Reaction Details Report a problem with these data
Target
Growth hormone secretagogue receptor type 1
Ligand
BDBM50096214
Substrate
n/a
Meas. Tech.
ChEMBL_1505778 (CHEMBL3595016)
IC50
3.0±n/a nM
Citation
 Takahashi, B; Funami, H; Iwaki, T; Maruoka, H; Shibata, M; Koyama, M; Nagahira, A; Kamiide, Y; Kanki, S; Igawa, Y; Muto, T Orally active ghrelin receptor inverse agonists and their actions on a rat obesity model. Bioorg Med Chem 23:4792-803 (2015) [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:
BDBM50096214
Synonyms:
CHEMBL3593814
Type:
Small organic molecule
Emp. Form.:
C29H29ClN4O5
Mol. Mass.:
549.017
SMILES:
COc1ccc(CNC(=O)c2cc(cnc2NCc2ccc3OCOc3c2)C#CC(C)(C)NC(C)=O)cc1Cl
Structure:
Search PDB for entries with ligand similarity: