Target
Growth hormone secretagogue receptor type 1
Ligand
BDBM50232278
Substrate
n/a
Meas. Tech.
ChEMBL_460934 (CHEMBL944882)
IC50
96±n/a nM
Citation
 Moulin, ADemange, LRyan, JMousseaux, DSanchez, PBergé, GGagne, DPerrissoud, DLocatelli, VTorsello, AGalleyrand, JCFehrentz, JAMartinez, J New trisubstituted 1,2,4-triazole derivatives as potent ghrelin receptor antagonists. 3. Synthesis and pharmacological in vitro and in vivo evaluations. J Med Chem 51:689-93 (2008) [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:
BDBM50232278
Synonyms:
(R)-N-((5-(2-(1H-indol-3-yl)ethyl)-4-(4-ethylphenyl)-4H-1,2,4-triazol-3-yl)(1H-indol-3-yl)methyl)-2-(pyridin-2-yl)acetamide | CHEMBL266961
Type:
Small organic molecule
Emp. Form.:
C36H33N7O
Mol. Mass.:
579.6935
SMILES:
CCc1ccc(cc1)-n1c(CCc2c[nH]c3ccccc23)nnc1[C@H](NC(=O)Cc1ccccn1)c1c[nH]c2ccccc12
Structure:
Search PDB for entries with ligand similarity: