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Assay Detail

CHEMBL840102

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

Binding
Effective concentration against human PPARgamma expressed in HepG2 cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HepG2
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Synthesis, biological evaluation, and molecular modeling investigation of new chiral fibrates with PPARalpha and PPARgamma agonist activity.
Pinelli A, Godio C, Laghezza A, Mitro N, Fracchiolla G, Tortorella V, Lavecchia A, Novellino E, Fruchart JC, Staels B, Crestani M, Loiodice F.
J Med Chem (2005) 48 : 5509 -5519
PubMed 16107150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 5.46 7.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL121 ROSIGLITAZONE 4.0 1 7.41
CHEMBL191275 1 6.30
CHEMBL192518 1 6.05
CHEMBL426632 1 5.82
CHEMBL189116 1 5.80
CHEMBL364748 1 5.57
CHEMBL191060 1 5.44
CHEMBL360420 1 5.27
CHEMBL366157 1 5.14
CHEMBL369890 1 5.05
CHEMBL190905 1 4.98
CHEMBL190368 1 4.91
CHEMBL364254 1 4.90
CHEMBL371320 1 4.70
CHEMBL370054 1 4.59
CHEMBL683 CLOFIBRIC ACID 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL121 ROSIGLITAZONE EC50 = 39.0 nM 7.41
CHEMBL191275 EC50 = 500.0 nM 6.30
CHEMBL192518 EC50 = 900.0 nM 6.05
CHEMBL426632 EC50 = 1500.0 nM 5.82
CHEMBL189116 EC50 = 1600.0 nM 5.80
CHEMBL364748 EC50 = 2700.0 nM 5.57
CHEMBL191060 EC50 = 3600.0 nM 5.44
CHEMBL360420 EC50 = 5400.0 nM 5.27
CHEMBL366157 EC50 = 7200.0 nM 5.14
CHEMBL369890 EC50 = 8900.0 nM 5.05
CHEMBL190905 EC50 = 10500.0 nM 4.98
CHEMBL190368 EC50 = 12400.0 nM 4.91
CHEMBL364254 EC50 = 12500.0 nM 4.90
CHEMBL371320 EC50 = 20100.0 nM 4.70
CHEMBL370054 EC50 = 25700.0 nM 4.59
CHEMBL683 CLOFIBRIC ACID EC50 = 309000.0 nM -