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TargetPeroxisome proliferator-activated receptor gamma
LigandBDBM50610167
Substrate/Competitorn/a
Meas. Tech.ChEMBL_2280278
IC50 14±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 Chem78:0 (2023) [PubMed]
More Info.:Get all data from this article,  Assay Method
 
Peroxisome proliferator-activated receptor gamma
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:
MGETLGDSPIDPESDSFTDTLSANISQEMTMVDTEMPFWPTNFGISSVDLSVMEDHSHSF
DIKPFTTVDFSSISTPHYEDIPFTRTDPVVADYKYDLKLQEYQSAIKVEPASPPYYSEKT
QLYNKPHEEPSNSLMAIECRVCGDKASGFHYGVHACEGCKGFFRRTIRLKLIYDRCDLNC
RIHKKSRNKCQYCRFQKCLAVGMSHNAIRFGRMPQAEKEKLLAEISSDIDQLNPESADLR
ALAKHLYDSYIKSFPLTKAKARAILTGKTTDKSPFVIYDMNSLMMGEDKIKFKHITPLQE
QSKEVAIRIFQGCQFRSVEAVQEITEYAKSIPGFVNLDLNDQVTLLKYGVHEIIYTMLAS
LMNKDGVLISEGQGFMTREFLKSLRKPFGDFMEPKFEFAVKFNALELDDSDLAIFIAVII
LSGDRPGLLNVKPIEDIQDNLLQALELQLKLNHPESSQLFAKLLQKMTDLRQIVTEHVQL
LQVIKKTETDMSLHPLLQEIYKDLY
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50610167
n/a
NameBDBM50610167
Synonyms:CHEMBL5271038
TypeSmall organic molecule
Emp. Form.C25H22ClF3N4O3
Mol. Mass.518.915
SMILESCc1cc(cnc1NC(=O)c1cc(C(=O)NCc2ccc(F)c(F)c2)c(F)cc1Cl)N1CCOCC1
Structure
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