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ChEMBL ligand: CHEMBL224864 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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sirtuin 1/NAD-dependent deacetylase sirtuin 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4506] [GtoPdb: 2707] [UniProtKB: Q96EB6] | ||||||||
ChEMBL | Inhibition of N-terminal His-tagged recombinant human SIRT-1 expressed in Escherichia coli using Fluor-de-Lys-SIRT1 as substrate after 15 mins by fluorescence assay | B | 4.01 | pIC50 | 98100 | nM | IC50 | J Med Chem (2017) 60: 4714-4733 [PMID:28475330] |
ChEMBL | Inhibition of recombinant human N-terminal GST-tagged SIRT1 (193 to 741 residues) using human p53 derived peptides as substrate incubated for 45 mins by fluorescence assay | B | 4.17 | pIC50 | 68000 | nM | IC50 | Medchemcomm (2015) 6: 1857-1863 |
ChEMBL | Inhibition of human recombinant SIRT1 using fluorescent peptide substrate by fluorescent assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Science (2007) 317: 516-519 [PMID:17588900] |
ChEMBL | Inhibition of human recombinant SIRT1 by Flour de Lys assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2010) 53: 1407-1411 [PMID:20041717] |
ChEMBL | Inhibition of human SIRT1 | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem (2015) 23: 328-339 [PMID:25515955] |
ChEMBL | Inhibition of human SIRT1 | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2017) 60: 1928-1945 [PMID:28135086] |
ChEMBL | Inhibition of human recombinant SIRT1 expressed in Escherichia coli cells using acetylated Lys side chain amino acids 379-382 (Arg-His-Lys-Lys(Ac)) p53 conjugated with aminomethylcoumarin as substrate by fluorescence assay | B | 4.42 | pIC50 | 38000 | nM | IC50 | J Med Chem (2012) 55: 8193-8197 [PMID:22931526] |
ChEMBL | Inhibition of human recombinant SIRT1 using Fluor-de-Lys as substrate incubated for 60 mins prior to substrate addition measured after 60 mins by fluorometric analysis | B | 4.52 | pIC50 | 30000 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 1871-1874 [PMID:24675380] |
ChEMBL | Inhibition of human recombinant SIRT1 using Fluor de Lys-SIRT as substrate incubated for 60 mins prior to substrate addition measured after 60 mins by fluorimetric analysis | B | 4.52 | pIC50 | 30000 | nM | IC50 | J Med Chem (2012) 55: 5760-5773 [PMID:22642300] |
sirtuin 2/NAD-dependent deacetylase sirtuin 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4462] [GtoPdb: 2708] [UniProtKB: Q8IXJ6] | ||||||||
ChEMBL | Inhibition of GST-tagged SIRT2 (unknown origin) by HPLC assay | B | 4.26 | pIC50 | 55000 | nM | IC50 | Medchemcomm (2010) 1: 233-238 |
ChEMBL | Inhibition of human recombinant SIRT2 assessed as deacetylation of N-acetyl lysine residue in p53 (317 to 320) after 30 mins by luciferase-mediated luminescence assay | B | 4.86 | pIC50 | 13900 | nM | IC50 | Eur J Med Chem (2015) 92: 145-155 [PMID:25549554] |
ChEMBL | Inhibition of human recombinant SIRT2 using AMC-p53 (317 to 320 residues) as substrate incubated for 45 mins followed by NAD+ addition measured after 30 mins by fluorescence assay | B | 5.08 | pIC50 | 8340 | nM | IC50 | Medchemcomm (2016) 7: 2094-2099 |
ChEMBL | Inhibition of human recombinant SIRT2 using p53 (317 to 320 residues) conjugated to AMC as substrate incubated for 45 mins in presence of NAD+ by fluorescence assay | B | 5.08 | pIC50 | 8340 | nM | IC50 | Medchemcomm (2019) 10: 2140-2145 [PMID:32904142] |
ChEMBL | Inhibition of recombinant human C-terminal His-tagged SIRT2 (13 to 319 residues) using human p53 derived peptides as substrate incubated for 45 mins by fluorescence assay | B | 5.1 | pIC50 | 7900 | nM | IC50 | Medchemcomm (2015) 6: 1857-1863 |
ChEMBL | Inhibition of human recombinant SIRT2 expressed in Escherichia coli cells using acetylated Lys side chain amino acids 379-382 (Arg-His-Lys-Lys(Ac)) p53 conjugated with aminomethylcoumarin as substrate by fluorescence assay | B | 5.26 | pIC50 | 5500 | nM | IC50 | J Med Chem (2012) 55: 8193-8197 [PMID:22931526] |
ChEMBL | Inhibition of human recombinant SIRT2 by Flour de Lys assay | B | 5.45 | pIC50 | 3540 | nM | IC50 | J Med Chem (2010) 53: 1407-1411 [PMID:20041717] |
ChEMBL | Inhibition of human recombinant SIRT2 | B | 5.46 | pIC50 | 3500 | nM | IC50 | Bioorg Med Chem (2015) 23: 328-339 [PMID:25515955] |
