Reaction Details Report a problem with these data
Target
Growth hormone secretagogue receptor type 1
Ligand
BDBM50181180
Substrate
n/a
Meas. Tech.
ChEMBL_345662 (CHEMBL870659)
IC50
0.4±n/a nM
Citation
 Liu, B; Liu, M; Xin, Z; Zhao, H; Serby, MD; Kosogof, C; Nelson, LT; Szczepankiewicz, BG; Kaszubska, W; Schaefer, VG; Falls, HD; Lin, CW; Collins, CA; Sham, HL; Liu, G Optimization of 2,4-diaminopyrimidines as GHS-R antagonists: side chain exploration. Bioorg Med Chem Lett 16:1864-8 (2006) [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:
BDBM50181180
Synonyms:
CHEMBL377514 | N-(3,5-dimethylbenzyl)-3-(5-(4-(4-(methylsulfonyl)benzylamino)phenyl)-2,6-diaminopyrimidin-4-yl)propanamide
Type:
Small organic molecule
Emp. Form.:
C30H34N6O3S
Mol. Mass.:
558.694
SMILES:
Cc1cc(C)cc(CNC(=O)CCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(cc3)S(C)(=O)=O)cc2)c1
Structure:
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