ChEMBL ligand: CHEMBL273264 (Nafamostat)
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!
coagulation factor XII/Coagulation factor XII in Human [ChEMBL: CHEMBL2821] [GtoPdb: 2361] [UniProtKB: P00748] There should be some charts here, you may need to enable JavaScript!
complement C1r/Complement C1r in Human [ChEMBL: CHEMBL4611] [GtoPdb: 2334] [UniProtKB: P00736] There should be some charts here, you may need to enable JavaScript!
complement C1s/Complement C1s in Human [ChEMBL: CHEMBL3913] [GtoPdb: 2335] [UniProtKB: P09871] There should be some charts here, you may need to enable JavaScript!
Hepatocyte growth factor activator in Human [ChEMBL: CHEMBL3351190] [UniProtKB: Q04756] There should be some charts here, you may need to enable JavaScript!
integrin, beta 3 subunit (platelet glycoprotein IIIa, antigen CD61)/integrin, alpha IIb subunit (platelet glycoprotein IIb of IIb/IIIa complex, antigen CD41)/Integrin alpha-IIb/beta-3 in Human [ChEMBL: CHEMBL2093869] [GtoPdb: 2457, 2441] [UniProtKB: P05106, P08514] There should be some charts here, you may need to enable JavaScript!
kallikrein 1/Kallikrein 1 in Human [ChEMBL: CHEMBL2319] [GtoPdb: 2865] [UniProtKB: P06870] There should be some charts here, you may need to enable JavaScript!
ST14 transmembrane serine protease matriptase /Matriptase in Human [ChEMBL: CHEMBL3018] [GtoPdb: 2418] [UniProtKB: Q9Y5Y6] 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!
Serine protease hepsin in Human [ChEMBL: CHEMBL2079849] [UniProtKB: P05981] 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!
serine protease 1/Trypsin I in Human [ChEMBL: CHEMBL209] [GtoPdb: 2397] [UniProtKB: P07477] Trypsin I in Bovine [ChEMBL: CHEMBL3769] [UniProtKB: P00760] There should be some charts here, you may need to enable JavaScript!
TRPM7 in Human [GtoPdb: 499] [UniProtKB: Q96QT4] There should be some charts here, you may need to enable JavaScript!
ASIC1 in Human [GtoPdb: 684] [UniProtKB: P78348] There should be some charts here, you may need to enable JavaScript!
ASIC2 in Human [GtoPdb: 685] [UniProtKB: Q16515] There should be some charts here, you may need to enable JavaScript!
ASIC3 in Human [GtoPdb: 686] [UniProtKB: Q9UHC3] There should be some charts here, you may need to enable JavaScript!
transmembrane serine protease 2 in Human [GtoPdb: 2421] [UniProtKB: O15393] There should be some charts here, you may need to enable JavaScript!
tryptase alpha/beta 1 in Human [GtoPdb: 2424] [UniProtKB: Q15661] 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	Inhibitory concentration against Coagulation factor X	B	4.68	pIC50	21100	nM	IC50	J. Med. Chem. (2000) 43: 305-341 [PMID:10669559]
coagulation factor XII/Coagulation factor XII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2821] [GtoPdb: 2361] [UniProtKB: P00748]
ChEMBL	Inhibition of human factor 12a using chromogenic substrate by Lineweaver-Burk analysis	B	6.98	pKi	105	nM	Ki	Eur J Med Chem (2020) 208: 112753-112753 [PMID:32883641]
complement C1r/Complement C1r in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4611] [GtoPdb: 2334] [UniProtKB: P00736]
GtoPdb	-	-	4.92	pIC50	12000	nM	IC50	J Med Chem (1998) 41: 1060-7 [PMID:9544206]
ChEMBL	Inhibition of 50% of human C1r Serine Protease by initially using Cbz-Gly-Arg-S-Bzl as substrate	B	4.92	pIC50	12000	nM	IC50	J. Med. Chem. (1998) 41: 1060-1067 [PMID:9544206]
ChEMBL	The compound was evaluated to inhibit 50% of Clr Serine Protease after 60 mins and is expressed in IC50 (uM).	B	4.92	pIC50	12000	nM	IC50	J. Med. Chem. (1998) 41: 1060-1067 [PMID:9544206]
ChEMBL	Inhibitory activity against C1r serine protease	B	4.92	pIC50	12000	nM	IC50	Bioorg. Med. Chem. Lett. (1996) 6: 679-682
