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Assay Detail

CHEMBL743989

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Functional
Agonist activity for murine PPAR alpha receptor in transcriptional activation assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Peroxisome proliferator-activated receptor alpha (CHEMBL2128)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

The PPARs: from orphan receptors to drug discovery.
Willson TM, Brown PJ, Sternbach DD, Henke BR.
J Med Chem (2000) 43 : 527 -550
PubMed 10691680 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 5.57 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL278590 GSK-9578 1 8.30
CHEMBL435278 1 6.57
CHEMBL295416 PIRINIXIC ACID 2.0 1 6.20
CHEMBL306229 1 6.03
CHEMBL293526 REGLITAZAR 2.0 1 5.37
CHEMBL278994 L-796449 1 5.12
CHEMBL24458 1 5.00
CHEMBL672 FENOFIBRATE 4.0 1 4.75
CHEMBL565 CLOFIBRATE 4.0 1 4.30
CHEMBL264374 BEZAFIBRATE 3.0 1 4.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL278590 GSK-9578 EC50 = 5.0 nM 8.30
CHEMBL435278 EC50 = 270.0 nM 6.57
CHEMBL295416 PIRINIXIC ACID EC50 = 630.0 nM 6.20
CHEMBL306229 EC50 = 930.0 nM 6.03
CHEMBL293526 REGLITAZAR EC50 = 4300.0 nM 5.37
CHEMBL278994 L-796449 EC50 = 7600.0 nM 5.12
CHEMBL24458 EC50 = 10000.0 nM 5.00
CHEMBL672 FENOFIBRATE EC50 = 18000.0 nM 4.75
CHEMBL565 CLOFIBRATE EC50 = 50000.0 nM 4.30
CHEMBL264374 BEZAFIBRATE EC50 = 90000.0 nM 4.05