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Target
Growth hormone secretagogue receptor type 1
Ligand
BDBM19340
Substrate
125I-His9-ghrelin
Meas. Tech.
Receptor Binding Studies
IC50
63±n/a nM
EC50
14±n/a nM
Citation
 Moulin, A; Demange, L; Bergé, G; Gagne, D; Ryan, J; Mousseaux, D; Heitz, A; Perrissoud, D; Locatelli, V; Torsello, A; Galleyrand, JC; Fehrentz, JA; Martinez, J Toward Potent Ghrelin Receptor Ligands Based on Trisubstituted 1,2,4-Triazole Structure. 2. Synthesis and Pharmacological in Vitro and in Vivo Evaluations. J Med Chem 50:5790-5806 (2007) [PubMed]  Article 
Target
Name:
Growth hormone secretagogue receptor type 1
Synonyms:
GH-releasing peptide receptor | GHRP | GHS-R | GHSR | GHSR_HUMAN | Ghrelin Receptor (Growth Hormone Secretagogue Receptor Type 1) | Ghrelin receptor | Ghrelin receptor 1a (GHS-R1a)
Type:
Receptor
Mol. Mass.:
41334.57
Organism:
Homo sapiens (Human)
Description:
Receptor binding studies use plasma membranes from LLC PK-1 cells transiently transfected with hGHSR1a.
Residue:
366
Sequence:
MWNATPSEEPGFNLTLADLDWDASPGNDSLGDELLQLFPAPLLAGVTATCVALFVVGIAGNLLTMLVVSRFRELRTTTNLYLSSMAFSDLLIFLCMPLDLVRLWQYRPWNFGDLLCKLFQFVSESCTYATVLTITALSVERYFAICFPLRAKVVVTKGRVKLVIFVIWAVAFCSAGPIFVLVGVEHENGTDPWDTNECRPTEFAVRSGLLTVMVWVSSIFFFLPVFCLTVLYSLIGRKLWRRRRGDAVVGASLRDQNHKQTVKMLAVVVFAFILCWLPFHVGRYLFSKSFEPGSLEIAQISQYCNLVSFVLFYLSAAINPILYNIMSKKYRVAVFRLLGFEPFSQRKLSTLKDESSRAWTESSINT
  
Inhibitor
Name:
BDBM19340
Synonyms:
N-[(1R)-1-[4-(2,4-dimethoxyphenyl)-5-(2-phenylethyl)-4H-1,2,4-triazol-3-yl]-2-(1H-indol-3-yl)ethyl]piperidine-4-carboxamide | Trisubstituted 1,2,4-Triazole, 48
Type:
Small organic molecule
Emp. Form.:
C34H38N6O3
Mol. Mass.:
578.7039
SMILES:
COc1ccc(c(OC)c1)-n1c(CCc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCNCC1 |r,wU:23.38,(4.57,-2.49,;3.09,-2.1,;2.48,-.68,;.95,-.51,;.33,.91,;1.25,2.14,;2.78,1.97,;3.7,3.2,;5.24,3.2,;3.39,.55,;.85,3.63,;2.12,4.51,;3.57,4,;4.74,5.01,;4.74,6.55,;3.4,7.32,;3.4,8.86,;4.74,9.63,;6.07,8.86,;6.07,7.32,;1.67,5.98,;.13,6.02,;-.37,4.56,;-1.71,3.79,;-2.48,2.46,;-2.48,.92,;-1,.49,;-.95,-1.05,;-2.41,-1.57,;-2.99,-3,;-4.52,-3.2,;-5.46,-1.98,;-4.87,-.56,;-3.35,-.35,;-3.04,4.56,;-4.38,3.79,;-4.38,2.25,;-5.71,4.56,;-7.04,3.79,;-8.38,4.56,;-8.38,6.1,;-7.04,6.87,;-5.71,6.1,)|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
125I-His9-ghrelin
Synonyms:
radiolabeled peptide ligand
Type:
Peptide
Mol. Mass.:
9033.11
Organism:
n/a
Description:
n/a
Residue:
82
Sequence:
GLYSERSERCTANYLPHELESERPRGLHISGLNARGVALGLNGLNARGLYSGLSERLYSLYSPRPRALALYSLEGLNPRARG