Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2184802

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

Binding
Reversible inhibition of human erythrocyte derived 20S proteasome subunit beta1 after 30 mins by fluorogenic 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

Proteasome component C5 (CHEMBL4208)
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 3 7.05 7.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2141296 IXAZOMIB 3.0 1 7.51
CHEMBL325041 BORTEZOMIB 3.0 1 7.28
CHEMBL371405 MARIZOMIB 3.0 1 6.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2141296 IXAZOMIB IC50 = 31.0 nM 7.51
CHEMBL325041 BORTEZOMIB IC50 = 53.0 nM 7.28
CHEMBL371405 MARIZOMIB IC50 = 430.0 nM 6.37