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Assay Detail

CHEMBL3602054

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

Binding
Agonist activity at human PPARgamma transfected in human MCF7 cells after 16 hrs by luciferase reporter gene assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MCF7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Novel Oxazolidinone-Based Peroxisome Proliferator Activated Receptor Agonists: Molecular Modeling, Synthesis, and Biological Evaluation.
Fresno N, Macías-González M, Torres-Zaguirre A, Romero-Cuevas M, Sanz-Camacho P, Elguero J, Pavón FJ, Rodríguez de Fonseca F, Goya P, Pérez-Fernández R.
J Med Chem (2015) 58 : 6639 -6652
PubMed 26226490 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.25 7.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL121 ROSIGLITAZONE 4.0 1 7.06
CHEMBL3601087 1 5.89
CHEMBL3601089 1 5.79
CHEMBL3601092 1 -
CHEMBL3601090 1 -
CHEMBL3601088 1 -
CHEMBL3600934 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL121 ROSIGLITAZONE EC50 = 87.0 nM 7.06
CHEMBL3601087 EC50 = 1298.0 nM 5.89
CHEMBL3601089 EC50 = 1622.0 nM 5.79
CHEMBL3601092 EC50 > 100000.0 nM -
CHEMBL3601090 EC50 > 100000.0 nM -
CHEMBL3601088 EC50 > 100000.0 nM -
CHEMBL3600934 EC50 > 100000.0 nM -