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Assay Detail

CHEMBL3817039

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Binding
Agonist activity at LXR in human HepG2 cells assessed as upregulation of SREBP1C gene expression after 24 hrs by RT-PCR analysis
3
Total Activities
1
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HepG2
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Liver X receptor (CHEMBL3706564)
Type PROTEIN FAMILY
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 1 8.22 8.22
Efficacy 1 - -
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3814206 3 8.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3814206 EC50 = 6.0 nM 8.22
CHEMBL3814206 Efficacy = 91.0 % -
CHEMBL3814206 Activity - -