Reaction Details
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Growth hormone secretagogue receptor type 1
Ligand
BDBM21944
Substrate
BDBM10852
Meas. Tech.
Fluorescence Imaging Plate Reader (FLIPR) Assay
pH
7.2000±n/a
Temperature
295.1500±n/a K
EC50
14.6±n/a nM
Citation
Li, J; Chen, SY; Li, JJ; Wang, H; Hernandez, AS; Tao, S; Musial, CM; Qu, F; Swartz, S; Chao, ST; Flynn, N; Murphy, BJ; Slusarchyk, DA; Seethala, R; Yan, M; Sleph, P; Grover, G; Smith, MA; Beehler, B; Giupponi, L; Dickinson, KE; Zhang, H; Humphreys, WG; Patel, BP; Schwinden, M; Stouch, T; Cheng, PT; Biller, SA; Ewing, WR; Gordon, D; Robl, JA; Tino, JA Discovery of a tetrazole-based growth hormone secretagogue: 4-(hydroxybutyl)carbamic acid 2-{5-[1-(2-amino-2-methylpropionylamino)-2- benzyloxyethyl]tetrazol-1-yl}ethyl ester (BMS-317180). J Med Chem 50:5890-3 (2007) [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:
BDBM21944
Synonyms:
2-{5-[(1S)-1-(2-amino-2-methylpropanamido)-2-(benzyloxy)ethyl]-1H-1,2,3,4-tetrazol-1-yl}ethyl N-(5-hydroxypentyl)carbamate | Tetrazole-based compound, 10
Type:
Small organic molecule
Emp. Form.:
C22H35N7O5
Mol. Mass.:
477.27
SMILES:
CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCCO |r|
Structure:
Substrate