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Assay Detail

CHEMBL4433385

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

Binding
Inhibition of chymotrypsin-like activity of purified human erythrocyte 20S proteasome assessed as decrease in AMC hydrolysis using Suc-LLVY-AMC as substrate preincubated for 10 mins and measured by fluorescence based method
7
Total Activities
7
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 7 5.21 5.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129795 ISOLIQUIRITIGENIN 1 5.31
CHEMBL402744 1 5.28
CHEMBL44 GENISTEIN 2.0 1 5.03
CHEMBL252642 LIQUIRTIGENIN 1 -
CHEMBL238845 1 -
CHEMBL8145 DAIDZEIN 2.0 1 -
CHEMBL242341 FORMONONETIN 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129795 ISOLIQUIRITIGENIN IC50 = 4880.0 nM 5.31
CHEMBL402744 IC50 = 5210.0 nM 5.28
CHEMBL44 GENISTEIN IC50 = 9260.0 nM 5.03
CHEMBL252642 LIQUIRTIGENIN IC50 > 100000.0 nM -
CHEMBL238845 IC50 > 100000.0 nM -
CHEMBL8145 DAIDZEIN IC50 > 100000.0 nM -
CHEMBL242341 FORMONONETIN IC50 > 100000.0 nM -