Target
Growth hormone secretagogue receptor type 1
Ligand
BDBM50153551
Substrate
n/a
Meas. Tech.
ChEMBL_306821 (CHEMBL831012)
IC50
47±n/a nM
Citation
 Liu, BLiu, GXin, ZSerby, MDZhao, HSchaefer, VGFalls, HDKaszubska, WCollins, CASham, HL Novel isoxazole carboxamides as growth hormone secretagogue receptor (GHS-R) antagonists. Bioorg Med Chem Lett 14:5223-6 (2004) [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:
BDBM50153551
Synonyms:
5-(2-Benzo[1,3]dioxol-5-yl-ethyl)-3-(2,6-dichloro-phenyl)-isoxazole-4-carboxylic acid (4-diethylamino-phenyl)-amide | CHEMBL440939
Type:
Small organic molecule
Emp. Form.:
C29H27Cl2N3O4
Mol. Mass.:
552.448
SMILES:
CCN(CC)c1ccc(NC(=O)c2c(CCc3ccc4OCOc4c3)onc2-c2c(Cl)cccc2Cl)cc1 |(8.6,-1.55,;7.13,-1.06,;5.98,-2.11,;6.31,-3.61,;7.77,-4.07,;4.52,-1.64,;3.37,-2.67,;1.92,-2.2,;1.59,-.69,;.1,-.22,;-1.03,-1.25,;-.7,-2.77,;-2.52,-.78,;-2.97,.69,;-2.07,1.93,;-2.7,3.33,;-1.8,4.6,;-2.43,6,;-1.54,7.26,;.01,7.1,;1.15,8.11,;2.48,7.35,;2.16,5.83,;.63,5.67,;-.27,4.43,;-4.51,.68,;-4.99,-.78,;-3.74,-1.68,;-3.73,-3.23,;-5.06,-4,;-6.4,-3.23,;-5.06,-5.55,;-3.73,-6.32,;-2.38,-5.55,;-2.38,-4,;-.84,-4,;2.72,.34,;4.18,-.12,)|
Structure:
Search PDB for entries with ligand similarity: