Reaction Details Report a problem with these data
Target
Growth hormone secretagogue receptor type 1 [E24Q]
Ligand
BDBM212436
Substrate
n/a
Meas. Tech.
GHS Ligand Binding Assay
Ki
993±0 nM
Citation
 Mary, S; Fehrentz, JA; Damian, M; Gaibelet, G; Orcel, H; Verdié, P; Mouillac, B; Martinez, J; Marie, J; Banères, JL Heterodimerization with Its splice variant blocks the ghrelin receptor 1a in a non-signaling conformation: a study with a purified heterodimer assembled into lipid discs. J Biol Chem 288:24656-65 (2013) [PubMed]  Article 
Target
Name:
Growth hormone secretagogue receptor type 1 [E24Q]
Synonyms:
GHSR | GHSR_HUMAN | Ghrelin receptor 1a (GHS-R1a E124Q)
Type:
Protein
Mol. Mass.:
41334.59
Organism:
Homo sapiens (Human)
Description:
Human ghrelin receptor 1a E124Q mutant
Residue:
366
Sequence:
MWNATPSEEPGFNLTLADLDWDASPGNDSLGDELLQLFPAPLLAGVTATCVALFVVGIAGNLLTMLVVSRFRELRTTTNLYLSSMAFSDLLIFLCMPLDLVRLWQYRPWNFGDLLCKLFQFVSQSCTYATVLTITALSVERYFAICFPLRAKVVVTKGRVKLVIFVIWAVAFCSAGPIFVLVGVEHENGTDPWDTNECRPTEFAVRSGLLTVMVWVSSIFFFLPVFCLTVLYSLIGRKLWRRRRGDAVVGASLRDQNHKQTVKMLAVVVFAFILCWLPFHVGRYLFSKSFEPGSLEIAQISQYCNLVSFVLFYLSAAINPILYNIMSKKYRVAVFRLLGFEPFSQRKLSTLKDESSRAWTESSINT
  
Inhibitor
Name:
BDBM212436
Synonyms:
JMV 3002 | N-[1-[4-[(2,4-dimethoxyphenyl)methyl]-5-(2-phenylethyl)-1,2,4-triazol-3-yl]-2-(1H-indol-3-yl)ethyl]pyridine-2-carboxamide
Type:
Small organic molecule
Emp. Form.:
C35H34N6O3
Mol. Mass.:
586.6829
SMILES:
COc1ccc(Cn2c(CCc3ccccc3)nnc2C(Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)c(OC)c1
Structure:
Search PDB for entries with ligand similarity: