Reaction Details Report a problem with these data
Target
Growth hormone secretagogue receptor type 1
Ligand
BDBM50260268
Substrate
n/a
Meas. Tech.
ChEMBL_509093 (CHEMBL1007237)
IC50
3.2±n/a nM
Citation
 Holst, B; Mokrosinski, J; Lang, M; Brandt, E; Nygaard, R; Frimurer, TM; Beck-Sickinger, AG; Schwartz, TW Identification of an efficacy switch region in the ghrelin receptor responsible for interchange between agonism and inverse agonism. J Biol Chem 282:15799-811 (2007) [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:
BDBM50260268
Synonyms:
CHEMBL501261 | rPKPfQwFwLL-NH2
Type:
Small organic molecule
Emp. Form.:
C79H109N19O12
Mol. Mass.:
1516.8309
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](Cc1ccccc1)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 |r,wU:91.97,75.80,55.65,41.56,82.94,30.40,16.28,64.77,8.12,wD:98.106,4.4,(32.88,-5.76,;32.94,-4.22,;34.29,-3.5,;31.62,-3.41,;31.68,-1.87,;30.37,-1.06,;29.01,-1.78,;28.96,-3.32,;27.71,-.97,;27.76,.56,;29.12,1.29,;29.17,2.83,;30.43,.48,;26.35,-1.69,;25.04,-.88,;25.1,.66,;23.69,-1.6,;23.63,-3.15,;24.94,-3.96,;26.37,-3.38,;27.35,-4.56,;26.54,-5.87,;26.96,-7.34,;25.9,-8.45,;24.4,-8.08,;23.97,-6.6,;25.05,-5.49,;22.38,-.79,;21.02,-1.51,;20.96,-3.05,;19.71,-.7,;19.76,.84,;21.12,1.56,;22.43,.75,;23.78,1.47,;23.84,3.02,;22.53,3.83,;21.17,3.11,;18.35,-1.43,;17.04,-.62,;17.09,.93,;15.68,-1.35,;15.63,-2.87,;16.93,-3.7,;18.37,-3.12,;19.35,-4.3,;18.54,-5.61,;18.97,-7.08,;17.9,-8.18,;16.4,-7.82,;15.97,-6.33,;17.04,-5.23,;14.38,-.52,;13,-1.22,;12.96,-2.76,;11.71,-.4,;11.75,1.13,;13.11,1.86,;13.16,3.4,;11.88,4.19,;14.52,4.12,;10.36,-1.15,;9.06,-.33,;9.1,1.22,;7.7,-1.05,;7.65,-2.58,;8.95,-3.4,;10.31,-2.68,;11.61,-3.49,;11.56,-5.03,;10.21,-5.76,;8.9,-4.94,;6.39,-.23,;5.03,-.95,;4.99,-2.49,;3.73,-.14,;3.87,1.41,;2.24,1.8,;1.35,.37,;2.44,-.91,;2.19,-2.43,;3.32,-3.48,;.73,-2.89,;-.6,-2.09,;-1.94,-2.83,;-3.26,-2.04,;-4.61,-2.78,;-5.93,-1.99,;.76,-4.43,;2.1,-5.19,;3.43,-4.4,;2.12,-6.72,;.73,-7.44,;1.29,-9.03,;2.96,-8.99,;3.46,-7.39,;4.8,-6.61,;4.78,-5.08,;6.14,-7.36,;7.47,-6.6,;6.16,-8.91,;7.48,-9.68,;7.48,-11.23,;8.8,-12.02,;8.78,-13.56,;7.44,-14.33,;10.1,-14.35,;33.03,-1.15,;34.35,-1.96,;33.09,.39,)|
Structure:
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