Reaction Details |
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Target | Dipeptidyl peptidase 8 |
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Ligand | BDBM11701 |
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Substrate/Competitor | BDBM11526 |
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Meas. Tech. | Dipeptidyl Peptidase Inhibition Assay |
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IC50 | 202±n/a nM |
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Citation | Tsu, H; Chen, X; Chen, CT; Lee, SJ; Chang, CN; Kao, KH; Coumar, MS; Yeh, YT; Chien, CH; Wang, HS; Lin, KT; Chang, YY; Wu, SH; Chen, YS; Lu, IL; Wu, SY; Tsai, TY; Chen, WC; Hsieh, HP; Chao, YS; Jiaang, WT 2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]-1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV. J Med Chem49:373-80 (2006) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Dipeptidyl peptidase 8 |
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Name: | Dipeptidyl peptidase 8 |
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 |
Type: | Enzyme |
Mol. Mass.: | 103342.62 |
Organism: | Homo sapiens (Human) |
Description: | Q6V1X1 |
Residue: | 898 |
Sequence: | MWKRSEQMKIKSGKCNMAAAMETEQLGVEIFETADCEENIESQDRPKLEPFYVERYSWSQ
LKKLLADTRKYHGYMMAKAPHDFMFVKRNDPDGPHSDRIYYLAMSGENRENTLFYSEIPK
TINRAAVLMLSWKPLLDLFQATLDYGMYSREEELLRERKRIGTVGIASYDYHQGSGTFLF
QAGSGIYHVKDGGPQGFTQQPLRPNLVETSCPNIRMDPKLCPADPDWIAFIHSNDIWISN
IVTREERRLTYVHNELANMEEDARSAGVATFVLQEEFDRYSGYWWCPKAETTPSGGKILR
ILYEENDESEVEIIHVTSPMLETRRADSFRYPKTGTANPKVTFKMSEIMIDAEGRIIDVI
DKELIQPFEILFEGVEYIARAGWTPEGKYAWSILLDRSQTRLQIVLISPELFIPVEDDVM
ERQRLIESVPDSVTPLIIYEETTDIWINIHDIFHVFPQSHEEEIEFIFASECKTGFRHLY
KITSILKESKYKRSSGGLPAPSDFKCPIKEEIAITSGEWEVLGRHGSNIQVDEVRRLVYF
EGTKDSPLEHHLYVVSYVNPGEVTRLTDRGYSHSCCISQHCDFFISKYSNQKNPHCVSLY
KLSSPEDDPTCKTKEFWATILDSAGPLPDYTPPEIFSFESTTGFTLYGMLYKPHDLQPGK
KYPTVLFIYGGPQVQLVNNRFKGVKYFRLNTLASLGYVVVVIDNRGSCHRGLKFEGAFKY
KMGQIEIDDQVEGLQYLASRYDFIDLDRVGIHGWSYGGYLSLMALMQRSDIFRVAIAGAP
VTLWIFYDTGYTERYMGHPDQNEQGYYLGSVAMQAEKFPSEPNRLLLLHGFLDENVHFAH
TSILLSFLVRAGKPYDLQIYPQERHSIRVPESGEHYELHLLHYLQENLGSRIAALKVI
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BDBM11701 |
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BDBM11526 |
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Name | BDBM11701 |
Synonyms: | (2S)-1-{2-[(3-{4-[(3,5-difluorophenyl)carbonyl]piperazin-1-yl}-3-oxopropyl)amino]acetyl}pyrrolidine-2-carbonitrile | (2S)-Cyanopyrrolidine analogue 18e | 1-[3-[2-[2-Cyano-(S)-pyrrolidin-1-yl]-2-oxoethylamino]-1-oxo-propyl]-4-[3,5-difluorobenzoyl]piperazine |
Type | Small organic molecule |
Emp. Form. | C21H25F2N5O3 |
Mol. Mass. | 433.4517 |
SMILES | Fc1cc(F)cc(c1)C(=O)N1CCN(CC1)C(=O)CCNCC(=O)N1CCC[C@H]1C#N |r| |
Structure |
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