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

CHEMBL4479416

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

Binding
Inhibition of catalytic activity of constitutive proteasome 20s subunit beta5 in human RPMI8226 cells incubated for 1 hr by BODIPY(TMR)-NC-005-VS probe based competitive activity based protein profiling assay
2
Total Activities
2
Compounds Tested
2
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

Structure-Based Design of β5c Selective Inhibitors of Human Constitutive Proteasomes.
Xin BT, de Bruin G, Huber EM, Besse A, Florea BI, Filippov DV, van der Marel GA, Kisselev AF, van der Stelt M, Driessen C, Groll M, Overkleeft HS.
J Med Chem (2016) 59 : 7177 -7187
PubMed 27438186 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.56 6.56
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4522536 1 6.56
CHEMBL4581001 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4522536 IC50 = 274.0 nM 6.56
CHEMBL4581001 Inhibition - % -