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Assay Detail

CHEMBL4015837

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

Binding
Inhibition of full length FLAG-tagged XIAP (unknown origin) interaction with full length untagged caspase-9 expressed in HEK293 cells after 2 hrs by immunoprecipitation 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

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

Publication

Discovery of a Potent Nonpeptidomimetic, Small-Molecule Antagonist of Cellular Inhibitor of Apoptosis Protein 1 (cIAP1) and X-Linked Inhibitor of Apoptosis Protein (XIAP).
Tamanini E, Buck IM, Chessari G, Chiarparin E, Day JEH, Frederickson M, Griffiths-Jones CM, Hearn K, Heightman TD, Iqbal A, Johnson CN, Lewis EJ, Martins V, Peakman T, Reader M, Rich SJ, Ward GA, Williams PA, Wilsher NE.
J Med Chem (2017) 60 : 4611 -4625
PubMed 28492317 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 7.40 8.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4064619 1 8.29
CHEMBL3700093 1 7.89
CHEMBL3700084 1 7.85
CHEMBL4081831 1 7.77
CHEMBL3700072 1 7.77
CHEMBL3700071 1 7.62
CHEMBL4090609 1 7.50
CHEMBL2431768 LCL-161 2.0 1 7.46
CHEMBL3700098 1 7.43
CHEMBL4062646 1 7.17
CHEMBL3700068 1 7.16
CHEMBL4092217 1 7.14
CHEMBL3700052 1 6.92
CHEMBL3700059 1 6.89
CHEMBL3700061 1 6.82
CHEMBL3700085 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4064619 EC50 = 5.1 nM 8.29
CHEMBL3700093 EC50 = 13.0 nM 7.89
CHEMBL3700084 EC50 = 14.0 nM 7.85
CHEMBL4081831 EC50 = 17.0 nM 7.77
CHEMBL3700072 EC50 = 17.0 nM 7.77
CHEMBL3700071 EC50 = 24.0 nM 7.62
CHEMBL4090609 EC50 = 32.0 nM 7.50
CHEMBL2431768 LCL-161 EC50 = 35.0 nM 7.46
CHEMBL3700098 EC50 = 37.0 nM 7.43
CHEMBL4062646 EC50 = 67.0 nM 7.17
CHEMBL3700068 EC50 = 69.0 nM 7.16
CHEMBL4092217 EC50 = 73.0 nM 7.14
CHEMBL3700052 EC50 = 120.0 nM 6.92
CHEMBL3700059 EC50 = 130.0 nM 6.89
CHEMBL3700061 EC50 = 150.0 nM 6.82
CHEMBL3700085 EC50 = 180.0 nM 6.75