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Assay Detail

CHEMBL759727

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

Binding
Transcriptional activation of reporter assay by PPAR gamma receptor in CV-1 cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CV-1
Confidence 9 — Direct single protein target
Curated By Expert

Target

Peroxisome proliferator-activated receptor gamma (CHEMBL235)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of alpha-aryloxy-alpha-methylhydrocinnamic acids: a novel class of dual peroxisome proliferator-activated receptor alpha/gamma agonists.
Xu Y, Rito CJ, Etgen GJ, Ardecky RJ, Bean JS, Bensch WR, Bosley JR, Broderick CL, Brooks DA, Dominianni SJ, Hahn PJ, Liu S, Mais DE, Montrose-Rafizadeh C, Ogilvie KM, Oldham BA, Peters M, Rungta DK, Shuker AJ, Stephenson GA, Tripp AE, Wilson SB, Winneroski LL, Zink R, Kauffman RF, McCarthy JR.
J Med Chem (2004) 47 : 2422 -2425
PubMed 15115385 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 7.45 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL264385 1 9.00
CHEMBL81248 1 8.52
CHEMBL77502 LY-510929 1 8.40
CHEMBL82602 1 8.22
CHEMBL81676 1 8.22
CHEMBL312717 1 8.15
CHEMBL82034 1 8.10
CHEMBL309882 1 8.05
CHEMBL79426 1 6.92
CHEMBL78529 1 6.54
CHEMBL412371 1 6.42
CHEMBL81208 1 6.41
CHEMBL81592 1 5.75
CHEMBL82193 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL264385 EC50 = 1.0 nM 9.00
CHEMBL81248 EC50 = 3.0 nM 8.52
CHEMBL77502 LY-510929 EC50 = 4.0 nM 8.40
CHEMBL82602 EC50 = 6.0 nM 8.22
CHEMBL81676 EC50 = 6.0 nM 8.22
CHEMBL312717 EC50 = 7.0 nM 8.15
CHEMBL82034 EC50 = 8.0 nM 8.10
CHEMBL309882 EC50 = 9.0 nM 8.05
CHEMBL79426 EC50 = 121.0 nM 6.92
CHEMBL78529 EC50 = 285.0 nM 6.54
CHEMBL412371 EC50 = 382.0 nM 6.42
CHEMBL81208 EC50 = 390.0 nM 6.41
CHEMBL81592 EC50 = 1776.0 nM 5.75
CHEMBL82193 EC50 = 2507.0 nM 5.60