| Reaction Details |
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 | Report a problem with these data |
| Target | Dipeptidyl peptidase 8 |
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| Ligand | BDBM50206058 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_850198 (CHEMBL2149804) |
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| IC50 | 40±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 8 |
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| Name: | Dipeptidyl peptidase 8 |
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| Synonyms: | DPP8 | DPP8_HUMAN | DPRP-1 | DPRP1 | Dipeptidyl peptidase 8 (DPP-8) | Dipeptidyl peptidase 8 (DPP8) | Dipeptidyl peptidase 8/9 | Dipeptidyl peptidase IV-related protein 1 | Dipeptidyl peptidase VIII | Dipeptidyl peptidase VIII (DDP-VIII) | Prolyl dipeptidase DPP8 |
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| Type: | Enzyme |
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| Mol. Mass.: | 103342.62 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q6V1X1 |
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| Residue: | 898 |
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| Sequence: | MWKRSEQMKIKSGKCNMAAAMETEQLGVEIFETADCEENIESQDRPKLEPFYVERYSWSQ
LKKLLADTRKYHGYMMAKAPHDFMFVKRNDPDGPHSDRIYYLAMSGENRENTLFYSEIPK
TINRAAVLMLSWKPLLDLFQATLDYGMYSREEELLRERKRIGTVGIASYDYHQGSGTFLF
QAGSGIYHVKDGGPQGFTQQPLRPNLVETSCPNIRMDPKLCPADPDWIAFIHSNDIWISN
IVTREERRLTYVHNELANMEEDARSAGVATFVLQEEFDRYSGYWWCPKAETTPSGGKILR
ILYEENDESEVEIIHVTSPMLETRRADSFRYPKTGTANPKVTFKMSEIMIDAEGRIIDVI
DKELIQPFEILFEGVEYIARAGWTPEGKYAWSILLDRSQTRLQIVLISPELFIPVEDDVM
ERQRLIESVPDSVTPLIIYEETTDIWINIHDIFHVFPQSHEEEIEFIFASECKTGFRHLY
KITSILKESKYKRSSGGLPAPSDFKCPIKEEIAITSGEWEVLGRHGSNIQVDEVRRLVYF
EGTKDSPLEHHLYVVSYVNPGEVTRLTDRGYSHSCCISQHCDFFISKYSNQKNPHCVSLY
KLSSPEDDPTCKTKEFWATILDSAGPLPDYTPPEIFSFESTTGFTLYGMLYKPHDLQPGK
KYPTVLFIYGGPQVQLVNNRFKGVKYFRLNTLASLGYVVVVIDNRGSCHRGLKFEGAFKY
KMGQIEIDDQVEGLQYLASRYDFIDLDRVGIHGWSYGGYLSLMALMQRSDIFRVAIAGAP
VTLWIFYDTGYTERYMGHPDQNEQGYYLGSVAMQAEKFPSEPNRLLLLHGFLDENVHFAH
TSILLSFLVRAGKPYDLQIYPQERHSIRVPESGEHYELHLLHYLQENLGSRIAALKVI
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| BDBM50206058 |
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| n/a |
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| Name | BDBM50206058 |
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| Synonyms: | 6-(4-((3S,5S)-5-(thiazolidine-3-carbonyl)pyrrolidin-3-yl)piperazin-1-yl)nicotinonitrile | CHEMBL241253 |
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| Type | Small organic molecule |
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| Emp. Form. | C18H24N6OS |
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| Mol. Mass. | 372.488 |
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| SMILES | O=C([C@@H]1C[C@@H](CN1)N1CCN(CC1)c1ccc(cn1)C#N)N1CCSC1 |
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| Structure | 
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