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Assay Detail

CHEMBL885569

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Functional
Agonist activity at human Gal4-PPARalpha expressed in CV1 cells by transactivation assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CV-1
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Design and synthesis of a novel class of dual PPARgamma/delta agonists.
Gonzalez IC, Lamar J, Iradier F, Xu Y, Winneroski LL, York J, Yumibe N, Zink R, Montrose-Rafizadeh C, Etgen GJ, Broderick CL, Oldham BA, Mantlo N.
Bioorg Med Chem Lett (2007) 17 : 1052 -1055
PubMed 17129725 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 5.60 6.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL212911 1 6.06
CHEMBL241478 1 5.63
CHEMBL238970 1 5.58
CHEMBL241286 1 5.57
CHEMBL241078 1 5.57
CHEMBL241298 1 5.55
CHEMBL391264 1 5.55
CHEMBL391470 1 5.54
CHEMBL241479 1 5.54
CHEMBL241472 1 5.54
CHEMBL241471 1 5.54
CHEMBL393926 1 5.54
CHEMBL241299 1 5.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL212911 EC50 = 877.0 nM 6.06
CHEMBL241478 EC50 = 2340.0 nM 5.63
CHEMBL238970 EC50 = 2630.0 nM 5.58
CHEMBL241286 EC50 = 2680.0 nM 5.57
CHEMBL241078 EC50 = 2690.0 nM 5.57
CHEMBL241298 EC50 = 2810.0 nM 5.55
CHEMBL391264 EC50 = 2800.0 nM 5.55
CHEMBL391470 EC50 = 2890.0 nM 5.54
CHEMBL241479 EC50 = 2850.0 nM 5.54
CHEMBL241472 EC50 = 2900.0 nM 5.54
CHEMBL241471 EC50 = 2870.0 nM 5.54
CHEMBL393926 EC50 = 2880.0 nM 5.54
CHEMBL241299 EC50 = 2980.0 nM 5.53