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Assay Detail

CHEMBL4433382

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 assessed as decrease in AMC hydrolysis using Suc-Leu-Leu-Val-Tyr-AMC as substrate incubated for 30 mins by fluorometric analysis
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

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 6 6.86 7.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL297453 EPIGALOCATECHIN GALLATE 3.0 1 7.07
CHEMBL129451 (-)-CATECHINGALLATE 1 6.91
CHEMBL264938 GALLOCATECHIN GALLATE 1 6.73
CHEMBL36327 EPICATECHIN GALLATE 1 6.71
CHEMBL47386 EPIGALLOCATECHIN 1 -
CHEMBL288114 GALLIC ACID 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL297453 EPIGALOCATECHIN GALLATE IC50 = 86.0 nM 7.07
CHEMBL129451 (-)-CATECHINGALLATE IC50 = 124.0 nM 6.91
CHEMBL264938 GALLOCATECHIN GALLATE IC50 = 187.0 nM 6.73
CHEMBL36327 EPICATECHIN GALLATE IC50 = 194.0 nM 6.71
CHEMBL47386 EPIGALLOCATECHIN IC50 = 1200000.0 nM -
CHEMBL288114 GALLIC ACID IC50 = 7100000.0 nM -