Reaction Details |
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Target | Enteropeptidase |
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Ligand | BDBM50595346 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2216353 (CHEMBL5129485) |
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IC50 | 7.4±n/a nM |
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Citation | Ikeda, Z; Kakegawa, K; Kikuchi, F; Itono, S; Oki, H; Yashiro, H; Hiyoshi, H; Tsuchimori, K; Hamagami, K; Watanabe, M; Sasaki, M; Ishihara, Y; Tohyama, K; Kitazaki, T; Maekawa, T; Sasaki, M Design, Synthesis, and Biological Evaluation of a Novel Series of 4-Guanidinobenzoate Derivatives as Enteropeptidase Inhibitors with Low Systemic Exposure for the Treatment of Obesity. J Med Chem65:8456-8477 (2022) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Enteropeptidase |
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Name: | Enteropeptidase |
Synonyms: | ENTK | ENTK_HUMAN | PRSS7 | TMPRSS15 |
Type: | Enzyme |
Mol. Mass.: | 112901.62 |
Organism: | Homo sapiens (Human) |
Description: | P98073 |
Residue: | 1019 |
Sequence: | MGSKRGISSRHHSLSSYEIMFAALFAILVVLCAGLIAVSCLTIKESQRGAALGQSHEARA
TFKITSGVTYNPNLQDKLSVDFKVLAFDLQQMIDEIFLSSNLKNEYKNSRVLQFENGSII
VVFDLFFAQWVSDENVKEELIQGLEANKSSQLVTFHIDLNSVDILDKLTTTSHLATPGNV
SIECLPGSSPCTDALTCIKADLFCDGEVNCPDGSDEDNKMCATVCDGRFLLTGSSGSFQA
THYPKPSETSVVCQWIIRVNQGLSIKLSFDDFNTYYTDILDIYEGVGSSKILRASIWETN
PGTIRIFSNQVTATFLIESDESDYVGFNATYTAFNSSELNNYEKINCNFEDGFCFWVQDL
NDDNEWERIQGSTFSPFTGPNFDHTFGNASGFYISTPTGPGGRQERVGLLSLPLDPTLEP
ACLSFWYHMYGENVHKLSINISNDQNMEKTVFQKEGNYGDNWNYGQVTLNETVKFKVAFN
AFKNKILSDIALDDISLTYGICNGSLYPEPTLVPTPPPELPTDCGGPFELWEPNTTFSST
NFPNSYPNLAFCVWILNAQKGKNIQLHFQEFDLENINDVVEIRDGEEADSLLLAVYTGPG
PVKDVFSTTNRMTVLLITNDVLARGGFKANFTTGYHLGIPEPCKADHFQCKNGECVPLVN
LCDGHLHCEDGSDEADCVRFFNGTTNNNGLVRFRIQSIWHTACAENWTTQISNDVCQLLG
LGSGNSSKPIFPTDGGPFVKLNTAPDGHLILTPSQQCLQDSLIRLQCNHKSCGKKLAAQD
ITPKIVGGSNAKEGAWPWVVGLYYGGRLLCGASLVSSDWLVSAAHCVYGRNLEPSKWTAI
LGLHMKSNLTSPQTVPRLIDEIVINPHYNRRRKDNDIAMMHLEFKVNYTDYIQPICLPEE
NQVFPPGRNCSIAGWGTVVYQGTTANILQEADVPLLSNERCQQQMPEYNITENMICAGYE
EGGIDSCQGDSGGPLMCQENNRWFLAGVTSFGYKCALPNRPGVYARVSRFTEWIQSFLH
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BDBM50595346 |
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n/a |
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Name | BDBM50595346 |
Synonyms: | CHEMBL5189108 |
Type | Small organic molecule |
Emp. Form. | C20H19FN4O7 |
Mol. Mass. | 446.3859 |
SMILES | NC(=N)Nc1ccc(C(=O)Oc2ccc(CC(=O)N[C@@H](CC(O)=O)C(O)=O)cc2)c(F)c1 |r| |
Structure |
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