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ChEMBL ligand: CHEMBL19902 (DX-9065A) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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]