DX-9065a [Ligand Id: 11365] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL19902 (DX-9065A)
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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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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 factor 10a in human plasma B 7.39 pKi 41 nM Ki Bioorg Med Chem Lett (2008) 18: 4682-4687 [PMID:18667303]
ChEMBL Inhibitory concentration against human Coagulation factor Xa (fXa) B 7.39 pKi 41 nM Ki J Med Chem (2002) 45: 1221-1232 [PMID:11881991]
ChEMBL Binding affinity against Coagulation factor X B 7.39 pKi 41 nM Ki J Med Chem (2000) 43: 305-341 [PMID:10669559]
ChEMBL Inhibition of Factor Xa B 7.39 pKi 41 nM Ki Bioorg Med Chem Lett (1997) 7: 2813-2818
ChEMBL Inhibition of factor 10a B 7.39 pKi 41 nM Ki J Med Chem (2010) 53: 6243-6274 [PMID:20503967]
ChEMBL Inhibition of human factor 10a by Lineweaver-Burke plot B 7.39 pKi 41 nM Ki Bioorg Med Chem (2009) 17: 1193-1206 [PMID:19128974]
GtoPdb Dissociation constant for FXa - 7.39 pKi 41 nM Ki J Thromb Haemost (2004) 2: 612-8 [PMID:15102016];
Thromb Haemost (1994) 71: 314-9 [PMID:8029795]
ChEMBL In vitro inhibition of human coagulation factor Xa (Xa) in a purified enzyme system. B 7.4 pKi 40 nM Ki J Med Chem (1999) 42: 5415-5425 [PMID:10639283]
ChEMBL Compound was tested for inhibition activity against factor Xa (FXa) B 7.66 pKi 22 nM Ki J Med Chem (1999) 42: 1749-1756 [PMID:10346927]
ChEMBL Binding affinity towards Coagulation factor X B 8.15 pKi 7 nM Ki J Med Chem (1998) 41: 4240-4250 [PMID:9784099]
ChEMBL Inhibition of human factor 10a B 6.89 pIC50 130 nM IC50 Bioorg Med Chem (2008) 16: 2243-2260 [PMID:18077174]
ChEMBL Inhibition of human factor 10a B 6.89 pIC50 130 nM IC50 Bioorg Med Chem (2008) 16: 3125-3140 [PMID:18164204]
ChEMBL In vitro evaluation for the concentration needed for inhibiting factor Xa by 50% B 7.15 pIC50 70 nM IC50 J Med Chem (1994) 37: 1200-1207 [PMID:8164262]
ChEMBL Inhibitory Activity against human Coagulation factor X B 7.15 pIC50 70 nM IC50 J Med Chem (2000) 43: 3033-3044 [PMID:10956211]
ChEMBL Inhibition of human factor 10a B 7.15 pIC50 70 nM IC50 Bioorg Med Chem (2009) 17: 1193-1206 [PMID:19128974]
ChEMBL Inhibition of human factor 10a B 7.4 pIC50 40 nM IC50 Bioorg Med Chem (2007) 15: 4175-4192 [PMID:17416533]
Coagulation factor X in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3656] [UniProtKB: P00743]
ChEMBL Binding affinity towards Coagulation factor X B 7.39 pKi 41 nM Ki J Med Chem (1998) 41: 4240-4250 [PMID:9784099]
Coagulation factor X in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5062] [UniProtKB: O19045]
ChEMBL Compound was tested for the inhibition of serine protease factor Xa enzyme. B 7.39 pIC50 41 nM IC50 Bioorg Med Chem Lett (1998) 8: 3143-3148 [PMID:9873692]
plasminogen/Plasminogen in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1801] [GtoPdb: 2394] [UniProtKB: P00747]
ChEMBL Inhibition of human plasmin by Lineweaver-Burke plot B 4.64 pKi 23000 nM Ki Bioorg Med Chem (2009) 17: 1193-1206 [PMID:19128974]
coagulation factor II, thrombin/Thrombin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
ChEMBL Compound was tested for inhibition activity against human thrombin (FIIa) B 5.3 pKi >5000 nM Ki J Med Chem (1999) 42: 1749-1756 [PMID:10346927]
ChEMBL Inhibitory concentration against thrombin. B 5.7 pKi >2000 nM Ki J Med Chem (2002) 45: 1221-1232 [PMID:11881991]
ChEMBL Inhibition of human thrombin B 4 pIC50 >100000 nM IC50 Bioorg Med Chem (2007) 15: 4175-4192 [PMID:17416533]
plasminogen activator, tissue type/Tissue-type plasminogen activator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1873] [GtoPdb: 2392] [UniProtKB: P00750]
ChEMBL Inhibition of human recombinant tissue plasminogen activator by Lineweaver-Burke plot B 4.68 pKi 21000 nM Ki Bioorg Med Chem (2009) 17: 1193-1206 [PMID:19128974]
serine protease 1/Trypsin I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL209] [GtoPdb: 2397] [UniProtKB: P07477]
ChEMBL Binding affinity against Trypsin B 6.21 pKi 620 nM Ki J Med Chem (2000) 43: 305-341 [PMID:10669559]
Trypsin I in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3769] [UniProtKB: P00760]
ChEMBL Inhibitory concentration against bovine trypsin B 6.2 pKi 630 nM Ki J Med Chem (2002) 45: 1221-1232 [PMID:11881991]
ChEMBL Compound was tested for inhibition activity against bovine trypsin. B 6.72 pKi 190 nM Ki J Med Chem (1999) 42: 1749-1756 [PMID:10346927]
Trypsin II in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4472] [UniProtKB: Q29463]
ChEMBL Binding affinity towards Trypsin. B 6.21 pKi 620 nM Ki J Med Chem (1998) 41: 4240-4250 [PMID:9784099]

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]