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Assay Detail

CHEMBL759725

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

Binding
In vitro transcriptional activation in CV-1 cells expressing human Gal4-PPAR delta ligand binding domain
13
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CV-1
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis.
Brown PJ, Stuart LW, Hurley KP, Lewis MC, Winegar DA, Wilson JG, Wilkison WO, Ittoop OR, Willson TM.
Bioorg Med Chem Lett (2001) 11 : 1225 -1227
PubMed 11354382 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 5.57 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20392 1 5.96
CHEMBL278590 GSK-9578 1 5.85
CHEMBL20125 2 5.70
CHEMBL20495 1 5.40
CHEMBL280897 1 5.30
CHEMBL21241 GW7647 1 5.21
CHEMBL21105 1 -
CHEMBL21706 1 -
CHEMBL281791 1 -
CHEMBL279211 1 -
CHEMBL20280 1 -
CHEMBL281608 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20392 EC50 = 1100.0 nM 5.96
CHEMBL278590 GSK-9578 EC50 = 1400.0 nM 5.85
CHEMBL20125 EC50 = 2000.0 nM 5.70
CHEMBL20495 EC50 = 4000.0 nM 5.40
CHEMBL280897 EC50 = 5000.0 nM 5.30
CHEMBL21241 GW7647 EC50 = 6200.0 nM 5.21
CHEMBL21105 EC50 > 10000.0 nM -
CHEMBL21706 EC50 > 10000.0 nM -
CHEMBL20125 EC50 > 10000.0 nM -
CHEMBL281791 EC50 > 10000.0 nM -
CHEMBL279211 EC50 > 10000.0 nM -
CHEMBL20280 EC50 > 10000.0 nM -
CHEMBL281608 EC50 > 10000.0 nM -