nafamostat [Ligand Id: 4262] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL273264 (Nafamostat)
  • coagulation factor X/Coagulation factor X in Human [ChEMBL: CHEMBL244] [GtoPdb: 2359] [UniProtKB: P00742]
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  • coagulation factor XII/Coagulation factor XII in Human [ChEMBL: CHEMBL2821] [GtoPdb: 2361] [UniProtKB: P00748]
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  • 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: 24572441] [UniProtKB: P05106P08514]
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  • ST14 transmembrane serine protease matriptase /Matriptase in Human [ChEMBL: CHEMBL3018] [GtoPdb: 2418] [UniProtKB: Q9Y5Y6]
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  • coagulation factor II, thrombin/Thrombin in Human [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
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  • TRPM7 in Human [GtoPdb: 499] [UniProtKB: Q96QT4]
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  • ASIC1 in Human [GtoPdb: 684] [UniProtKB: P78348]
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  • ASIC2 in Human [GtoPdb: 685] [UniProtKB: Q16515]
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  • ASIC3 in Human [GtoPdb: 686] [UniProtKB: Q9UHC3]
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  • transmembrane serine protease 2 in Human [GtoPdb: 2421] [UniProtKB: O15393]
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  • tryptase alpha/beta 1 in Human [GtoPdb: 2424] [UniProtKB: Q15661]
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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: 24572441] [UniProtKB: P05106P08514]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]