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Assay Detail

CHEMBL854664

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

Functional
Activity at PPARbeta/delta by luciferase reporter gene transactivation assay in COS7 cells
12
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Studies towards the conception of new selective PPARbeta/delta ligands.
Basséne CE, Suzenet F, Hennuyer N, Staels B, Caignard DH, Dacquet C, Renard P, Guillaumet G.
Bioorg Med Chem Lett (2006) 16 : 4528 -4532
PubMed 16797985 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 7.11 9.00
Activity 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38943 GW501516 2.0 1 9.00
CHEMBL213355 1 8.15
CHEMBL425431 1 7.82
CHEMBL214394 1 7.80
CHEMBL212993 1 7.09
CHEMBL211963 1 7.01
CHEMBL153057 1 6.90
CHEMBL373785 1 6.34
CHEMBL213132 1 5.98
CHEMBL212808 1 5.00
CHEMBL213411 1 -
CHEMBL213410 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38943 GW501516 EC50 = 1.0 nM 9.00
CHEMBL213355 EC50 = 7.0 nM 8.15
CHEMBL425431 EC50 = 15.0 nM 7.82
CHEMBL214394 EC50 = 16.0 nM 7.80
CHEMBL212993 EC50 = 82.0 nM 7.09
CHEMBL211963 EC50 = 98.0 nM 7.01
CHEMBL153057 EC50 = 125.0 nM 6.90
CHEMBL373785 EC50 = 457.0 nM 6.34
CHEMBL213132 EC50 = 1046.0 nM 5.98
CHEMBL212808 EC50 = 10000.0 nM 5.00
CHEMBL213411 Activity - -
CHEMBL213410 Activity - -