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Target
Peroxisome proliferator-activated receptor gamma
Ligand
BDBM50610148
Substrate
n/a
Meas. Tech.
ChEMBL_2280261
IC50
94±n/a nM
Citation
 Orsi, DL; Ferrara, SJ; Siegel, S; Friberg, A; Bouché, L; Pook, E; Lienau, P; Bluck, JP; Lemke, CT; Akcay, G; Stellfeld, T; Meyer, H; Pütter, V; Holton, SJ; Korr, D; Jerchel-Furau, I; Pantelidou, C; Strathdee, CA; Meyerson, M; Eis, K; Goldstein, 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:
BDBM50610148
Synonyms:
CHEMBL5287868
Type:
Small organic molecule
Emp. Form.:
C21H16ClFN2O2
Mol. Mass.:
382.815
SMILES:
Fc1cc(Cl)c(cc1C(=O)NCc1ccccc1)C(=O)Nc1ccccc1
Structure:
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