Reaction Details |
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Target | Muscarinic acetylcholine receptor M1 |
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Ligand | BDBM50228403 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_803994 (CHEMBL1954974) |
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IC50 | 295±n/a nM |
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Citation | Sutton, JM; Clark, DE; Dunsdon, SJ; Fenton, G; Fillmore, A; Harris, NV; Higgs, C; Hurley, CA; Krintel, SL; MacKenzie, RE; Duttaroy, A; Gangl, E; Maniara, W; Sedrani, R; Namoto, K; Ostermann, N; Gerhartz, B; Sirockin, F; Trappe, J; Hassiepen, U; Baeschlin, DK Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes. Bioorg Med Chem Lett22:1464-8 (2012) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Muscarinic acetylcholine receptor M1 |
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Name: | Muscarinic acetylcholine receptor M1 |
Synonyms: | ACM1_HUMAN | CHRM1 | Cholinergic receptor, muscarinic 1 | Cholinergic, muscarinic M1 |
Type: | Protein |
Mol. Mass.: | 51442.54 |
Organism: | Homo sapiens (Human) |
Description: | P11229 |
Residue: | 460 |
Sequence: | MNTSAPPAVSPNITVLAPGKGPWQVAFIGITTGLLSLATVTGNLLVLISFKVNTELKTVN
NYFLLSLACADLIIGTFSMNLYTTYLLMGHWALGTLACDLWLALDYVASNASVMNLLLIS
FDRYFSVTRPLSYRAKRTPRRAALMIGLAWLVSFVLWAPAILFWQYLVGERTVLAGQCYI
QFLSQPIITFGTAMAAFYLPVTVMCTLYWRIYRETENRARELAALQGSETPGKGGGSSSS
SERSQPGAEGSPETPPGRCCRCCRAPRLLQAYSWKEEEEEDEGSMESLTSSEGEEPGSEV
VIKMPMVDPEAQAPTKQPPRSSPNTVKRPTKKGRDRAGKGQKPRGKEQLAKRKTFSLVKE
KKAARTLSAILLAFILTWTPYNIMVLVSTFCKDCVPETLWELGYWLCYVNSTINPMCYAL
CNKAFRDTFRLLLLCRWDKRRWRKIPKRPGSVHRTPSRQC
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BDBM50228403 |
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n/a |
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Name | BDBM50228403 |
Synonyms: | (R)-8-(3-aminopiperidin-1-yl)-7-(but-2-ynyl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione | 8-[(3R)-3-Aminopiperidin-1-yl]-7-but-2-yn-1-yl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione | CHEMBL237500 | LINAGLIPTIN | US10202383, Example 2(142) | US10358449, Linagliptin | US9255098, Linagliptin | US9321791, 2(142) | US9556175, 2(142) |
Type | Small organic molecule |
Emp. Form. | C25H28N8O2 |
Mol. Mass. | 472.5422 |
SMILES | CC#CCn1c(nc2n(C)c(=O)n(Cc3nc(C)c4ccccc4n3)c(=O)c12)N1CCC[C@@H](N)C1 |
Structure |
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