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Assay Detail

CHEMBL1777015

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

Binding
Competitive inhibition of human cIAP1 BIR3 domain after 2 to 3 hrs by fluorescence polarization assay
16
Total Activities
16
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

Potent bivalent Smac mimetics: effect of the linker on binding to inhibitor of apoptosis proteins (IAPs) and anticancer activity.
Sun H, Liu L, Lu J, Bai L, Li X, Nikolovska-Coleska Z, McEachern D, Yang CY, Qiu S, Yi H, Sun D, Wang S.
J Med Chem (2011) 54 : 3306 -3318
PubMed 21462933 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 8.15 8.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1774157 1 8.59
CHEMBL1774031 1 8.55
CHEMBL1774160 1 8.49
CHEMBL1774154 1 8.34
CHEMBL1774163 1 8.31
CHEMBL1774158 1 8.27
CHEMBL1774156 1 8.21
CHEMBL1774161 1 8.21
CHEMBL1774162 1 8.17
CHEMBL1774164 1 8.12
CHEMBL1773083 1 8.00
CHEMBL1774159 1 7.89
CHEMBL1774165 1 7.89
CHEMBL1774166 1 7.80
CHEMBL481422 1 7.42
CHEMBL1774155 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1774157 IC50 = 2.6 nM 8.59
CHEMBL1774031 IC50 = 2.8 nM 8.55
CHEMBL1774160 IC50 = 3.2 nM 8.49
CHEMBL1774154 IC50 = 4.6 nM 8.34
CHEMBL1774163 IC50 = 4.9 nM 8.31
CHEMBL1774158 IC50 = 5.4 nM 8.27
CHEMBL1774156 IC50 = 6.2 nM 8.21
CHEMBL1774161 IC50 = 6.2 nM 8.21
CHEMBL1774162 IC50 = 6.8 nM 8.17
CHEMBL1774164 IC50 = 7.5 nM 8.12
CHEMBL1773083 IC50 = 10.0 nM 8.00
CHEMBL1774159 IC50 = 13.0 nM 7.89
CHEMBL1774165 IC50 = 13.0 nM 7.89
CHEMBL1774166 IC50 = 16.0 nM 7.80
CHEMBL481422 IC50 = 38.0 nM 7.42
CHEMBL1774155 IC50 > 50000.0 nM -