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Assay Detail

CHEMBL3540468

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ADMET
Mechanism-based inhibition of recombinant human CYP2C9 expressed in microsomes isolated from Saccharomyces cerevisiae AH22 cells assessed as diclofenac 4'-hydroxylation preincubated for 5 to 10 mins followed by substrate addition measured after 15 mins by HPLC analysis
3
Total Activities
1
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type AH22
Subcellular Microsomes
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 2C9 (CHEMBL3397)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Comparison of metabolism of sesamin and episesamin by drug-metabolizing enzymes in human liver.
Yasuda K, Ikushiro S, Wakayama S, Itoh T, Yamamoto K, Kamakura M, Munetsuna E, Ohta M, Sakaki T.
Drug Metab Dispos (2012) 40 : 1917 -1926
PubMed 22752007 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 5.17 5.17
Inhibition 1 - -
Kinact 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL43469 ASARININ 3 5.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL43469 ASARININ Ki = 6800.0 nM 5.17
CHEMBL43469 ASARININ Inhibition - % -
CHEMBL43469 ASARININ Kinact = 0.17 /min -