WX-UK1 [Ligand Id: 6498] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL107955
  • coagulation factor X/Coagulation factor X in Human [ChEMBL: CHEMBL244] [GtoPdb: 2359] [UniProtKB: P00742]
  • Coagulation factor X in Bovine [ChEMBL: CHEMBL3656] [UniProtKB: P00743]
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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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  • plasminogen activator, tissue type/Tissue-type plasminogen activator in Human [ChEMBL: CHEMBL1873] [GtoPdb: 2392] [UniProtKB: P00750]
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  • plasminogen activator, urokinase/Urokinase-type plasminogen activator in Human [ChEMBL: CHEMBL3286] [GtoPdb: 2393] [UniProtKB: P00749]
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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 f10a B 5.77 pKi 1700 nM Ki J Med Chem (2006) 49: 4116-4126 [PMID:16821772]
Coagulation factor X in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3656] [UniProtKB: P00743]
ChEMBL Compound was tested for inhibition of Coagulation factor X B 5.77 pKi 1700 nM Ki Bioorg Med Chem Lett (1999) 9: 3147-3152 [PMID:10560742]
ST14 transmembrane serine protease matriptase /Matriptase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3018] [GtoPdb: 2418] [UniProtKB: Q9Y5Y6]
ChEMBL Inhibition of matriptase B 6.49 pKi 320 nM Ki J Med Chem (2006) 49: 4116-4126 [PMID:16821772]
kallikrein B1/Plasma kallikrein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2000] [GtoPdb: 2379] [UniProtKB: P03952]
ChEMBL Compound was tested for inhibition of plasma kallikrein B 5.14 pKi 7200 nM Ki Bioorg Med Chem Lett (1999) 9: 3147-3152 [PMID:10560742]
plasminogen/Plasminogen in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1801] [GtoPdb: 2394] [UniProtKB: P00747]
GtoPdb - - 5.84 pKi 1460 nM Ki Thromb Haemost (2005) 93: 779-86 [PMID:15841327]
ChEMBL Compound was tested for inhibition of plasmin B 6.41 pKi 390 nM Ki Bioorg Med Chem Lett (1999) 9: 3147-3152 [PMID:10560742]
ChEMBL Inhibition of plasmin B 6.41 pKi 390 nM Ki J Med Chem (2006) 49: 4116-4126 [PMID:16821772]
ChEMBL Inhibition of human plasma plasmin using pyroGlu-Pro-Arg-p-NA.HCl as substrate preincubated for 15 mins prior substrate addition measured for 10 mins by spectrophotometry B 6.41 pKi 390 nM Ki Bioorg Med Chem (2012) 20: 1557-1568 [PMID:22285569]
ChEMBL Inhibition of human plasmin B 6.41 pKi 390 nM Ki J Med Chem (2020) 63: 1445-1472 [PMID:31658420]
coagulation factor II, thrombin/Thrombin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
GtoPdb - - 6.3 pKi 500 nM Ki Thromb Haemost (2005) 93: 779-86 [PMID:15841327]
ChEMBL Compound was tested for inhibition of thrombin B 6.31 pKi 490 nM Ki Bioorg Med Chem Lett (1999) 9: 3147-3152 [PMID:10560742]
ChEMBL Inhibition of thrombin B 6.31 pKi 490 nM Ki J Med Chem (2006) 49: 4116-4126 [PMID:16821772]
ChEMBL Inhibition of human plasma thrombin using pyroGlu-Pro-Arg-p-NA.HCl as substrate preincubated for 15 mins prior substrate addition measured for 10 mins by spectrophotometry B 6.31 pKi 490 nM Ki Bioorg Med Chem (2012) 20: 1557-1568 [PMID:22285569]
plasminogen activator, tissue type/Tissue-type plasminogen activator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1873] [GtoPdb: 2392] [UniProtKB: P00750]
ChEMBL Inhibition of recombinant tPA using H-D-Ile-Pro-Arg-pNA.2HCl as substrate preincubated for 15 mins prior substrate addition measured for 10 mins by spectrophotometry B 5.31 pKi 4900 nM Ki Bioorg Med Chem (2012) 20: 1557-1568 [PMID:22285569]
Trypsin I in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3769] [UniProtKB: P00760]
ChEMBL Compound was tested for inhibition of trypsin B 7.43 pKi 37 nM Ki Bioorg Med Chem Lett (1999) 9: 3147-3152 [PMID:10560742]
tryptase gamma 1/Tryptase gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4955] [GtoPdb: 2425] [UniProtKB: Q9NRR2]
ChEMBL Compound was tested for inhibition of tryptase B 5.2 pKi 6300 nM Ki Bioorg Med Chem Lett (1999) 9: 3147-3152 [PMID:10560742]
plasminogen activator, urokinase/Urokinase-type plasminogen activator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3286] [GtoPdb: 2393] [UniProtKB: P00749]
GtoPdb - - 6.19 pKi 650 nM Ki Thromb Haemost (2005) 93: 779-86 [PMID:15841327]
ChEMBL Compound was tested for inhibition of plasminogen activator urokinase (microPa) B 6.39 pKi 410 nM Ki Bioorg Med Chem Lett (1999) 9: 3147-3152 [PMID:10560742]
ChEMBL Inhibition of uPA B 6.39 pKi 410 nM Ki J Med Chem (2006) 49: 4116-4126 [PMID:16821772]
ChEMBL Inhibition of human uPA using pyroGlu-Gly-Arg-p-NA.HCl as substrate preincubated for 15 mins prior substrate addition measured for 10 mins by spectrophotometry B 6.39 pKi 410 nM Ki Bioorg Med Chem (2012) 20: 1557-1568 [PMID:22285569]
ChEMBL Inhibition of uPA (unknown origin) B 6.39 pKi 410 nM Ki J Med Chem (2015) 58: 9238-9257 [PMID:26575094]
ChEMBL Inhibition of uPA B 6.39 pIC50 410 nM IC50 J Med Chem (2008) 51: 183-186 [PMID:18163548]
GtoPdb - - 6.4 pIC50 410 nM IC50 Bioorg Med Chem Lett (1999) 9: 3147-52 [PMID:10560742]

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]