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Assay Detail

CHEMBL4325679

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

Binding
Inhibition of CYP3A5 in doxycycline-induced CYP3A5 overexpressing wild type human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate pretreated with doxycycline for 24 hrs followed by incubation with compound for 24 hrs by LC-MS/MS analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type ASPC1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 3A5 (CHEMBL3019)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5.
Wright WC, Chenge J, Wang J, Girvan HM, Yang L, Chai SC, Huber AD, Wu J, Oladimeji PO, Munro AW, Chen T.
J Med Chem (2020) 63 : 1415 -1433
PubMed 31965799 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.27 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1159650 CLOBETASOL PROPIONATE 4.0 1 7.68
CHEMBL157101 KETOCONAZOLE 4.0 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1159650 CLOBETASOL PROPIONATE IC50 = 21.0 nM 7.68
CHEMBL157101 KETOCONAZOLE IC50 = 141.0 nM 6.85