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Assay Detail

CHEMBL2162880

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

Binding
Binding affinity to His6-tagged human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) assessed as dissociation constant after 2 to 3 hrs by fluorescence polarization assay
1
Total Activities
1
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

E3 ubiquitin-protein ligase XIAP (CHEMBL4198)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
Cai Q, Sun H, Peng Y, Lu J, Nikolovska-Coleska Z, McEachern D, Liu L, Qiu S, Yang CY, Miller R, Yi H, Zhang T, Sun D, Kang S, Guo M, Leopold L, Yang D, Wang S.
J Med Chem (2011) 54 : 2714 -2726
PubMed 21443232 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 8.36 8.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2158054 1 8.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2158054 Kd = 4.4 nM 8.36