Reaction Details |
| Report a problem with these data |
Target | Dipeptidyl peptidase 4 |
---|
Ligand | BDBM11150 |
---|
Substrate/Competitor | BDBM11057 |
---|
Meas. Tech. | Dipeptidyl Peptidase Inhibition Assay |
---|
pH | 7.5±n/a |
---|
Temperature | 310.15±n/a K |
---|
IC50 | 150±n/a nM |
---|
Citation | Edmondson, SD; Mastracchio, A; Mathvink, RJ; He, J; Harper, B; Park, YJ; Beconi, M; Di Salvo, J; Eiermann, GJ; He, H; Leiting, B; Leone, JF; Levorse, DA; Lyons, K; Patel, RA; Patel, SB; Petrov, A; Scapin, G; Shang, J; Roy, RS; Smith, A; Wu, JK; Xu, S; Zhu, B; Thornberry, NA; Weber, AE (2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]-pyridin-6-ylphenyl)butanamide: a selective alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. J Med Chem49:3614-27 (2006) [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 | 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: | Homo sapiens (Human) |
Description: | P27487 |
Residue: | 766 |
Sequence: | MKTPWKVLLGLLGAAALVTIITVPVVLLNKGTDDATADSRKTYTLTDYLKNTYRLKLYSL
RWISDHEYLYKQENNILVFNAEYGNSSVFLENSTFDEFGHSINDYSISPDGQFILLEYNY
VKQWRHSYTASYDIYDLNKRQLITEERIPNNTQWVTWSPVGHKLAYVWNNDIYVKIEPNL
PSYRITWTGKEDIIYNGITDWVYEEEVFSAYSALWWSPNGTFLAYAQFNDTEVPLIEYSF
YSDESLQYPKTVRVPYPKAGAVNPTVKFFVVNTDSLSSVTNATSIQITAPASMLIGDHYL
CDVTWATQERISLQWLRRIQNYSVMDICDYDESSGRWNCLVARQHIEMSTTGWVGRFRPS
EPHFTLDGNSFYKIISNEEGYRHICYFQIDKKDCTFITKGTWEVIGIEALTSDYLYYISN
EYKGMPGGRNLYKIQLSDYTKVTCLSCELNPERCQYYSVSFSKEAKYYQLRCSGPGLPLY
TLHSSVNDKGLRVLEDNSALDKMLQNVQMPSKKLDFIILNETKFWYQMILPPHFDKSKKY
PLLLDVYAGPCSQKADTVFRLNWATYLASTENIIVASFDGRGSGYQGDKIMHAINRRLGT
FEVEDQIEAARQFSKMGFVDNKRIAIWGWSYGGYVTSMVLGSGSGVFKCGIAVAPVSRWE
YYDSVYTERYMGLPTPEDNLDHYRNSTVMSRAENFKQVEYLLIHGTADDNVHFQQSAQIS
KALVDVGVDFQAMWYTDEDHGIASSTAHQHIYTHMSHFIKQCFSLP
|
|
|
BDBM11150 |
---|
BDBM11057 |
---|
Name | BDBM11150 |
Synonyms: | (1S,2S)-1-(dimethylcarbamoyl)-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-(4-{8-methyl-[1,2,4]triazolo[1,5-a]pyridin-6-yl}phenyl)-3-oxopropan-2-aminium; 2,2,2-trifluoroacetate | (2S,3S)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-[4-(8-methyl[1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]-1,4-dioxobutan-2-aminium trifluoroacetate | Biarylphenylalanine (S)-Fluoropyrrolidide Amide 29 |
Type | Small organic molecule |
Emp. Form. | C23H28FN6O2 |
Mol. Mass. | 439.5053 |
SMILES | CN(C)C(=O)[C@H]([C@H]([NH3+])C(=O)N1CC[C@H](F)C1)c1ccc(cc1)-c1cc(C)c2ncnn2c1 |r| |
Structure |
|