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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 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]