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Assay Detail

CHEMBL759387

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Functional
Agonist activity on Gal4 chimeric human Peroxisome proliferator activated receptor delta expressed in CHO-K1 cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Design, synthesis, and evaluation of substituted phenylpropanoic acid derivatives as human peroxisome proliferator activated receptor activators. Discovery of potent and human peroxisome proliferator activated receptor alpha subtype-selective activators.
Nomura M, Tanase T, Ide T, Tsunoda M, Suzuki M, Uchiki H, Murakami K, Miyachi H.
J Med Chem (2003) 46 : 3581 -3599
PubMed 12904063 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 5.76 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL118939 1 6.92
CHEMBL120748 1 6.40
CHEMBL262558 1 6.19
CHEMBL116540 1 6.05
CHEMBL120611 1 5.82
CHEMBL332465 1 5.62
CHEMBL120456 1 5.55
CHEMBL325723 1 5.52
CHEMBL120744 1 5.52
CHEMBL122070 1 5.52
CHEMBL120009 1 5.44
CHEMBL120676 1 5.18
CHEMBL118976 1 5.10
CHEMBL264374 BEZAFIBRATE 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL118939 EC50 = 120.0 nM 6.92
CHEMBL120748 EC50 = 400.0 nM 6.40
CHEMBL262558 EC50 = 640.0 nM 6.19
CHEMBL116540 EC50 = 900.0 nM 6.05
CHEMBL120611 EC50 = 1500.0 nM 5.82
CHEMBL332465 EC50 = 2400.0 nM 5.62
CHEMBL120456 EC50 = 2800.0 nM 5.55
CHEMBL325723 EC50 = 3000.0 nM 5.52
CHEMBL120744 EC50 = 3000.0 nM 5.52
CHEMBL122070 EC50 = 3000.0 nM 5.52
CHEMBL120009 EC50 = 3600.0 nM 5.44
CHEMBL120676 EC50 = 6600.0 nM 5.18
CHEMBL118976 EC50 = 8000.0 nM 5.10
CHEMBL264374 BEZAFIBRATE EC50 > 143000.0 nM -