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Target
Growth hormone secretagogue receptor type 1
Ligand
BDBM19386
Substrate
125I-His9-ghrelin
Meas. Tech.
Receptor Binding Studies and GHS-R Ca2+ Flux Assay
pH
7.4±n/a
Temperature
295.15±n/a K
IC50
0.2±0.1 nM
EC50
5.8±2.6 nM
Citation
 Serby, MD; Zhao, H; Szczepankiewicz, BG; Kosogof, C; Xin, Z; Liu, B; Liu, M; Nelson, LT; Kaszubska, W; Falls, HD; Schaefer, V; Bush, EN; Shapiro, R; Droz, BA; Knourek-Segel, VE; Fey, TA; Brune, ME; Beno, DW; Turner, TM; Collins, CA; Jacobson, PB; Sham, HL; Liu, G 2,4-diaminopyrimidine derivatives as potent growth hormone secretagogue receptor antagonists. J Med Chem 49:2568-78 (2006) [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:
BDBM19386
Synonyms:
2,4-diaminopyrimidine derivative, 8b | 6-[(benzyloxy)methyl]-5-(4-{[(4-nitrophenyl)methyl]amino}phenyl)pyrimidine-2,4-diamine
Type:
Small organic molecule
Emp. Form.:
C25H24N6O3
Mol. Mass.:
456.4965
SMILES:
Nc1nc(N)c(c(COCc2ccccc2)n1)-c1ccc(NCc2ccc(cc2)[N+]([O-])=O)cc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
125I-His9-ghrelin
Synonyms:
radiolabeled peptide ligand
Type:
Peptide
Mol. Mass.:
9033.11
Organism:
n/a
Description:
n/a
Residue:
82
Sequence:
GLYSERSERCTANYLPHELESERPRGLHISGLNARGVALGLNGLNARGLYSGLSERLYSLYSPRPRALALYSLEGLNPRARG