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Assay Detail

CHEMBL2027596

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Functional
Agonist activity at human PPARalpha expressed in MCF7 cells co-transfected CPTI DR1-type RE after 16 hrs by luciferase reporter gene assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MCF7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of Potent Dual PPARα Agonists/CB1 Ligands.
Pérez-Fernández R, Fresno N, Macías-González M, Elguero J, Decara J, Girón R, Rodríguez-Álvarez A, Martín MI, Rodríguez de Fonseca F, Goya P.
ACS Med Chem Lett (2011) 2 : 793 -797
PubMed 24936232 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.29 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL280065 OLEOYLETHANOLAMIDE 1 6.82
CHEMBL295416 PIRINIXIC ACID 2.0 1 6.19
CHEMBL2022404 1 6.13
CHEMBL2022403 1 6.00
CHEMBL2022405 1 -
CHEMBL2022406 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL280065 OLEOYLETHANOLAMIDE EC50 = 152.0 nM 6.82
CHEMBL295416 PIRINIXIC ACID EC50 = 650.0 nM 6.19
CHEMBL2022404 EC50 = 743.0 nM 6.13
CHEMBL2022403 EC50 = 989.0 nM 6.00
CHEMBL2022405 EC50 - -
CHEMBL2022406 EC50 - -