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Target
Growth hormone secretagogue receptor type 1
Ligand
BDBM50232287
Substrate
n/a
Meas. Tech.
ChEMBL_460934 (CHEMBL944882)
IC50
120±n/a nM
Citation
 Moulin, A; Demange, L; Ryan, J; Mousseaux, D; Sanchez, P; Bergé, G; Gagne, D; Perrissoud, D; Locatelli, V; Torsello, A; Galleyrand, JC; Fehrentz, JA; Martinez, 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:
BDBM50232287
Synonyms:
CHEMBL428314 | N-((R)-(4-(2,4-dimethoxyphenyl)-5-phenethyl-4H-1,2,4-triazol-3-yl)(1H-indol-3-yl)methyl)-2-(pyridin-2-yl)acetamide
Type:
Small organic molecule
Emp. Form.:
C34H32N6O3
Mol. Mass.:
572.6563
SMILES:
COc1ccc(c(OC)c1)-n1c(CCc2ccccc2)nnc1[C@H](NC(=O)Cc1ccccn1)c1c[nH]c2ccccc12 |wD:23.26,(8.33,-38.92,;9.66,-39.7,;11,-38.95,;11.02,-37.41,;12.36,-36.65,;13.68,-37.44,;13.67,-38.97,;15,-39.75,;14.99,-41.29,;12.33,-39.73,;15.02,-36.68,;16.36,-37.45,;16.39,-38.99,;17.74,-39.74,;17.77,-41.28,;16.45,-42.07,;16.48,-43.61,;17.83,-44.35,;19.15,-43.55,;19.12,-42.01,;17.64,-36.35,;16.88,-35.02,;15.35,-35.17,;14.32,-34.03,;12.82,-34.34,;11.48,-33.58,;11.47,-32.04,;10.15,-34.36,;8.81,-33.6,;8.8,-32.06,;7.47,-31.3,;6.14,-32.08,;6.15,-33.63,;7.49,-34.38,;14.8,-32.56,;13.9,-31.31,;14.81,-30.06,;16.28,-30.54,;17.6,-29.77,;18.94,-30.54,;18.95,-32.09,;17.61,-32.86,;16.28,-32.09,)|
Structure:
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