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Assay Detail

CHEMBL760609

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

Functional
In vitro activity in human Peroxisome proliferator activated receptor alpha-transactivation assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Peroxisome proliferator-activated receptor alpha (CHEMBL239)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Aryloxazolidinediones: identification of potent orally active PPAR dual alpha/gamma agonists.
Desai RC, Gratale DF, Han W, Koyama H, Metzger E, Lombardo VK, MacNaul KL, Doebber TW, Berger JP, Leung K, Franklin R, Moller DE, Heck JV, Sahoo SP.
Bioorg Med Chem Lett (2003) 13 : 3541 -3544
PubMed 14505666 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 6.98 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL94306 1 7.58
CHEMBL122417 1 7.28
CHEMBL118251 1 7.27
CHEMBL118756 1 7.26
CHEMBL122418 1 7.12
CHEMBL119496 1 6.89
CHEMBL117738 1 6.77
CHEMBL280293 1 5.70
CHEMBL119066 1 -
CHEMBL117578 1 -
CHEMBL331071 1 -
CHEMBL332018 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL94306 EC50 = 26.0 nM 7.58
CHEMBL122417 EC50 = 53.0 nM 7.28
CHEMBL118251 EC50 = 54.0 nM 7.27
CHEMBL118756 EC50 = 55.0 nM 7.26
CHEMBL122418 EC50 = 76.0 nM 7.12
CHEMBL119496 EC50 = 130.0 nM 6.89
CHEMBL117738 EC50 = 170.0 nM 6.77
CHEMBL280293 EC50 = 2000.0 nM 5.70
CHEMBL119066 EC50 > 3000.0 nM -
CHEMBL117578 EC50 > 3000.0 nM -
CHEMBL331071 EC50 > 3000.0 nM -
CHEMBL332018 EC50 > 3000.0 nM -