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Target
Growth hormone secretagogue receptor type 1
Ligand
BDBM50386955
Substrate
n/a
Meas. Tech.
ChEMBL_982014 (CHEMBL2428369)
Ki
5.5±n/a nM
Citation
 McClure, KF; Jackson, M; Cameron, KO; Kung, DW; Perry, DA; Orr, ST; Zhang, Y; Kohrt, J; Tu, M; Gao, H; Fernando, D; Jones, R; Erasga, N; Wang, G; Polivkova, J; Jiao, W; Swartz, R; Ueno, H; Bhattacharya, SK; Stock, IA; Varma, S; Bagdasarian, V; Perez, S; Kelly-Sullivan, D; Wang, R; Kong, J; Cornelius, P; Michael, L; Lee, E; Janssen, A; Steyn, SJ; Lapham, K; Goosen, T Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor. Bioorg Med Chem Lett 23:5410-4 (2013) [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:
BDBM50386955
Synonyms:
CHEMBL2048820
Type:
Small organic molecule
Emp. Form.:
C24H26ClN7OS
Mol. Mass.:
496.028
SMILES:
Cc1cn2cc(CC(=O)N3CCC4(CN(Cc5ccc(cc5Cl)-n5nccn5)C4)CC3)nc2s1
Structure:
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