telaprevir [Ligand Id: 7871] 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: CHEMBL231813 (Incivek, Incivo, LY 570310, LY-570310, MP 424, MP-424, Telaprevir, VRT 111950, VRT-111950, VX 950, VX-950) |
|---|
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 |
|---|---|---|---|---|---|---|---|---|
| cathepsin B/Cathepsin B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4072] [GtoPdb: 2343] [UniProtKB: P07858] | ||||||||
| ChEMBL | Inhibition of human Cathepsin B | B | 5.36 | pIC50 | 4400 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 305-311 [PMID:19841155] |
| ChEMBL | Inhibition of human CatB after 60 mins fluorescence assay | B | 5.64 | pIC50 | 2300 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 4611-4618 [PMID:20823284] |
| ChEMBL | Inhibition of cathepsin B | B | 6.68 | pIC50 | 210 | nM | IC50 | J Med Chem (2011) 54: 2529-2591 [PMID:21413808] |
| cathepsin F/Cathepsin F in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2517] [GtoPdb: 2347] [UniProtKB: Q9UBX1] | ||||||||
| ChEMBL | Inhibition of human Cathepsin F | B | 5 | pIC50 | >10000 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 305-311 [PMID:19841155] |
| cathepsin K/Cathepsin K in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL268] [GtoPdb: 2350] [UniProtKB: P43235] | ||||||||
| ChEMBL | Inhibition of human Cathepsin K | B | 6.2 | pIC50 | 630 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 305-311 [PMID:19841155] |
| cathepsin L/Cathepsin L in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3837] [GtoPdb: 2351] [UniProtKB: P07711] | ||||||||
| ChEMBL | Inhibition of human Cathepsin L | B | 5.46 | pIC50 | 3500 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 305-311 [PMID:19841155] |
| cathepsin V/Cathepsin L2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3272] [GtoPdb: 2352] [UniProtKB: O60911] | ||||||||
| ChEMBL | Inhibition of human Cathepsin V | B | 5.87 | pIC50 | 1350 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 305-311 [PMID:19841155] |
| cathepsin S/Cathepsin S in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2954] [GtoPdb: 2353] [UniProtKB: P25774] | ||||||||
| ChEMBL | Inhibition of human cathepsin S | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 6325-6330 [PMID:24135727] |
| ChEMBL | Inhibition of human Cathepsin S | B | 6.52 | pIC50 | 300 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 305-311 [PMID:19841155] |
| chymase 1/Chymase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4068] [GtoPdb: 2340] [UniProtKB: P23946] | ||||||||
| ChEMBL | Inhibition of human Chymase | B | 7.59 | pIC50 | 26 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 305-311 [PMID:19841155] |
| chymotrypsin like elastase 1/Elastase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3000] [GtoPdb: 2338] [UniProtKB: Q9UNI1] | ||||||||
| GtoPdb | - | - | 7.52 | pIC50 | 30 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 305-11 [PMID:19841155] |
| ChEMBL | Inhibition of human Pancreatic elastase 1 | B | 7.52 | pIC50 | 30 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 305-311 [PMID:19841155] |
| elastase, neutrophil expressed/Leukocyte elastase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL248] [GtoPdb: 2358] [UniProtKB: P08246] | ||||||||
| ChEMBL | Inhibition of human Neutrophil elastase 2 | B | 5.1 | pIC50 | 8000 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 305-311 [PMID:19841155] |
| ChEMBL | Inhibition of human neutrophil elastase | B | 5.1 | pIC50 | 8000 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 6325-6330 [PMID:24135727] |
| ChEMBL | Inhibition of human leukocyte elastase after 60 mins fluorescence assay | B | 6.17 | pIC50 | 680 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 4611-4618 [PMID:20823284] |
