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

CHEMBL4433375

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

Binding
Inhibition of chymotrypsin-like activity of human 26S proteasome in human Jurkat cells assessed as decrease in AMC hydrolysis using Z-Gly-Gly-Leu-AMC as substrate after 24 hrs by fluorescence based method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Jurkat
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Another look at phenolic compounds in cancer therapy the effect of polyphenols on ubiquitin-proteasome system.
Golonko A, Pienkowski T, Swislocka R, Lazny R, Roszko M, Lewandowski W.
Eur J Med Chem (2019) 167 : 291 -311
PubMed 30776692 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.24 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL28 APIGENIN 1 6.00
CHEMBL151 LUTEOLIN 2.0 1 5.89
CHEMBL50 QUERCETIN 3.0 1 5.70
CHEMBL117 CHRYSIN 1 5.21
CHEMBL150 KAEMPFEROL 1.0 1 4.96
CHEMBL164 MYRICETIN 1 4.92
CHEMBL8996 ERIODICTYOL 1 4.84
CHEMBL9352 NARINGENIN 1 4.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL28 APIGENIN IC50 = 1000.0 nM 6.00
CHEMBL151 LUTEOLIN IC50 = 1300.0 nM 5.89
CHEMBL50 QUERCETIN IC50 = 2000.0 nM 5.70
CHEMBL117 CHRYSIN IC50 = 6100.0 nM 5.21
CHEMBL150 KAEMPFEROL IC50 = 11000.0 nM 4.96
CHEMBL164 MYRICETIN IC50 = 12000.0 nM 4.92
CHEMBL8996 ERIODICTYOL IC50 = 14600.0 nM 4.84
CHEMBL9352 NARINGENIN IC50 = 41600.0 nM 4.38