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Assay Detail

CHEMBL4269160

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

Binding
Agonist activity at human GAL4 fused PPARdelta-LBD expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay
23
Total Activities
23
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 delta (CHEMBL3979)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.
Li Z, Zhou Z, Deng F, Li Y, Zhang D, Zhang L.
Eur J Med Chem (2018) 159 : 267 -276
PubMed 30296685 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 5.72 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38508 1 7.89
CHEMBL374234 1 6.77
CHEMBL4281724 1 5.82
CHEMBL4289610 1 5.76
CHEMBL4291932 1 5.76
CHEMBL4292189 1 5.71
CHEMBL4281988 1 5.71
CHEMBL4281316 1 5.70
CHEMBL4284723 1 5.68
CHEMBL4276781 1 5.67
CHEMBL4292598 1 5.62
CHEMBL4288124 1 5.62
CHEMBL4284280 1 5.49
CHEMBL4295200 1 5.47
CHEMBL4284549 1 5.34
CHEMBL4280212 1 5.32
CHEMBL4288513 1 5.26
CHEMBL4288770 1 5.10
CHEMBL4277858 1 5.02
CHEMBL4291763 1 -
CHEMBL121 ROSIGLITAZONE 4.0 1 -
CHEMBL21241 GW7647 1 -
CHEMBL1829174 FASIGLIFAM 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38508 EC50 = 13.0 nM 7.89
CHEMBL374234 EC50 = 170.0 nM 6.77
CHEMBL4281724 EC50 = 1520.0 nM 5.82
CHEMBL4289610 EC50 = 1730.0 nM 5.76
CHEMBL4291932 EC50 = 1750.0 nM 5.76
CHEMBL4292189 EC50 = 1930.0 nM 5.71
CHEMBL4281988 EC50 = 1950.0 nM 5.71
CHEMBL4281316 EC50 = 1980.0 nM 5.70
CHEMBL4284723 EC50 = 2090.0 nM 5.68
CHEMBL4276781 EC50 = 2160.0 nM 5.67
CHEMBL4292598 EC50 = 2420.0 nM 5.62
CHEMBL4288124 EC50 = 2370.0 nM 5.62
CHEMBL4284280 EC50 = 3260.0 nM 5.49
CHEMBL4295200 EC50 = 3350.0 nM 5.47
CHEMBL4284549 EC50 = 4560.0 nM 5.34
CHEMBL4280212 EC50 = 4840.0 nM 5.32
CHEMBL4288513 EC50 = 5490.0 nM 5.26
CHEMBL4288770 EC50 = 7930.0 nM 5.10
CHEMBL4277858 EC50 = 9570.0 nM 5.02
CHEMBL4291763 EC50 > 10000.0 nM -
CHEMBL121 ROSIGLITAZONE EC50 - -
CHEMBL21241 GW7647 EC50 - -
CHEMBL1829174 FASIGLIFAM EC50 - -