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Name | Glucose-dependent insulinotropic receptor |
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Species | Homo sapiens (Human) |
Gene | GPR119 |
Synonym | GPCR2 GPR119 G-protein coupled receptor 2 G-protein coupled receptor 119 G protein-coupled receptor 119 [ Show all ] |
Disease | Type 2 diabetes Diabetes Peripheral arterial disease; Type 2 diabetes Non-insulin dependent diabetes Gastric cancer; Type 2 diabetes |
Length | 335 |
Amino acid sequence | MESSFSFGVILAVLASLIIATNTLVAVAVLLLIHKNDGVSLCFTLNLAVADTLIGVAISGLLTDQLSSPSRPTQKTLCSLRMAFVTSSAAASVLTVMLITFDRYLAIKQPFRYLKIMSGFVAGACIAGLWLVSYLIGFLPLGIPMFQQTAYKGQCSFFAVFHPHFVLTLSCVGFFPAMLLFVFFYCDMLKIASMHSQQIRKMEHAGAMAGGYRSPRTPSDFKALRTVSVLIGSFALSWTPFLITGIVQVACQECHLYLVLERYLWLLGVGNSLLNPLIYAYWQKEVRLQLYHMALGVKKVLTSFLLFLSARNCGPERPRESSCHIVTISSSEFDG |
UniProt | Q8TDV5 |
Protein Data Bank | N/A |
GPCR-HGmod model | Q8TDV5 |
3D structure model | This predicted structure model is from GPCR-EXP Q8TDV5. |
BioLiP | N/A |
Therapeutic Target Database | T93788 |
ChEMBL | CHEMBL5652 |
IUPHAR | 126 |
DrugBank | N/A |
Name | CHEMBL2204984 |
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Molecular formula | C23H24N10O |
IUPAC name | 2-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]-4-[[4-(tetrazol-1-yl)phenoxy]methyl]pyrazole-3-carbonitrile |
Molecular weight | 456.514 |
Hydrogen bond acceptor | 9 |
Hydrogen bond donor | 0 |
XlogP | 2.7 |
Synonyms | BDBM50400773 SCHEMBL9883082 |
Inchi Key | BGLRWXCBFWYRFO-UHFFFAOYSA-N |
Inchi ID | InChI=1S/C23H24N10O/c1-2-17-12-25-23(26-13-17)31-9-7-20(8-10-31)33-22(11-24)18(14-28-33)15-34-21-5-3-19(4-6-21)32-16-27-29-30-32/h3-6,12-14,16,20H,2,7-10,15H2,1H3 |
PubChem CID | 67950429 |
ChEMBL | CHEMBL2204984 |
IUPHAR | N/A |
BindingDB | 50400773 |
DrugBank | N/A |
Structure | |
Lipinski's druglikeness | This ligand satisfies Lipinski's rule of five. |
Parameter | Value | Reference | Database source |
---|---|---|---|
EC50 | 5.3 nM | PMID24900416 | BindingDB |
EC50 | 5.32 nM | PMID24900416 | ChEMBL |
EC50 | 10.7 nM | PMID24900416 | ChEMBL |
EC50 | 11.0 nM | PMID24900416 | BindingDB |
Intrinsic activity | 76.8 % | PMID24900416 | ChEMBL |
Intrinsic activity | 86.1 % | PMID24900416 | ChEMBL |
Ki | 14.9 nM | PMID24900416 | ChEMBL |
Ki | 15.0 nM | PMID24900416 | BindingDB |
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