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Assay Detail

CHEMBL1026574

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Functional
Agonist activity at LXRbeta by FRET assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and SAR of potent LXR agonists containing an indole pharmacophore.
Washburn DG, Hoang TH, Campobasso N, Smallwood A, Parks DJ, Webb CL, Frank KA, Nord M, Duraiswami C, Evans C, Jaye M, Thompson SK.
Bioorg Med Chem Lett (2009) 19 : 1097 -1100
PubMed 19167885 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 7.44 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL446208 1 8.40
CHEMBL505808 1 8.15
CHEMBL505520 1 7.92
CHEMBL471641 1 7.82
CHEMBL457452 1 7.82
CHEMBL513949 1 7.64
CHEMBL59030 1 7.60
CHEMBL518000 1 7.58
CHEMBL480493 1 7.22
CHEMBL499550 1 6.54
CHEMBL451889 1 6.29
CHEMBL450200 1 6.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL446208 EC50 = 4.0 nM 8.40
CHEMBL505808 EC50 = 7.0 nM 8.15
CHEMBL505520 EC50 = 12.0 nM 7.92
CHEMBL471641 EC50 = 15.0 nM 7.82
CHEMBL457452 EC50 = 15.0 nM 7.82
CHEMBL513949 EC50 = 23.0 nM 7.64
CHEMBL59030 EC50 = 25.0 nM 7.60
CHEMBL518000 EC50 = 26.0 nM 7.58
CHEMBL480493 EC50 = 60.0 nM 7.22
CHEMBL499550 EC50 = 288.0 nM 6.54
CHEMBL451889 EC50 = 510.0 nM 6.29
CHEMBL450200 EC50 = 560.0 nM 6.25