ChEMBL	In vitro inhibition of purified human C1r protease.	B	4.92	pIC50	12000	nM	IC50	Bioorg. Med. Chem. Lett. (1999) 9: 815-820 [PMID:10206542]
ChEMBL	Evaluated in vitro for inhibitory activity against purified human C1r protease incubated in buffer for 60 minutes	B	4.92	pIC50	12000	nM	IC50	Bioorg. Med. Chem. Lett. (1999) 9: 815-820 [PMID:10206542]
ChEMBL	Inhibitory activity against C1r serine protease	B	4.92	pIC50	12000	nM	IC50	Bioorg. Med. Chem. Lett. (1996) 6: 679-682
ChEMBL	Compound was evaluated for inhibitory activity against C1r serine protease.	B	5.98	pIC50	1040	nM	IC50	Bioorg. Med. Chem. Lett. (1996) 6: 679-682
ChEMBL	Inhibition of C1r serine protease	B	6	pIC50	1000	nM	IC50	Bioorg. Med. Chem. Lett. (1996) 6: 679-682
ChEMBL	Inhibition of human serum C1r using AAME as substrate after 30 mins	B	6.1	pIC50	800	nM	IC50	J Med Chem (2018) 61: 3253-3276 [PMID:28977749]
complement C1s/Complement C1s in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3913] [GtoPdb: 2335] [UniProtKB: P09871]
ChEMBL	Compound was evaluated for inhibitory activity against C1s serine protease.	B	6.85	pIC50	140	nM	IC50	Bioorg. Med. Chem. Lett. (1996) 6: 679-682
ChEMBL	Inhibition of human serum C1s using AGLME as substrate after 30 mins	B	7.54	pIC50	29	nM	IC50	J Med Chem (2018) 61: 3253-3276 [PMID:28977749]
Hepatocyte growth factor activator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3351190] [UniProtKB: Q04756]
ChEMBL	Inhibition of recombinant HGFA (unknown origin) using Boc-QLR-AMC as substrate by chromogenic proteolytic assay	B	7.6	pKi	25	nM	Ki	ACS Med. Chem. Lett. (2014) 5: 1219-1224 [PMID:25408834]
ChEMBL	Inhibition of recombinant N-terminal His-tagged HGFA (unknown origin) expressed in baculovirus-infected Sf9 cells using Boc-QLR-AMC as substrate incubated for 30 mins prior to substrate addition by fluorescence assay	B	7.6	pKi	25	nM	Ki	Bioorg. Med. Chem. (2015) 23: 2328-2343 [PMID:25882520]
ChEMBL	Inhibition of recombinant N-terminal His-tagged HGFA (unknown origin) expressed in baculovirus-infected Sf9 cells incubated for 30 mins prior to cromogenic substrate addition by spectrophotometry	B	6.82	pIC50	150	nM	IC50	Bioorg. Med. Chem. (2015) 23: 2328-2343 [PMID:25882520]
ChEMBL	Inhibition of HGFA in human MDA-MB-231 cells assessed as inhibition of c-MET phosphorylation after 15 mins by immunoblotting	B	6.31	pEC50	490	nM	EC50	ACS Med. Chem. Lett. (2014) 5: 1219-1224 [PMID:25408834]
integrin, beta 3 subunit (platelet glycoprotein IIIa, antigen CD61)/integrin, alpha IIb subunit (platelet glycoprotein IIb of IIb/IIIa complex, antigen CD41)/Integrin alpha-IIb/beta-3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2093869] [GtoPdb: 2457, 2441] [UniProtKB: P05106, P08514]
ChEMBL	Antagonist activity against integrin alpha2bbeta3 in human platelet rich plasma	B	4.9	pIC50	12500	nM	IC50	J. Med. Chem. (2015) 58: 7681-7694 [PMID:26367138]
ChEMBL	Antagonist activity at integrin alpha2b beta3 receptor in citrated human platelet-rich plasma assessed as inhibition of ADP-induced platelet aggregation	B	4.92	pIC50	12000	nM	IC50	J Med Chem (2017) 60: 3241-3251 [PMID:28135089]
kallikrein 1/Kallikrein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2319] [GtoPdb: 2865] [UniProtKB: P06870]
ChEMBL	Compound was evaluated for inhibitory activity against Kallikrein.	B	6.19	pIC50	650	nM	IC50	Bioorg. Med. Chem. Lett. (1996) 6: 679-682
ST14 transmembrane serine protease matriptase /Matriptase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3018] [GtoPdb: 2418] [UniProtKB: Q9Y5Y6]
ChEMBL	Inhibition of matriptase (unknown origin) using Boc-QAR-AMC as substrate by fluorescence assay	B	10.7	pKi	0.02	nM	Ki	ACS Med. Chem. Lett. (2014) 5: 1219-1224 [PMID:25408834]
