nafamostat [Ligand Id: 4262] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL273264 (Nafamostat) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
|
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 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]
