| Reaction Details |
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 | Report a problem with these data |
| Target | Serine protease hepsin |
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| Ligand | BDBM14142 |
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| Substrate/Competitor | BDBM13573 |
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| Meas. Tech. | Enzyme Assay and Determination of the Inhibition Constants |
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| Ki | 85±n/a nM |
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| Citation |  Katz, BA; Luong, C; Ho, JD; Somoza, JR; Gjerstad, E; Tang, J; Williams, SR; Verner, E; Mackman, RL; Young, WB; Sprengeler, PA; Chan, H; Mortara, K; Janc, JW; McGrath, ME Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA). J Mol Biol344:527-47 (2004) [PubMed] Article |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| Serine protease hepsin |
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| Name: | Serine protease hepsin |
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| Synonyms: | HEPS_HUMAN | HPN | Hepsin | Serine protease hepsin | TMPRSS1 | Transmembrane protease serine 11E | Transmembrane protease, serine 1 |
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| Type: | Enzyme |
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| Mol. Mass.: | 45016.98 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Human deglycosylated hepsin was expressed in Pichia pastoris. |
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| Residue: | 417 |
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| Sequence: | MAQKEGGRTVPCCSRPKVAALTAGTLLLLTAIGAASWAIVAVLLRSDQEPLYPVQVSSAD
ARLMVFDKTEGTWRLLCSSRSNARVAGLSCEEMGFLRALTHSELDVRTAGANGTSGFFCV
DEGRLPHTQRLLEVISVCDCPRGRFLAAICQDCGRRKLPVDRIVGGRDTSLGRWPWQVSL
RYDGAHLCGGSLLSGDWVLTAAHCFPERNRVLSRWRVFAGAVAQASPHGLQLGVQAVVYH
GGYLPFRDPNSEENSNDIALVHLSSPLPLTEYIQPVCLPAAGQALVDGKICTVTGWGNTQ
YYGQQAGVLQEARVPIISNDVCNGADFYGNQIKPKMFCAGYPEGGIDACQGDSGGPFVCE
DSISRTPRWRLCGIVSWGTGCALAQKPGVYTKVSDFREWIFQAIKTHSEASGMVTQL
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| BDBM14142 |
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| BDBM13573 |
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| Name | BDBM14142 |
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| Synonyms: | 2-{5-[amino(iminiumyl)methyl]-1H-indol-2-yl}-6-phenylbenzen-1-olate | 3-{5-[AMINO(IMINIO)METHYL]-1H-INDOL-2-YL}-1,1-BIPHENYL-2-OLATE) | APC-8696 | CA-04 | CRA-8696 |
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| Type | Small organic molecule |
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| Emp. Form. | C21H17N3O |
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| Mol. Mass. | 327.3792 |
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| SMILES | NC(=[NH2+])c1ccc2[nH]c(cc2c1)-c1cccc(-c2ccccc2)c1[O-] |
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| Structure | 
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