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ChEMBL ligand: CHEMBL87563 (Gabexate, Gabexate mesilate) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]