AGK2 [Ligand Id: 8099] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL224864
  • sirtuin 1/NAD-dependent deacetylase sirtuin 1 in Human [ChEMBL: CHEMBL4506] [GtoPdb: 2707] [UniProtKB: Q96EB6]
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  • sirtuin 2/NAD-dependent deacetylase sirtuin 2 in Human [ChEMBL: CHEMBL4462] [GtoPdb: 2708] [UniProtKB: Q8IXJ6]
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  • sirtuin 3/NAD-dependent deacetylase sirtuin 3 in Human [ChEMBL: CHEMBL4461] [GtoPdb: 2709] [UniProtKB: Q9NTG7]
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  • sirtuin 5/NAD-dependent protein deacylase sirtuin-5, mitochondrial in Human [ChEMBL: CHEMBL2163183] [GtoPdb: 2711] [UniProtKB: Q9NXA8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 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 using fluorescent peptide substrate by fluorescent assay B 5.46 pIC50 3500 nM IC50 Science (2007) 317: 516-519 [PMID:17588900]
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 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 SIRT2 B 5.46 pIC50 3500 nM IC50 J Med Chem (2017) 60: 1928-1945 [PMID:28135086]
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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]