SRT1720 [Ligand Id: 7703] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL257991 (SRT-1720)
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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  • 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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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Inhibition of adrenergic alpha2A receptor B 5.55 pIC50 2830 nM IC50 J Med Chem (2009) 52: 1275-1283 [PMID:19199480]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG by patch clamp method B 5 pIC50 >10000 nM IC50 J Med Chem (2009) 52: 1275-1283 [PMID:19199480]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL Inhibition of muscarinic M1 receptor B 5.1 pIC50 8020 nM IC50 J Med Chem (2009) 52: 1275-1283 [PMID:19199480]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Inhibition of muscarinic M2 receptor B 5.2 pIC50 6280 nM IC50 J Med Chem (2009) 52: 1275-1283 [PMID:19199480]
sirtuin 1/NAD-dependent deacetylase sirtuin 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4506] [GtoPdb: 2707] [UniProtKB: Q96EB6]
ChEMBL Activation of human SIRT1 expressed in Escherichia coli BL21 by mass spectrometry assay B 6.8 pEC50 160 nM EC50 Nature (2007) 450: 712-716 [PMID:18046409]
ChEMBL Activation of N-terminal His6-tagged SIRT1 (156 to 664 amino acid residues) (unknown origin) expressed in Escherichia coli BL21(DE3) using ac-RHKKac-AMC as substrate after 45 mins by fluorometric analysis B 6.8 pEC50 160 nM EC50 J Med Chem (2013) 56: 761-780 [PMID:23316803]
ChEMBL Inhibition of SIRT1 (unknown origin) B 6.8 pEC50 160 nM EC50 Eur J Med Chem (2021) 226: 113867-113867 [PMID:34607244]
GtoPdb - - 6.8 pEC50 160 nM EC50 Nature (2007) 450: 712-6 [PMID:18046409]
sirtuin 2/NAD-dependent deacetylase sirtuin 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4462] [GtoPdb: 2708] [UniProtKB: Q8IXJ6]
ChEMBL Activation of SIRT2 by mass spectrometry assay B 4.43 pEC50 37000 nM EC50 Nature (2007) 450: 712-716 [PMID:18046409]
ChEMBL Activation of human SirT2 protein fluorescence polarization assay B 6.8 pEC50 160 nM EC50 Nat Chem Biol (2008) 4: 590-597 [PMID:18800048]
sirtuin 3/NAD-dependent deacetylase sirtuin 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4461] [GtoPdb: 2709] [UniProtKB: Q9NTG7]
ChEMBL Inhibition of SIRT3 (unknown origin) B 6.07 pIC50 850 nM IC50 Eur J Med Chem (2017) 134: 230-241 [PMID:28415012]
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL Inhibition of norepinephrine transporter B 5.61 pIC50 2470 nM IC50 J Med Chem (2009) 52: 1275-1283 [PMID:19199480]

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]