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Assay Detail

CHEMBL3602053

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

Binding
Agonist activity at human PPARalpha transfected in human MCF7 cells after 16 hrs by luciferase reporter gene assay
16
Total Activities
16
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 alpha (CHEMBL239)
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 16 6.19 8.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL21241 GW7647 1 8.19
CHEMBL280065 OLEOYLETHANOLAMIDE 1 6.82
CHEMBL3601087 1 6.17
CHEMBL3601093 1 6.12
CHEMBL3601089 1 6.09
CHEMBL3601098 1 6.06
CHEMBL3601099 1 6.01
CHEMBL3601096 1 6.01
CHEMBL3601097 1 5.72
CHEMBL3601091 1 5.70
CHEMBL3601090 1 5.18
CHEMBL3601095 1 -
CHEMBL3601094 1 -
CHEMBL3601092 1 -
CHEMBL3601088 1 -
CHEMBL3600934 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL21241 GW7647 EC50 = 6.5 nM 8.19
CHEMBL280065 OLEOYLETHANOLAMIDE EC50 = 152.0 nM 6.82
CHEMBL3601087 EC50 = 670.0 nM 6.17
CHEMBL3601093 EC50 = 756.0 nM 6.12
CHEMBL3601089 EC50 = 821.0 nM 6.09
CHEMBL3601098 EC50 = 866.0 nM 6.06
CHEMBL3601099 EC50 = 981.0 nM 6.01
CHEMBL3601096 EC50 = 966.0 nM 6.01
CHEMBL3601097 EC50 = 1922.0 nM 5.72
CHEMBL3601091 EC50 = 1978.0 nM 5.70
CHEMBL3601090 EC50 = 6623.0 nM 5.18
CHEMBL3601095 EC50 > 100000.0 nM -
CHEMBL3601094 EC50 > 100000.0 nM -
CHEMBL3601092 EC50 > 100000.0 nM -
CHEMBL3601088 EC50 > 100000.0 nM -
CHEMBL3600934 EC50 > 100000.0 nM -