gabexate [Ligand Id: 7863] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL87563 (Gabexate, Gabexate mesilate)
  • amine oxidase copper containing 3/Amine oxidase, copper containing in Rat [ChEMBL: CHEMBL4592] [GtoPdb: 2767] [UniProtKB: O08590]
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  • coagulation factor X/Coagulation factor X in Human [ChEMBL: CHEMBL244] [GtoPdb: 2359] [UniProtKB: P00742]
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  • coagulation factor XII/Coagulation factor XII in Human [ChEMBL: CHEMBL2821] [GtoPdb: 2361] [UniProtKB: P00748]
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  • Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8]
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  • MATE2/Multidrug and toxin extrusion protein 2 in Human [ChEMBL: CHEMBL1743127] [GtoPdb: 1217] [UniProtKB: Q86VL8]
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  • Organic cation transporter 2/Solute carrier family 22 member 2 in Human [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244]
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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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  • tryptase alpha/beta 1 in Human [GtoPdb: 2424] [UniProtKB: Q15661]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
amine oxidase copper containing 3/Amine oxidase, copper containing in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4592] [GtoPdb: 2767] [UniProtKB: O08590]
ChEMBL Inhibitory activity against porcine kidney amine oxidase B 4.57 pKi 27000 nM Ki Bioorg Med Chem Lett (2001) 11: 2565-2568 [PMID:11551750]
coagulation factor X/Coagulation factor X in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL244] [GtoPdb: 2359] [UniProtKB: P00742]
ChEMBL Inhibition of purified human factor 10a using Suc-Ile-Glu(gammaPip)-GlyArg-pNa-HCl as substrate measured for 5 mins by spectrophotometric assay B 5.34 pIC50 4610 nM IC50 J Med Chem (2015) 58: 9238-9257 [PMID:26575094]
coagulation factor XII/Coagulation factor XII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2821] [GtoPdb: 2361] [UniProtKB: P00748]
ChEMBL Inhibition of human factor 12a using chromogenic substrate by Lineweaver-Burk analysis B 5.53 pKi 2920 nM Ki Eur J Med Chem (2020) 208: 112753-112753 [PMID:32883641]
Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8]
ChEMBL Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay B 6.3 pIC50 500 nM IC50 J Med Chem (2013) 56: 781-795 [PMID:23241029]
MATE2/Multidrug and toxin extrusion protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743127] [GtoPdb: 1217] [UniProtKB: Q86VL8]
ChEMBL Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay B 4.97 pIC50 10800 nM IC50 J Med Chem (2013) 56: 781-795 [PMID:23241029]
kallikrein B1/Plasma kallikrein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2000] [GtoPdb: 2379] [UniProtKB: P03952]
ChEMBL Inhibition of human plasma kallikrein using D-Pro-Phe-Arg-pNA-2HCl as substrate measured for 5 mins by spectrophotometric assay B 5.87 pIC50 1350 nM IC50 J Med Chem (2015) 58: 9238-9257 [PMID:26575094]
plasminogen/Plasminogen in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1801] [GtoPdb: 2394] [UniProtKB: P00747]
ChEMBL Competitive inhibition of human plasmin assessed as reduction in hydrolytic activity using S-2251 as substrate by spectrophotometric method B 5.72 pKi 1900 nM Ki J Med Chem (2020) 63: 1445-1472 [PMID:31658420]
ChEMBL Inhibition of human plasma plasmin using pyroGlu-Pro-Arg-pNA-HCl as substrate measured for 5 mins by spectrophotometric assay B 5.81 pIC50 1550 nM IC50 J Med Chem (2015) 58: 9238-9257 [PMID:26575094]
Serine protease hepsin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2079849] [UniProtKB: P05981]
ChEMBL Inhibition of recombinant C-terminal His10-tagged human Hepsin (R45 to L17 residues) D161E/ R162K double mutant expressed in mouse NS0 cells using Boc-QRR-AMC as substrate after 15 mins by automated fluorescence assay B 6.42 pIC50 383 nM IC50 J Med Chem (2018) 61: 4335-4347 [PMID:29701962]
Organic cation transporter 2/Solute carrier family 22 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244]
ChEMBL Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay B 6.05 pIC50 900 nM IC50 J Med Chem (2013) 56: 781-795 [PMID:23241029]
coagulation factor II, thrombin/Thrombin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
ChEMBL Inhibition of human plasma thrombin using pyroGlu-Pro-Arg-pNA-HCl as substrate measured for 5 mins by spectrophotometric assay B 6.16 pIC50 687 nM IC50 J Med Chem (2015) 58: 9238-9257 [PMID:26575094]
plasminogen activator, tissue type/Tissue-type plasminogen activator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1873] [GtoPdb: 2392] [UniProtKB: P00750]
ChEMBL Inhibition of recombinant human tPA using H-D-Ile-Pro-L-Arg-pNA-2HCl as substrate measured for 5 mins by spectrophotometric assay B 4.81 pIC50 15360 nM IC50 J Med Chem (2015) 58: 9238-9257 [PMID:26575094]
plasminogen activator, urokinase/Urokinase-type plasminogen activator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3286] [GtoPdb: 2393] [UniProtKB: P00749]
ChEMBL Inhibition of human uPA using pyro-Glu-Gly-Arg-pNA as substrate assessed as para-nitroaniline release from substrate measured for 5 mins by spectrophotometric assay B 6.37 pIC50 431 nM IC50 J Med Chem (2015) 58: 9238-9257 [PMID:26575094]
tryptase alpha/beta 1 in Human [GtoPdb: 2424] [UniProtKB: Q15661]
GtoPdb - - 8.47 pIC50 3.4 nM IC50 Biochem Pharmacol (2001) 61: 271-6 [PMID:11172730]

ChEMBL data shown on this page come from version 32:

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]