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Assay Detail

CHEMBL886476

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

Binding
Activity at RXR-LXR heterodimer in human THP1 cells assessed as induction of ABCA1 mRNA
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type THP-1
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

RXR-LXR heterodimer modulators for the potential treatment of dyslipidemia.
Lagu B, Pio B, Lebedev R, Yang M, Pelton PD.
Bioorg Med Chem Lett (2007) 17 : 3497 -3503
PubMed 17485209 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 7.11 8.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL246821 1 8.44
CHEMBL428930 1 8.00
CHEMBL247856 1 7.40
CHEMBL247819 1 7.36
CHEMBL248191 1 6.79
CHEMBL248415 1 6.75
CHEMBL247836 1 6.70
CHEMBL400557 1 6.53
CHEMBL246805 1 6.01
CHEMBL400380 1 -
CHEMBL246806 1 -
CHEMBL399765 1 -
CHEMBL246629 1 -
CHEMBL247005 1 -
CHEMBL247855 1 -
CHEMBL400490 1 -
CHEMBL247857 1 -
CHEMBL247011 1 -
CHEMBL247012 1 -
CHEMBL246625 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL246821 EC50 = 3.6 nM 8.44
CHEMBL428930 EC50 = 10.0 nM 8.00
CHEMBL247856 EC50 = 39.7 nM 7.40
CHEMBL247819 EC50 = 44.0 nM 7.36
CHEMBL248191 EC50 = 163.0 nM 6.79
CHEMBL248415 EC50 = 180.0 nM 6.75
CHEMBL247836 EC50 = 200.0 nM 6.70
CHEMBL400557 EC50 = 296.0 nM 6.53
CHEMBL246805 EC50 = 975.0 nM 6.01
CHEMBL400380 EC50 > 3000.0 nM -
CHEMBL246806 EC50 > 3000.0 nM -
CHEMBL399765 EC50 > 3000.0 nM -
CHEMBL246629 EC50 > 3000.0 nM -
CHEMBL247005 EC50 > 3000.0 nM -
CHEMBL247855 EC50 > 3000.0 nM -
CHEMBL400490 EC50 > 3000.0 nM -
CHEMBL247857 EC50 > 3000.0 nM -
CHEMBL247011 EC50 > 3000.0 nM -
CHEMBL247012 EC50 > 3000.0 nM -
CHEMBL246625 EC50 > 3000.0 nM -