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Assay Detail

CHEMBL757882

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

Functional
In vitro agonist activity tested for transactivation in human PPAR gamma-Gal4 chimeric COS-1 cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type COS-1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Peroxisome proliferator-activated receptor gamma (CHEMBL235)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.
Koyama H, Boueres JK, Han W, Metzger EJ, Bergman JP, Gratale DF, Miller DJ, Tolman RL, MacNaul KL, Berger JP, Doebber TW, Leung K, Moller DE, Heck JV, Sahoo SP.
Bioorg Med Chem Lett (2003) 13 : 1801 -1804
PubMed 12729668 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 6.95 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL430970 1 7.70
CHEMBL121 ROSIGLITAZONE 4.0 1 7.70
CHEMBL50885 1 7.52
CHEMBL53746 1 7.52
CHEMBL300026 1 7.22
CHEMBL52426 1 7.10
CHEMBL54097 1 7.00
CHEMBL52633 1 6.92
CHEMBL50143 1 6.70
CHEMBL299958 1 6.52
CHEMBL301156 1 6.52
CHEMBL50755 1 6.40
CHEMBL50984 1 6.30
CHEMBL298187 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL430970 EC50 = 20.0 nM 7.70
CHEMBL121 ROSIGLITAZONE EC50 = 20.0 nM 7.70
CHEMBL50885 EC50 = 30.0 nM 7.52
CHEMBL53746 EC50 = 30.0 nM 7.52
CHEMBL300026 EC50 = 60.0 nM 7.22
CHEMBL52426 EC50 = 80.0 nM 7.10
CHEMBL54097 EC50 = 100.0 nM 7.00
CHEMBL52633 EC50 = 120.0 nM 6.92
CHEMBL50143 EC50 = 200.0 nM 6.70
CHEMBL299958 EC50 = 300.0 nM 6.52
CHEMBL301156 EC50 = 300.0 nM 6.52
CHEMBL50755 EC50 = 400.0 nM 6.40
CHEMBL50984 EC50 = 500.0 nM 6.30
CHEMBL298187 EC50 = 700.0 nM 6.16