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Assay Detail

CHEMBL763845

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

Functional
In vitro effective concentration for agonist activity on human Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor in transfected KRP-297 cells
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type KRP-297
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Peroxisome proliferator-activated receptor alpha (CHEMBL239)
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 38 6.13 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL118329 1 7.70
CHEMBL118939 1 7.40
CHEMBL120009 1 7.40
CHEMBL116540 1 7.37
CHEMBL107789 1 7.22
CHEMBL122070 1 7.05
CHEMBL119791 1 6.96
CHEMBL120243 1 6.89
CHEMBL119911 1 6.64
CHEMBL120456 1 6.62
CHEMBL120246 1 6.54
CHEMBL331469 1 6.50
CHEMBL332465 1 6.44
CHEMBL116947 1 6.40
CHEMBL120748 1 6.17
CHEMBL120611 1 6.13
CHEMBL262558 1 6.07
CHEMBL331206 1 6.00
CHEMBL24458 1 6.00
CHEMBL120676 1 5.92
CHEMBL118413 1 5.89
CHEMBL120444 1 5.82
CHEMBL120744 1 5.80
CHEMBL325723 1 5.80
CHEMBL331464 1 5.75
CHEMBL122009 1 5.66
CHEMBL118198 1 5.64
CHEMBL118483 1 5.57
CHEMBL333778 1 5.55
CHEMBL331557 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL118329 EC50 = 20.0 nM 7.70
CHEMBL118939 EC50 = 40.0 nM 7.40
CHEMBL120009 EC50 = 40.0 nM 7.40
CHEMBL116540 EC50 = 43.0 nM 7.37
CHEMBL107789 EC50 = 60.0 nM 7.22
CHEMBL122070 EC50 = 90.0 nM 7.05
CHEMBL119791 EC50 = 110.0 nM 6.96
CHEMBL120243 EC50 = 130.0 nM 6.89
CHEMBL119911 EC50 = 230.0 nM 6.64
CHEMBL120456 EC50 = 240.0 nM 6.62
CHEMBL120246 EC50 = 290.0 nM 6.54
CHEMBL331469 EC50 = 320.0 nM 6.50
CHEMBL332465 EC50 = 360.0 nM 6.44
CHEMBL116947 EC50 = 400.0 nM 6.40
CHEMBL120748 EC50 = 680.0 nM 6.17
CHEMBL120611 EC50 = 740.0 nM 6.13
CHEMBL262558 EC50 = 860.0 nM 6.07
CHEMBL331206 EC50 = 1000.0 nM 6.00
CHEMBL24458 EC50 = 1000.0 nM 6.00
CHEMBL120676 EC50 = 1200.0 nM 5.92
CHEMBL118413 EC50 = 1300.0 nM 5.89
CHEMBL120444 EC50 = 1500.0 nM 5.82
CHEMBL120744 EC50 = 1600.0 nM 5.80
CHEMBL325723 EC50 = 1600.0 nM 5.80
CHEMBL331464 EC50 = 1800.0 nM 5.75
CHEMBL122009 EC50 = 2200.0 nM 5.66
CHEMBL118198 EC50 = 2300.0 nM 5.64
CHEMBL118483 EC50 = 2700.0 nM 5.57
CHEMBL333778 EC50 = 2800.0 nM 5.55
CHEMBL331557 EC50 = 2900.0 nM 5.54
CHEMBL118492 EC50 = 3000.0 nM 5.52
CHEMBL119682 EC50 = 3100.0 nM 5.51
CHEMBL118976 EC50 = 4900.0 nM 5.31
CHEMBL118279 EC50 = 5600.0 nM 5.25
CHEMBL120620 EC50 = 6000.0 nM 5.22
CHEMBL326777 EC50 = 9400.0 nM 5.03
CHEMBL672 FENOFIBRATE EC50 = 41000.0 nM 4.39
CHEMBL264374 BEZAFIBRATE EC50 > 78000.0 nM -