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Assay Detail

CHEMBL5098733

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

Binding
Antagonist activity at N-terminal His-tagged cIAP1-BIR3 domain (unknown origin) expressed in Escherichia coli BL21 using AVPIAQKSEK-biotinylated peptide as substrate preincubated for 2 hrs with protein followed by substrate addition measured after 2 hrs by DELFIA assay
3
Total Activities
3
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 2 (CHEMBL5462)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Lysine Covalent Antagonists of Melanoma Inhibitors of Apoptosis Protein.
Udompholkul P, Baggio C, Gambini L, Alboreggia G, Pellecchia M.
J Med Chem (2021) 64 : 16147 -16158
PubMed 34705456 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.09 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2431768 LCL-161 2.0 1 7.80
CHEMBL5174454 1 7.03
CHEMBL5195146 1 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2431768 LCL-161 IC50 = 16.0 nM 7.80
CHEMBL5174454 IC50 = 94.0 nM 7.03
CHEMBL5195146 IC50 = 370.0 nM 6.43