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Assay Detail

CHEMBL2033943

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

Binding
Inhibition of biotin-labelled Bcl-xL using [FAM]-IWIAQELRRIGDEFNAYY-NH2 as substrate after 60 mins by FRET analysis
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Bcl-2-like protein 1 (CHEMBL4625)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyrazole and pyrimidine phenylacylsulfonamides as dual Bcl-2/Bcl-xL antagonists.
Schroeder GM, Wei D, Banfi P, Cai ZW, Lippy J, Menichincheri M, Modugno M, Naglich J, Penhallow B, Perez HL, Sack J, Schmidt RJ, Tebben A, Yan C, Zhang L, Galvani A, Lombardo LJ, Borzilleri RM.
Bioorg Med Chem Lett (2012) 22 : 3951 -3956
PubMed 22608393 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 7.27 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2030856 1 8.22
CHEMBL2030860 1 8.15
CHEMBL2030857 1 8.15
CHEMBL2030859 1 8.10
CHEMBL2031009 1 8.05
CHEMBL2030847 1 7.96
CHEMBL2030855 1 7.89
CHEMBL2030861 1 7.89
CHEMBL2031008 1 7.85
CHEMBL2030864 1 7.82
CHEMBL2030858 1 7.82
CHEMBL2030853 1 7.75
CHEMBL2030854 1 7.58
CHEMBL2030846 1 7.52
CHEMBL2030852 1 7.46
CHEMBL2030851 1 7.46
CHEMBL2030845 1 7.38
CHEMBL2030848 1 7.32
CHEMBL2030850 1 7.26
CHEMBL2030863 1 6.92
CHEMBL2031006 1 6.92
CHEMBL2031004 1 6.89
CHEMBL2030862 1 6.85
CHEMBL2031003 1 6.80
CHEMBL2031005 1 6.64
CHEMBL2031007 1 6.60
CHEMBL2030849 1 6.33
CHEMBL2030866 1 6.32
CHEMBL2030865 1 6.30
CHEMBL2030844 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2030856 IC50 = 6.0 nM 8.22
CHEMBL2030860 IC50 = 7.0 nM 8.15
CHEMBL2030857 IC50 = 7.0 nM 8.15
CHEMBL2030859 IC50 = 8.0 nM 8.10
CHEMBL2031009 IC50 = 9.0 nM 8.05
CHEMBL2030847 IC50 = 11.0 nM 7.96
CHEMBL2030855 IC50 = 13.0 nM 7.89
CHEMBL2030861 IC50 = 13.0 nM 7.89
CHEMBL2031008 IC50 = 14.0 nM 7.85
CHEMBL2030864 IC50 = 15.0 nM 7.82
CHEMBL2030858 IC50 = 15.0 nM 7.82
CHEMBL2030853 IC50 = 18.0 nM 7.75
CHEMBL2030854 IC50 = 26.0 nM 7.58
CHEMBL2030846 IC50 = 30.0 nM 7.52
CHEMBL2030851 IC50 = 35.0 nM 7.46
CHEMBL2030852 IC50 = 35.0 nM 7.46
CHEMBL2030845 IC50 = 42.0 nM 7.38
CHEMBL2030848 IC50 = 48.0 nM 7.32
CHEMBL2030850 IC50 = 55.0 nM 7.26
CHEMBL2030863 IC50 = 120.0 nM 6.92
CHEMBL2031006 IC50 = 120.0 nM 6.92
CHEMBL2031004 IC50 = 130.0 nM 6.89
CHEMBL2030862 IC50 = 140.0 nM 6.85
CHEMBL2031003 IC50 = 160.0 nM 6.80
CHEMBL2031005 IC50 = 230.0 nM 6.64
CHEMBL2031007 IC50 = 250.0 nM 6.60
CHEMBL2030849 IC50 = 470.0 nM 6.33
CHEMBL2030866 IC50 = 480.0 nM 6.32
CHEMBL2030865 IC50 = 500.0 nM 6.30
CHEMBL2030844 IC50 = 640.0 nM 6.19
CHEMBL2031002 IC50 = 710.0 nM 6.15
CHEMBL2031001 IC50 = 970.0 nM 6.01