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Assay Detail

CHEMBL911541

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

Functional
Transactivation of human PPARdelta in CV1 cells by luciferase reporter gene assay
15
Total Activities
15
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 Expert

Target

Peroxisome proliferator-activated receptor delta (CHEMBL3979)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of dual peroxisome proliferator-activated receptors gamma and delta agonists as novel euglycemic agents with a reduced weight gain profile.
Xu Y, Etgen GJ, Broderick CL, Canada E, Gonzalez I, Lamar J, Montrose-Rafizadeh C, Oldham BA, Osborne JJ, Xie C, Shi Q, Winneroski LL, York J, Yumibe N, Zink R, Mantlo N.
J Med Chem (2006) 49 : 5649 -5652
PubMed 16970391 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 7.77 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL213315 1 9.00
CHEMBL214921 1 8.70
CHEMBL377660 1 8.30
CHEMBL212911 1 8.30
CHEMBL215701 1 8.22
CHEMBL378068 1 8.15
CHEMBL214026 1 8.10
CHEMBL215127 1 7.60
CHEMBL215245 1 7.47
CHEMBL215582 1 7.35
CHEMBL213314 1 7.33
CHEMBL212023 1 7.28
CHEMBL212591 1 7.16
CHEMBL213361 1 7.14
CHEMBL215126 1 6.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL213315 EC50 = 1.0 nM 9.00
CHEMBL214921 EC50 = 2.0 nM 8.70
CHEMBL377660 EC50 = 5.0 nM 8.30
CHEMBL212911 EC50 = 5.0 nM 8.30
CHEMBL215701 EC50 = 6.0 nM 8.22
CHEMBL378068 EC50 = 7.0 nM 8.15
CHEMBL214026 EC50 = 8.0 nM 8.10
CHEMBL215127 EC50 = 25.0 nM 7.60
CHEMBL215245 EC50 = 34.0 nM 7.47
CHEMBL215582 EC50 = 45.0 nM 7.35
CHEMBL213314 EC50 = 47.0 nM 7.33
CHEMBL212023 EC50 = 52.0 nM 7.28
CHEMBL212591 EC50 = 70.0 nM 7.16
CHEMBL213361 EC50 = 73.0 nM 7.14
CHEMBL215126 EC50 = 339.0 nM 6.47