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Assay Detail

CHEMBL800472

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

Binding
Transcriptional activation in CV-1 cells expressing Retinoid X receptor alpha
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CV-1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Retinoic acid receptor RXR-alpha (CHEMBL2061)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and structure-activity relationship of novel RXR-selective modulators.
Michellys PY, D'Arrigo J, Grese TA, Karanewsky DS, Leibowitz MD, Mais DA, Mapes CM, Reifel-Miller A, Rungta D, Boehm MF.
Bioorg Med Chem Lett (2004) 14 : 1593 -1598
PubMed 15006411 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 7.14 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41890 1 7.70
CHEMBL44420 1 7.41
CHEMBL289057 1 7.13
CHEMBL2372524 1 7.07
CHEMBL417520 1 6.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41890 EC50 = 20.0 nM 7.70
CHEMBL44420 EC50 = 39.0 nM 7.41
CHEMBL289057 EC50 = 74.0 nM 7.13
CHEMBL2372524 EC50 = 86.0 nM 7.07
CHEMBL417520 EC50 = 390.0 nM 6.41