ChEMBL | Inhibition of human SIRT2 | B | 5.46 | pIC50 | 3500 | nM | IC50 | J Med Chem (2017) 60: 1928-1945 [PMID:28135086] |
ChEMBL | Inhibition of SIRT-2 (unknown origin) | B | 5.46 | pIC50 | 3500 | nM | IC50 | Medchemcomm (2012) 3: 135-161 |
ChEMBL | Inhibition of SirT2 | B | 5.46 | pIC50 | 3500 | nM | IC50 | Nat Chem Biol (2008) 4: 590-597 [PMID:18800048] |
ChEMBL | Inhibition of SIRT2 | B | 5.46 | pIC50 | 3500 | nM | IC50 | Bioorg Med Chem (2011) 19: 3616-3624 [PMID:21306906] |
ChEMBL | Inhibition of Sirt2 | B | 5.46 | pIC50 | 3500 | nM | IC50 | Bioorg Med Chem (2011) 19: 3605-3615 [PMID:21316248] |
ChEMBL | Inhibition of human recombinant SIRT2 using Fluor de Lys-SIRT as substrate incubated for 60 mins prior to substrate addition measured after 60 mins by fluorimetric analysis | B | 5.46 | pIC50 | 3500 | nM | IC50 | J Med Chem (2012) 55: 5760-5773 [PMID:22642300] |
ChEMBL | Inhibition of human recombinant SIRT2 using Fluor-de-Lys as substrate incubated for 60 mins prior to substrate addition measured after 60 mins by fluorometric analysis | B | 5.46 | pIC50 | 3500 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 1871-1874 [PMID:24675380] |
ChEMBL | Inhibition of human recombinant SIRT2 using fluorescent peptide substrate by fluorescent assay | B | 5.46 | pIC50 | 3500 | nM | IC50 | Science (2007) 317: 516-519 [PMID:17588900] |
ChEMBL | Inhibition of GST-tagged human recombinant SIRT2 (34 to 356 residues) expressed in Escherichia coli BL21 using Fluor de Lys-SIRT as substrate incubated for 60 mins prior to substrate addition measured after 45 mins by fluorimetric analysis | B | 5.52 | pIC50 | 3000 | nM | IC50 | Bioorg Med Chem (2015) 23: 328-339 [PMID:25515955] |
ChEMBL | Inhibition of N-terminal His-tagged recombinant human SIRT-2 expressed in Escherichia coli using Fluor-de-Lys-SIRT1 as substrate after 15 mins by fluorescence assay | B | 5.55 | pIC50 | 2800 | nM | IC50 | J Med Chem (2017) 60: 4714-4733 [PMID:28475330] |
ChEMBL | Inhibition of full length human SIRT2 expressed in Escherichia coli BL21 (DE3) cells using fluorogenic 7-amino-4-methylcoumarin (AMC)-labeled peptide by fluorescence assay | B | 5.81 | pIC50 | 1560 | nM | IC50 | J Med Chem (2014) 57: 8340-8357 [PMID:25275824] |
GtoPdb | - | - | 5.81 | pIC50 | 1560 | nM | IC50 |
Science (2007) 317: 516-9 [PMID:17588900]; J Med Chem (2014) 57: 8340-57 [PMID:25275824] |
sirtuin 3/NAD-dependent deacetylase sirtuin 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4461] [GtoPdb: 2709] [UniProtKB: Q9NTG7] | ||||||||
ChEMBL | Inhibition of human recombinant SIRT3 using Fluor de Lys-SIRT as substrate incubated for 60 mins prior to substrate addition measured after 60 mins by fluorimetric analysis | B | 4.04 | pIC50 | 91000 | nM | IC50 | J Med Chem (2012) 55: 5760-5773 [PMID:22642300] |
ChEMBL | Inhibition of human recombinant SIRT3 using Fluor-de-Lys as substrate incubated for 60 mins prior to substrate addition measured after 60 mins by fluorometric analysis | B | 4.04 | pIC50 | 91000 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 1871-1874 [PMID:24675380] |
ChEMBL | Inhibition of catalytically active human SIRT3 (102 to 399 amino acids) expressed in Escherichia coli BL21 (DE3) cells using fluorogenic 7-amino-4-methylcoumarin (AMC)-labeled peptide by fluorescence assay | B | 4.28 | pIC50 | 52800 | nM | IC50 | J Med Chem (2014) 57: 8340-8357 [PMID:25275824] |
ChEMBL | Inhibition of human recombinant SIRT3 using fluorescent peptide substrate by fluorescent assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Science (2007) 317: 516-519 [PMID:17588900] |
ChEMBL | Inhibition of human SIRT3 | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem (2015) 23: 328-339 [PMID:25515955] |
sirtuin 5/NAD-dependent protein deacylase sirtuin-5, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2163183] [GtoPdb: 2711] [UniProtKB: Q9NXA8] | ||||||||
ChEMBL | Inhibition of SIRT5 | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2012) 55: 5582-5590 [PMID:22583019] |
ChEMBL | Inhibition of human SIRT5 assessed as reduction in desuccinylase activity using KQTAR(SuK)STGGKA substrate | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 1671-1674 [PMID:25818461] |
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]