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Target
Growth hormone secretagogue receptor type 1
Ligand
BDBM19293
Substrate
125I-His9-ghrelin
Meas. Tech.
Receptor Binding Studies
pH
7.3±n/a
Temperature
298.15±n/a K
IC50
15±5 nM
EC50
64±14 nM
Comments
73 +/- 13 % of max [Ca2+] response @ 10 uM.
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:
BDBM19293
Synonyms:
(R)-N-(1-(5-(2-(1H-Indol-3-yl)ethyl)-4-benzyl-4H-1,2,4-triazol-3-yl)-2-(1H-indol-3-yl)ethyl)-2-amino-2-methylpropanamide | 2-amino-N-[(1R)-1-{4-benzyl-5-[2-(1H-indol-3-yl)ethyl]-4H-1,2,4-triazol-3-yl}-2-(1H-indol-3-yl)ethyl]-2-methylpropanamide | CHEMBL374073 | Trisubstituted 1,2,4-Triazole, 1
Type:
Small organic molecule
Emp. Form.:
C33H35N7O
Mol. Mass.:
545.6773
SMILES:
CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 |r|
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