AKK(thioAc)LM21 [Ligand Id: 8816] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL504711 |
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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 preincubated for 5 mins before addition of substrate measured after 1 hr by fluorescence-based assay | B | 6.42 | pIC50 | 380 | nM | IC50 | J Med Chem (2009) 52: 2153-2156 [PMID:19296597] |
| sirtuin 2/NAD-dependent deacetylase sirtuin 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4462] [GtoPdb: 2708] [UniProtKB: Q8IXJ6] | ||||||||
| ChEMBL | Inhibition of recombinant SIRT2 preincubated for 5 mins before addition of substrate measured after 3 hrs by fluorescence-based assay | B | 5.07 | pIC50 | 8500 | nM | IC50 | J Med Chem (2009) 52: 2153-2156 [PMID:19296597] |
| sirtuin 6/NAD-dependent protein deacetylase sirtuin-6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2163182] [GtoPdb: 2712] [UniProtKB: Q8N6T7] | ||||||||
| ChEMBL | Inhibition of human recombinant SIRT6 assessed as 7-amino-4-methylcoumarin labelled Arg-His-Lys-Lys(epsilon-acetyl) substrate deacetylation after 90 mins by Fluor-de-Lys assay | B | 4.33 | pIC50 | 47000 | nM | IC50 | ACS Med Chem Lett (2012) 3: 969-974 [PMID:24900419] |
| GtoPdb | - | - | 4.33 | pIC50 | 47000 | nM | IC50 | ACS Med Chem Lett (2012) 3: 969-74 [PMID:24900419] |
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]
