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Assay Detail

CHEMBL2033581

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

Functional
Inverse agonist activity at PPARbeta/delta in mouse C2C12 cells assessed as inhibition of Angptl4 expression after 24 hrs by RT-qPCR analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type C2C12
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 4 7.54 8.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2030550 1 8.02
CHEMBL592652 1 7.32
CHEMBL2030543 1 7.28
CHEMBL1998001 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2030550 IC50 = 9.5 nM 8.02
CHEMBL592652 IC50 = 48.0 nM 7.32
CHEMBL2030543 IC50 = 52.0 nM 7.28
CHEMBL1998001 IC50 > 500.0 nM -