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ChEMBL ligand: CHEMBL2012938 (Vialinin A) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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SUMO specific peptidase 1/Sentrin-specific protease 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1909484] [GtoPdb: 2414] [UniProtKB: Q9P0U3] | ||||||||
ChEMBL | Binding affinity to full-length recombinant human 6His-tagged SENP1 expressed in Escherichia coli BL21 (DE3) | B | 5.97 | pKi | 1070 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 4237-4240 [PMID:27491710] |
ChEMBL | Binding affinity to recombinant human 6His-tagged SENP1 catalytic domain expressed in Escherichia coli | B | 6.03 | pKi | 930 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 4237-4240 [PMID:27491710] |
ChEMBL | Inhibition of human SENP1 catalytic domain assessed as reduction in deSUMOylation of RanGAP1-SUMO2 using RanGAP1-SUMO2 as substrate by fluorescence based analysis | B | 5.72 | pIC50 | 1900 | nM | IC50 | Eur J Med Chem (2022) 241: 114650-114650 [PMID:35939992] |
ChEMBL | Inhibition of recombinant human 6His-tagged SENP1 catalytic domain expressed in Escherichia coli preincubated for 15 mins followed by addition of SUMO1-AMC as substrate measured after 1 hr by fluorescence analysis | B | 5.72 | pIC50 | 1890 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4237-4240 [PMID:27491710] |
ChEMBL | Inhibition of full-length recombinant human 6His-tagged SENP1 expressed in Escherichia coli BL21 (DE3) preincubated for 15 mins followed by addition of SUMO1-AMC as substrate measured after 1 hr by fluorescence analysis | B | 5.79 | pIC50 | 1640 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4237-4240 [PMID:27491710] |
ChEMBL | Inhibition of human full-length recombinant SENP1 | B | 5.8 | pIC50 | 1600 | nM | IC50 | Eur J Med Chem (2022) 241: 114650-114650 [PMID:35939992] |
Ubiquitin carboxyl-terminal hydrolase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2406900] [UniProtKB: Q13107] | ||||||||
ChEMBL | Inhibition of human USP4 using Ub-AMC as substrate after 60 mins by fluorometric analysis | B | 5.82 | pIC50 | 1500 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 4328-4331 [PMID:23791076] |
ubiquitin specific peptidase 5/Ubiquitin carboxyl-terminal hydrolase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6158] [GtoPdb: 2431] [UniProtKB: P45974] | ||||||||
ChEMBL | Competitive inhibition of wild type human USP5 expressed in Escherichia coli BL21(DE3) using Ub-AMC as substrate | B | 4.9 | pKi | 12500 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 4328-4331 [PMID:23791076] |
ChEMBL | Inhibition of wild type human USP5 expressed in Escherichia coli BL21(DE3) using Ub-AMC as substrate after 60 mins by fluorometric analysis | B | 5.4 | pKi | 4000 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 4328-4331 [PMID:23791076] |
GtoPdb | - | - | 5.4 | pKi | 4000 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 4328-31 [PMID:23791076] |
ChEMBL | Inhibition of wild type human USP5 expressed in Escherichia coli BL21(DE3) using Ub-AMC as substrate after 60 mins by fluorometric analysis | B | 5.23 | pIC50 | 5900 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 4328-4331 [PMID:23791076] |
ubiquitin C-terminal hydrolase L1/Ubiquitin carboxyl-terminal hydrolase isozyme L1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6159] [GtoPdb: 2426] [UniProtKB: P09936] | ||||||||
ChEMBL | Inhibition of human UCH-L1 using Ub-AMC as substrate after 60 mins by fluorometric analysis | B | 4.65 | pIC50 | 22300 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 4328-4331 [PMID:23791076] |
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]