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Assay Detail

CHEMBL1019894

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

Binding
Inhibition of GST fused Bcl-2 binding to biotinylated 26 mer Bak-BH3 peptide by HTRF-LANCE assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Tetrahydroisoquinoline amide substituted phenyl pyrazoles as selective Bcl-2 inhibitors.
Porter J, Payne A, de Candole B, Ford D, Hutchinson B, Trevitt G, Turner J, Edwards C, Watkins C, Whitcombe I, Davis J, Stubberfield C.
Bioorg Med Chem Lett (2009) 19 : 230 -233
PubMed 19027294 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.30 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL508392 1 7.52
CHEMBL503454 1 7.00
CHEMBL473446 1 6.89
CHEMBL504480 1 6.89
CHEMBL481581 1 6.80
CHEMBL509788 1 6.68
CHEMBL449546 1 6.57
CHEMBL509208 1 6.48
CHEMBL518649 1 6.42
CHEMBL460173 1 6.32
CHEMBL451856 1 6.29
CHEMBL502066 1 6.22
CHEMBL498873 1 6.19
CHEMBL481775 1 6.16
CHEMBL467229 1 6.11
CHEMBL513318 1 5.70
CHEMBL450954 1 5.50
CHEMBL446802 1 5.25
CHEMBL520607 1 4.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL508392 IC50 = 30.0 nM 7.52
CHEMBL503454 IC50 = 100.0 nM 7.00
CHEMBL473446 IC50 = 130.0 nM 6.89
CHEMBL504480 IC50 = 130.0 nM 6.89
CHEMBL481581 IC50 = 160.0 nM 6.80
CHEMBL509788 IC50 = 210.0 nM 6.68
CHEMBL449546 IC50 = 270.0 nM 6.57
CHEMBL509208 IC50 = 330.0 nM 6.48
CHEMBL518649 IC50 = 380.0 nM 6.42
CHEMBL460173 IC50 = 480.0 nM 6.32
CHEMBL451856 IC50 = 510.0 nM 6.29
CHEMBL502066 IC50 = 600.0 nM 6.22
CHEMBL498873 IC50 = 650.0 nM 6.19
CHEMBL481775 IC50 = 700.0 nM 6.16
CHEMBL467229 IC50 = 780.0 nM 6.11
CHEMBL513318 IC50 = 2010.0 nM 5.70
CHEMBL450954 IC50 = 3150.0 nM 5.50
CHEMBL446802 IC50 = 5660.0 nM 5.25
CHEMBL520607 IC50 = 17300.0 nM 4.76