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TargetDipeptidyl peptidase 4
LigandBDBM11529
Substrate/CompetitorBDBM11526
Meas. Tech.In Vitro DPP-IV Inhibition Assays
pH7.4±n/a
Temperature295.15±n/a K
Ki 3.9±0.6 nM
Citation Augeri, DJRobl, JABetebenner, DAMagnin, DRKhanna, ARobertson, JGWang, ASimpkins, LMTaunk, PHuang, QHan, SPAbboa-Offei, BCap, MXin, LTao, LTozzo, EWelzel, GEEgan, DMMarcinkeviciene, JChang, SYBiller, SAKirby, MSParker, RAHamann, LG Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. J Med Chem48:5025-37 (2005) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  Assay Method
 
Dipeptidyl peptidase 4
Name:Dipeptidyl peptidase 4
Synonyms:ADABP | ADCP2 | Adenosine deaminase complexing protein 2 | CD26 | CD_antigen=CD26 | DPP IV | DPP4 | DPPIV | Dipeptidyl peptidase 4 (DDP-IV) | Dipeptidyl peptidase 4 (DPP IV) | Dipeptidyl peptidase 4 (DPP-4) | Dipeptidyl peptidase 4 (DPP4) | Dipeptidyl peptidase 4 (DPPIV) | Dipeptidyl peptidase 4 membrane form | Dipeptidyl peptidase 4 soluble form | Dipeptidyl peptidase IV | Dipeptidyl peptidase IV (DDP-4) | Dipeptidyl peptidase IV (DDP-IV) | Dipeptidyl peptidase IV (DPP IV) | Dipeptidyl peptidase IV membrane form | Dipeptidyl peptidase IV soluble form | Dipeptidyl peptidase-IV (DPP-4) | Dipeptidyl peptidase-IV (DPP-IV) | T-cell activation antigen CD26 | TP103
Type:Enzyme
Mol. Mass.:88271.01
Organism:Homo sapiens (Human)
Description:P27487
Residue:766
Sequence:
MKTPWKVLLGLLGAAALVTIITVPVVLLNKGTDDATADSRKTYTLTDYLKNTYRLKLYSL
RWISDHEYLYKQENNILVFNAEYGNSSVFLENSTFDEFGHSINDYSISPDGQFILLEYNY
VKQWRHSYTASYDIYDLNKRQLITEERIPNNTQWVTWSPVGHKLAYVWNNDIYVKIEPNL
PSYRITWTGKEDIIYNGITDWVYEEEVFSAYSALWWSPNGTFLAYAQFNDTEVPLIEYSF
YSDESLQYPKTVRVPYPKAGAVNPTVKFFVVNTDSLSSVTNATSIQITAPASMLIGDHYL
CDVTWATQERISLQWLRRIQNYSVMDICDYDESSGRWNCLVARQHIEMSTTGWVGRFRPS
EPHFTLDGNSFYKIISNEEGYRHICYFQIDKKDCTFITKGTWEVIGIEALTSDYLYYISN
EYKGMPGGRNLYKIQLSDYTKVTCLSCELNPERCQYYSVSFSKEAKYYQLRCSGPGLPLY
TLHSSVNDKGLRVLEDNSALDKMLQNVQMPSKKLDFIILNETKFWYQMILPPHFDKSKKY
PLLLDVYAGPCSQKADTVFRLNWATYLASTENIIVASFDGRGSGYQGDKIMHAINRRLGT
FEVEDQIEAARQFSKMGFVDNKRIAIWGWSYGGYVTSMVLGSGSGVFKCGIAVAPVSRWE
YYDSVYTERYMGLPTPEDNLDHYRNSTVMSRAENFKQVEYLLIHGTADDNVHFQQSAQIS
KALVDVGVDFQAMWYTDEDHGIASSTAHQHIYTHMSHFIKQCFSLP
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BDBM11529
NameBDBM11529
Synonyms:(1S,3S,5S)-2-[(2S)-2-amino-2-(1-ethenylcyclopentyl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile; 2,2,2-trifluoroacetic acid | (S)-2-(1-Ethenylcyclopent-1-yl)glycine-L-cis-4,5-methanoprolinenitrile | BMS-477118 analogue | Saxagliptin Analogue 8d
TypeSmall organic molecule
Emp. Form.C15H21N3O
Mol. Mass.259.3467
SMILESN[C@H](C(=O)N1[C@H]2C[C@H]2C[C@H]1C#N)C1(CCCC1)C=C |r|
Structure
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BDBM11526
NameBDBM11526
Synonyms:1-(2-aminoacetyl)-N-(4-nitrophenyl)pyrrolidine-2-carboxamide | Gly-Pro-p-nitroaniline | Gly-Pro-pNA
TypeSmall organic molecule
Emp. Form.C13H16N4O4
Mol. Mass.292.2905
SMILESNCC(=O)N1CCCC1C(=O)Nc1ccc(cc1)[N+]([O-])=O
Structure
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