ChEMBL ligand: CHEMBL224864
sirtuin 1/NAD-dependent deacetylase sirtuin 1 in Human [ChEMBL: CHEMBL4506] [GtoPdb: 2707] [UniProtKB: Q96EB6] There should be some charts here, you may need to enable JavaScript!
sirtuin 2/NAD-dependent deacetylase sirtuin 2 in Human [ChEMBL: CHEMBL4462] [GtoPdb: 2708] [UniProtKB: Q8IXJ6] There should be some charts here, you may need to enable JavaScript!
sirtuin 3/NAD-dependent deacetylase sirtuin 3 in Human [ChEMBL: CHEMBL4461] [GtoPdb: 2709] [UniProtKB: Q9NTG7] There should be some charts here, you may need to enable JavaScript!
sirtuin 5/NAD-dependent protein deacylase sirtuin-5, mitochondrial in Human [ChEMBL: CHEMBL2163183] [GtoPdb: 2711] [UniProtKB: Q9NXA8] 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
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 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]