Target
Growth hormone secretagogue receptor type 1
Ligand
BDBM50019924
Substrate
n/a
Meas. Tech.
ChEMBL_1361892 (CHEMBL3293067)
Ki
15±n/a nM
Citation
 Bhattacharya, SKAndrews, KBeveridge, RCameron, KOChen, CDunn, MFernando, DGao, HHepworth, DJackson, VMKhot, VKong, JKosa, RELapham, KLoria, PMLondregan, ATMcClure, KFOrr, STPatel, JRose, CSaenz, JStock, IAStorer, GVanVolkenburg, MVrieze, DWang, GXiao, JZhang, Y Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate. ACS Med Chem Lett 5:474-9 (2014) [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:
BDBM50019924
Synonyms:
CHEMBL3287216
Type:
Small organic molecule
Emp. Form.:
C29H33N5O2
Mol. Mass.:
483.6046
SMILES:
COc1ccc(CC(=O)N2CCC3(CN(C3)[C@@H]3CCc4cc(ccc34)-c3nccc(C)n3)CC2)nc1 |r|
Structure:
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