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Assay Detail

CHEMBL799677

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Functional
Antagonist activity for Retinoic X receptor alpha in CV1 cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
IC50 15 7.45 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL288436 1 8.10
CHEMBL41146 1 8.10
CHEMBL290246 1 7.96
CHEMBL41260 1 7.85
CHEMBL43238 1 7.80
CHEMBL41742 1 7.80
CHEMBL2372524 1 7.70
CHEMBL41422 1 7.66
CHEMBL290761 1 7.62
CHEMBL291034 1 7.08
CHEMBL41675 1 6.89
CHEMBL290399 1 6.71
CHEMBL265051 1 6.52
CHEMBL39206 1 6.46
CHEMBL42314 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL288436 IC50 = 8.0 nM 8.10
CHEMBL41146 IC50 = 8.0 nM 8.10
CHEMBL290246 IC50 = 11.0 nM 7.96
CHEMBL41260 IC50 = 14.0 nM 7.85
CHEMBL43238 IC50 = 16.0 nM 7.80
CHEMBL41742 IC50 = 16.0 nM 7.80
CHEMBL2372524 IC50 = 20.0 nM 7.70
CHEMBL41422 IC50 = 22.0 nM 7.66
CHEMBL290761 IC50 = 24.0 nM 7.62
CHEMBL291034 IC50 = 83.0 nM 7.08
CHEMBL41675 IC50 = 128.0 nM 6.89
CHEMBL290399 IC50 = 194.0 nM 6.71
CHEMBL265051 IC50 = 300.0 nM 6.52
CHEMBL39206 IC50 = 347.0 nM 6.46
CHEMBL42314 IC50 = - nM -