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Assay Detail

CHEMBL5223569

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

Binding
Inhibition of beta5 proteasome (unknown origin)
8
Total Activities
8
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 Macropain subunit MB1 (CHEMBL4662)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Proteases and Their Modulators in Cancer Therapy: Challenges and Opportunities.
Song R, Qiao W, He J, Huang J, Luo Y, Yang T.
J Med Chem (2021) 64 : 2851 -2877
PubMed 33656892 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.44 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64925 MG-132 1 8.92
CHEMBL270515 DELANZOMIB 2.0 1 8.82
CHEMBL325041 BORTEZOMIB 3.0 1 8.62
CHEMBL5283576 1 8.59
CHEMBL2103884 OPROZOMIB 2.0 1 8.52
CHEMBL2141296 IXAZOMIB 3.0 1 8.47
CHEMBL451887 CARFILZOMIB 4.0 1 8.22
CHEMBL5269437 1 7.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64925 MG-132 IC50 = 1.2 nM 8.92
CHEMBL270515 DELANZOMIB IC50 = 1.5 nM 8.82
CHEMBL325041 BORTEZOMIB IC50 = 2.4 nM 8.62
CHEMBL5283576 IC50 = 2.6 nM 8.59
CHEMBL2103884 OPROZOMIB IC50 = 3.0 nM 8.52
CHEMBL2141296 IXAZOMIB IC50 = 3.4 nM 8.47
CHEMBL451887 CARFILZOMIB IC50 = 6.0 nM 8.22
CHEMBL5269437 IC50 = 47.0 nM 7.33