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]
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 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]