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Assay Detail

CHEMBL4311828

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

Binding
Inhibition of chymotrypsin like activity of 26S proteasome beta 5 subunit (unknown origin) by fluorescence assay
6
Total Activities
6
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

Tripeptide analogues of MG132 as protease inhibitors.
Pehere AD, Nguyen S, Garlick SK, Wilson DW, Hudson I, Sykes MJ, Morton JD, Abell AD.
Bioorg Med Chem (2019) 27 : 436 -441
PubMed 30581047 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.00 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64925 MG-132 1 8.92
CHEMBL4590466 1 6.86
CHEMBL4574306 1 6.72
CHEMBL4475662 1 6.66
CHEMBL4531762 1 6.57
CHEMBL4540394 1 6.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64925 MG-132 IC50 = 1.2 nM 8.92
CHEMBL4590466 IC50 = 139.0 nM 6.86
CHEMBL4574306 IC50 = 189.0 nM 6.72
CHEMBL4475662 IC50 = 220.0 nM 6.66
CHEMBL4531762 IC50 = 269.0 nM 6.57
CHEMBL4540394 IC50 = 514.0 nM 6.29