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Assay Detail

CHEMBL651610

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

Functional
Transcriptional activity against RXR:PPAR-gamma synergy was determined in vitro
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cercopithecidae
Confidence 6 — Multiple protein complex / RNA
Curated By Expert

Target

RXR alpha/PPAR gamma (CHEMBL2111394)
Type PROTEIN COMPLEX
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 17 8.15 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL88740 1 9.00
CHEMBL92487 1 8.70
CHEMBL92050 1 8.70
CHEMBL42314 1 8.52
CHEMBL423503 1 8.52
CHEMBL92430 1 8.40
CHEMBL91779 1 8.30
CHEMBL91185 1 8.22
CHEMBL329334 1 8.15
CHEMBL90824 1 8.10
CHEMBL315986 1 8.05
CHEMBL88931 1 8.00
CHEMBL313647 1 7.96
CHEMBL414218 1 7.92
CHEMBL90254 1 7.72
CHEMBL288436 1 7.42
CHEMBL420249 1 6.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL88740 EC50 = 1.0 nM 9.00
CHEMBL92487 EC50 = 2.0 nM 8.70
CHEMBL92050 EC50 = 2.0 nM 8.70
CHEMBL42314 EC50 = 3.0 nM 8.52
CHEMBL423503 EC50 = 3.0 nM 8.52
CHEMBL92430 EC50 = 4.0 nM 8.40
CHEMBL91779 EC50 = 5.0 nM 8.30
CHEMBL91185 EC50 = 6.0 nM 8.22
CHEMBL329334 EC50 = 7.0 nM 8.15
CHEMBL90824 EC50 = 8.0 nM 8.10
CHEMBL315986 EC50 = 9.0 nM 8.05
CHEMBL88931 EC50 = 10.0 nM 8.00
CHEMBL313647 EC50 = 11.0 nM 7.96
CHEMBL414218 EC50 = 12.0 nM 7.92
CHEMBL90254 EC50 = 19.0 nM 7.72
CHEMBL288436 EC50 = 38.0 nM 7.42
CHEMBL420249 EC50 = 154.0 nM 6.81