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Assay Detail

CHEMBL4307144

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

Binding
Agonist activity at PPARalpha (unknown origin) incubated for 3 to 16 hrs by pathhunter nuclear hormone receptor assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of a Novel Selective Dual Peroxisome Proliferator-Activated Receptor α/δ Agonist for the Treatment of Primary Biliary Cirrhosis.
Jiang Z, Liu X, Yuan Z, He H, Wang J, Zhang X, Gong Z, Hou L, Shen L, Guo F, Zhang J, Wang J, Xu D, Liu Z, Li H, Chen X, Long C, Li J, Chen S.
ACS Med Chem Lett (2019) 10 : 1068 -1073
PubMed 31312410 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 6.46 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL21241 GW7647 1 8.30
CHEMBL4470753 1 8.10
CHEMBL4436335 1 7.57
CHEMBL3707395 ELAFIBRANOR 4.0 1 6.65
CHEMBL4516239 1 6.42
CHEMBL4566817 1 5.55
CHEMBL4460024 1 5.47
CHEMBL4483327 1 5.05
CHEMBL4587533 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL21241 GW7647 EC50 = 5.0 nM 8.30
CHEMBL4470753 EC50 = 8.0 nM 8.10
CHEMBL4436335 EC50 = 27.0 nM 7.57
CHEMBL3707395 ELAFIBRANOR EC50 = 225.0 nM 6.65
CHEMBL4516239 EC50 = 385.0 nM 6.42
CHEMBL4566817 EC50 = 2821.0 nM 5.55
CHEMBL4460024 EC50 = 3423.0 nM 5.47
CHEMBL4483327 EC50 = 8974.0 nM 5.05
CHEMBL4587533 EC50 = 10000.0 nM 5.00