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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 | APD597 |
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Molecular formula | C21H29N5O6S |
IUPAC name | propan-2-yl 4-[5-methoxy-6-[(2-methyl-6-methylsulfonylpyridin-3-yl)amino]pyrimidin-4-yl]oxypiperidine-1-carboxylate |
Molecular weight | 479.552 |
Hydrogen bond acceptor | 10 |
Hydrogen bond donor | 1 |
XlogP | 2.5 |
Synonyms | HY-15566 propan-2-yl 4-[5-methoxy-6-[(2-methyl-6-methylsulfonylpyridin-3-yl)amino]pyrimidin-4-yl]oxypiperidine-1-carboxylate ADP-597 JNJ-38431055 UNII-345354O7AT [ Show all ] |
Inchi Key | WPDCHTSXOPUOII-UHFFFAOYSA-N |
Inchi ID | InChI=1S/C21H29N5O6S/c1-13(2)31-21(27)26-10-8-15(9-11-26)32-20-18(30-4)19(22-12-23-20)25-16-6-7-17(24-14(16)3)33(5,28)29/h6-7,12-13,15H,8-11H2,1-5H3,(H,22,23,25) |
PubChem CID | 11691484 |
ChEMBL | CHEMBL1951032 |
IUPHAR | 5727 |
BindingDB | 50364559 |
DrugBank | N/A |
Structure | |
Lipinski's druglikeness | This ligand satisfies Lipinski's rule of five. |
Parameter | Value | Reference | Database source |
---|---|---|---|
EC50 | 46.0 nM | PMID26048791, PMID25088191, PMID22264481 | BindingDB,ChEMBL |
EC50 | 50.1187 nM | PMID22264481 | IUPHAR |
Efficacy | 75.0 % | PMID25088191 | ChEMBL |
Emax | 75.0 % | PMID26048791 | ChEMBL |
Intrinsic activity | 75.0 % | PMID22264481 | ChEMBL |
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