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Assay Detail

CHEMBL3294824

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

Binding
Antagonist activity at human PXR transfected in African green monkey CV1 cells assessed as inhibition of SR12813-induced transactivation after 24 hrs by luciferase reporter gene assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CV-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Nuclear receptor subfamily 1 group I member 2 (CHEMBL3401)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Bazedoxifene-scaffold-based mimetics of solomonsterols A and B as novel pregnane X receptor antagonists.
Hodnik Ž, Peterlin Mašič L, Tomašić T, Smodiš D, D'Amore C, Fiorucci S, Kikelj D.
J Med Chem (2014) 57 : 4819 -4833
PubMed 24828006 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.92 4.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL30707 COUMESTROL 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL30707 COUMESTROL IC50 = 12000.0 nM 4.92