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Assay Detail

CHEMBL1805306

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

Binding
Transactivation of human PXR expressed in HepG2 cells after 18 hrs by luciferase reporter gene assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HepG2
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

Total synthesis and pharmacological characterization of solomonsterol A, a potent marine pregnane-X-receptor agonist endowed with anti-inflammatory activity.
Sepe V, Ummarino R, D'Auria MV, Mencarelli A, D'Amore C, Renga B, Zampella A, Fiorucci S.
J Med Chem (2011) 54 : 4590 -4599
PubMed 21599020 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 5.47 5.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1617 RIFAXIMIN 4.0 1 5.66
CHEMBL1649712 SOLOMONSTEROL A 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1617 RIFAXIMIN EC50 = 2200.0 nM 5.66
CHEMBL1649712 SOLOMONSTEROL A EC50 = 5200.0 nM 5.28