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Target
Growth hormone secretagogue receptor type 1/Isoform 1B of Growth hormone secretagogue receptor type 1 (1B)
Ligand
BDBM50049478
Substrate
n/a
Meas. Tech.
GHS Ligand Binding Assay
Ki
90.6±5.3 nM
Citation
 Mary, S; Fehrentz, JA; Damian, M; Gaibelet, G; Orcel, H; Verdié, P; Mouillac, B; Martinez, J; Marie, J; Banères, JL Heterodimerization with Its splice variant blocks the ghrelin receptor 1a in a non-signaling conformation: a study with a purified heterodimer assembled into lipid discs. J Biol Chem 288:24656-65 (2013) [PubMed]  Article 
Target
Name:
Growth hormone secretagogue receptor type 1/Isoform 1B of Growth hormone secretagogue receptor type 1 (1B)
Synonyms:
GHS-R1a:GHS-R1b | Growth hormone secretagogue receptor type 1 (1B)
Type:
Dimeric receptor
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
Name:
Growth hormone secretagogue receptor type 1
Synonyms:
Ghrelin receptor 1a (GHS-R1a) | GH-releasing peptide receptor | Ghrelin Receptor (Growth Hormone Secretagogue Receptor Type 1) | GHS-R | GHRP | GHSR_HUMAN | GHSR | Ghrelin receptor
Type:
Receptor
Mol. Mass.:
41334.57
Organism:
Human
Description:
Receptor binding studies use plasma membranes from LLC PK-1 cells transiently transfected with hGHSR1a.
Residue:
366
Sequence:
MWNATPSEEPGFNLTLADLDWDASPGNDSLGDELLQLFPAPLLAGVTATCVALFVVGIAGNLLTMLVVSRFRELRTTTNLYLSSMAFSDLLIFLCMPLDLVRLWQYRPWNFGDLLCKLFQFVSESCTYATVLTITALSVERYFAICFPLRAKVVVTKGRVKLVIFVIWAVAFCSAGPIFVLVGVEHENGTDPWDTNECRPTEFAVRSGLLTVMVWVSSIFFFLPVFCLTVLYSLIGRKLWRRRRGDAVVGASLRDQNHKQTVKMLAVVVFAFILCWLPFHVGRYLFSKSFEPGSLEIAQISQYCNLVSFVLFYLSAAINPILYNIMSKKYRVAVFRLLGFEPFSQRKLSTLKDESSRAWTESSINT
  
Component 2
Name:
Isoform 1B of Growth hormone secretagogue receptor type 1 (1B)
Synonyms:
Ghrelin receptor 1b (GHS-R1b) | GHSR_HUMAN | GHSR | Growth hormone secretagogue receptor type 1 (1B)
Type:
Protein
Mol. Mass.:
32156.55
Organism:
Human
Description:
Q92847-2
Residue:
289
Sequence:
MWNATPSEEPGFNLTLADLDWDASPGNDSLGDELLQLFPAPLLAGVTATCVALFVVGIAGNLLTMLVVSRFRELRTTTNLYLSSMAFSDLLIFLCMPLDLVRLWQYRPWNFGDLLCKLFQFVSESCTYATVLTITALSVERYFAICFPLRAKVVVTKGRVKLVIFVIWAVAFCSAGPIFVLVGVEHENGTDPWDTNECRPTEFAVRSGLLTVMVWVSSIFFFLPVFCLTVLYSLIGRKLWRRRRGDAVVGASLRDQNHKQTVKMLGGSQRALRLSLAGPILSLCLLPSL
  
Inhibitor
Name:
BDBM50049478
Synonyms:
1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-dihydrospiro[indole-3,4'-piperidine]-1'-yl}-1-oxopropan-2-yl]carbamoyl}-1-methylethan-1-aminium | MK-0677 | 1N-[1-benzyloxymethyl-2-[1-methylsulfonylspiro[2,3-dihydro-1H-indole-3,4'-(hexahydropyridine)]-1-yl]-2-oxo-(1R)-ethyl]-2-amino-2-methylpropanamide [3a(MK-0677)] | MK-677 | 1N-[1-benzyloxymethyl-2-[1-methylsulfonylspiro[2,3-dihydro-1H-indole-3,4'-(hexahydropyridine)]-1-yl]-2-oxo-(1R)-ethyl]-2-amino-2-methylpropanamide | 1N-[1-benzyloxymethyl-2-[1-methylsulfonylspiro[2,3-dihydro-1H-indole-3,4'-(hexahydropyridine)]-1-yl]-2-oxo-(1R)-ethyl]-2-amino-2-methylpropanamide(MK-0677) | CHEMBL13817 | MK 0677
Type:
Small organic molecule
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
CC(C)(C(=O)N[C@H](COCc1ccccc1)C(=O)N2CCC3(CC2)CN(c4c3cccc4)S(=O)(=O)C)N
Structure:
Search PDB for entries with ligand similarity: