compound 5 [PMID: 21741839] [Ligand Id: 8670] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1229259
  • coagulation factor X/Coagulation factor X in Human [ChEMBL: CHEMBL244] [GtoPdb: 2359] [UniProtKB: P00742]
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  • ST14 transmembrane serine protease matriptase /Matriptase in Human [ChEMBL: CHEMBL3018] [GtoPdb: 2418] [UniProtKB: Q9Y5Y6]
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  • coagulation factor II, thrombin/Thrombin in Human [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
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  • transmembrane serine protease 11D/Transmembrane protease serine 11D in Human [ChEMBL: CHEMBL1795138] [GtoPdb: 2420] [UniProtKB: O60235]
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  • transmembrane serine protease 2/Transmembrane protease serine 2 in Human [ChEMBL: CHEMBL1795140] [GtoPdb: 2421] [UniProtKB: O15393]
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  • transmembrane serine protease 6/Transmembrane protease serine 6 in Human [ChEMBL: CHEMBL1795139] [GtoPdb: 2422] [UniProtKB: Q8IU80]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
coagulation factor X/Coagulation factor X in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL244] [GtoPdb: 2359] [UniProtKB: P00742]
ChEMBL Inhibition of factor 10a B 8.62 pKi 2.4 nM Ki Bioorg Med Chem Lett (2011) 21: 4860-4864 [PMID:21741839]
ST14 transmembrane serine protease matriptase /Matriptase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3018] [GtoPdb: 2418] [UniProtKB: Q9Y5Y6]
ChEMBL Inhibition of matriptase B 7.26 pKi 55 nM Ki Bioorg Med Chem Lett (2011) 21: 4860-4864 [PMID:21741839]
kallikrein B1/Plasma kallikrein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2000] [GtoPdb: 2379] [UniProtKB: P03952]
ChEMBL Inhibition of plasma kallikrein B 8.08 pKi 8.3 nM Ki Bioorg Med Chem Lett (2011) 21: 4860-4864 [PMID:21741839]
plasminogen/Plasminogen in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1801] [GtoPdb: 2394] [UniProtKB: P00747]
ChEMBL Inhibition of plasmin B 7.41 pKi 39 nM Ki Bioorg Med Chem Lett (2011) 21: 4860-4864 [PMID:21741839]
coagulation factor II, thrombin/Thrombin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
ChEMBL Inhibition of thrombin B 8.46 pKi 3.5 nM Ki Bioorg Med Chem Lett (2011) 21: 4860-4864 [PMID:21741839]
transmembrane serine protease 11D/Transmembrane protease serine 11D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795138] [GtoPdb: 2420] [UniProtKB: O60235]
GtoPdb - - 7.72 pKi 19 nM Ki Bioorg Med Chem Lett (2011) 21: 4860-4 [PMID:21741839]
ChEMBL Inhibition of human recombinant airway trypsin-like protease HAT using D-cyclohexylalanine-Pro-Arg-AMC as substrate by fluorescence plate reader analysis B 7.72 pKi 19 nM Ki Bioorg Med Chem Lett (2011) 21: 4860-4864 [PMID:21741839]
transmembrane serine protease 2/Transmembrane protease serine 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795140] [GtoPdb: 2421] [UniProtKB: O15393]
ChEMBL Inhibition of recombinant catalytic domain of TMPRSS2 expressed in Escherichia coli using Dcyclohexylalanine- Pro-Arg-AMC as substrate by fluorescence plate reader analysis B 7.7 pKi 20 nM Ki Bioorg Med Chem Lett (2011) 21: 4860-4864 [PMID:21741839]
GtoPdb - - 7.7 pKi 20 nM Ki Bioorg Med Chem Lett (2011) 21: 4860-4 [PMID:21741839]
transmembrane serine protease 6/Transmembrane protease serine 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795139] [GtoPdb: 2422] [UniProtKB: Q8IU80]
ChEMBL Inhibition of matriptase 2 B 6.77 pKi 170 nM Ki Bioorg Med Chem Lett (2011) 21: 4860-4864 [PMID:21741839]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]