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Assay Detail

CHEMBL1113508

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Functional
Agonist activity at human GAL4-tagged PPARalpha chimeric receptor expressed in HEK cells by transactivation assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Peroxisome proliferator-activated receptor alpha (CHEMBL239)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

(S)-3-(4-(2-(5-Methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-(piperazin-1-yl) propanoic acid compounds: synthesis and biological evaluation of dual PPARalpha/gamma agonists.
Zhou X, Chen W, Xu C, Fan S, Xie Y, Zhong W, Wang L, Li S.
Bioorg Med Chem Lett (2010) 20 : 2605 -2608
PubMed 20299214 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 6.09 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL410478 1 8.00
CHEMBL1089633 1 7.92
CHEMBL1089634 1 5.87
CHEMBL1089632 1 5.84
CHEMBL1089177 1 5.05
CHEMBL121 ROSIGLITAZONE 4.0 1 4.98
CHEMBL1090859 1 4.95
CHEMBL1090860 1 -
CHEMBL1090861 1 -
CHEMBL1090557 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL410478 EC50 = 10.0 nM 8.00
CHEMBL1089633 EC50 = 12.0 nM 7.92
CHEMBL1089634 EC50 = 1350.0 nM 5.87
CHEMBL1089632 EC50 = 1450.0 nM 5.84
CHEMBL1089177 EC50 = 8980.0 nM 5.05
CHEMBL121 ROSIGLITAZONE EC50 = 10580.0 nM 4.98
CHEMBL1090859 EC50 = 11130.0 nM 4.95
CHEMBL1090860 EC50 > 100000.0 nM -
CHEMBL1090861 EC50 > 100000.0 nM -
CHEMBL1090557 EC50 > 100000.0 nM -