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Target
Gastrin-releasing peptide receptor
Ligand
BDBM50336886
Substrate
n/a
Meas. Tech.
ChEMBL_718886 (CHEMBL1681380)
IC50
>10000±n/a nM
Citation
 Sebhat, IK; Franklin, C; Lo, MM; Chen, D; Jewell, JP; Miller, R; Pang, J; Palyha, O; Kan, Y; Kelly, TM; Guan, XM; Marsh, DJ; Kosinski, JA; Metzger, JM; Lyons, K; Dragovic, J; Guzzo, PR; Henderson, AJ; Reitman, ML; Nargund, RP; Wyvratt, MJ Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity ACS Med Chem Lett 2:43-47 (2011) [PubMed]  Article
Target
Name:
Gastrin-releasing peptide receptor
Synonyms:
Bombesin 2 | GRP-R | GRP-preferring bombesin receptor | GRPR | GRPR_HUMAN | Gastrin releasing peptide receptor | Gastrin-releasing peptide receptor
Type:
Enzyme Catalytic Domain
Mol. Mass.:
43214.53
Organism:
Homo sapiens (Human)
Description:
Bombesin 2 GRPR 0::P30550
Residue:
384
Sequence:
MALNDCFLLNLEVDHFMHCNISSHSADLPVNDDWSHPGILYVIPAVYGVIILIGLIGNITLIKIFCTVKSMRNVPNLFISSLALGDLLLLITCAPVDASRYLADRWLFGRIGCKLIPFIQLTSVGVSVFTLTALSADRYKAIVRPMDIQASHALMKICLKAAFIWIISMLLAIPEAVFSDLHPFHEESTNQTFISCAPYPHSNELHPKIHSMASFLVFYVIPLSIISVYYYFIAKNLIQSAYNLPVEGNIHVKKQIESRKRLAKTVLVFVGLFAFCWLPNHVIYLYRSYHYSEVDTSMLHFVTSICARLLAFTNSCVNPFALYLLSKSFRKQFNTQLLCCQPGLIIRSHSTGRSTTCMTSLKSTNPSVATFSLINGNICHERYV
  
Inhibitor
Name:
BDBM50336886
Synonyms:
1-[4-(2,2-dimethylpropyl)-1H-imidazol-2-yl]-2-[4-(5-fluoropyridin-2-yl)phenyl]propan-2-ol | CHEMBL1672352
Type:
Small organic molecule
Emp. Form.:
C22H26FN3O
Mol. Mass.:
367.4597
SMILES:
CC(C)(C)Cc1cnc(CC(C)(O)c2ccc(cc2)-c2ccc(F)cn2)[nH]1
Structure:
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