Reaction Details |
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Target | Serine protease hepsin |
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Ligand | BDBM14482 |
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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 | 2100±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 |
Synonyms: | HEPS_HUMAN | HPN | Hepsin | Serine protease hepsin | TMPRSS1 | Transmembrane protease serine 11E | Transmembrane protease, serine 1 |
Type: | Enzyme |
Mol. Mass.: | 45016.98 |
Organism: | Homo sapiens (Human) |
Description: | Human deglycosylated hepsin was expressed in Pichia pastoris. |
Residue: | 417 |
Sequence: | MAQKEGGRTVPCCSRPKVAALTAGTLLLLTAIGAASWAIVAVLLRSDQEPLYPVQVSSAD
ARLMVFDKTEGTWRLLCSSRSNARVAGLSCEEMGFLRALTHSELDVRTAGANGTSGFFCV
DEGRLPHTQRLLEVISVCDCPRGRFLAAICQDCGRRKLPVDRIVGGRDTSLGRWPWQVSL
RYDGAHLCGGSLLSGDWVLTAAHCFPERNRVLSRWRVFAGAVAQASPHGLQLGVQAVVYH
GGYLPFRDPNSEENSNDIALVHLSSPLPLTEYIQPVCLPAAGQALVDGKICTVTGWGNTQ
YYGQQAGVLQEARVPIISNDVCNGADFYGNQIKPKMFCAGYPEGGIDACQGDSGGPFVCE
DSISRTPRWRLCGIVSWGTGCALAQKPGVYTKVSDFREWIFQAIKTHSEASGMVTQL
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BDBM14482 |
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BDBM13573 |
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Name | BDBM14482 |
Synonyms: | 2-amino-5-[(3-hydroxynaphthalene-2-)amido]-1H-1,3-benzodiazol-3-ium | CA-24 |
Type | Small organic molecule |
Emp. Form. | C18H15N4O2 |
Mol. Mass. | 319.3368 |
SMILES | Nc1[nH]c2ccc(NC(=O)c3cc4ccccc4cc3O)cc2[nH+]1 |
Structure |
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