Reaction Details |
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Target | Dipeptidyl peptidase 4 |
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Ligand | BDBM50391573 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_850195 (CHEMBL2149801) |
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IC50 | 2.3±n/a nM |
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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 Chem20:5705-19 (2012) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Dipeptidyl peptidase 4 |
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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: | MKTPWKVLLGLLGVAALVTIITVPVVLLNKDEAAADSRRTYTLADYLKNTFRVKSYSLRW
VSDSEYLYKQENNILLFNAEHGNSSIFLENSTFEIFGDSISDYSVSPDRLFVLLEYNYVK
QWRHSYTASYSIYDLNKRQLITEEKIPNNTQWITWSQEGHKLAYVWKNDIYVKIEPHLPS
HRITSTGKENVIFNGINDWVYEEEIFGAYSALWWSPNGTFLAYAQFNDTGVPLIEYSFYS
DESLQYPKTVWIPYPKAGAVNPTVKFFIVNTDSLSSTTTTIPMQITAPASVTTGDHYLCD
VAWVSEDRISLQWLRRIQNYSVMAICDYDKTTLVWNCPTTQEHIETSATGWCGRFRPAEP
HFTSDGSSFYKIVSDKDGYKHICQFQKDRKPEQVCTFITKGAWEVISIEALTSDYLYYIS
NEYKEMPGGRNLYKIQLTDHTNKKCLSCDLNPERCQYYSVSLSKEAKYYQLGCRGPGLPL
YTLHRSTDQKELRVLEDNSALDKMLQDVQMPSKKLDFIVLNETRFWYQMILPPHFDKSKK
YPLLIDVYAGPCSQKADAAFRLNWATYLASTENIIVASFDGRGSGYQGDKIMHAINKRLG
TLEVEDQIEAARQFLKMGFVDSKRVAIWGWSYGGYVTSMVLGSGSGVFKCGIAVAPVSRW
EYYDSVYTERYMGLPTPEDNLDHYRNSTVMSRAENFKQVEYLLIHGTADDNVHFQQSAQI
SKALVDAGVDFQAMWYTDEDHGIASSTAHQHIYSHMSHFLQQCFSLR
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BDBM50391573 |
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n/a |
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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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