Target
Peroxisome proliferator-activated receptor gamma
Ligand
BDBM50610161
Substrate
n/a
Meas. Tech.
ChEMBL_2280261
IC50
6.6±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 gamma
Synonyms:
NR1C3 | Nuclear receptor subfamily 1 group C member 3 | PPAR-gamma | PPARG | PPARG_HUMAN | Peroxisome proliferator-activated receptor | Peroxisome proliferator-activated receptor gamma (PPAR gamma) | Peroxisome proliferator-activated receptor gamma (PPARG) | Peroxisome proliferator-activated receptor gamma (PPARγ) | Peroxisome proliferator-activated receptor gamma/Nuclear receptor corepressor 2 | peroxisome proliferator-activated receptor gamma isoform 2
Type:
Nuclear Receptor
Mol. Mass.:
57613.46
Organism:
Homo sapiens (Human)
Description:
P37231
Residue:
505
Sequence:
MGETLGDSPIDPESDSFTDTLSANISQEMTMVDTEMPFWPTNFGISSVDLSVMEDHSHSFDIKPFTTVDFSSISTPHYEDIPFTRTDPVVADYKYDLKLQEYQSAIKVEPASPPYYSEKTQLYNKPHEEPSNSLMAIECRVCGDKASGFHYGVHACEGCKGFFRRTIRLKLIYDRCDLNCRIHKKSRNKCQYCRFQKCLAVGMSHNAIRFGRMPQAEKEKLLAEISSDIDQLNPESADLRALAKHLYDSYIKSFPLTKAKARAILTGKTTDKSPFVIYDMNSLMMGEDKIKFKHITPLQEQSKEVAIRIFQGCQFRSVEAVQEITEYAKSIPGFVNLDLNDQVTLLKYGVHEIIYTMLASLMNKDGVLISEGQGFMTREFLKSLRKPFGDFMEPKFEFAVKFNALELDDSDLAIFIAVIILSGDRPGLLNVKPIEDIQDNLLQALELQLKLNHPESSQLFAKLLQKMTDLRQIVTEHVQLLQVIKKTETDMSLHPLLQEIYKDLY
  
Inhibitor
Name:
BDBM50610161
Synonyms:
CHEMBL5281842
Type:
Small organic molecule
Emp. Form.:
C29H19ClF3N3O3
Mol. Mass.:
549.928
SMILES:
Cc1cccc(c1)-c1nc2cc(NC(=O)c3cc(C(=O)NCc4ccc(F)c(F)c4)c(F)cc3Cl)ccc2o1
Structure:
Search PDB for entries with ligand similarity: