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Assay Detail

CHEMBL2184801

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

Binding
Irreversible inhibition of constitutive 20S proteasome subunit beta5 chymotrypsin-like activity in human WM cells using suc-LLVY-amc as substrate after 2 hrs by fluorescence assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type WM
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Proteasome Macropain subunit MB1 (CHEMBL4662)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Molecular mechanisms of acquired proteasome inhibitor resistance.
Kale AJ, Moore BS.
J Med Chem (2012) 55 : 10317 -10327
PubMed 22978849 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.00 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2103884 OPROZOMIB 2.0 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2103884 OPROZOMIB IC50 = 10.0 nM 8.00