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Assay Detail

CHEMBL1777016

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

Binding
Binding affinity to human cIAP1 BIR3 domain after 2 to 3 hrs by fluorescence polarization-based 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
Ki 16 8.77 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1774156 1 9.00
CHEMBL1774158 1 9.00
CHEMBL1774161 1 9.00
CHEMBL1774162 1 9.00
CHEMBL1774164 1 9.00
CHEMBL1773083 1 8.70
CHEMBL1774165 1 8.70
CHEMBL1774159 1 8.60
CHEMBL1774166 1 8.52
CHEMBL481422 1 8.17
CHEMBL1774154 1 -
CHEMBL1774157 1 -
CHEMBL1774031 1 -
CHEMBL1774160 1 -
CHEMBL1774163 1 -
CHEMBL1774155 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1774156 Ki = 1.0 nM 9.00
CHEMBL1774158 Ki = 1.0 nM 9.00
CHEMBL1774161 Ki = 1.0 nM 9.00
CHEMBL1774162 Ki = 1.0 nM 9.00
CHEMBL1774164 Ki = 1.0 nM 9.00
CHEMBL1773083 Ki = 2.0 nM 8.70
CHEMBL1774165 Ki = 2.0 nM 8.70
CHEMBL1774159 Ki = 2.5 nM 8.60
CHEMBL1774166 Ki = 3.0 nM 8.52
CHEMBL481422 Ki = 6.8 nM 8.17
CHEMBL1774154 Ki < 1.0 nM -
CHEMBL1774157 Ki < 1.0 nM -
CHEMBL1774031 Ki < 1.0 nM -
CHEMBL1774160 Ki < 1.0 nM -
CHEMBL1774163 Ki < 1.0 nM -
CHEMBL1774155 Ki > 9000.0 nM -