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Target
Growth hormone secretagogue receptor type 1
Ligand
BDBM102975
Substrate
n/a
Meas. Tech.
Competitive Binding Assay
IC50
0.6±n/a nM
Citation
 Aicher, B; Mueller, G; Paulini, K; Blumenstein, L; Schmidt, P; Gerlach, M; Teifel, M; Martinez, J; Fehrentz, J; Blayo, A Triazole derivatives with improved receptor activity and bioavailability properties as ghrelin antagonists of growth hormone secretagogue receptors US Patent  US8546435 Publication Date 10/1/2013 
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:
BDBM102975
Synonyms:
US8546435, 3
Type:
Small organic molecule
Emp. Form.:
C38H36N8O3
Mol. Mass.:
652.7442
SMILES:
COc1ccc(Cn2c(nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)[C@@H](Cc2c[nH]c3ccccc23)NC(C)=O)cc1 |r|
Structure:
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