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Assay Detail

CHEMBL2089717

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

Functional
Agonist activity at PPARalpha-LBD expressed in HEK293 cells co-expressing GAL4-DBD after 16 to 19 hrs by beta lactamase reporter gene assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis, radiolabeling and initial in vivo evaluation of [(11)C]KSM-01 for imaging PPAR-α receptors.
Solingapuram Sai KK, Kil KE, Tu Z, Chu W, Finck BN, Rothfuss JM, Shoghi KI, Welch MJ, Gropler RJ, Mach RH.
Bioorg Med Chem Lett (2012) 22 : 6233 -6236
PubMed 22939697 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 9.21 9.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2088421 1 9.55
CHEMBL21241 GW7647 1 9.34
CHEMBL2088422 1 9.23
CHEMBL20392 1 8.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2088421 IC50 = 0.28 nM 9.55
CHEMBL21241 GW7647 IC50 = 0.46 nM 9.34
CHEMBL2088422 IC50 = 0.59 nM 9.23
CHEMBL20392 IC50 = 1.93 nM 8.71