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Assay Detail

CHEMBL3602896

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

Binding
Antagonist activity at cIAP1-BIR3 domain (unknown origin) assessed as inhibition of interaction with SMAC by fluorescence polarization assay
8
Total Activities
8
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

Baculoviral IAP repeat-containing protein 2 (CHEMBL5462)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Fragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP.
Chessari G, Buck IM, Day JE, Day PJ, Iqbal A, Johnson CN, Lewis EJ, Martins V, Miller D, Reader M, Rees DC, Rich SJ, Tamanini E, Vitorino M, Ward GA, Williams PA, Williams G, Wilsher NE, Woolford AJ.
J Med Chem (2015) 58 : 6574 -6588
PubMed 26218264 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.43 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3600717 1 8.00
CHEMBL3600735 1 6.50
CHEMBL3600734 1 6.19
CHEMBL3600733 1 5.43
CHEMBL3600732 1 4.70
CHEMBL181785 1 4.62
CHEMBL3600720 1 4.57
CHEMBL3600721 1 3.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3600717 IC50 = 10.0 nM 8.00
CHEMBL3600735 IC50 = 320.0 nM 6.50
CHEMBL3600734 IC50 = 650.0 nM 6.19
CHEMBL3600733 IC50 = 3700.0 nM 5.43
CHEMBL3600732 IC50 = 20000.0 nM 4.70
CHEMBL181785 IC50 = 24000.0 nM 4.62
CHEMBL3600720 IC50 = 27000.0 nM 4.57
CHEMBL3600721 IC50 = 410000.0 nM 3.39