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Assay Detail

CHEMBL885567

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]2-(4-{2-[3-(2,4-difluoro-phenyl)-1-heptyl-ureido]-ethyl}-phenoxy)-2-methyl butyric acid from human PPARdelta
17
Total Activities
17
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Peroxisome proliferator-activated receptor delta (CHEMBL3979)
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
IC50 16 8.29 8.70
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL241299 1 8.70
CHEMBL238970 1 8.52
CHEMBL241479 1 8.52
CHEMBL212911 1 8.52
CHEMBL241286 1 8.52
CHEMBL241471 1 8.52
CHEMBL241478 1 8.40
CHEMBL391470 1 8.30
CHEMBL241472 1 8.30
CHEMBL391283 1 8.30
CHEMBL393926 1 8.30
CHEMBL392063 1 8.10
CHEMBL241078 1 8.05
CHEMBL400024 1 7.92
CHEMBL241298 1 7.89
CHEMBL391264 1 7.85
CHEMBL121 ROSIGLITAZONE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL241299 IC50 = 2.0 nM 8.70
CHEMBL238970 IC50 = 3.0 nM 8.52
CHEMBL241479 IC50 = 3.0 nM 8.52
CHEMBL212911 IC50 = 3.0 nM 8.52
CHEMBL241286 IC50 = 3.0 nM 8.52
CHEMBL241471 IC50 = 3.0 nM 8.52
CHEMBL241478 IC50 = 4.0 nM 8.40
CHEMBL391470 IC50 = 5.0 nM 8.30
CHEMBL241472 IC50 = 5.0 nM 8.30
CHEMBL391283 IC50 = 5.0 nM 8.30
CHEMBL393926 IC50 = 5.0 nM 8.30
CHEMBL392063 IC50 = 8.0 nM 8.10
CHEMBL241078 IC50 = 9.0 nM 8.05
CHEMBL400024 IC50 = 12.0 nM 7.92
CHEMBL241298 IC50 = 13.0 nM 7.89
CHEMBL391264 IC50 = 14.0 nM 7.85
CHEMBL121 ROSIGLITAZONE Activity - -