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Assay Detail

CHEMBL763850

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

Functional
In vitro transactivation of human Peroxisome proliferator activated receptor alpha measured in PPAR-GAL4 chimeric COS-1 cell
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type COS-1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents.
Desai RC, Han W, Metzger EJ, Bergman JP, Gratale DF, MacNaul KL, Berger JP, Doebber TW, Leung K, Moller DE, Heck JV, Sahoo SP.
Bioorg Med Chem Lett (2003) 13 : 2795 -2798
PubMed 12873517 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 6.98 7.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL96451 1 7.18
CHEMBL318684 1 7.09
CHEMBL96143 1 7.07
CHEMBL328615 1 6.81
CHEMBL420441 1 6.75
CHEMBL94496 1 -
CHEMBL121 ROSIGLITAZONE 4.0 1 -
CHEMBL94397 1 -
CHEMBL97529 1 -
CHEMBL96758 1 -
CHEMBL92130 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL96451 EC50 = 66.0 nM 7.18
CHEMBL318684 EC50 = 82.0 nM 7.09
CHEMBL96143 EC50 = 85.0 nM 7.07
CHEMBL328615 EC50 = 156.0 nM 6.81
CHEMBL420441 EC50 = 180.0 nM 6.75
CHEMBL94496 EC50 > 3000.0 nM -
CHEMBL121 ROSIGLITAZONE EC50 > 3000.0 nM -
CHEMBL94397 EC50 > 3000.0 nM -
CHEMBL97529 EC50 > 3000.0 nM -
CHEMBL96758 EC50 > 3000.0 nM -
CHEMBL92130 EC50 > 3000.0 nM -