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Assay Detail

CHEMBL947320

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

Functional
Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type THP-1
Confidence 1 — Organism
Curated By Autocuration

Target

THP-1 (CHEMBL614245)
Type CELL-LINE
Organism Homo sapiens

Publication

Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.
Wrobel J, Steffan R, Bowen SM, Magolda R, Matelan E, Unwalla R, Basso M, Clerin V, Gardell SJ, Nambi P, Quinet E, Reminick JI, Vlasuk GP, Wang S, Feingold I, Huselton C, Bonn T, Farnegardh M, Hansson T, Nilsson AG, Wilhelmsson A, Zamaratski E, Evans MJ.
J Med Chem (2008) 51 : 7161 -7168
PubMed 18973288 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 7.28 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL62136 T091317 1 8.52
CHEMBL214719 1 8.22
CHEMBL59030 1 7.51
CHEMBL457977 1 6.26
CHEMBL456237 LXR-623 1.0 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL62136 T091317 EC50 = 3.0 nM 8.52
CHEMBL214719 EC50 = 6.0 nM 8.22
CHEMBL59030 EC50 = 31.0 nM 7.51
CHEMBL457977 EC50 = 549.0 nM 6.26
CHEMBL456237 LXR-623 EC50 = 1275.0 nM 5.89