ChEMBL	Inhibition of matripase (unknown origin) using Boc-QAR-AMC as substrate incubated for 30 mins prior to substrate addition by fluorescence assay	B	10.7	pKi	0.02	nM	Ki	Bioorg. Med. Chem. (2015) 23: 2328-2343 [PMID:25882520]
plasminogen/Plasminogen in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1801] [GtoPdb: 2394] [UniProtKB: P00747]
ChEMBL	Inhibition of human plasmin assessed as reduction in hydrolytic activity using TAME as substrate after 5 mins by spectrophotometric method	B	6.39	pKi	410	nM	Ki	J Med Chem (2020) 63: 1445-1472 [PMID:31658420]
ChEMBL	Inhibitory concentration against plasmin	B	5.54	pIC50	2900	nM	IC50	J. Med. Chem. (2000) 43: 305-341 [PMID:10669559]
ChEMBL	Compound was evaluated for inhibitory activity against plasmin.	B	6.62	pIC50	240	nM	IC50	Bioorg. Med. Chem. Lett. (1996) 6: 679-682
Serine protease hepsin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2079849] [UniProtKB: P05981]
ChEMBL	Inhibition of recombinant hepsin (unknown origin) using Boc-QAR-AMC as substrate by fluorescence assay	B	9.28	pKi	0.53	nM	Ki	ACS Med. Chem. Lett. (2014) 5: 1219-1224 [PMID:25408834]
ChEMBL	Inhibition of hepsin (unknown origin) using Boc-QAR-AMC as substrate after 30 mins prior to substrate addition by fluorescence assay	B	9.28	pKi	0.53	nM	Ki	Bioorg. Med. Chem. (2015) 23: 2328-2343 [PMID:25882520]
ChEMBL	Inhibition of recombinant C-terminal His10-tagged human Hepsin (R45 to L17 residues) D161E/ R162K double mutant expressed in mouse NS0 cells using Boc-QRR-AMC as substrate after 15 mins by automated fluorescence assay	B	8.3	pIC50	5	nM	IC50	J Med Chem (2018) 61: 4335-4347 [PMID:29701962]
coagulation factor II, thrombin/Thrombin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
ChEMBL	Inhibitory concentration against thrombin	B	5.72	pIC50	1900	nM	IC50	J. Med. Chem. (2000) 43: 305-341 [PMID:10669559]
ChEMBL	Compound was evaluated for inhibitory activity against Thrombin.	B	6.54	pIC50	290	nM	IC50	Bioorg. Med. Chem. Lett. (1996) 6: 679-682
serine protease 1/Trypsin I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL209] [GtoPdb: 2397] [UniProtKB: P07477]
ChEMBL	Compound was evaluated for inhibitory activity against Trypsin.	B	7.7	pIC50	20	nM	IC50	Bioorg. Med. Chem. Lett. (1996) 6: 679-682
ChEMBL	In vitro for inhibition of purified bovine trypsin.	B	7.77	pIC50	17	nM	IC50	Bioorg. Med. Chem. Lett. (1999) 9: 815-820 [PMID:10206542]
GtoPdb	-	-	7.77	pIC50	17	nM	IC50	J Med Chem (1998) 41: 1060-7 [PMID:9544206]
Trypsin I in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3769] [UniProtKB: P00760]
ChEMBL	The compound was evaluated to inhibit trypsin and is expressed in IC50 (The concentration required to inhibit 50% of the enzyme).	B	7.77	pIC50	17	nM	IC50	J. Med. Chem. (1998) 41: 1060-1067 [PMID:9544206]
TRPM7 in Human [GtoPdb: 499] [UniProtKB: Q96QT4]
GtoPdb	-	-	3.21	pIC50	617000	nM	IC50	Mol Brain (2010) 3: 38 [PMID:21122141]
ASIC1 in Human [GtoPdb: 684] [UniProtKB: P78348]
GtoPdb	-	-	4.9	pIC50	~13000	nM	IC50	Biochem Biophys Res Commun (2007) 363: 203-8 [PMID:17826743]
ASIC2 in Human [GtoPdb: 685] [UniProtKB: Q16515]
GtoPdb	-	-	4.2	pIC50	~70000	nM	IC50	Biochem Biophys Res Commun (2007) 363: 203-8 [PMID:17826743]
ASIC3 in Human [GtoPdb: 686] [UniProtKB: Q9UHC3]
GtoPdb	-	-	5.6	pIC50	~2500	nM	IC50	Biochem Biophys Res Commun (2007) 363: 203-8 [PMID:17826743]
transmembrane serine protease 2 in Human [GtoPdb: 2421] [UniProtKB: O15393]
GtoPdb	Inhibition of TMPRSS2-dependent MERS-S-mediated membrane fusion in an in vitro reporter assay.	-	7	pIC50	100	nM	IC50	Antimicrob Agents Chemother (2016) 60: 6532-6539 [PMID:27550352]
tryptase alpha/beta 1 in Human [GtoPdb: 2424] [UniProtKB: Q15661]
GtoPdb	-	-	10	pIC50	0.1	nM	IC50	J Pharmacol Sci (2003) 92: 420-3 [PMID:12939527]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]