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Assay Detail

CHEMBL764507

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

Functional
Displacement of PPAR-alpha/delta agonist from human Peroxisome proliferator activated receptor alpha
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Peroxisome proliferator-activated receptor alpha (CHEMBL239)
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
IC50 14 6.72 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL264385 1 7.75
CHEMBL81248 1 7.68
CHEMBL77502 LY-510929 1 7.55
CHEMBL82034 1 7.38
CHEMBL82602 1 7.35
CHEMBL309882 1 7.14
CHEMBL81676 1 6.78
CHEMBL78529 1 6.33
CHEMBL312717 1 6.30
CHEMBL79426 1 6.21
CHEMBL81592 1 6.17
CHEMBL81208 1 5.96
CHEMBL412371 1 5.81
CHEMBL82193 1 5.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL264385 IC50 = 18.0 nM 7.75
CHEMBL81248 IC50 = 21.0 nM 7.68
CHEMBL77502 LY-510929 IC50 = 28.0 nM 7.55
CHEMBL82034 IC50 = 42.0 nM 7.38
CHEMBL82602 IC50 = 45.0 nM 7.35
CHEMBL309882 IC50 = 73.0 nM 7.14
CHEMBL81676 IC50 = 167.0 nM 6.78
CHEMBL78529 IC50 = 473.0 nM 6.33
CHEMBL312717 IC50 = 503.0 nM 6.30
CHEMBL79426 IC50 = 618.0 nM 6.21
CHEMBL81592 IC50 = 678.0 nM 6.17
CHEMBL81208 IC50 = 1106.0 nM 5.96
CHEMBL412371 IC50 = 1546.0 nM 5.81
CHEMBL82193 IC50 = 1846.0 nM 5.73