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TargetDipeptidyl peptidase VIII
LigandBDBM12654
Substrate/CompetitorBDBM11057
Meas. Tech.DPP Inhibition Assay
pH7.5±n/a
Temperature295.15±n/a K
Ki 560±n/a nM
CommentsResult is from racemic analogues.
Citation Pei ZLi Xvon Geldern TWMadar DJLongenecker KYong HLubben THStewart KDZinker BABackes BJJudd ASMulhern MBallaron SJStashko MAMika AKBeno DWReinhart GAFryer RMPreusser LCKempf-Grote AJSham HLTrevillyan JM Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. J Med Chem 49:6439-42 (2006) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Dipeptidyl peptidase VIII
Name:Dipeptidyl peptidase VIII
Synonyms:DPP8 | DPRP-1 | Dipeptidyl peptidase 8 (DPP-8) | Dipeptidyl peptidase 8 (DPP8) | Dipeptidyl peptidase IV-related protein 1 | 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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  Blast E-value cutoff:
BDBM12654
BDBM11057
NameBDBM12654
Synonyms:(1S,6R)-3-(3-carbamoylphenoxymethyl)-6-(2,4,5-trifluorophenyl)cyclohex-3-en-1-aminium; 2,2,2-trifluoroacetate | 3-{[trans-5-Amino-4-(2,4,5-trifluorophenyl)cyclohex-1-en-1-yl]methoxy}benzamide | ABT-341 analogue 17
TypeSmall organic molecule
Emp. Form.C20H20F3N2O2
Mol. Mass.377.3797
SMILESNC(=O)c1cccc(OCC2=CC[C@@H]([C@@H]([NH3+])C2)c2cc(F)c(F)cc2F)c1 |r,t:10|
Structure
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