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Assay Detail

CHEMBL5223566

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

Binding
Inhibition of beta 1 proteasome (unknown origin)
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 component C5 (CHEMBL4208)
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 5 7.03 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL325041 BORTEZOMIB 3.0 1 7.62
CHEMBL2141296 IXAZOMIB 3.0 1 7.51
CHEMBL5283576 1 7.49
CHEMBL64925 MG-132 1 6.92
CHEMBL451887 CARFILZOMIB 4.0 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL325041 BORTEZOMIB IC50 = 24.0 nM 7.62
CHEMBL2141296 IXAZOMIB IC50 = 31.0 nM 7.51
CHEMBL5283576 IC50 = 32.7 nM 7.49
CHEMBL64925 MG-132 IC50 = 120.0 nM 6.92
CHEMBL451887 CARFILZOMIB IC50 = 2400.0 nM 5.62