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Assay Detail

CHEMBL3859720

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

Binding
Inhibition of 5-FAM-Bid peptide binding to Bcl-XL (unknown origin) by fluorescence polarization assay
21
Total Activities
21
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-like protein 1 (CHEMBL4625)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and activity evaluation of selective inhibitors of anti-apoptotic Bcl-2 proteins: The effects on the selectivity of the P1 pockets in the active sites.
Wang M, Tian W, Wang C, Lu S, Yang C, Wang J, Song Y, Zhou Y, Zhu J, Li Z, Zheng C.
Bioorg Med Chem Lett (2016) 26 : 5207 -5211
PubMed 27712939 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 6.80 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL376408 ABT 737 1.0 1 9.00
CHEMBL3891088 1 7.16
CHEMBL3980363 1 7.05
CHEMBL3926515 1 6.96
CHEMBL3933727 1 6.92
CHEMBL3951428 1 6.89
CHEMBL3900077 1 6.85
CHEMBL3909131 1 6.80
CHEMBL3971723 1 6.77
CHEMBL3960206 1 6.68
CHEMBL3979383 1 6.68
CHEMBL3961198 1 6.54
CHEMBL3902269 1 6.54
CHEMBL51483 GOSSYPOL 3.0 1 6.51
CHEMBL3971226 1 6.50
CHEMBL3947409 1 6.48
CHEMBL3976674 1 6.35
CHEMBL3960600 1 6.29
CHEMBL1940668 1 6.20
CHEMBL3918541 1 -
CHEMBL3895790 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL376408 ABT 737 Ki = 1.0 nM 9.00
CHEMBL3891088 Ki = 70.0 nM 7.16
CHEMBL3980363 Ki = 90.0 nM 7.05
CHEMBL3926515 Ki = 110.0 nM 6.96
CHEMBL3933727 Ki = 120.0 nM 6.92
CHEMBL3951428 Ki = 130.0 nM 6.89
CHEMBL3900077 Ki = 140.0 nM 6.85
CHEMBL3909131 Ki = 160.0 nM 6.80
CHEMBL3971723 Ki = 170.0 nM 6.77
CHEMBL3960206 Ki = 210.0 nM 6.68
CHEMBL3979383 Ki = 210.0 nM 6.68
CHEMBL3961198 Ki = 290.0 nM 6.54
CHEMBL3902269 Ki = 290.0 nM 6.54
CHEMBL51483 GOSSYPOL Ki = 310.0 nM 6.51
CHEMBL3971226 Ki = 320.0 nM 6.50
CHEMBL3947409 Ki = 330.0 nM 6.48
CHEMBL3976674 Ki = 450.0 nM 6.35
CHEMBL3960600 Ki = 510.0 nM 6.29
CHEMBL1940668 Ki = 630.0 nM 6.20
CHEMBL3918541 Ki > 20000.0 nM -
CHEMBL3895790 Ki > 20000.0 nM -