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Assay Detail

CHEMBL5098730

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

Binding
Antagonist activity at N-terminal His-tagged cIAP2-BIR3 domain (unknown origin) expressed in Escherichia coli BL21 using AVPIAQKSEK-biotinylated peptide as substrate incubated for 2 hrs by DELFIA assay
12
Total Activities
12
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

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 12 6.73 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2431768 LCL-161 2.0 1 7.77
CHEMBL5174454 1 7.23
CHEMBL5191180 1 6.85
CHEMBL5170823 1 6.75
CHEMBL5186855 1 6.62
CHEMBL5175233 1 6.54
CHEMBL5193194 1 6.43
CHEMBL5195146 1 6.40
CHEMBL5181541 1 6.37
CHEMBL5203019 1 6.29
CHEMBL5169527 1 -
CHEMBL5200297 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2431768 LCL-161 IC50 = 17.0 nM 7.77
CHEMBL5174454 IC50 = 59.0 nM 7.23
CHEMBL5191180 IC50 = 140.0 nM 6.85
CHEMBL5170823 IC50 = 177.0 nM 6.75
CHEMBL5186855 IC50 = 240.0 nM 6.62
CHEMBL5175233 IC50 = 288.0 nM 6.54
CHEMBL5193194 IC50 = 371.0 nM 6.43
CHEMBL5195146 IC50 = 397.0 nM 6.40
CHEMBL5181541 IC50 = 431.0 nM 6.37
CHEMBL5203019 IC50 = 519.0 nM 6.29
CHEMBL5169527 IC50 > 2000.0 nM -
CHEMBL5200297 IC50 > 1500.0 nM -