Target
Peroxisome proliferator-activated receptor delta
Ligand
BDBM50610167
Substrate
n/a
Meas. Tech.
ChEMBL_2280282
IC50
>5000±n/a nM
Citation
 Orsi, DLFerrara, SJSiegel, SFriberg, ABouché, LPook, ELienau, PBluck, JPLemke, CTAkcay, GStellfeld, TMeyer, HPütter, VHolton, SJKorr, DJerchel-Furau, IPantelidou, CStrathdee, CAMeyerson, MEis, KGoldstein, JT Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists. Bioorg Med Chem 78:0 (2023) [PubMed]
Target
Name:
Peroxisome proliferator-activated receptor delta
Synonyms:
NR1C2 | NUC1 | NUCI | Nuclear hormone receptor 1 | Nuclear receptor subfamily 1 group C member 2 | PPAR delta | PPAR-beta | PPARB | PPARD | PPARD_HUMAN | Peroxisome proliferator-activated receptor | Peroxisome proliferator-activated receptor beta | Peroxisome proliferator-activated receptor delta
Type:
Enzyme
Mol. Mass.:
49910.45
Organism:
Homo sapiens (Human)
Description:
Q03181
Residue:
441
Sequence:
MEQPQEEAPEVREEEEKEEVAEAEGAPELNGGPQHALPSSSYTDLSRSSSPPSLLDQLQMGCDGASCGSLNMECRVCGDKASGFHYGVHACEGCKGFFRRTIRMKLEYEKCERSCKIQKKNRNKCQYCRFQKCLALGMSHNAIRFGRMPEAEKRKLVAGLTANEGSQYNPQVADLKAFSKHIYNAYLKNFNMTKKKARSILTGKASHTAPFVIHDIETLWQAEKGLVWKQLVNGLPPYKEISVHVFYRCQCTTVETVRELTEFAKSIPSFSSLFLNDQVTLLKYGVHEAIFAMLASIVNKDGLLVANGSGFVTREFLRSLRKPFSDIIEPKFEFAVKFNALELDDSDLALFIAAIILCGDRPGLMNVPRVEAIQDTILRALEFHLQANHPDAQYLFPKLLQKMADLRQLVTEHAQMMQRIKKTETETSLHPLLQEIYKDMY
  
Inhibitor
Name:
BDBM50610167
Synonyms:
CHEMBL5271038
Type:
Small organic molecule
Emp. Form.:
C25H22ClF3N4O3
Mol. Mass.:
518.915
SMILES:
Cc1cc(cnc1NC(=O)c1cc(C(=O)NCc2ccc(F)c(F)c2)c(F)cc1Cl)N1CCOCC1
Structure:
Search PDB for entries with ligand similarity: