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TargetGhrelin receptor
LigandBDBM50019921
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1361893
Ki 6.6±n/a nM
Citation Bhattacharya, SKAndrews, KBeveridge, RCameron, KOChen, CDunn, MFernando, DGao, HHepworth, DJackson, VMKhot, VKong, JKosa, RELapham, KLoria, PMLondregan, ATMcClure, KFOrr, STPatel, JRose, CSaenz, JStock, IAStorer, GVanVolkenburg, MVrieze, DWang, GXiao, JZhang, Y Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate. ACS Med Chem Lett5:474-9 (2014) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Ghrelin receptor
Name:Ghrelin receptor
Synonyms:GH-releasing peptide receptor | GHRP | GHS-R | Ghrelin Receptor (Growth Hormone Secretagogue Receptor Type 1) | 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:
MWNATPSEEPGFNLTLADLDWDASPGNDSLGDELLQLFPAPLLAGVTATCVALFVVGIAG
NLLTMLVVSRFRELRTTTNLYLSSMAFSDLLIFLCMPLDLVRLWQYRPWNFGDLLCKLFQ
FVSESCTYATVLTITALSVERYFAICFPLRAKVVVTKGRVKLVIFVIWAVAFCSAGPIFV
LVGVEHENGTDPWDTNECRPTEFAVRSGLLTVMVWVSSIFFFLPVFCLTVLYSLIGRKLW
RRRRGDAVVGASLRDQNHKQTVKMLAVVVFAFILCWLPFHVGRYLFSKSFEPGSLEIAQI
SQYCNLVSFVLFYLSAAINPILYNIMSKKYRVAVFRLLGFEPFSQRKLSTLKDESSRAWT
ESSINT
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  Blast E-value cutoff:
BDBM50019921
NameBDBM50019921
Synonyms:CHEMBL3287213
TypeSmall organic molecule
Emp. Form.C28H30N6OS
Mol. Mass.498.642
SMILESCc1cn2cc(CC(=O)N3CCC4(CN(C4)[C@@H]4CCc5cc(ccc45)-c4ncccn4)CC3)nc2s1 |r|
Structure
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