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Assay Detail

CHEMBL2033577

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

Binding
Displacement of fluormone Pan-PPAR Green from mouse recombinant GST-tagged PPARbeta/delta LBD after 60 mins by TR-FRET assay
4
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Peroxisome proliferator-activated receptor delta (CHEMBL2458)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

(Z)-2-(2-bromophenyl)-3-{[4-(1-methyl-piperazine)amino]phenyl}acrylonitrile (DG172): an orally bioavailable PPARβ/δ-selective ligand with inverse agonistic properties.
Lieber S, Scheer F, Meissner W, Naruhn S, Adhikary T, Müller-Brüsselbach S, Diederich WE, Müller R.
J Med Chem (2012) 55 : 2858 -2868
PubMed 22369181 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.16 7.57
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2030550 1 7.57
CHEMBL2030543 2 6.75
CHEMBL592652 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2030550 IC50 = 26.9 nM 7.57
CHEMBL2030543 IC50 = 180.0 nM 6.75
CHEMBL2030543 Activity - -
CHEMBL592652 IC50 >= 300.0 nM -