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Target
Dipeptidyl peptidase 8
Ligand
BDBM11198
Substrate
BDBM11561
Meas. Tech.
Dipeptidyl Peptidase Inhibition Assay
IC50
>100000±n/a nM
Citation
 Edmondson, SD; Mastracchio, A; Duffy, JL; Eiermann, GJ; He, H; Ita, I; Leiting, B; Leone, JF; Lyons, KA; Makarewicz, AM; Patel, RA; Petrov, A; Wu, JK; Thornberry, NA; Weber, AE Discovery of potent and selective orally bioavailable beta-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors. Bioorg Med Chem Lett 15:3048-52 (2005) [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:
BDBM11198
Synonyms:
(1S,2S)-1-[4-(4-fluorophenyl)phenyl]-3-[(3S)-3-fluoropyrrolidin-1-yl]-3-oxo-1-(1H-1,2,3,4-tetrazol-5-yl)propan-2-aminium; 2,2,2-trifluoroacetate | beta-substituted phenylalanine deriv. 23
Type:
Small organic molecule
Emp. Form.:
C20H21F2N6O
Mol. Mass.:
399.4166
SMILES:
[NH3+][C@@H]([C@@H](c1nnn[nH]1)c1ccc(cc1)-c1ccc(F)cc1)C(=O)N1CC[C@H](F)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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