ChEMBL ligand: CHEMBL2016873
coagulation factor X/Coagulation factor X in Human [ChEMBL: CHEMBL244] [GtoPdb: 2359] [UniProtKB: P00742] There should be some charts here, you may need to enable JavaScript!
kallikrein B1/Plasma kallikrein in Human [ChEMBL: CHEMBL2000] [GtoPdb: 2379] [UniProtKB: P03952] There should be some charts here, you may need to enable JavaScript!
plasminogen/Plasminogen in Human [ChEMBL: CHEMBL1801] [GtoPdb: 2394] [UniProtKB: P00747] There should be some charts here, you may need to enable JavaScript!
coagulation factor II, thrombin/Thrombin in Human [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734] There should be some charts here, you may need to enable JavaScript!
protein C, inactivator of coagulation factors Va and VIIIa/Vitamin K-dependent protein C in Human [ChEMBL: CHEMBL4444] [GtoPdb: 2396] [UniProtKB: P04070] There should be some charts here, you may need to enable JavaScript!

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 by dixon plot method	B	6.69	pKi	206	nM	Ki	J Med Chem (2012) 55: 1171-1180 [PMID:22276953]
ChEMBL	Enzyme Assay: The inhibition constants for human plasmin (h plasmin), human plasma kallikrein (h PK), thrombin and factor Xa were determined in analogy to a previously disclosed method (Stürzebecher et al., J. Med. Chem., 40, 3091-3099 (1997)), using a microplate reader (Multiscan Ascent, Thermo Scientific) at 405 nm. The reactions to determine the inhibition of human plasmin and human plasma kallikrein were carried out at 25° C. in 200 μl 50 mM Tris×HCl buffer pH 8.0 (containing 0.154 M NaCl, 2% ethanol and inhibitor in appropriate concentrations) and 25 μl substrate solution. Reactions were started by addition of 50 μl of enzyme solution.	B	6.69	pKi	206	nM	Ki	US-8921319-B2. Serine protease inhibitors (2014)
kallikrein B1/Plasma kallikrein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2000] [GtoPdb: 2379] [UniProtKB: P03952]
ChEMBL	Inhibition of plasma kallikrein by dixon plot method	B	8.62	pKi	2.4	nM	Ki	J Med Chem (2012) 55: 1171-1180 [PMID:22276953]
ChEMBL	Enzyme Assay: The inhibition constants for human plasmin (h plasmin), human plasma kallikrein (h PK), thrombin and factor Xa were determined in analogy to a previously disclosed method (Stürzebecher et al., J. Med. Chem., 40, 3091-3099 (1997)), using a microplate reader (Multiscan Ascent, Thermo Scientific) at 405 nm. The reactions to determine the inhibition of human plasmin and human plasma kallikrein were carried out at 25° C. in 200 μl 50 mM Tris×HCl buffer pH 8.0 (containing 0.154 M NaCl, 2% ethanol and inhibitor in appropriate concentrations) and 25 μl substrate solution. Reactions were started by addition of 50 μl of enzyme solution.	B	8.62	pKi	2.4	nM	Ki	US-8921319-B2. Serine protease inhibitors (2014)
plasminogen/Plasminogen in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1801] [GtoPdb: 2394] [UniProtKB: P00747]
GtoPdb	-	-	9.1	pKi	0.77	nM	Ki	J Med Chem (2012) 55: 1171-80 [PMID:22276953]
ChEMBL	Inhibition of plasmin by dixon plot method	B	9.11	pKi	0.77	nM	Ki	J Med Chem (2012) 55: 1171-1180 [PMID:22276953]
ChEMBL	Enzyme Assay: The inhibition constants for human plasmin (h plasmin), human plasma kallikrein (h PK), thrombin and factor Xa were determined in analogy to a previously disclosed method (Stürzebecher et al., J. Med. Chem., 40, 3091-3099 (1997)), using a microplate reader (Multiscan Ascent, Thermo Scientific) at 405 nm. The reactions to determine the inhibition of human plasmin and human plasma kallikrein were carried out at 25° C. in 200 μl 50 mM Tris×HCl buffer pH 8.0 (containing 0.154 M NaCl, 2% ethanol and inhibitor in appropriate concentrations) and 25 μl substrate solution. Reactions were started by addition of 50 μl of enzyme solution.	B	9.11	pKi	0.77	nM	Ki	US-8921319-B2. Serine protease inhibitors (2014)
coagulation factor II, thrombin/Thrombin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
ChEMBL	Inhibition of thrombin by dixon plot method	B	5.02	pKi	9490	nM	Ki	J Med Chem (2012) 55: 1171-1180 [PMID:22276953]
ChEMBL	Enzyme Assay: The inhibition constants for human plasmin (h plasmin), human plasma kallikrein (h PK), thrombin and factor Xa were determined in analogy to a previously disclosed method (Stürzebecher et al., J. Med. Chem., 40, 3091-3099 (1997)), using a microplate reader (Multiscan Ascent, Thermo Scientific) at 405 nm. The reactions to determine the inhibition of human plasmin and human plasma kallikrein were carried out at 25° C. in 200 μl 50 mM Tris×HCl buffer pH 8.0 (containing 0.154 M NaCl, 2% ethanol and inhibitor in appropriate concentrations) and 25 μl substrate solution. Reactions were started by addition of 50 μl of enzyme solution.	B	5.37	pKi	4300	nM	Ki	US-8921319-B2. Serine protease inhibitors (2014)
protein C, inactivator of coagulation factors Va and VIIIa/Vitamin K-dependent protein C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4444] [GtoPdb: 2396] [UniProtKB: P04070]
ChEMBL	Inhibition of activated protein C by dixon plot method	B	5.52	pKi	3000	nM	Ki	J Med Chem (2012) 55: 1171-1180 [PMID:22276953]

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]