 1110.0 nM 5.96
CHEMBL3265294 Ki = 2340.0 nM 5.63
CHEMBL3265295 Ki = 3180.0 nM 5.50
CHEMBL3265299 Ki = 3360.0 nM 5.47
CHEMBL1331211 Ki = 5330.0 nM 5.27
CHEMBL2030270 Ki = 6140.0 nM 5.21
CHEMBL3265296 Ki = 17260.0 nM 4.76