compound 2 [Maurer et al., 2012] [Ligand Id: 8823] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2203548
  • 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 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 recombinant SIRT1 using ZMAL substrate after 4 hrs by homogeneous fluorescence assay B 5.28 pIC50 5300 nM IC50 ACS Med Chem Lett (2012) 3: 1050-1053 [PMID:24900427]
ChEMBL Inhibition of sirtuin 1 (unknown origin) B 5.3 pIC50 5000 nM IC50 Eur J Med Chem (2019) 161: 48-77 [PMID:30342425]
sirtuin 2/NAD-dependent deacetylase sirtuin 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4462] [GtoPdb: 2708] [UniProtKB: Q8IXJ6]
ChEMBL Inhibition of sirtuin 2 (unknown origin) B 5 pIC50 10000 nM IC50 Eur J Med Chem (2019) 161: 48-77 [PMID:30342425]
ChEMBL Inhibition of recombinant SIRT2 using ZMAL substrate after 4 hrs by homogeneous fluorescence assay B 5.01 pIC50 9700 nM IC50 ACS Med Chem Lett (2012) 3: 1050-1053 [PMID:24900427]
ChEMBL Inhibition of human recombinant Sirt2 using ZMAL as substrate after 4 hrs by fluorescent deacetylase assay B 5.55 pIC50 2818.38 nM IC50 Medchemcomm (2012) 3: 167-173
ChEMBL Inhibition of human recombinant Sirt2 using ZMAL as substrate after 4 hrs by fluorescent deacetylase assay B 5.55 pIC50 2800 nM IC50 Medchemcomm (2012) 3: 167-173
sirtuin 5/NAD-dependent protein deacylase sirtuin-5, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2163183] [GtoPdb: 2711] [UniProtKB: Q9NXA8]
ChEMBL Inhibition of human recombinant N-terminal Strep2-tagged SIRT5 expressed in Escherichia coli BL21 (DE3) using Abz-GVLK(glutaryl)AY(NO2)GV-NH2 as substrate in presence of NAD+ by fluorescence assay B 4.6 pIC50 25200 nM IC50 J Med Chem (2018) 61: 2460-2471 [PMID:29494161]
ChEMBL Inhibition of SIRT5 using ZK(suc)A substrate after 1 hr by homogeneous fluorescence assay B 5.64 pIC50 2300 nM IC50 ACS Med Chem Lett (2012) 3: 1050-1053 [PMID:24900427]
GtoPdb - - 5.64 pIC50 2300 nM IC50 ACS Med Chem Lett (2012) 3: 1050-3 [PMID:24900427]

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]