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Assay Detail

CHEMBL918997

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Functional
Agonist activity at mouse PPAR delta expressed in HEK293 cells by PPAR-GAL4 transactivation assay
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

Peroxisome proliferator-activated receptor delta (CHEMBL2458)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Identification and synthesis of a novel selective partial PPARdelta agonist with full efficacy on lipid metabolism in vitro and in vivo.
Sauerberg P, Olsen GS, Jeppesen L, Mogensen JP, Pettersson I, Jeppesen CB, Daugaard JR, Galsgaard ED, Ynddal L, Fleckner J, Panajotova V, Polivka Z, Pihera P, Havranek M, Wulff EM.
J Med Chem (2007) 50 : 1495 -1503
PubMed 17343371 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.90 7.27
Activity 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38943 GW501516 2.0 2 7.27
CHEMBL222880 2 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38943 GW501516 EC50 = 54.0 nM 7.27
CHEMBL222880 EC50 = 300.0 nM 6.52
CHEMBL38943 GW501516 Activity = 269.0 % -
CHEMBL222880 Activity = 167.0 % -