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Assay Detail

CHEMBL806515

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

Binding
In vitro evaluation against RXR-alpha in CV-1 cells by cotransfection assay was determined
14
Total Activities
14
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 (CHEMBL4431)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design, synthesis, and structure-activity relationship studies of novel 6,7-locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic acids.
Michellys PY, Ardecky RJ, Chen JH, D'Arrigo J, Grese TA, Karanewsky DS, Leibowitz MD, Liu S, Mais DA, Mapes CM, Montrose-Rafizadeh C, Ogilvie KM, Reifel-Miller A, Rungta D, Thompson AW, Tyhonas JS, Boehm MF.
J Med Chem (2003) 46 : 4087 -4103
PubMed 12954061 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.83 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL337719 1 8.64
CHEMBL336086 1 8.48
CHEMBL340074 1 8.29
CHEMBL131561 1 8.17
CHEMBL335762 1 8.06
CHEMBL339298 1 7.99
CHEMBL132488 1 7.98
CHEMBL340555 1 7.94
CHEMBL335751 1 7.94
CHEMBL129887 1 7.81
CHEMBL129976 1 7.33
CHEMBL445634 1 7.30
CHEMBL130230 1 7.10
CHEMBL130577 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL337719 IC50 = 2.3 nM 8.64
CHEMBL336086 IC50 = 3.3 nM 8.48
CHEMBL340074 IC50 = 5.1 nM 8.29
CHEMBL131561 IC50 = 6.8 nM 8.17
CHEMBL335762 IC50 = 8.7 nM 8.06
CHEMBL339298 IC50 = 10.3 nM 7.99
CHEMBL132488 IC50 = 10.4 nM 7.98
CHEMBL340555 IC50 = 11.4 nM 7.94
CHEMBL335751 IC50 = 11.6 nM 7.94
CHEMBL129887 IC50 = 15.5 nM 7.81
CHEMBL129976 IC50 = 46.3 nM 7.33
CHEMBL445634 IC50 = 49.6 nM 7.30
CHEMBL130230 IC50 = 79.9 nM 7.10
CHEMBL130577 IC50 = 271.2 nM 6.57