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Target
Dipeptidyl peptidase 8
Ligand
BDBM11186
Substrate
BDBM11561
Meas. Tech.
Dipeptidyl Peptidase Inhibition Assay
IC50
>100000±n/a nM
Citation
 Xu, J; Wei, L; Mathvink, R; Edmondson, SD; Mastracchio, A; Eiermann, GJ; He, H; Leone, JF; Leiting, B; Lyons, KA; Marsilio, F; Patel, RA; Petrov, A; Wu, JK; Thornberry, NA; Weber, AE Discovery of potent, selective, and orally bioavailable pyridone-based dipeptidyl peptidase-4 inhibitors. Bioorg Med Chem Lett 16:1346-9 (2006) [PubMed]  Article 
Target
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:
MWKRSEQMKIKSGKCNMAAAMETEQLGVEIFETADCEENIESQDRPKLEPFYVERYSWSQLKKLLADTRKYHGYMMAKAPHDFMFVKRNDPDGPHSDRIYYLAMSGENRENTLFYSEIPKTINRAAVLMLSWKPLLDLFQATLDYGMYSREEELLRERKRIGTVGIASYDYHQGSGTFLFQAGSGIYHVKDGGPQGFTQQPLRPNLVETSCPNIRMDPKLCPADPDWIAFIHSNDIWISNIVTREERRLTYVHNELANMEEDARSAGVATFVLQEEFDRYSGYWWCPKAETTPSGGKILRILYEENDESEVEIIHVTSPMLETRRADSFRYPKTGTANPKVTFKMSEIMIDAEGRIIDVIDKELIQPFEILFEGVEYIARAGWTPEGKYAWSILLDRSQTRLQIVLISPELFIPVEDDVMERQRLIESVPDSVTPLIIYEETTDIWINIHDIFHVFPQSHEEEIEFIFASECKTGFRHLYKITSILKESKYKRSSGGLPAPSDFKCPIKEEIAITSGEWEVLGRHGSNIQVDEVRRLVYFEGTKDSPLEHHLYVVSYVNPGEVTRLTDRGYSHSCCISQHCDFFISKYSNQKNPHCVSLYKLSSPEDDPTCKTKEFWATILDSAGPLPDYTPPEIFSFESTTGFTLYGMLYKPHDLQPGKKYPTVLFIYGGPQVQLVNNRFKGVKYFRLNTLASLGYVVVVIDNRGSCHRGLKFEGAFKYKMGQIEIDDQVEGLQYLASRYDFIDLDRVGIHGWSYGGYLSLMALMQRSDIFRVAIAGAPVTLWIFYDTGYTERYMGHPDQNEQGYYLGSVAMQAEKFPSEPNRLLLLHGFLDENVHFAHTSILLSFLVRAGKPYDLQIYPQERHSIRVPESGEHYELHLLHYLQENLGSRIAALKVI
  
Inhibitor
Name:
BDBM11186
Synonyms:
(2S,3S)-1-(3-fluoroazetidin-1-yl)-3-[4-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)phenyl]-1-oxobutan-2-aminium; 2,2,2-trifluoroacetate | pyridone-based inhibitor 29
Type:
Small organic molecule
Emp. Form.:
C19H23FN3O2
Mol. Mass.:
344.4027
SMILES:
C[C@H]([C@H]([NH3+])C(=O)N1CC(F)C1)c1ccc(cc1)-c1ccc(=O)n(C)c1 |r|
Structure:
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Substrate
Name:
BDBM11561
Synonyms:
1-(2-aminopropanoyl)-N-[2-oxo-4-(trifluoromethyl)-2H-chromen-7-yl]pyrrolidine-2-carboxamide | Ala-Pro-7-amido-4-trifluoromethylcoumarin
Type:
Small organic molecule
Emp. Form.:
C18H18F3N3O4
Mol. Mass.:
397.3484
SMILES:
CC(N)C(=O)N1CCCC1C(=O)Nc1ccc2c(cc(=O)oc2c1)C(F)(F)F
Structure:
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