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Assay Detail

CHEMBL958321

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

Binding
Agonist activity at LXRbeta ligand binding domain by FRET based SRC1 recruitment assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Liver X receptor agonists with selectivity for LXRbeta; N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides.
Swahn BM, Macsari I, Viklund J, Ohberg L, Sjödin J, Neelissen J, Lindquist J.
Bioorg Med Chem Lett (2009) 19 : 2009 -2012
PubMed 19264481 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 6.20 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL62136 T091317 1 8.10
CHEMBL59030 1 7.11
CHEMBL434302 24(S),25-EPOXYCHOLESTEROL 1 6.54
CHEMBL522370 1 6.24
CHEMBL495173 1 6.20
CHEMBL523211 1 6.10
CHEMBL494843 1 6.06
CHEMBL495020 1 6.03
CHEMBL521866 1 5.82
CHEMBL492798 1 5.72
CHEMBL495197 1 5.63
CHEMBL495196 1 5.58
CHEMBL521811 1 5.46
CHEMBL522668 1 -
CHEMBL492563 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL62136 T091317 EC50 = 8.0 nM 8.10
CHEMBL59030 EC50 = 78.0 nM 7.11
CHEMBL434302 24(S),25-EPOXYCHOLESTEROL EC50 = 286.0 nM 6.54
CHEMBL522370 EC50 = 580.0 nM 6.24
CHEMBL495173 EC50 = 626.0 nM 6.20
CHEMBL523211 EC50 = 790.0 nM 6.10
CHEMBL494843 EC50 = 880.0 nM 6.06
CHEMBL495020 EC50 = 940.0 nM 6.03
CHEMBL521866 EC50 = 1500.0 nM 5.82
CHEMBL492798 EC50 = 1900.0 nM 5.72
CHEMBL495197 EC50 = 2320.0 nM 5.63
CHEMBL495196 EC50 = 2600.0 nM 5.58
CHEMBL521811 EC50 = 3500.0 nM 5.46
CHEMBL522668 EC50 > 100000.0 nM -
CHEMBL492563 EC50 > 100000.0 nM -