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Target
Growth hormone secretagogue receptor type 1/Isoform 1B of Growth hormone secretagogue receptor type 1 (1B)
Ligand
BDBM212438
Substrate
n/a
Meas. Tech.
GHS Ligand Binding Assay
Ki
291.8±9.2 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:
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
  
Component 2
Name:
Isoform 1B of Growth hormone secretagogue receptor type 1 (1B)
Synonyms:
GHSR | GHSR_HUMAN | Ghrelin receptor 1b (GHS-R1b) | Growth hormone secretagogue receptor type 1 (1B)
Type:
Protein
Mol. Mass.:
32156.55
Organism:
Homo sapiens (Human)
Description:
Q92847-2
Residue:
289
Sequence:
MWNATPSEEPGFNLTLADLDWDASPGNDSLGDELLQLFPAPLLAGVTATCVALFVVGIAGNLLTMLVVSRFRELRTTTNLYLSSMAFSDLLIFLCMPLDLVRLWQYRPWNFGDLLCKLFQFVSESCTYATVLTITALSVERYFAICFPLRAKVVVTKGRVKLVIFVIWAVAFCSAGPIFVLVGVEHENGTDPWDTNECRPTEFAVRSGLLTVMVWVSSIFFFLPVFCLTVLYSLIGRKLWRRRRGDAVVGASLRDQNHKQTVKMLGGSQRALRLSLAGPILSLCLLPSL
  
Inhibitor
Name:
BDBM212438
Synonyms:
SPA | Substance P [DArg1, DTrp5,7,9, Leu11]
Type:
Small organic molecule
Emp. Form.:
C81H110N20O12
Mol. Mass.:
1555.8669
SMILES:
CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@H](N)CCCN=C(N)N)C(N)=O |wU:85.98,64.81,101.110,55.65,78.84,94.101,wD:41.56,30.40,8.12,16.28,4.4,(5.24,8.85,;5.24,7.31,;3.91,6.54,;6.57,6.54,;6.57,5,;7.91,4.23,;9.24,5,;9.24,6.54,;10.58,4.23,;11.91,5,;11.91,6.54,;13.24,7.31,;10.58,7.31,;10.58,2.69,;11.91,1.92,;13.24,2.69,;11.91,.38,;10.58,-.39,;10.18,-1.87,;10.8,-3.28,;9.66,-4.31,;8.33,-3.54,;6.86,-4.02,;5.72,-2.99,;6.04,-1.48,;7.5,-1.01,;8.65,-2.04,;13.24,-.39,;14.58,.38,;14.58,1.92,;15.91,-.39,;17.24,.38,;17.24,1.92,;15.91,2.69,;15.91,4.23,;17.24,5,;18.58,4.23,;18.58,2.69,;15.91,-1.93,;17.24,-2.7,;18.58,-1.93,;17.24,-4.24,;15.91,-5.01,;15.91,-6.55,;17.16,-7.45,;16.68,-8.92,;15.14,-8.92,;14.11,-10.06,;12.6,-9.74,;12.13,-8.28,;13.16,-7.13,;14.66,-7.45,;18.58,-5.01,;19.91,-4.24,;19.91,-2.7,;21.25,-5.01,;21.25,-6.55,;22.58,-7.32,;22.58,-8.86,;23.91,-9.63,;21.25,-9.63,;22.58,-4.24,;23.91,-5.01,;23.91,-6.55,;25.25,-4.24,;25.25,-2.7,;24.16,-1.61,;22.64,-1.85,;21.94,-.48,;23.03,.61,;22.95,2.15,;24.24,2.99,;25.61,2.29,;25.69,.75,;24.4,-.09,;26.58,-5.01,;27.91,-4.24,;27.91,-2.7,;29.25,-5.01,;29.41,-6.54,;30.91,-6.86,;31.68,-5.53,;30.65,-4.38,;30.97,-2.87,;29.83,-1.84,;32.44,-2.4,;33.58,-3.43,;35.05,-2.95,;36.19,-3.98,;37.66,-3.51,;38.8,-4.54,;32.76,-.89,;34.22,-.42,;35.37,-1.45,;34.54,1.09,;35.95,1.72,;35.79,3.25,;34.28,3.57,;33.51,2.23,;31.98,2.07,;31.36,.67,;31.08,3.32,;31.7,4.73,;29.55,3.16,;28.64,4.4,;29.27,5.81,;28.36,7.06,;28.99,8.46,;30.52,8.62,;28.08,9.71,;5.24,4.23,;3.91,5,;5.24,2.69,)|
Structure:
Search PDB for entries with ligand similarity: