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Assay Detail

CHEMBL872989

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

Functional
Inhibitory activity against Retinoic acid receptor RXR-alpha antagonist was determined in vitro
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous 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
IC50 12 8.13 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL88931 1 9.00
CHEMBL414218 1 8.40
CHEMBL91779 1 8.40
CHEMBL92430 1 8.40
CHEMBL423503 1 8.22
CHEMBL42314 1 8.10
CHEMBL92050 1 8.10
CHEMBL92487 1 8.10
CHEMBL90254 1 7.89
CHEMBL313647 1 7.80
CHEMBL315986 1 7.77
CHEMBL420249 1 7.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL88931 IC50 = 1.0 nM 9.00
CHEMBL414218 IC50 = 4.0 nM 8.40
CHEMBL91779 IC50 = 4.0 nM 8.40
CHEMBL92430 IC50 = 4.0 nM 8.40
CHEMBL423503 IC50 = 6.0 nM 8.22
CHEMBL42314 IC50 = 8.0 nM 8.10
CHEMBL92050 IC50 = 8.0 nM 8.10
CHEMBL92487 IC50 = 8.0 nM 8.10
CHEMBL90254 IC50 = 13.0 nM 7.89
CHEMBL313647 IC50 = 16.0 nM 7.80
CHEMBL315986 IC50 = 17.0 nM 7.77
CHEMBL420249 IC50 = 43.0 nM 7.37