Target
Growth hormone secretagogue receptor type 1
Ligand
BDBM50165582
Substrate
n/a
Meas. Tech.
ChEMBL_1574213 (CHEMBL3802218)
Temperature
298.15±n/a K
Ki
2.5±n/a nM
Comments
extracted
Citation
 Maingot, MBlayo, ALDenoyelle, SM'Kadmi, CDamian, MMary, SGagne, DSanchez, PAicher, BSchmidt, PMüller, GTeifel, MGünther, EMarie, JBanères, JLMartinez, JFehrentz, JA New ligands of the ghrelin receptor based on the 1,2,4-triazole scaffold by introduction of a second chiral center. Bioorg Med Chem Lett 26:2408-12 (2016) [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:
BDBM50165582
Synonyms:
CHEMBL3797225
Type:
Small organic molecule
Emp. Form.:
C38H45N9O3
Mol. Mass.:
675.8224
SMILES:
COc1ccc(Cn2c(nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)[C@@H](Cc2c[nH]c3ccccc23)NC(C)=O)cc1 |r|
Structure:
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