Reaction Details |
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Target | Dipeptidyl peptidase 4 |
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Ligand | BDBM50391571 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_850194 (CHEMBL2149800) |
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IC50 | 0.85±n/a nM |
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Citation | Yoshida, T; Akahoshi, F; Sakashita, H; Kitajima, H; Nakamura, M; Sonda, S; Takeuchi, M; Tanaka, Y; Ueda, N; Sekiguchi, S; Ishige, T; Shima, K; Nabeno, M; Abe, Y; Anabuki, J; Soejima, A; Yoshida, K; Takashina, Y; Ishii, S; Kiuchi, S; Fukuda, S; Tsutsumiuchi, R; Kosaka, K; Murozono, T; Nakamaru, Y; Utsumi, H; Masutomi, N; Kishida, H; Miyaguchi, I; Hayashi, Y Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine): a highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. Bioorg Med Chem20:5705-19 (2012) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Dipeptidyl peptidase 4 |
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Name: | Dipeptidyl peptidase 4 |
Synonyms: | ADABP | ADCP2 | Adenosine deaminase complexing protein 2 | CD26 | CD_antigen=CD26 | DPP IV | DPP4 | DPP4_HUMAN | DPPIV | Dipeptidyl peptidase 4 (DDP-IV) | Dipeptidyl peptidase 4 (DPP IV) | Dipeptidyl peptidase 4 (DPP-4) | Dipeptidyl peptidase 4 (DPP4) | Dipeptidyl peptidase 4 (DPPIV) | Dipeptidyl peptidase 4 membrane form | Dipeptidyl peptidase 4 soluble form | Dipeptidyl peptidase IV | Dipeptidyl peptidase IV (DDP-4) | Dipeptidyl peptidase IV (DDP-IV) | Dipeptidyl peptidase IV (DPP IV) | Dipeptidyl peptidase IV membrane form | Dipeptidyl peptidase IV soluble form | Dipeptidyl peptidase-IV (DPP-4) | Dipeptidyl peptidase-IV (DPP-IV) | T-cell activation antigen CD26 | TP103 |
Type: | Enzyme |
Mol. Mass.: | 88271.01 |
Organism: | Homo sapiens (Human) |
Description: | P27487 |
Residue: | 766 |
Sequence: | MKTPWKVLLGLLGAAALVTIITVPVVLLNKGTDDATADSRKTYTLTDYLKNTYRLKLYSL
RWISDHEYLYKQENNILVFNAEYGNSSVFLENSTFDEFGHSINDYSISPDGQFILLEYNY
VKQWRHSYTASYDIYDLNKRQLITEERIPNNTQWVTWSPVGHKLAYVWNNDIYVKIEPNL
PSYRITWTGKEDIIYNGITDWVYEEEVFSAYSALWWSPNGTFLAYAQFNDTEVPLIEYSF
YSDESLQYPKTVRVPYPKAGAVNPTVKFFVVNTDSLSSVTNATSIQITAPASMLIGDHYL
CDVTWATQERISLQWLRRIQNYSVMDICDYDESSGRWNCLVARQHIEMSTTGWVGRFRPS
EPHFTLDGNSFYKIISNEEGYRHICYFQIDKKDCTFITKGTWEVIGIEALTSDYLYYISN
EYKGMPGGRNLYKIQLSDYTKVTCLSCELNPERCQYYSVSFSKEAKYYQLRCSGPGLPLY
TLHSSVNDKGLRVLEDNSALDKMLQNVQMPSKKLDFIILNETKFWYQMILPPHFDKSKKY
PLLLDVYAGPCSQKADTVFRLNWATYLASTENIIVASFDGRGSGYQGDKIMHAINRRLGT
FEVEDQIEAARQFSKMGFVDNKRIAIWGWSYGGYVTSMVLGSGSGVFKCGIAVAPVSRWE
YYDSVYTERYMGLPTPEDNLDHYRNSTVMSRAENFKQVEYLLIHGTADDNVHFQQSAQIS
KALVDVGVDFQAMWYTDEDHGIASSTAHQHIYTHMSHFIKQCFSLP
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BDBM50391571 |
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n/a |
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Name | BDBM50391571 |
Synonyms: | CHEMBL2147713 |
Type | Small organic molecule |
Emp. Form. | C22H29FN6OS |
Mol. Mass. | 444.569 |
SMILES | Cc1cc(N2CCN(CC2)[C@@H]2CN[C@@H](C2)C(=O)N2CCSC2)n(n1)-c1ccccc1F |r| |
Structure |
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