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Assay Detail

CHEMBL1109729

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

Binding
Agonist activity at LXRbeta ligand binding domain-mediated transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay
10
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CV-1
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Discovery of tertiary sulfonamides as potent liver X receptor antagonists.
Zuercher WJ, Buckholz RG, Campobasso N, Collins JL, Galardi CM, Gampe RT, Hyatt SM, Merrihew SL, Moore JT, Oplinger JA, Reid PR, Spearing PK, Stanley TB, Stewart EL, Willson TM.
J Med Chem (2010) 53 : 3412 -3416
PubMed 20345102 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 7.66 9.00
pEC50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1093554 1 9.00
CHEMBL1091034 1 8.50
CHEMBL1091976 1 8.50
CHEMBL1093523 1 7.80
CHEMBL1093840 1 7.70
CHEMBL1092952 1 7.10
CHEMBL62136 T091317 1 7.00
CHEMBL1093828 1 7.00
CHEMBL59030 1 6.30
CHEMBL1093266 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1093554 EC50 = 1.0 nM 9.00
CHEMBL1091034 EC50 = 3.162 nM 8.50
CHEMBL1091976 EC50 = 3.162 nM 8.50
CHEMBL1093523 EC50 = 15.85 nM 7.80
CHEMBL1093840 EC50 = 19.95 nM 7.70
CHEMBL1092952 EC50 = 79.43 nM 7.10
CHEMBL62136 T091317 EC50 = 100.0 nM 7.00
CHEMBL1093828 EC50 = 100.0 nM 7.00
CHEMBL59030 EC50 = 501.19 nM 6.30
CHEMBL1093266 pEC50 - -