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Assay Detail

CHEMBL896823

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Functional
Agonist activity at human LXRalpha receptor after 1 hr by HTRF cofactor recruitment assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Oxysterols receptor LXR-alpha (CHEMBL2808)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists.
Kher S, Lake K, Sircar I, Pannala M, Bakir F, Zapf J, Xu K, Zhang SH, Liu J, Morera L, Sakurai N, Jack R, Cheng JF.
Bioorg Med Chem Lett (2007) 17 : 4442 -4446
PubMed 17587573 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.30 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL62136 T091317 1 7.40
CHEMBL392996 1 6.66
CHEMBL59030 1 6.43
CHEMBL393966 1 5.96
CHEMBL397612 1 5.94
CHEMBL397564 1 5.92
CHEMBL233369 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL62136 T091317 EC50 = 40.0 nM 7.40
CHEMBL392996 EC50 = 220.0 nM 6.66
CHEMBL59030 EC50 = 367.0 nM 6.43
CHEMBL393966 EC50 = 1110.0 nM 5.96
CHEMBL397612 EC50 = 1150.0 nM 5.94
CHEMBL397564 EC50 = 1190.0 nM 5.92
CHEMBL233369 EC50 = 1500.0 nM 5.82