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Assay Detail

CHEMBL886106

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

Functional
Activation of LXRbeta co-transfected in COS7 cells with RXRalpha by reporter transactivation assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type COS-7
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Oxysterols receptor LXR-beta (CHEMBL4093)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists.
Bakir F, Kher S, Pannala M, Wilson N, Nguyen T, Sircar I, Takedomi K, Fukushima C, Zapf J, Xu K, Zhang SH, Liu J, Morera L, Schneider L, Sakurai N, Jack R, Cheng JF.
Bioorg Med Chem Lett (2007) 17 : 3473 -3479
PubMed 17416521 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 7.15 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL62136 T091317 1 7.96
CHEMBL59030 1 7.82
CHEMBL251331 1 7.28
CHEMBL233369 1 7.19
CHEMBL398680 1 6.92
CHEMBL400937 1 6.47
CHEMBL251538 1 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL62136 T091317 EC50 = 11.0 nM 7.96
CHEMBL59030 EC50 = 15.0 nM 7.82
CHEMBL251331 EC50 = 52.0 nM 7.28
CHEMBL233369 EC50 = 65.0 nM 7.19
CHEMBL398680 EC50 = 120.0 nM 6.92
CHEMBL400937 EC50 = 336.0 nM 6.47
CHEMBL251538 EC50 = 363.0 nM 6.44