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Assay Detail

CHEMBL4416033

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

Binding
Inhibition of N-terminal 6x-His-tagged recombinant human cIAP2-BIR3 (244 to 349 residues) expressed in Escherichia coli 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

Baculoviral IAP repeat-containing protein 3 (CHEMBL5335)
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 7.58 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4581366 1 8.05
CHEMBL4552412 1 7.90
CHEMBL2431768 LCL-161 2.0 1 7.72
CHEMBL4437401 1 7.33
CHEMBL2158051 XEVINAPANT 3.0 1 6.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4581366 IC50 = 9.0 nM 8.05
CHEMBL4552412 IC50 = 12.5 nM 7.90
CHEMBL2431768 LCL-161 IC50 = 19.0 nM 7.72
CHEMBL4437401 IC50 = 47.0 nM 7.33
CHEMBL2158051 XEVINAPANT IC50 = 133.0 nM 6.88