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Assay Detail

CHEMBL807383

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

Binding
In vitro evaluation against RXR-alpha/PPAR-gamma in CV-1 cells by cotransfection assay was determined
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CV-1
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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
EC50 17 6.51 8.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL340074 1 8.06
CHEMBL133176 1 7.72
CHEMBL288436 1 7.00
CHEMBL132488 1 6.96
CHEMBL42314 1 6.88
CHEMBL335751 1 6.76
CHEMBL339298 1 6.69
CHEMBL121 ROSIGLITAZONE 4.0 1 6.49
CHEMBL335762 1 6.29
CHEMBL129887 1 6.25
CHEMBL131561 1 6.21
CHEMBL445634 1 6.13
CHEMBL337719 1 6.10
CHEMBL130577 1 5.89
CHEMBL336086 1 5.79
CHEMBL130230 1 5.76
CHEMBL340555 1 5.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL340074 EC50 = 8.8 nM 8.06
CHEMBL133176 EC50 = 19.2 nM 7.72
CHEMBL288436 EC50 = 99.0 nM 7.00
CHEMBL132488 EC50 = 110.0 nM 6.96
CHEMBL42314 EC50 = 131.5 nM 6.88
CHEMBL335751 EC50 = 173.6 nM 6.76
CHEMBL339298 EC50 = 202.6 nM 6.69
CHEMBL121 ROSIGLITAZONE EC50 = 325.0 nM 6.49
CHEMBL335762 EC50 = 508.7 nM 6.29
CHEMBL129887 EC50 = 556.2 nM 6.25
CHEMBL131561 EC50 = 623.9 nM 6.21
CHEMBL445634 EC50 = 736.7 nM 6.13
CHEMBL337719 EC50 = 802.0 nM 6.10
CHEMBL130577 EC50 = 1272.7 nM 5.89
CHEMBL336086 EC50 = 1604.0 nM 5.79
CHEMBL130230 EC50 = 1723.8 nM 5.76
CHEMBL340555 EC50 = 1716.1 nM 5.76