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Assay Detail

CHEMBL5033439

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

Binding
Agonist activity at Gal4-fused human PPARalpha LBD transfected in HEK293T cells assessed as transcriptional activation incubated for 14 to 16 hrs by dual-Glo luciferase assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

A Photohormone for Light-Dependent Control of PPARα in Live Cells.
Willems S, Morstein J, Hinnah K, Trauner D, Merk D.
J Med Chem (2021) 64 : 10393 -10402
PubMed 34213899 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 6.65 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5077172 1 8.15
CHEMBL5075710 1 8.05
CHEMBL5079792 1 7.54
CHEMBL5078989 1 7.44
CHEMBL5090762 1 7.40
CHEMBL5093897 1 7.40
CHEMBL5091066 1 7.16
CHEMBL5078096 1 7.15
CHEMBL5090355 1 6.72
CHEMBL5087538 1 6.62
CHEMBL5093865 1 6.55
CHEMBL5090334 1 6.54
CHEMBL5085675 1 6.33
CHEMBL5090373 1 6.19
CHEMBL5090949 1 6.18
CHEMBL4471853 1 6.10
CHEMBL5087457 1 6.10
CHEMBL5078286 1 5.96
CHEMBL5075561 1 5.96
CHEMBL2204696 1 5.96
CHEMBL5079941 1 5.46
CHEMBL2204695 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5077172 EC50 = 7.0 nM 8.15
CHEMBL5075710 EC50 = 9.0 nM 8.05
CHEMBL5079792 EC50 = 29.0 nM 7.54
CHEMBL5078989 EC50 = 36.0 nM 7.44
CHEMBL5090762 EC50 = 40.0 nM 7.40
CHEMBL5093897 EC50 = 40.0 nM 7.40
CHEMBL5091066 EC50 = 70.0 nM 7.16
CHEMBL5078096 EC50 = 71.0 nM 7.15
CHEMBL5090355 EC50 = 190.0 nM 6.72
CHEMBL5087538 EC50 = 240.0 nM 6.62
CHEMBL5093865 EC50 = 280.0 nM 6.55
CHEMBL5090334 EC50 = 290.0 nM 6.54
CHEMBL5085675 EC50 = 470.0 nM 6.33
CHEMBL5090373 EC50 = 640.0 nM 6.19
CHEMBL5090949 EC50 = 660.0 nM 6.18
CHEMBL4471853 EC50 = 790.0 nM 6.10
CHEMBL5087457 EC50 = 800.0 nM 6.10
CHEMBL5078286 EC50 = 1100.0 nM 5.96
CHEMBL5075561 EC50 = 1100.0 nM 5.96
CHEMBL2204696 EC50 = 1090.0 nM 5.96
CHEMBL5079941 EC50 = 3500.0 nM 5.46
CHEMBL2204695 EC50 = 3700.0 nM 5.43