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Assay Detail

CHEMBL3868528

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

Binding
Agonist activity at human PXR expressed in human HepG2 cells assessed as induction of CYP3A4 measured after 24 hrs by AlamarBlue dye-based 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

Discovery of Highly Potent Liver X Receptor β Agonists.
Kick EK, Busch BB, Martin R, Stevens WC, Bollu V, Xie Y, Boren BC, Nyman MC, Nanao MH, Nguyen L, Plonowski A, Schulman IG, Yan G, Zhang H, Hou X, Valente MN, Narayanan R, Behnia K, Rodrigues AD, Brock B, Smalley J, Cantor GH, Lupisella J, Sleph P, Grimm D, Ostrowski J, Wexler RR, Kirchgessner T, Mohan R.
ACS Med Chem Lett (2016) 7 : 1207 -1212
PubMed 27994765 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 5.76 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3945199 BMS-852927 1.0 1 6.00
CHEMBL3953927 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3945199 BMS-852927 EC50 = 1000.0 nM 6.00
CHEMBL3953927 EC50 = 3000.0 nM 5.52