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: CHEMBL590799 (Camostat) |
---|
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 |
---|---|---|---|---|---|---|---|---|
cathepsin L/Cathepsin L in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3837] [GtoPdb: 2351] [UniProtKB: P07711] | ||||||||
ChEMBL | Inhibition of human recombinant Cathepsin L assessed as Kinact using Z-FR-AMC as substrate incubated for 30 mins by fluorometric assay | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2020) 63: 12256-12274 [PMID:32539378] |
Hepatocyte growth factor activator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3351190] [UniProtKB: Q04756] | ||||||||
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 | 4.49 | pIC50 | 32000 | nM | IC50 | Bioorg Med Chem (2015) 23: 2328-2343 [PMID:25882520] |
Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8] | ||||||||
ChEMBL | Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | B | 5.54 | pIC50 | 2900 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
MATE2/Multidrug and toxin extrusion protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743127] [GtoPdb: 1217] [UniProtKB: Q86VL8] | ||||||||
ChEMBL | Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | B | 4.9 | pIC50 | 12700 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
CoV Replicase polyprotein 1ab/CoV RNA-dependent RNA polymerase/CoV Non-structural protein 15/CoV Non-structural protein 13/Replicase polyprotein 1ab in Severe acute respiratory syndrome coronavirus 2 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523582] [GtoPdb: 3125, 3139, 3206, 3261] [UniProtKB: P0DTD1] | ||||||||
ChEMBL | Inhibition of SARS-CoV-2 MPro | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem (2021) 29: 115860-115860 [PMID:33191083] |
Serine protease hepsin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2079849] [UniProtKB: P05981] | ||||||||
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 | 7.54 | pIC50 | 29 | nM | IC50 | J Med Chem (2018) 61: 4335-4347 [PMID:29701962] |
Organic cation transporter 2/Solute carrier family 22 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244] | ||||||||
ChEMBL | Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay | B | 4.78 | pIC50 | 16500 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
coagulation factor II, thrombin/Thrombin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734] | ||||||||
ChEMBL | Inhibition of thrombin (unknown origin) using Boc-Val-Pro-Arg-AMC as substrate preincubated with enzyme for 15 mins followed by addition of substrate by fluorescence plate reader analysis | B | 6.11 | pIC50 | 780 | nM | IC50 | Eur J Med Chem (2019) 176: 187-194 [PMID:31103899] |
transmembrane serine protease 2/Transmembrane protease serine 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795140] [GtoPdb: 2421] [UniProtKB: O15393] | ||||||||
GtoPdb | Inhibition of TMPRSS2-dependent MERS-S-mediated membrane fusion in an in vitro reporter assay. | - | 6 | pIC50 | 1000 | nM | IC50 | Antimicrob Agents Chemother (2016) 60: 6532-6539 [PMID:27550352] |
ChEMBL | Inhibition of human TMPRSS2-mediated SARS-CoV-2 entry into human Caco-2 cells | B | 6 | pEC50 | 1000 | nM | EC50 | J Med Chem (2020) 63: 13205-13227 [PMID:32845145] |
serine protease 1/Trypsin I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL209] [GtoPdb: 2397] [UniProtKB: P07477] | ||||||||
GtoPdb | - | - | 7.3 | pIC50 | 50.6 | nM | IC50 | J Med Chem (1995) 38: 2521-3 [PMID:7629790] |
ChEMBL | Inhibition Assay: The compound was dissolved in dimethyl sulfoxide (DMSO), and diluted to an arbitrary concentration (A). A was 100-fold diluted with a buffer (0.1 M Tris (pH 8.0), 0.15 M NaCl, 10 mM CaCl2, 0.05% Brij38) (B). The r-h trypsin was diluted with a buffer to 0.088 ug/mL, and the m-trypsin was diluted with a buffer to 1/50 (C). The dilution ratio of the m-trypsin (1/50) was set to exhibit the same activity as the 0.088 ug/mL r-h trypsin as determined by kinetic analysis. The substrate solution of a substrate for the enzyme reaction, BZiPAR, (Rhodamine Reference Substrate) was diluted with a buffer to 5 umol/L (D). B; 5 uL, C; 5 uL, and D; 10 uL were added to a 384-plate, and incubated at room temperature for 30 minutes. The fluorescent signals were detected with Ex/Em = 497/520 using Tecan Safire Fluorometer. The compound was reviewed from 2500 nM to its 3-fold value, 0.0075 nM, at 12 concentrations, and the inhibitory rate of each compound was calculated. | B | 8.34 | pIC50 | 4.6 | nM | IC50 | US-9199927-B2. Guanidinobenzoic acid compound (2015) |
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]