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Assay Detail

CHEMBL1049545

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

Binding
Displacement of [3H]TO901317 from human recombinant LXRbeta expressed in Escherichia coli by flashplate method
20
Total Activities
20
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-beta (CHEMBL4093)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration.
Hu B, Bernotas R, Unwalla R, Collini M, Quinet E, Feingold I, Goos-Nilsson A, Wilhelmsson A, Nambi P, Evans M, Wrobel J.
Bioorg Med Chem Lett (2010) 20 : 689 -693
PubMed 19962892 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.20 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL595689 1 9.00
CHEMBL590098 1 8.70
CHEMBL600244 1 8.66
CHEMBL593739 1 8.30
CHEMBL62136 T091317 1 8.05
CHEMBL589613 1 7.96
CHEMBL593267 1 7.80
CHEMBL590828 1 7.75
CHEMBL591582 1 7.75
CHEMBL604259 1 7.55
CHEMBL606139 1 7.24
CHEMBL602446 1 7.21
CHEMBL590584 1 7.11
CHEMBL591815 1 6.43
CHEMBL593740 1 6.23
CHEMBL600851 1 6.14
CHEMBL590350 1 5.97
CHEMBL606862 1 5.54
CHEMBL590586 1 5.29
CHEMBL590351 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL595689 IC50 = 1.0 nM 9.00
CHEMBL590098 IC50 = 2.0 nM 8.70
CHEMBL600244 IC50 = 2.2 nM 8.66
CHEMBL593739 IC50 = 5.0 nM 8.30
CHEMBL62136 T091317 IC50 = 9.0 nM 8.05
CHEMBL589613 IC50 = 11.0 nM 7.96
CHEMBL593267 IC50 = 16.0 nM 7.80
CHEMBL590828 IC50 = 18.0 nM 7.75
CHEMBL591582 IC50 = 18.0 nM 7.75
CHEMBL604259 IC50 = 28.0 nM 7.55
CHEMBL606139 IC50 = 57.0 nM 7.24
CHEMBL602446 IC50 = 62.0 nM 7.21
CHEMBL590584 IC50 = 77.0 nM 7.11
CHEMBL591815 IC50 = 367.0 nM 6.43
CHEMBL593740 IC50 = 590.0 nM 6.23
CHEMBL600851 IC50 = 730.0 nM 6.14
CHEMBL590350 IC50 = 1076.0 nM 5.97
CHEMBL606862 IC50 = 2850.0 nM 5.54
CHEMBL590586 IC50 = 5133.0 nM 5.29
CHEMBL590351 IC50 = 5294.0 nM 5.28