| NS3 protease in Hepatitis C virus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4296313] [UniProtKB: C1KIQ2] | ||||||||
| ChEMBL | Inhibition of full-length HCV NS3 protease D168V mutant | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (2014) 57: 1790-1801 [PMID:23517538] |
| ChEMBL | Inhibition of HCV genotype 1a NS3 protease V36M/R155K double mutant expressed in Escherichia coli BL21 (DE3) | B | 5.47 | pIC50 | 3400 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 110-120 [PMID:17938182] |
| ChEMBL | Inhibition of HCV 1a NS3-4A protease R155S mutant after 60 mins | B | 5.94 | pIC50 | 1150 | nM | IC50 | J Biol Chem (2007) 282: 22619-22628 [PMID:17556358] |
| ChEMBL | Inhibition of HCV 1a NS3-4A R155I mutant protease after 60 mins | B | 6.06 | pIC50 | 880 | nM | IC50 | J Biol Chem (2007) 282: 22619-22628 [PMID:17556358] |
| ChEMBL | Inhibition of HCV 1a NS3-4A R155K mutant protease after 60 mins | B | 6.29 | pIC50 | 510 | nM | IC50 | J Biol Chem (2007) 282: 22619-22628 [PMID:17556358] |
| ChEMBL | Inhibition of HCV 1a NS3-4A R155T mutant protease after 60 mins | B | 6.31 | pIC50 | 490 | nM | IC50 | J Biol Chem (2007) 282: 22619-22628 [PMID:17556358] |
| ChEMBL | Inhibition of HCV genotype 1a NS3 protease V36M mutant expressed in Escherichia coli BL21 (DE3) | B | 6.57 | pIC50 | 270 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 110-120 [PMID:17938182] |
| ChEMBL | Inhibition of HCV genotype 1a NS3 protease V36L mutant expressed in Escherichia coli BL21 (DE3) | B | 6.89 | pIC50 | 130 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 110-120 [PMID:17938182] |
| NS3 protease in Hepatitis C virus subtype 1b (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4296325] [UniProtKB: Q0ZMF1] | ||||||||
| ChEMBL | Inhibition of full-length HCV NS3 protease A156T mutant | B | 5.21 | pKi | 6100 | nM | Ki | J Med Chem (2014) 57: 1790-1801 [PMID:23517538] |
| ChEMBL | Inhibition of full-length HCV NS3 protease R155K mutant | B | 7.09 | pKi | 82 | nM | Ki | J Med Chem (2014) 57: 1790-1801 [PMID:23517538] |
| plasminogen/Plasminogen in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1801] [GtoPdb: 2394] [UniProtKB: P00747] | ||||||||
| ChEMBL | Inhibition of human plasmin | B | 5.06 | pIC50 | 8700 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 6325-6330 [PMID:24135727] |
| 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 3CL protease using Dabcyl-KTSAVLQSGFRKME-Edans substrate measured by flourimetric plate reader method | B | 4.94 | pIC50 | 11470 | nM | IC50 | Bioorg Med Chem Lett (2021) 48: 128263-128263 [PMID:34271072] |
| ChEMBL | Inhibition of SARS-CoV-2 3CLpro preincubated for 30 mins followed by addition of (Dabcyl)KTSAVLQSGFRKM(Glu) peptide substrate and measured after 1.5 hrs by FRET assay | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2021) 48: 128263-128263 [PMID:34271072] |
| coagulation factor II, thrombin/Thrombin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734] | ||||||||
| ChEMBL | Inhibition of human thrombin | B | 6 | pIC50 | <1000 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 6325-6330 [PMID:24135727] |
| serine protease 1/Trypsin I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL209] [GtoPdb: 2397] [UniProtKB: P07477] | ||||||||
| ChEMBL | Inhibition of human Trypsin activity | B | 5 | pIC50 | >10000 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 305-311 [PMID:19841155] |
| Cathepsin A in Human [GtoPdb: 1581] [UniProtKB: P10619] | ||||||||
| GtoPdb | - | - | 7 | pIC50 | 100 | nM | IC50 | WO2013072328. Use of telaprevir and related compounds in atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases. (2013) |
| CoV 3C-like (main) protease in SARS-CoV-2 [GtoPdb: 3111] | ||||||||
| GtoPdb | - | - | 4.94 | pIC50 | 11470 | nM | IC50 | ACS Nano (2021) 15: 857-872 [PMID:33373194] |
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]
