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Assay Detail

CHEMBL927780

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

Functional
Agonist activity at mouse PPARalpha assessed as receptor activation by cell based assay
35
Total Activities
24
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, synthesis and evaluation of trifluoromethane sulfonamide derivatives as new potent and selective peroxisome proliferator-activated receptor alpha agonists.
Faucher N, Martres P, Laroze A, Pineau O, Potvain F, Grillot D.
Bioorg Med Chem Lett (2008) 18 : 710 -715
PubMed 18060776 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 24 6.98 8.70
Activity 11 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL253310 2 8.70
CHEMBL252675 2 7.70
CHEMBL219586 GW590735 2.0 2 7.70
CHEMBL427890 2 7.22
CHEMBL403637 2 7.10
CHEMBL438346 2 6.89
CHEMBL253486 2 6.70
CHEMBL253923 2 6.47
CHEMBL401562 2 6.16
CHEMBL254744 2 6.10
CHEMBL403909 2 6.00
CHEMBL402100 1 -
CHEMBL254946 1 -
CHEMBL404467 1 -
CHEMBL254743 1 -
CHEMBL254742 1 -
CHEMBL254540 1 -
CHEMBL253520 1 -
CHEMBL253522 1 -
CHEMBL401560 1 -
CHEMBL253490 1 -
CHEMBL401580 1 -
CHEMBL253109 1 -
CHEMBL253924 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL253310 EC50 = 2.0 nM 8.70
CHEMBL219586 GW590735 EC50 = 20.0 nM 7.70
CHEMBL252675 EC50 = 20.0 nM 7.70
CHEMBL427890 EC50 = 60.0 nM 7.22
CHEMBL403637 EC50 = 80.0 nM 7.10
CHEMBL438346 EC50 = 130.0 nM 6.89
CHEMBL253486 EC50 = 200.0 nM 6.70
CHEMBL253923 EC50 = 340.0 nM 6.47
CHEMBL401562 EC50 = 700.0 nM 6.16
CHEMBL254744 EC50 = 800.0 nM 6.10
CHEMBL403909 EC50 = 1000.0 nM 6.00
CHEMBL253109 EC50 > 10000.0 nM -
CHEMBL253520 EC50 > 10000.0 nM -
CHEMBL253310 Activity = 98.0 % -
CHEMBL253486 Activity = 152.0 % -
CHEMBL254744 Activity = 78.0 % -
CHEMBL254540 EC50 > 10000.0 nM -
CHEMBL254742 EC50 > 10000.0 nM -
CHEMBL254743 EC50 > 10000.0 nM -
CHEMBL404467 EC50 > 10000.0 nM -
CHEMBL254946 EC50 > 10000.0 nM -
CHEMBL402100 EC50 > 10000.0 nM -
CHEMBL219586 GW590735 Activity = 103.0 % -
CHEMBL401562 Activity = 116.0 % -
CHEMBL252675 Activity = 123.0 % -
CHEMBL403637 Activity = 96.0 % -
CHEMBL253923 Activity = 0.34 % -
CHEMBL427890 Activity = 74.0 % -
CHEMBL438346 Activity = 132.0 % -
CHEMBL253522 EC50 > 25000.0 nM -
CHEMBL403909 Activity = 130.0 % -
CHEMBL253490 EC50 > 25000.0 nM -
CHEMBL253924 EC50 > 25000.0 nM -
CHEMBL401580 EC50 > 25000.0 nM -
CHEMBL401560 EC50 > 25000.0 nM -