Reaction Details
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Report a problem with these dataTarget
Growth hormone secretagogue receptor type 1
Ligand
BDBM50049478
Substrate
n/a
Meas. Tech.
ChEMBL_1722251 (CHEMBL4137251)
EC50
0.398107±n/a nM
Citation
Gardelli, C; Wada, H; Ray, A; Caffrey, M; Llinas, A; Shamovsky, I; Tholander, J; Larsson, J; Sivars, U; Hultin, L; Andersson, U; Sanganee, HJ; Stenvall, K; Leidvik, B; Gedda, K; Jinton, L; Rydén Landergren, M; Karabelas, K Identification and Pharmacological Profile of an Indane Based Series of Ghrelin Receptor Full Agonists. J Med Chem 61:5974-5987 (2018) [PubMed] Article More Info.:
Target
Name:
Growth hormone secretagogue receptor type 1
Synonyms:
Ghrelin receptor 1a (GHS-R1a) | GH-releasing peptide receptor | Ghrelin Receptor (Growth Hormone Secretagogue Receptor Type 1) | GHS-R | GHRP | GHSR_HUMAN | GHSR | Ghrelin receptor
Type:
Receptor
Mol. Mass.:
41334.57
Organism:
Human
Description:
Receptor binding studies use plasma membranes from LLC PK-1 cells transiently transfected with hGHSR1a.
Residue:
366
Sequence:
MWNATPSEEPGFNLTLADLDWDASPGNDSLGDELLQLFPAPLLAGVTATCVALFVVGIAGNLLTMLVVSRFRELRTTTNLYLSSMAFSDLLIFLCMPLDLVRLWQYRPWNFGDLLCKLFQFVSESCTYATVLTITALSVERYFAICFPLRAKVVVTKGRVKLVIFVIWAVAFCSAGPIFVLVGVEHENGTDPWDTNECRPTEFAVRSGLLTVMVWVSSIFFFLPVFCLTVLYSLIGRKLWRRRRGDAVVGASLRDQNHKQTVKMLAVVVFAFILCWLPFHVGRYLFSKSFEPGSLEIAQISQYCNLVSFVLFYLSAAINPILYNIMSKKYRVAVFRLLGFEPFSQRKLSTLKDESSRAWTESSINT
Inhibitor
Name:
BDBM50049478
Synonyms:
1-{[(2R)-3-(benzyloxy)-1-{1-methanesulfonyl-1,2-dihydrospiro[indole-3,4'-piperidine]-1'-yl}-1-oxopropan-2-yl]carbamoyl}-1-methylethan-1-aminium | MK-0677 | 1N-[1-benzyloxymethyl-2-[1-methylsulfonylspiro[2,3-dihydro-1H-indole-3,4'-(hexahydropyridine)]-1-yl]-2-oxo-(1R)-ethyl]-2-amino-2-methylpropanamide [3a(MK-0677)] | MK-677 | 1N-[1-benzyloxymethyl-2-[1-methylsulfonylspiro[2,3-dihydro-1H-indole-3,4'-(hexahydropyridine)]-1-yl]-2-oxo-(1R)-ethyl]-2-amino-2-methylpropanamide | 1N-[1-benzyloxymethyl-2-[1-methylsulfonylspiro[2,3-dihydro-1H-indole-3,4'-(hexahydropyridine)]-1-yl]-2-oxo-(1R)-ethyl]-2-amino-2-methylpropanamide(MK-0677) | CHEMBL13817 | MK 0677
Type:
Small organic molecule
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
CC(C)(C(=O)N[C@H](COCc1ccccc1)C(=O)N2CCC3(CC2)CN(c4c3cccc4)S(=O)(=O)C)N
