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Target
Growth hormone secretagogue receptor type 1
Ligand
BDBM19358
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
66±23 nM
EC50
188±30 nM
Citation
 Xin, Z; Serby, MD; Zhao, H; Kosogof, C; Szczepankiewicz, BG; Liu, M; Liu, B; Hutchins, CW; Sarris, KA; Hoff, ED; Falls, HD; Lin, CW; Ogiela, CA; Collins, CA; Brune, ME; Bush, EN; Droz, BA; Fey, TA; Knourek-Segel, VE; Shapiro, R; Jacobson, PB; Beno, DW; Turner, TM; Sham, HL; Liu, G Discovery and pharmacological evaluation of growth hormone secretagogue receptor antagonists. J Med Chem 49:4459-69 (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:
BDBM19358
Synonyms:
2,4-diaminopyrimidine-based antagonist, 13d | N-(4-{2,4-diamino-6-[(benzyloxy)methyl]pyrimidin-5-yl}phenyl)cyclopropanecarboxamide
Type:
Small organic molecule
Emp. Form.:
C22H23N5O2
Mol. Mass.:
389.4503
SMILES:
Nc1nc(N)c(c(COCc2ccccc2)n1)-c1ccc(NC(=O)C2CC2)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