Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL800545

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

Functional
Inhibition of Retinoic acid receptor RXR-alpha agonist activity in vitro
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Novel (2E,4E,6Z)-7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta-2,4,6-trienoic acid retinoid X receptor modulators are active in models of type 2 diabetes.
Michellys PY, Ardecky RJ, Chen JH, Crombie DL, Etgen GJ, Faul MM, Faulkner AL, Grese TA, Heyman RA, Karanewsky DS, Klausing K, Leibowitz MD, Liu S, Mais DA, Mapes CM, Marschke KB, Reifel-Miller A, Ogilvie KM, Rungta D, Thompson AW, Tyhonas JS, Boehm MF.
J Med Chem (2003) 46 : 2683 -2696
PubMed 12801232 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 7.86 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL90824 1 8.70
CHEMBL88740 1 8.70
CHEMBL92430 1 8.15
CHEMBL288436 1 7.96
CHEMBL92050 1 7.75
CHEMBL329334 1 7.44
CHEMBL91185 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL90824 EC50 = 2.0 nM 8.70
CHEMBL88740 EC50 = 2.0 nM 8.70
CHEMBL92430 EC50 = 7.0 nM 8.15
CHEMBL288436 EC50 = 11.0 nM 7.96
CHEMBL92050 EC50 = 18.0 nM 7.75
CHEMBL329334 EC50 = 36.0 nM 7.44
CHEMBL91185 EC50 = 506.0 nM 6.30