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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]