Target
Growth hormone secretagogue receptor type 1
Ligand
BDBM50161054
Substrate
n/a
Meas. Tech.
ChEMBL_306206 (CHEMBL830164)
IC50
1900±n/a nM
Citation
 Xin, ZZhao, HSerby, MDLiu, BSchaefer, VGFalls, DHKaszubska, WColins, CASham, HLLiu, G Synthesis and structure-activity relationships of isoxazole carboxamides as growth hormone secretagogue receptor antagonists. Bioorg Med Chem Lett 15:1201-4 (2005) [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:
BDBM50161054
Synonyms:
3-(2,6-Dichloro-phenyl)-5-methyl-isoxazole-4-carboxylic acid (2-diethylcarbamoyl-phenyl)-amide | CHEMBL178138
Type:
Small organic molecule
Emp. Form.:
C22H21Cl2N3O3
Mol. Mass.:
446.326
SMILES:
CCN(CC)C(=O)c1ccccc1NC(=O)c1c(C)onc1-c1c(Cl)cccc1Cl |(6.28,5.08,;5.21,3.97,;3.67,3.97,;2.88,5.34,;3.97,6.42,;2.57,2.89,;1.48,3.97,;2.57,1.35,;4.14,1.35,;4.91,.04,;4.16,-1.31,;2.62,-1.31,;1.83,,;.33,.37,;-.76,-.71,;-.34,-2.2,;-2.23,-.33,;-2.63,1.16,;-1.67,2.38,;-4.17,1.24,;-4.71,-.17,;-3.52,-1.15,;-3.42,-2.69,;-2.05,-3.39,;-.58,-3.8,;-1.98,-4.95,;-3.26,-5.79,;-4.64,-5.09,;-4.73,-3.55,;-6.11,-2.87,)|
Structure:
Search PDB for entries with ligand similarity: