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Assay Detail

CHEMBL4344573

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

Binding
Agonist activity at human PPARdelta expressed in nonhuman mammalian cells assessed as increase in receptor transcriptional activity incubated for 22 to 24 hrs by luciferase reporter gene assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Evolution of a 4-Benzyloxy-benzylamino Chemotype to Provide Efficacious, Potent, and Isoform Selective PPARα Agonists as Leads for Retinal Disorders.
Dou X, Nath D, Shin H, Nurmemmedov E, Bourne PC, Ma JX, Duerfeldt AS.
J Med Chem (2020) 63 : 2854 -2876
PubMed 32096640 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 8.72 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38508 1 8.72
CHEMBL4237449 1 -
CHEMBL4564731 1 -
CHEMBL4466987 1 -
CHEMBL4454550 1 -
CHEMBL4476782 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38508 EC50 = 1.9 nM 8.72
CHEMBL4237449 EC50 > 100000.0 nM -
CHEMBL4564731 EC50 > 100000.0 nM -
CHEMBL4466987 EC50 > 100000.0 nM -
CHEMBL4454550 EC50 > 100000.0 nM -
CHEMBL4476782 EC50 > 100000.0 nM -