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Assay Detail

CHEMBL4351153

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Binding
Binding affinity to XIAP-BIR3 domain (241 to 356 residues) (unknown origin) by fluorescence polarization-based competition assay
10
Total Activities
10
Compounds Tested
2
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

Inhibitor of Apoptosis Protein (IAP) Antagonists in Anticancer Agent Discovery: Current Status and Perspectives.
Cong H, Xu L, Wu Y, Qu Z, Bian T, Zhang W, Xing C, Zhuang C.
J Med Chem (2019) 62 : 5750 -5772
PubMed 30676015 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 9 7.51 8.30
IC50 1 7.78 7.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4460352 1 8.30
CHEMBL2096803 1 7.92
CHEMBL4459769 1 7.80
CHEMBL1230673 1 7.80
CHEMBL4452928 1 7.78
CHEMBL2063869 GDC-0152 1.0 1 7.55
CHEMBL189768 1 7.54
CHEMBL2431768 LCL-161 2.0 1 7.28
CHEMBL4518625 1 6.70
CHEMBL4460096 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4460352 Kd = 5.0 nM 8.30
CHEMBL2096803 Kd = 12.0 nM 7.92
CHEMBL4459769 Kd = 16.0 nM 7.80
CHEMBL1230673 Kd = 16.0 nM 7.80
CHEMBL4452928 IC50 = 16.6 nM 7.78
CHEMBL2063869 GDC-0152 Kd = 28.0 nM 7.55
CHEMBL189768 Kd = 29.0 nM 7.54
CHEMBL2431768 LCL-161 Kd = 52.7 nM 7.28
CHEMBL4518625 Kd = 200.0 nM 6.70
CHEMBL4460096 Kd = 220.0 nM 6.66