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Assay Detail

CHEMBL3817033

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

Binding
Agonist activity at human LXRbeta ligand binding domain(155 to 460 residues) transfected in HEK293 cells after 16 hrs by Gal4-luciferase reporter gene assay
14
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR) β Agonist.
Zheng Y, Zhuang L, Fan KY, Tice CM, Zhao W, Dong C, Lotesta SD, Leftheris K, Lindblom PR, Liu Z, Shimada J, Noto PB, Meng S, Hardy A, Howard L, Krosky P, Guo J, Lipinski K, Kandpal G, Bukhtiyarov Y, Zhao Y, Lala D, Van Orden R, Zhou J, Chen G, Wu Z, McKeever BM, McGeehan GM, Gregg RE, Claremon DA, Singh SB.
J Med Chem (2016) 59 : 3264 -3271
PubMed 26990539 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 6.72 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3814501 1 7.68
CHEMBL3814206 1 7.68
CHEMBL3814006 1 7.52
CHEMBL3815014 1 7.28
CHEMBL3814153 1 7.28
CHEMBL3815001 1 7.17
CHEMBL3814478 1 7.10
CHEMBL3813863 1 6.30
CHEMBL3814372 3 6.00
CHEMBL3813875 2 5.89
CHEMBL3815113 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3814501 EC50 = 21.0 nM 7.68
CHEMBL3814206 EC50 = 21.0 nM 7.68
CHEMBL3814006 EC50 = 30.0 nM 7.52
CHEMBL3815014 EC50 = 53.0 nM 7.28
CHEMBL3814153 EC50 = 53.0 nM 7.28
CHEMBL3815001 EC50 = 68.0 nM 7.17
CHEMBL3814478 EC50 = 80.0 nM 7.10
CHEMBL3813863 EC50 = 503.0 nM 6.30
CHEMBL3814372 EC50 = 990.0 nM 6.00
CHEMBL3813875 EC50 = 1289.0 nM 5.89
CHEMBL3814372 EC50 = 2135.0 nM 5.67
CHEMBL3814372 EC50 = 9200.0 nM 5.04
CHEMBL3815113 EC50 > 20000.0 nM -
CHEMBL3813875 EC50 > 10000.0 nM -