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

CHEMBL3240089

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

Binding
Inhibition of beta5i subunit of immunoproteasome (unknown origin) by active-site ELISA
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

Proteasome subunit beta type-8 (CHEMBL5620)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structurally novel highly potent proteasome inhibitors created by the structure-based hybridization of nonpeptidic belactosin derivatives and peptide boronates.
Kawamura S, Unno Y, Asai A, Arisawa M, Shuto S.
J Med Chem (2014) 57 : 2726 -2735
PubMed 24524217 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.05 7.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3237863 1 7.51
CHEMBL3237873 1 7.23
CHEMBL325041 BORTEZOMIB 3.0 1 7.11
CHEMBL3237875 1 6.35
CHEMBL374308 LACTACYSTIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3237863 IC50 = 31.0 nM 7.51
CHEMBL3237873 IC50 = 59.0 nM 7.23
CHEMBL325041 BORTEZOMIB IC50 = 78.0 nM 7.11
CHEMBL3237875 IC50 = 450.0 nM 6.35
CHEMBL374308 LACTACYSTIN IC50 > 3000.0 nM -