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Assay Detail

CHEMBL760611

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 alpha ligand binding domain
13
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CV-1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Peroxisome proliferator-activated receptor alpha (CHEMBL239)
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 7.90 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL21706 1 9.00
CHEMBL20392 1 8.30
CHEMBL21241 GW7647 1 8.22
CHEMBL20495 1 8.22
CHEMBL280897 1 8.10
CHEMBL279211 1 8.05
CHEMBL20280 1 8.05
CHEMBL20125 2 7.77
CHEMBL281791 1 7.70
CHEMBL281608 1 7.30
CHEMBL278590 GSK-9578 1 7.30
CHEMBL21105 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL21706 EC50 = 1.0 nM 9.00
CHEMBL20392 EC50 = 5.0 nM 8.30
CHEMBL21241 GW7647 EC50 = 6.0 nM 8.22
CHEMBL20495 EC50 = 6.0 nM 8.22
CHEMBL280897 EC50 = 8.0 nM 8.10
CHEMBL279211 EC50 = 9.0 nM 8.05
CHEMBL20280 EC50 = 9.0 nM 8.05
CHEMBL20125 EC50 = 17.0 nM 7.77
CHEMBL281791 EC50 = 20.0 nM 7.70
CHEMBL20125 EC50 = 20.0 nM 7.70
CHEMBL281608 EC50 = 50.0 nM 7.30
CHEMBL278590 GSK-9578 EC50 = 50.0 nM 7.30
CHEMBL21105 EC50 = 100.0 nM 7.00