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Target
Dipeptidyl peptidase 4
Ligand
BDBM50391573
Substrate
n/a
Meas. Tech.
ChEMBL_850195 (CHEMBL2149801)
IC50
2.3±n/a nM
Citation
 Yoshida, T; Akahoshi, F; Sakashita, H; Kitajima, H; Nakamura, M; Sonda, S; Takeuchi, M; Tanaka, Y; Ueda, N; Sekiguchi, S; Ishige, T; Shima, K; Nabeno, M; Abe, Y; Anabuki, J; Soejima, A; Yoshida, K; Takashina, Y; Ishii, S; Kiuchi, S; Fukuda, S; Tsutsumiuchi, R; Kosaka, K; Murozono, T; Nakamaru, Y; Utsumi, H; Masutomi, N; Kishida, H; Miyaguchi, I; Hayashi, Y Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine): a highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. Bioorg Med Chem 20:5705-19 (2012) [PubMed]  Article 
Target
Name:
Dipeptidyl peptidase 4
Synonyms:
Bile canaliculus domain-specific membrane glycoprotein | CD_antigen=CD26 | Cd26 | DPP IV | DPP4_RAT | Dipeptidyl Peptidase IV (DPP-IV) | Dipeptidyl peptidase 4 | Dipeptidyl peptidase 4 (DDPIV) | Dipeptidyl peptidase 4 60 kDa soluble form | Dipeptidyl peptidase 4 membrane form | Dipeptidyl peptidase 4 soluble form | Dipeptidyl peptidase IV | Dipeptidyl peptidase IV 60 kDa soluble form | Dipeptidyl peptidase IV membrane form | Dipeptidyl peptidase IV soluble form | Dpp4 | GP110 glycoprotein | T-cell activation antigen CD26
Type:
Enzyme
Mol. Mass.:
88084.94
Organism:
Rattus norvegicus (rat)
Description:
n/a
Residue:
767
Sequence:
MKTPWKVLLGLLGVAALVTIITVPVVLLNKDEAAADSRRTYTLADYLKNTFRVKSYSLRWVSDSEYLYKQENNILLFNAEHGNSSIFLENSTFEIFGDSISDYSVSPDRLFVLLEYNYVKQWRHSYTASYSIYDLNKRQLITEEKIPNNTQWITWSQEGHKLAYVWKNDIYVKIEPHLPSHRITSTGKENVIFNGINDWVYEEEIFGAYSALWWSPNGTFLAYAQFNDTGVPLIEYSFYSDESLQYPKTVWIPYPKAGAVNPTVKFFIVNTDSLSSTTTTIPMQITAPASVTTGDHYLCDVAWVSEDRISLQWLRRIQNYSVMAICDYDKTTLVWNCPTTQEHIETSATGWCGRFRPAEPHFTSDGSSFYKIVSDKDGYKHICQFQKDRKPEQVCTFITKGAWEVISIEALTSDYLYYISNEYKEMPGGRNLYKIQLTDHTNKKCLSCDLNPERCQYYSVSLSKEAKYYQLGCRGPGLPLYTLHRSTDQKELRVLEDNSALDKMLQDVQMPSKKLDFIVLNETRFWYQMILPPHFDKSKKYPLLIDVYAGPCSQKADAAFRLNWATYLASTENIIVASFDGRGSGYQGDKIMHAINKRLGTLEVEDQIEAARQFLKMGFVDSKRVAIWGWSYGGYVTSMVLGSGSGVFKCGIAVAPVSRWEYYDSVYTERYMGLPTPEDNLDHYRNSTVMSRAENFKQVEYLLIHGTADDNVHFQQSAQISKALVDAGVDFQAMWYTDEDHGIASSTAHQHIYSHMSHFLQQCFSLR
  
Inhibitor
Name:
BDBM50391573
Synonyms:
CHEMBL2147711
Type:
Small organic molecule
Emp. Form.:
C22H29FN6OS
Mol. Mass.:
444.569
SMILES:
Cc1cc(N2CCN(CC2)[C@@H]2CN[C@@H](C2)C(=O)N2CCSC2)n(n1)-c1ccc(F)cc1 |r|
Structure:
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