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Assay Detail

CHEMBL3817030

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

Binding
Displacement of [3H]TO901317 from LXRalpha ligand binding domain (unknown origin) after 30 mins by liquid scintillation counting
14
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Oxysterols receptor LXR-alpha (CHEMBL2808)
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
Ki 14 6.85 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3814501 1 8.52
CHEMBL3814006 1 7.70
CHEMBL3814153 1 7.60
CHEMBL3815014 1 7.37
CHEMBL3814206 1 7.09
CHEMBL3815001 1 6.84
CHEMBL3814478 1 6.80
CHEMBL3813863 1 5.97
CHEMBL3813875 2 5.96
CHEMBL3814372 3 5.66
CHEMBL3815113 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3814501 Ki = 3.0 nM 8.52
CHEMBL3814006 Ki = 20.0 nM 7.70
CHEMBL3814153 Ki = 25.0 nM 7.60
CHEMBL3815014 Ki = 43.0 nM 7.37
CHEMBL3814206 Ki = 81.0 nM 7.09
CHEMBL3815001 Ki = 146.0 nM 6.84
CHEMBL3814478 Ki = 157.0 nM 6.80
CHEMBL3813863 Ki = 1072.0 nM 5.97
CHEMBL3813875 Ki = 1100.0 nM 5.96
CHEMBL3813875 Ki = 1552.0 nM 5.81
CHEMBL3814372 Ki = 2200.0 nM 5.66
CHEMBL3814372 Ki > 3300.0 nM -
CHEMBL3814372 Ki > 3300.0 nM -
CHEMBL3815113 Ki - -