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

CHEMBL1073017

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

Binding
Inhibition of 26S proteasome beta 5 using LLVY as substrate
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Proteasome Macropain subunit MB1 (CHEMBL4662)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Incorporation of fluorinated phenylalanine generates highly specific inhibitor of proteasome's chymotrypsin-like sites.
Geurink PP, Liu N, Spaans MP, Downey SL, van den Nieuwendijk AM, van der Marel GA, Kisselev AF, Florea BI, Overkleeft HS.
J Med Chem (2010) 53 : 2319 -2323
PubMed 20131905 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.61 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL578478 1 9.00
CHEMBL578885 1 8.70
CHEMBL579296 1 8.52
CHEMBL592161 1 7.51
CHEMBL591777 1 7.00
CHEMBL578486 1 6.89
CHEMBL577867 1 6.70
CHEMBL578518 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL578478 IC50 = 1.0 nM 9.00
CHEMBL578885 IC50 = 2.0 nM 8.70
CHEMBL579296 IC50 = 3.0 nM 8.52
CHEMBL592161 IC50 = 31.0 nM 7.51
CHEMBL591777 IC50 = 100.0 nM 7.00
CHEMBL578486 IC50 = 130.0 nM 6.89
CHEMBL577867 IC50 = 200.0 nM 6.70
CHEMBL578518 IC50 = 300.0 nM 6.52