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Assay Detail

CHEMBL1068976

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Functional
Agonist activity at human PPARgamma expressed in african green monkey CV1 cells by Gal4 transactivation assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CV-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Peroxisome proliferator-activated receptor gamma (CHEMBL235)
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
EC50 13 7.54 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL602468 1 9.10
CHEMBL606422 1 9.00
CHEMBL601222 1 8.70
CHEMBL590983 1 8.52
CHEMBL434063 1 8.22
CHEMBL602263 1 7.77
CHEMBL602670 1 7.66
CHEMBL602469 1 7.33
CHEMBL606425 1 6.79
CHEMBL590984 1 6.70
CHEMBL601861 1 6.47
CHEMBL601678 1 6.05
CHEMBL1017 TELMISARTAN 4.0 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL602468 EC50 = 0.8 nM 9.10
CHEMBL606422 EC50 = 1.0 nM 9.00
CHEMBL601222 EC50 = 2.0 nM 8.70
CHEMBL590983 EC50 = 3.0 nM 8.52
CHEMBL434063 EC50 = 6.0 nM 8.22
CHEMBL602263 EC50 = 17.0 nM 7.77
CHEMBL602670 EC50 = 22.0 nM 7.66
CHEMBL602469 EC50 = 47.0 nM 7.33
CHEMBL606425 EC50 = 163.0 nM 6.79
CHEMBL590984 EC50 = 201.0 nM 6.70
CHEMBL601861 EC50 = 338.0 nM 6.47
CHEMBL601678 EC50 = 900.0 nM 6.05
CHEMBL1017 TELMISARTAN EC50 = 2020.0 nM 5.70