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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 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]