Reaction Details |
| Report a problem with these data |
Target | Growth hormone secretagogue receptor type 1 |
---|
Ligand | BDBM50440261 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_1361892 (CHEMBL3293067) |
---|
Ki | 6.3±n/a nM |
---|
Citation | Bhattacharya, SK; Andrews, K; Beveridge, R; Cameron, KO; Chen, C; Dunn, M; Fernando, D; Gao, H; Hepworth, D; Jackson, VM; Khot, V; Kong, J; Kosa, RE; Lapham, K; Loria, PM; Londregan, AT; McClure, KF; Orr, ST; Patel, J; Rose, C; Saenz, J; Stock, IA; Storer, G; VanVolkenburg, M; Vrieze, D; Wang, G; Xiao, J; Zhang, 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 |
---|
|
Growth hormone secretagogue receptor type 1 |
---|
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: | MWNATPSEEPGFNLTLADLDWDASPGNDSLGDELLQLFPAPLLAGVTATCVALFVVGIAG
NLLTMLVVSRFRELRTTTNLYLSSMAFSDLLIFLCMPLDLVRLWQYRPWNFGDLLCKLFQ
FVSESCTYATVLTITALSVERYFAICFPLRAKVVVTKGRVKLVIFVIWAVAFCSAGPIFV
LVGVEHENGTDPWDTNECRPTEFAVRSGLLTVMVWVSSIFFFLPVFCLTVLYSLIGRKLW
RRRRGDAVVGASLRDQNHKQTVKMLAVVVFAFILCWLPFHVGRYLFSKSFEPGSLEIAQI
SQYCNLVSFVLFYLSAAINPILYNIMSKKYRVAVFRLLGFEPFSQRKLSTLKDESSRAWT
ESSINT
|
|
|
BDBM50440261 |
---|
n/a |
---|
Name | BDBM50440261 |
Synonyms: | CHEMBL2426677 |
Type | Small organic molecule |
Emp. Form. | C29H32N4O2 |
Mol. Mass. | 468.59 |
SMILES | COc1ccc(CC(=O)N2CCC3(CN(C3)[C@@H]3CCc4cc(ccc34)-c3ncccn3)CC2)cc1 |r| |
Structure |
|