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ChEMBL ligand: CHEMBL273264 (Nafamostat) |
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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 | 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 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]