Target
Growth hormone secretagogue receptor type 1
Ligand
BDBM50153542
Substrate
n/a
Meas. Tech.
ChEMBL_312888 (CHEMBL826436)
IC50
102±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:
BDBM50153542
Synonyms:
3-(2,6-Dichloro-phenyl)-5-[2-(tetrahydro-pyran-2-yl)-ethyl]-isoxazole-4-carboxylic acid (4-diethylamino-phenyl)-amide | CHEMBL185399
Type:
Small organic molecule
Emp. Form.:
C27H31Cl2N3O3
Mol. Mass.:
516.459
SMILES:
CCN(CC)c1ccc(NC(=O)c2c(CCC3CCCCO3)onc2-c2c(Cl)cccc2Cl)cc1 |(7.95,-3.46,;6.48,-3.01,;6.15,-1.5,;7.29,-.45,;8.76,-.93,;4.68,-1.01,;3.53,-2.06,;2.08,-1.57,;1.75,-.08,;.29,.39,;-.86,-.64,;-.53,-2.13,;-2.33,-.17,;-2.8,1.28,;-1.91,2.54,;-2.54,3.96,;-1.63,5.2,;-.09,5.02,;.8,6.27,;.17,7.67,;-1.35,7.83,;-2.27,6.58,;-4.34,1.28,;-4.83,-.17,;-3.56,-1.07,;-3.56,-2.62,;-4.9,-3.39,;-6.23,-2.62,;-4.9,-4.93,;-3.56,-5.71,;-2.22,-4.93,;-2.22,-3.39,;-.68,-3.39,;2.88,.95,;4.35,.48,)|
Structure:
Search PDB for entries with ligand similarity: