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Assay Detail

CHEMBL885571

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Functional
Agonist activity at PPARgamma in CV1 cells by transactivation assay
17
Total Activities
17
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 gamma (CHEMBL235)
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 17 6.41 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL212911 1 8.40
CHEMBL241478 1 7.17
CHEMBL238970 1 6.96
CHEMBL241472 1 6.85
CHEMBL241479 1 6.78
CHEMBL241471 1 6.74
CHEMBL241299 1 6.52
CHEMBL121 ROSIGLITAZONE 4.0 1 6.51
CHEMBL391283 1 6.24
CHEMBL391470 1 6.16
CHEMBL393926 1 6.08
CHEMBL241286 1 6.08
CHEMBL392063 1 5.78
CHEMBL241078 1 5.70
CHEMBL241298 1 5.70
CHEMBL400024 1 5.64
CHEMBL391264 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL212911 EC50 = 4.0 nM 8.40
CHEMBL241478 EC50 = 67.0 nM 7.17
CHEMBL238970 EC50 = 111.0 nM 6.96
CHEMBL241472 EC50 = 140.0 nM 6.85
CHEMBL241479 EC50 = 167.0 nM 6.78
CHEMBL241471 EC50 = 182.0 nM 6.74
CHEMBL241299 EC50 = 304.0 nM 6.52
CHEMBL121 ROSIGLITAZONE EC50 = 308.0 nM 6.51
CHEMBL391283 EC50 = 576.0 nM 6.24
CHEMBL391470 EC50 = 696.0 nM 6.16
CHEMBL393926 EC50 = 836.0 nM 6.08
CHEMBL241286 EC50 = 837.0 nM 6.08
CHEMBL392063 EC50 = 1670.0 nM 5.78
CHEMBL241078 EC50 = 1990.0 nM 5.70
CHEMBL241298 EC50 = 1980.0 nM 5.70
CHEMBL400024 EC50 = 2270.0 nM 5.64
CHEMBL391264 EC50 = 2300.0 nM 5.64