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ChEMBL ligand: CHEMBL257991 (SRT-1720) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]