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Assay Detail

CHEMBL3756609

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

Binding
Transactivation of human PPARalpha expressed in HEK293 cells incubated for 18 hrs by dual luciferase reporter gene assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Peroxisome proliferator-activated receptor alpha (CHEMBL239)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

PPAR agonists based on stilbene and its bioisosteres: biological evaluation and docking studies
De Filippis B, Agamennone M, Ammazzalorso A, Bruno I, D'Angelo A, Di Matteo M, Fantacuzzi M, Giampietro L, Giancristofaro A, Maccallini C, Amoroso R
Medchemcomm (2015) 6 : 1513 -1517
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 5.24 6.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3753965 1 6.12
CHEMBL3752643 1 6.10
CHEMBL1828826 1 6.00
CHEMBL3753786 1 5.48
CHEMBL3752940 1 5.42
CHEMBL3753029 1 4.55
CHEMBL457 GEMFIBROZIL 4.0 1 4.23
CHEMBL3752362 1 4.05
CHEMBL3753947 1 -
CHEMBL3751969 1 -
CHEMBL3751930 1 -
CHEMBL3754669 1 -
CHEMBL3753819 1 -
CHEMBL3753640 1 -
CHEMBL3754569 1 -
CHEMBL121 ROSIGLITAZONE 4.0 1 -
CHEMBL153057 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3753965 EC50 = 760.0 nM 6.12
CHEMBL3752643 EC50 = 800.0 nM 6.10
CHEMBL1828826 EC50 = 1000.0 nM 6.00
CHEMBL3753786 EC50 = 3300.0 nM 5.48
CHEMBL3752940 EC50 = 3800.0 nM 5.42
CHEMBL3753029 EC50 = 28400.0 nM 4.55
CHEMBL457 GEMFIBROZIL EC50 = 59000.0 nM 4.23
CHEMBL3752362 EC50 = 90000.0 nM 4.05
CHEMBL3753947 EC50 - -
CHEMBL3751969 EC50 - -
CHEMBL3751930 EC50 = 103200.0 nM -
CHEMBL3754669 EC50 - -
CHEMBL3753819 EC50 - -
CHEMBL3753640 EC50 - -
CHEMBL3754569 EC50 - -
CHEMBL121 ROSIGLITAZONE EC50 - -
CHEMBL153057 EC50 - -