Target
Dipeptidyl peptidase 8
Ligand
BDBM15554
Substrate
BDBM11561
Meas. Tech.
Dipeptidyl Peptidase Inhibition Assay
IC50
5300±n/a nM
Citation
 Liang, GBQian, XFeng, DBiftu, TEiermann, GHe, HLeiting, BLyons, KPetrov, ASinha-Roy, RZhang, BWu, JZhang, XThornberry, NAWeber, AE Optimization of 1,4-diazepan-2-one containing dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes. Bioorg Med Chem Lett 17:1903-7 (2007) [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:
BDBM15554
Synonyms:
(3R,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-[(2-fluorophenyl)methyl]-7-methyl-1,4-diazepan-2-one | 7-methyl diazepanone 15e
Type:
Small organic molecule
Emp. Form.:
C23H25F4N3O2
Mol. Mass.:
451.4571
SMILES:
C[C@@H]1CCN([C@H](Cc2ccccc2F)C(=O)N1)C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F |r|
Structure:
Search PDB for entries with ligand similarity:
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:
Search PDB for entries with ligand similarity: