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Assay Detail

CHEMBL1100434

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

ADMET
Inhibition of CYP3A4 assessed as ratio of IC50 at 0 mins to IC50 at 10 mins using 7-benzyloxyquinoline substrate
2
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Cytochrome P450 3A4 (CHEMBL340)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Evaluation of basic, heterocyclic ring systems as templates for use as potassium competitive acid blockers (pCABs).
Panchal T, Bailey N, Bamford M, Demont E, Elliott R, Farre-Gutierrez I, Garton N, Hayhow T, Hutley G, Naylor A.
Bioorg Med Chem Lett (2009) 19 : 6813 -6817
PubMed 19846298 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.25 7.25
Ratio IC50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1087758 1 7.25
CHEMBL497011 LINAPRAZAN 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1087758 IC50 = 56.23 nM 7.25
CHEMBL497011 LINAPRAZAN Ratio IC50 = 10.0 -