Target
Growth hormone secretagogue receptor type 1
Ligand
BDBM50544379
Substrate
n/a
Meas. Tech.
ChEMBL_1992277 (CHEMBL4626012)
EC50
0.235000±n/a nM
Citation
 Cooper, MLlinas, AHansen, PCaffrey, MRay, ASjödin, SShamovsky, IWada, HJellesmark Jensen, TSivars, UHultin, LAndersson, ULundqvist, SGedda, KJinton, LKrutrök, NLewis, RJansson, PGardelli, C Identification and Optimization of Pyrrolidine Derivatives as Highly Potent Ghrelin Receptor Full Agonists. J Med Chem 63:9705-9730 (2020) [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:
BDBM50544379
Synonyms:
CHEMBL4643530
Type:
Small organic molecule
Emp. Form.:
C26H27Cl2N5O5S
Mol. Mass.:
592.494
SMILES:
Clc1ccc(-c2cc(no2)C(=O)N[C@H]2CN(C[C@@H]2C(=O)N[C@H]2CCCNC2)S(=O)(=O)c2ccccc2)c(Cl)c1 |r|
Structure:
Search PDB for entries with ligand similarity: