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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] |
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]