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Assay Detail

CHEMBL4416028

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

Binding
Inhibition of N-terminal His-tagged human XIAP-BIR3 (253 to 347 residues) expressed in Escherichia coli BL21-Gold(DE3) pLysS incubated for 2 hrs after 6 hrs pre-incubation with enzyme by biotinylated AVPI peptide based DELFIA
5
Total Activities
5
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

Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy.
Baggio C, Udompholkul P, Gambini L, Salem AF, Jossart J, Perry JJP, Pellecchia M.
J Med Chem (2019) 62 : 9188 -9200
PubMed 31550155 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.63 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4552412 1 7.96
CHEMBL4581366 1 7.92
CHEMBL4437401 1 7.55
CHEMBL2431768 LCL-161 2.0 1 7.40
CHEMBL2158051 XEVINAPANT 3.0 1 7.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4552412 IC50 = 11.0 nM 7.96
CHEMBL4581366 IC50 = 12.0 nM 7.92
CHEMBL4437401 IC50 = 28.0 nM 7.55
CHEMBL2431768 LCL-161 IC50 = 40.0 nM 7.40
CHEMBL2158051 XEVINAPANT IC50 = 47.8 nM 7.32