Target
Growth hormone secretagogue receptor type 1
Ligand
BDBM50539697
Substrate
n/a
Meas. Tech.
ChEMBL_1978553 (CHEMBL4611688)
IC50
27000±n/a nM
Citation
 Davidsson, ÖNilsson, KBrånalt, JAndersson, TBerggren, KChen, YFjellström, OGradén, HGustafsson, LHermansson, NOJansen, FJohannesson, POhlsson, BTyrchan, CWellner, AWellner, EÖlwegård-Halvarsson, M Identification of novel GPR81 agonist lead series for target biology evaluation. Bioorg Med Chem Lett 30:0 (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:
BDBM50539697
Synonyms:
CHEMBL4636832
Type:
Small organic molecule
Emp. Form.:
C30H40ClN5O5S2
Mol. Mass.:
650.252
SMILES:
CCOc1cc(Cl)c(cc1N1C[C@H](C)O[C@H](C)C1)C(=O)Nc1nc2ccc(cc2s1)S(=O)(=O)CCCN1CCN(C)CC1 |r|
Structure:
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