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Assay Detail

CHEMBL1019892

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

Binding
Inhibition of GST fused Bcl-2 binding to biotinylated 16 mer Bak-BH3 peptide by HTRF-LANCE assay
35
Total Activities
35
Compounds Tested
2
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 34 6.44 8.00
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL473446 1 8.00
CHEMBL509208 1 7.70
CHEMBL481581 1 7.70
CHEMBL503454 1 7.52
CHEMBL504480 1 7.40
CHEMBL449546 1 7.40
CHEMBL509788 1 7.40
CHEMBL460173 1 7.30
CHEMBL481775 1 7.05
CHEMBL467229 1 7.00
CHEMBL514298 1 6.96
CHEMBL453380 1 6.96
CHEMBL500866 1 6.85
CHEMBL500574 1 6.82
CHEMBL501871 1 6.80
CHEMBL444140 1 6.72
CHEMBL513318 1 6.64
CHEMBL450954 1 6.60
CHEMBL453466 1 6.55
CHEMBL510332 1 6.14
CHEMBL517577 1 6.10
CHEMBL446802 1 6.09
CHEMBL446607 1 5.98
CHEMBL516633 1 5.85
CHEMBL464268 1 5.82
CHEMBL480009 1 5.72
CHEMBL518858 1 5.64
CHEMBL466801 1 5.60
CHEMBL480008 1 5.52
CHEMBL520607 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL473446 IC50 = 10.0 nM 8.00
CHEMBL509208 IC50 = 20.0 nM 7.70
CHEMBL481581 IC50 = 20.0 nM 7.70
CHEMBL503454 IC50 = 30.0 nM 7.52
CHEMBL504480 IC50 = 40.0 nM 7.40
CHEMBL449546 IC50 = 40.0 nM 7.40
CHEMBL509788 IC50 = 40.0 nM 7.40
CHEMBL460173 IC50 = 50.0 nM 7.30
CHEMBL481775 IC50 = 90.0 nM 7.05
CHEMBL467229 IC50 = 100.0 nM 7.00
CHEMBL514298 IC50 = 110.0 nM 6.96
CHEMBL453380 IC50 = 110.0 nM 6.96
CHEMBL500866 IC50 = 140.0 nM 6.85
CHEMBL500574 IC50 = 150.0 nM 6.82
CHEMBL501871 IC50 = 160.0 nM 6.80
CHEMBL444140 IC50 = 190.0 nM 6.72
CHEMBL513318 IC50 = 230.0 nM 6.64
CHEMBL450954 IC50 = 250.0 nM 6.60
CHEMBL453466 IC50 = 280.0 nM 6.55
CHEMBL510332 IC50 = 730.0 nM 6.14
CHEMBL517577 IC50 = 800.0 nM 6.10
CHEMBL446802 IC50 = 810.0 nM 6.09
CHEMBL446607 IC50 = 1050.0 nM 5.98
CHEMBL516633 IC50 = 1400.0 nM 5.85
CHEMBL464268 IC50 = 1500.0 nM 5.82
CHEMBL480009 IC50 = 1900.0 nM 5.72
CHEMBL518858 IC50 = 2300.0 nM 5.64
CHEMBL466801 IC50 = 2500.0 nM 5.60
CHEMBL480008 IC50 = 3000.0 nM 5.52
CHEMBL520607 IC50 = 3670.0 nM 5.43
CHEMBL446480 IC50 = 5610.0 nM 5.25
CHEMBL480010 IC50 = 7700.0 nM 5.11
CHEMBL469305 IC50 = 10700.0 nM 4.97
CHEMBL464440 IC50 = 50000.0 nM 4.30
CHEMBL466802 Activity - -