Reaction Details Report a problem with these data
Target
Growth hormone secretagogue receptor type 1
Ligand
BDBM19369
Substrate
125I-His9-ghrelin
Meas. Tech.
Receptor Binding Studies and GHS-R Ca2+ Flux Assay
pH
7.4000±n/a
Temperature
295.1500±n/a K
EC50
>10000±n/a 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:
Ghrelin receptor 1a (GHS-R1a) | GH-releasing peptide receptor | Ghrelin Receptor (Growth Hormone Secretagogue Receptor Type 1) | GHS-R | GHRP | GHSR_HUMAN | GHSR | Ghrelin receptor
Type:
Receptor
Mol. Mass.:
41334.57
Organism:
Human
Description:
Receptor binding studies use plasma membranes from LLC PK-1 cells transiently transfected with hGHSR1a.
Residue:
366
Sequence:
MWNATPSEEPGFNLTLADLDWDASPGNDSLGDELLQLFPAPLLAGVTATCVALFVVGIAGNLLTMLVVSRFRELRTTTNLYLSSMAFSDLLIFLCMPLDLVRLWQYRPWNFGDLLCKLFQFVSESCTYATVLTITALSVERYFAICFPLRAKVVVTKGRVKLVIFVIWAVAFCSAGPIFVLVGVEHENGTDPWDTNECRPTEFAVRSGLLTVMVWVSSIFFFLPVFCLTVLYSLIGRKLWRRRRGDAVVGASLRDQNHKQTVKMLAVVVFAFILCWLPFHVGRYLFSKSFEPGSLEIAQISQYCNLVSFVLFYLSAAINPILYNIMSKKYRVAVFRLLGFEPFSQRKLSTLKDESSRAWTESSINT
  
Inhibitor
Name:
BDBM19369
Synonyms:
1-(4-{2,4-diamino-6-[(benzyloxy)methyl]pyrimidin-5-yl}phenyl)-3-methyl-3-propan-2-ylurea | 2,4-diaminopyrimidine-based antagonist, 14b
Type:
Small organic molecule
Emp. Form.:
C23H28N6O2
Mol. Mass.:
420.23
SMILES:
CC(C)N(C)C(=O)Nc1ccc(cc1)-c1c(N)nc(N)nc1COCc1ccccc1
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