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Assay Detail

CHEMBL3528260

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ADMET
Substrate inhibition of human UGT1A3-mediated T-5224 acyl O-glucuronide formation after 10 to 60 mins in presence of UDP-glucuronic acid by HPLC method
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

UDP-glucuronosyltransferase 1A3 (CHEMBL3542435)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Metabolism of the c-Fos/activator protein-1 inhibitor T-5224 by multiple human UDP-glucuronosyltransferase isoforms.
Uchihashi S, Fukumoto H, Onoda M, Hayakawa H, Ikushiro S, Sakaki T.
Drug Metab Dispos (2011) 39 : 803 -813
PubMed 21346002 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 4.87 4.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3222137 1 4.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3222137 Ki = 13500.0 nM 4.87