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Assay Detail

CHEMBL972693

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

Functional
Agonist activity at PPARdelta transfected in HEK293 cells by GAL4 transactivation assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Peroxisome proliferator-activated receptor delta (CHEMBL3979)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Improvement of the transactivation activity of phenylpropanoic acid-type peroxisome proliferator-activated receptor pan agonists: effect of introduction of fluorine at the linker part.
Kasuga J, Oyama T, Hirakawa Y, Makishima M, Morikawa K, Hashimoto Y, Miyachi H.
Bioorg Med Chem Lett (2008) 18 : 4525 -4528
PubMed 18662876 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 6.95 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL462982 1 7.70
CHEMBL514264 1 7.60
CHEMBL457623 1 7.55
CHEMBL387914 1 7.54
CHEMBL457405 1 7.26
CHEMBL455957 1 7.23
CHEMBL514256 1 7.22
CHEMBL456974 1 7.03
CHEMBL402840 1 6.92
CHEMBL118939 1 6.89
CHEMBL456355 1 6.75
CHEMBL456973 1 6.55
CHEMBL456752 1 6.26
CHEMBL402161 1 6.03
CHEMBL456753 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL462982 EC50 = 20.0 nM 7.70
CHEMBL514264 EC50 = 25.0 nM 7.60
CHEMBL457623 EC50 = 28.0 nM 7.55
CHEMBL387914 EC50 = 29.0 nM 7.54
CHEMBL457405 EC50 = 55.0 nM 7.26
CHEMBL455957 EC50 = 59.0 nM 7.23
CHEMBL514256 EC50 = 60.0 nM 7.22
CHEMBL456974 EC50 = 94.0 nM 7.03
CHEMBL402840 EC50 = 120.0 nM 6.92
CHEMBL118939 EC50 = 130.0 nM 6.89
CHEMBL456355 EC50 = 180.0 nM 6.75
CHEMBL456973 EC50 = 280.0 nM 6.55
CHEMBL456752 EC50 = 550.0 nM 6.26
CHEMBL402161 EC50 = 940.0 nM 6.03
CHEMBL456753 EC50 = 2200.0 nM 5.66