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Assay Detail

CHEMBL4433374

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

Binding
Inhibition of chymotrypsin-like activity of purified human 20S proteasome expressed in human Jurkat cells assessed as decrease in AMC hydrolysis using Suc-Leu-Leu-Val-Tyr-AMC as substrate incubated for 2 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 5.18 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL151 LUTEOLIN 2.0 1 5.82
CHEMBL28 APIGENIN 1 5.75
CHEMBL50 QUERCETIN 3.0 1 5.46
CHEMBL117 CHRYSIN 1 5.31
CHEMBL164 MYRICETIN 1 5.00
CHEMBL150 KAEMPFEROL 1.0 1 4.98
CHEMBL8996 ERIODICTYOL 1 4.79
CHEMBL9352 NARINGENIN 1 4.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL151 LUTEOLIN IC50 = 1500.0 nM 5.82
CHEMBL28 APIGENIN IC50 = 1800.0 nM 5.75
CHEMBL50 QUERCETIN IC50 = 3500.0 nM 5.46
CHEMBL117 CHRYSIN IC50 = 4900.0 nM 5.31
CHEMBL164 MYRICETIN IC50 = 10000.0 nM 5.00
CHEMBL150 KAEMPFEROL IC50 = 10500.0 nM 4.98
CHEMBL8996 ERIODICTYOL IC50 = 16200.0 nM 4.79
CHEMBL9352 NARINGENIN IC50 = 48800.0 nM 4.31