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TargetGrowth hormone secretagogue receptor type 1
LigandBDBM19387
Substrate/Competitor125I-His9-ghrelin
Meas. Tech.Receptor Binding Studies and GHS-R Ca2+ Flux Assay
pH7.4±n/a
Temperature295.15±n/a K
IC50 0.3±0.1 nM
EC50 7.2±0.5 nM
Citation Serby, MDZhao, HSzczepankiewicz, BGKosogof, CXin, ZLiu, BLiu, MNelson, LTKaszubska, WFalls, HDSchaefer, VBush, ENShapiro, RDroz, BAKnourek-Segel, VEFey, TABrune, MEBeno, DWTurner, TMCollins, CAJacobson, PBSham, HLLiu, G 2,4-diaminopyrimidine derivatives as potent growth hormone secretagogue receptor antagonists. J Med Chem49:2568-78 (2006) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Growth hormone secretagogue receptor type 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:
MWNATPSEEPGFNLTLADLDWDASPGNDSLGDELLQLFPAPLLAGVTATCVALFVVGIAG
NLLTMLVVSRFRELRTTTNLYLSSMAFSDLLIFLCMPLDLVRLWQYRPWNFGDLLCKLFQ
FVSESCTYATVLTITALSVERYFAICFPLRAKVVVTKGRVKLVIFVIWAVAFCSAGPIFV
LVGVEHENGTDPWDTNECRPTEFAVRSGLLTVMVWVSSIFFFLPVFCLTVLYSLIGRKLW
RRRRGDAVVGASLRDQNHKQTVKMLAVVVFAFILCWLPFHVGRYLFSKSFEPGSLEIAQI
SQYCNLVSFVLFYLSAAINPILYNIMSKKYRVAVFRLLGFEPFSQRKLSTLKDESSRAWT
ESSINT
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM19387
125I-His9-ghrelin
Name:125I-His9-ghrelin
Synonyms:radiolabeled peptide ligand
Type:Peptide
Mol. Mass.:9033.11
Organism:n/a
Description:n/a
Residue:82
Sequence:
GLYSERSERCTANYLPHELESERPRGLHISGLNARGVALGLNGLNARGLYSGLSERLYSL
YSPRPRALALYSLEGLNPRARG