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Target
Dipeptidyl peptidase 4
Ligand
BDBM50232504
Substrate
n/a
Meas. Tech.
ChEMBL_461024 (CHEMBL944056)
IC50
11.0±n/a nM
Citation
Kim, D; Kowalchick, JE; Brockunier, LL; Parmee, ER; Eiermann, GJ; Fisher, MH; He, H; Leiting, B; Lyons, K; Scapin, G; Patel, SB; Petrov, A; Pryor, KD; Roy, RS; Wu, JK; Zhang, X; Wyvratt, MJ; Zhang, BB; Zhu, L; Thornberry, NA; Weber, AE Discovery of potent and selective dipeptidyl peptidase IV inhibitors derived from beta-aminoamides bearing subsituted triazolopiperazines. J Med Chem 51:589-602 (2008) [PubMed] Article
More Info.:
Target
Name:
Dipeptidyl peptidase 4
Synonyms:
ADABP | ADCP2 | Adenosine deaminase complexing protein 2 | CD26 | CD_antigen=CD26 | DPP IV | DPP4 | DPP4_HUMAN | 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:
Human
Description:
P27487
Residue:
766
Sequence:
MKTPWKVLLGLLGAAALVTIITVPVVLLNKGTDDATADSRKTYTLTDYLKNTYRLKLYSLRWISDHEYLYKQENNILVFNAEYGNSSVFLENSTFDEFGHSINDYSISPDGQFILLEYNYVKQWRHSYTASYDIYDLNKRQLITEERIPNNTQWVTWSPVGHKLAYVWNNDIYVKIEPNLPSYRITWTGKEDIIYNGITDWVYEEEVFSAYSALWWSPNGTFLAYAQFNDTEVPLIEYSFYSDESLQYPKTVRVPYPKAGAVNPTVKFFVVNTDSLSSVTNATSIQITAPASMLIGDHYLCDVTWATQERISLQWLRRIQNYSVMDICDYDESSGRWNCLVARQHIEMSTTGWVGRFRPSEPHFTLDGNSFYKIISNEEGYRHICYFQIDKKDCTFITKGTWEVIGIEALTSDYLYYISNEYKGMPGGRNLYKIQLSDYTKVTCLSCELNPERCQYYSVSFSKEAKYYQLRCSGPGLPLYTLHSSVNDKGLRVLEDNSALDKMLQNVQMPSKKLDFIILNETKFWYQMILPPHFDKSKKYPLLLDVYAGPCSQKADTVFRLNWATYLASTENIIVASFDGRGSGYQGDKIMHAINRRLGTFEVEDQIEAARQFSKMGFVDNKRIAIWGWSYGGYVTSMVLGSGSGVFKCGIAVAPVSRWEYYDSVYTERYMGLPTPEDNLDHYRNSTVMSRAENFKQVEYLLIHGTADDNVHFQQSAQISKALVDVGVDFQAMWYTDEDHGIASSTAHQHIYTHMSHFIKQCFSLP
Inhibitor
Name:
BDBM50232504
Synonyms:
(2R)-4-[5,8-dimethyl-3-(trifluoromethyl)-5,6-dihydro[[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine hydrochloride | CHEMBL536089
Type:
Small organic molecule
Emp. Form.:
C18H19F6N5O
Mol. Mass.:
435.3668
SMILES:
CC1CN(C(C)c2nnc(n12)C(F)(F)F)C(=O)C[C@H](N)Cc1cc(F)c(F)cc1F |w:1.0,4.4|