Reaction Details |
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Target | Serine protease hepsin |
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Ligand | BDBM50580342 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2148121 (CHEMBL5032467) |
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IC50 | 5.8±n/a nM |
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Citation | Damalanka, VC; Voss, JJLP; Mahoney, MW; Primeau, T; Li, S; Klampfer, L; Janetka, JW Macrocyclic Inhibitors of HGF-Activating Serine Proteases Overcome Resistance to Receptor Tyrosine Kinase Inhibitors and Block Lung Cancer Progression. J Med Chem64:18158-18174 (2021) [PubMed] Article |
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More Info.: | Get all data from this article, 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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BDBM50580342 |
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n/a |
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Name | BDBM50580342 |
Synonyms: | CHEMBL5088958 |
Type | Small organic molecule |
Emp. Form. | C29H41N9O7S |
Mol. Mass. | 659.757 |
SMILES | C[C@@H](O)[C@@H]1NC(=O)[C@H](CC(=O)NCCCC[C@H](NC1=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)c1nc2ccccc2s1)NC(C)=O |r| |
Structure |
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