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Assay Detail

CHEMBL760257

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Functional
In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type CV-1
Confidence 9 — Direct single protein target
Curated By Expert

Target

Peroxisome proliferator-activated receptor gamma (CHEMBL2459)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones.
Willson TM, Cobb JE, Cowan DJ, Wiethe RW, Correa ID, Prakash SR, Beck KD, Moore LB, Kliewer SA, Lehmann JM.
J Med Chem (1996) 39 : 665 -668
PubMed 8576907 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 6.25 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL17805 BRL-48482 1 7.89
CHEMBL121 ROSIGLITAZONE 4.0 1 7.22
CHEMBL128884 1 6.85
CHEMBL297312 1 6.72
CHEMBL595 PIOGLITAZONE 4.0 1 6.16
CHEMBL337973 1 6.00
CHEMBL7002 CIGLITAZONE 2.0 1 5.52
CHEMBL129562 1 5.00
CHEMBL17669 ENGLITAZONE 2.0 1 4.89
CHEMBL683 CLOFIBRIC ACID 2.0 1 -
CHEMBL346267 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL17805 BRL-48482 EC50 = 13.0 nM 7.89
CHEMBL121 ROSIGLITAZONE EC50 = 60.0 nM 7.22
CHEMBL128884 EC50 = 140.0 nM 6.85
CHEMBL297312 EC50 = 190.0 nM 6.72
CHEMBL595 PIOGLITAZONE EC50 = 690.0 nM 6.16
CHEMBL337973 EC50 = 1000.0 nM 6.00
CHEMBL7002 CIGLITAZONE EC50 = 3000.0 nM 5.52
CHEMBL129562 EC50 = 10000.0 nM 5.00
CHEMBL17669 ENGLITAZONE EC50 = 13000.0 nM 4.89
CHEMBL683 CLOFIBRIC ACID EC50 = 600000.0 nM -
CHEMBL346267 EC50 = 110000.0 nM -