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Assay Detail

CHEMBL1068982

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

Binding
Displacement of radiolabeled GW-2433 from human PPARalpha ligand binding domain expressed in Escherichia coli
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and biological activities of novel indole derivatives as potent and selective PPARgamma modulators.
Lamotte Y, Martres P, Faucher N, Laroze A, Grillot D, Ancellin N, Saintillan Y, Beneton V, Gampe RT.
Bioorg Med Chem Lett (2010) 20 : 1399 -1404
PubMed 20079636 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.15 5.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL602263 1 5.15
CHEMBL590984 1 -
CHEMBL590983 1 -
CHEMBL601222 1 -
CHEMBL601861 1 -
CHEMBL606422 1 -
CHEMBL602670 1 -
CHEMBL602469 1 -
CHEMBL602468 1 -
CHEMBL606425 1 -
CHEMBL1017 TELMISARTAN 4.0 1 -
CHEMBL601678 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL602263 IC50 = 7040.0 nM 5.15
CHEMBL590984 IC50 > 10000.0 nM -
CHEMBL590983 IC50 > 10000.0 nM -
CHEMBL601222 IC50 > 10000.0 nM -
CHEMBL601861 IC50 > 10000.0 nM -
CHEMBL606422 IC50 > 10000.0 nM -
CHEMBL602670 IC50 > 10000.0 nM -
CHEMBL602469 IC50 > 10000.0 nM -
CHEMBL602468 IC50 > 10000.0 nM -
CHEMBL606425 IC50 > 10000.0 nM -
CHEMBL1017 TELMISARTAN IC50 > 10000.0 nM -
CHEMBL601678 IC50 - -