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Assay Detail

CHEMBL3539570

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

ADMET
Inhibition of CYP3A4.1 (unknown origin)-mediated testosterone 6beta-hydroxylation incubated for 10 mins prior to NADPH addition measured after 20 mins by HPLC-UV analysis
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

ADMET (CHEMBL612558)
Type ADMET

Publication

Comparison of the inhibitory profiles of itraconazole and cimetidine in cytochrome P450 3A4 genetic variants.
Akiyoshi T, Saito T, Murase S, Miyazaki M, Murayama N, Yamazaki H, Guengerich FP, Nakamura K, Yamamoto K, Ohtani H.
Drug Metab Dispos (2011) 39 : 724 -728
PubMed 21212239 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 2 - -
Ki 2 7.12 7.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64391 ITRACONAZOLE 4.0 2 7.12
CHEMBL30 CIMETIDINE 4.0 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64391 ITRACONAZOLE Ki = 76.0 nM 7.12
CHEMBL64391 ITRACONAZOLE Inhibition - % -
CHEMBL30 CIMETIDINE Inhibition - % -
CHEMBL30 CIMETIDINE Ki = 367000.0 nM -