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Assay Detail

CHEMBL798929

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

Binding
Binding affinity against Retinoic acid receptor RXR-alpha was determined in vitro by using [3H]9-cis-RA as radioligand
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 17 8.36 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL92430 1 9.00
CHEMBL329334 1 9.00
CHEMBL90824 1 9.00
CHEMBL315986 1 8.70
CHEMBL88740 1 8.70
CHEMBL88931 1 8.70
CHEMBL91185 1 8.70
CHEMBL423503 1 8.52
CHEMBL91779 1 8.52
CHEMBL42314 1 8.52
CHEMBL414218 1 8.40
CHEMBL92050 1 7.96
CHEMBL420249 1 7.85
CHEMBL288436 1 7.75
CHEMBL90254 1 7.64
CHEMBL92487 1 7.57
CHEMBL313647 1 7.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL92430 Ki = 1.0 nM 9.00
CHEMBL329334 Ki = 1.0 nM 9.00
CHEMBL90824 Ki = 1.0 nM 9.00
CHEMBL315986 Ki = 2.0 nM 8.70
CHEMBL88740 Ki = 2.0 nM 8.70
CHEMBL88931 Ki = 2.0 nM 8.70
CHEMBL91185 Ki = 2.0 nM 8.70
CHEMBL423503 Ki = 3.0 nM 8.52
CHEMBL91779 Ki = 3.0 nM 8.52
CHEMBL42314 Ki = 3.0 nM 8.52
CHEMBL414218 Ki = 4.0 nM 8.40
CHEMBL92050 Ki = 11.0 nM 7.96
CHEMBL420249 Ki = 14.0 nM 7.85
CHEMBL288436 Ki = 18.0 nM 7.75
CHEMBL90254 Ki = 23.0 nM 7.64
CHEMBL92487 Ki = 27.0 nM 7.57
CHEMBL313647 Ki = 29.0 nM 7.54