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Assay Detail

CHEMBL830108

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

Binding
Effective concentration for Steroid receptor coactivator-1 (SRC1) recruitment to human LXRbeta (Liver X receptor)
11
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 Expert

Target

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

Publication

Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure.
Jaye MC, Krawiec JA, Campobasso N, Smallwood A, Qiu C, Lu Q, Kerrigan JJ, De Los Frailes Alvaro M, Laffitte B, Liu WS, Marino JP, Meyer CR, Nichols JA, Parks DJ, Perez P, Sarov-Blat L, Seepersaud SD, Steplewski KM, Thompson SK, Wang P, Watson MA, Webb CL, Haigh D, Caravella JA, Macphee CH, Willson TM, Collins JL.
J Med Chem (2005) 48 : 5419 -5422
PubMed 16107141 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 6.83 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL59030 1 7.70
CHEMBL62136 T091317 1 7.52
CHEMBL189938 1 7.40
CHEMBL364666 1 7.16
CHEMBL190901 1 6.96
CHEMBL191263 1 6.70
CHEMBL189228 1 6.58
CHEMBL191419 1 6.52
CHEMBL370285 1 6.25
CHEMBL189532 1 6.24
CHEMBL158781 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL59030 EC50 = 20.0 nM 7.70
CHEMBL62136 T091317 EC50 = 30.0 nM 7.52
CHEMBL189938 EC50 = 40.0 nM 7.40
CHEMBL364666 EC50 = 70.0 nM 7.16
CHEMBL190901 EC50 = 110.0 nM 6.96
CHEMBL191263 EC50 = 200.0 nM 6.70
CHEMBL189228 EC50 = 260.0 nM 6.58
CHEMBL191419 EC50 = 300.0 nM 6.52
CHEMBL370285 EC50 = 560.0 nM 6.25
CHEMBL189532 EC50 = 575.0 nM 6.24
CHEMBL158781 EC50 = 850.0 nM 6.07