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Target
Dipeptidyl peptidase 8
Ligand
BDBM50323174
Substrate
n/a
Meas. Tech.
ChEMBL_643843 (CHEMBL1211742)
Ki
6800±n/a nM
Citation
 Brigance, RP; Meng, W; Fura, A; Harrity, T; Wang, A; Zahler, R; Kirby, MS; Hamann, LG Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes. Bioorg Med Chem Lett 20:4395-8 (2010) [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:
BDBM50323174
Synonyms:
(2-(2-chlorophenyl)-7-(2,4-dichlorophenyl)-5-methylpyrazolo[1,5-a]pyrimidin-6-yl)methanamine | CHEMBL1209541
Type:
Small organic molecule
Emp. Form.:
C20H15Cl3N4
Mol. Mass.:
417.719
SMILES:
Cc1nc2cc(nn2c(c1CN)-c1ccc(Cl)cc1Cl)-c1ccccc1Cl |(16.35,-8.79,;15.02,-9.57,;13.69,-8.8,;12.35,-9.57,;10.88,-9.11,;9.98,-10.36,;10.9,-11.6,;12.36,-11.12,;13.69,-11.88,;15.03,-11.1,;16.36,-11.87,;17.69,-11.1,;13.7,-13.41,;12.37,-14.18,;12.37,-15.72,;13.71,-16.5,;13.71,-18.03,;15.04,-15.72,;15.04,-14.17,;16.37,-13.4,;8.44,-10.37,;7.67,-9.04,;6.13,-9.05,;5.37,-10.39,;6.15,-11.72,;7.69,-11.71,;8.47,-13.03,)|
Structure:
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