Reaction Details Report a problem with these data
Target
Growth hormone secretagogue receptor type 1
Ligand
BDBM50153547
Substrate
n/a
Meas. Tech.
ChEMBL_811973 (CHEMBL2013343)
IC50
8±n/a nM
Citation
 Mihalic, JT; Kim, YJ; Lizarzaburu, M; Chen, X; Deignan, J; Wanska, M; Yu, M; Fu, J; Chen, X; Zhang, A; Connors, R; Liang, L; Lindstrom, M; Ma, J; Tang, L; Dai, K; Li, L Discovery of a new class of ghrelin receptor antagonists. Bioorg Med Chem Lett 22:2046-51 (2012) [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:
BDBM50153547
Synonyms:
3-(2,6-Dichloro-phenyl)-5-[2-(2-oxo-piperidin-1-yl)-ethyl]-isoxazole-4-carboxylic acid (4-diethylamino-phenyl)-amide | CHEMBL363995
Type:
Small organic molecule
Emp. Form.:
C27H30Cl2N4O3
Mol. Mass.:
529.458
SMILES:
CCN(CC)c1ccc(NC(=O)c2c(CCN3CCCCC3=O)onc2-c2c(Cl)cccc2Cl)cc1 |(8.86,-1.12,;7.38,-.65,;6.25,-1.69,;6.56,-3.2,;8.05,-3.65,;4.77,-1.21,;3.64,-2.25,;2.18,-1.77,;1.85,-.28,;.4,.2,;-.75,-.84,;-.42,-2.33,;-2.22,-.36,;-2.7,1.1,;-1.8,2.35,;-2.43,3.77,;-1.53,5.01,;.01,4.83,;.89,6.06,;.28,7.49,;-1.25,7.63,;-2.16,6.39,;-3.7,6.57,;-4.24,1.1,;-4.71,-.37,;-3.45,-1.26,;-3.45,-2.8,;-4.78,-3.58,;-6.13,-2.8,;-4.78,-5.12,;-3.45,-5.88,;-2.11,-5.12,;-2.11,-3.57,;-.58,-3.57,;2.99,.76,;4.44,.3,)|
Structure:
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