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

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ChEMBL ligand: CHEMBL19902 (DX-9065A)
Created with Highcharts 10.3.3ValuesChart context menuCoagulation factor XpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd BovinepKi BovinepIC50 BovinepEC50 BovinepKd RabbitpKi RabbitpIC50 RabbitpEC50 Rabbit0246810Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuPlasminogenpKd HumanpKi HumanpIC50 HumanpEC50 Human012345Highcharts.com
  • coagulation factor II, thrombin/Thrombin in Human [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
Created with Highcharts 10.3.3ValuesChart context menuThrombinpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • plasminogen activator, tissue type/Tissue-type plasminogen activator in Human [ChEMBL: CHEMBL1873] [GtoPdb: 2392] [UniProtKB: P00750]
Created with Highcharts 10.3.3ValuesChart context menuTissue-type plasminogen activatorpKd HumanpKi HumanpIC50 HumanpEC50 Human012345Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuTrypsin IpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd BovinepKi BovinepIC50 BovinepEC50 Bovine02468Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuTrypsin IIpKd BovinepKi BovinepIC50 BovinepEC50 Bovine01234567Highcharts.com
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 35:

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]