splitomicin [Ligand Id: 8101] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL86537
  • Histone deacetylase in Plasmodium falciparum [ChEMBL: CHEMBL5541] [UniProtKB: Q9XYC7]
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  • histone deacetylase 3/Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) in Human [ChEMBL: CHEMBL2111363] [GtoPdb: 2617] [UniProtKB: O15379, Q9Y618]
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  • histone deacetylase 6/Histone deacetylase 6 in Human [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
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  • sirtuin 1/NAD-dependent deacetylase sirtuin 1 in Human [ChEMBL: CHEMBL4506] [GtoPdb: 2707] [UniProtKB: Q96EB6]
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  • NAD-dependent histone deacetylase SIR2 in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL3275] [UniProtKB: P06700]
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  • sirtuin 5/NAD-dependent protein deacylase sirtuin-5, mitochondrial in Human [ChEMBL: CHEMBL2163183] [GtoPdb: 2711] [UniProtKB: Q9NXA8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Histone deacetylase in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5541] [UniProtKB: Q9XYC7]
ChEMBL Inhibition of Plasmodium falciparum HDAC1 expressed in Drosophila melanogaster S2 cells B 5 pIC50 >10000 nM IC50 J Med Chem (2009) 52: 2185-2187 [PMID:19317450]
histone deacetylase 3/Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111363] [GtoPdb: 2617] [UniProtKB: O15379, Q9Y618]
ChEMBL Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from human HDAC3/NcoR2 by fluorescence polarization assay B 4.12 pKi >75000 nM Ki Bioorg Med Chem Lett (2008) 18: 2809-2812 [PMID:18430569]
ChEMBL Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from human HDAC3/NcoR2 by fluorescence polarization assay B 4.12 pIC50 >75000 nM IC50 Bioorg Med Chem Lett (2008) 18: 2809-2812 [PMID:18430569]
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
ChEMBL Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from human HDAC6 by fluorescence polarization assay B 4.12 pKi >75000 nM Ki Bioorg Med Chem Lett (2008) 18: 2809-2812 [PMID:18430569]
ChEMBL Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from human HDAC6 by fluorescence polarization assay B 4.12 pIC50 >75000 nM IC50 Bioorg Med Chem Lett (2008) 18: 2809-2812 [PMID:18430569]
sirtuin 1/NAD-dependent deacetylase sirtuin 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4506] [GtoPdb: 2707] [UniProtKB: Q96EB6]
ChEMBL Inhibition of human recombinant SIRT1 by Flour de Lys assay B 4.02 pIC50 96200 nM IC50 J Med Chem (2010) 53: 1407-1411 [PMID:20041717]
GtoPdb - - 4.02 pIC50 96200 nM IC50 J Med Chem (2010) 53: 1407-11 [PMID:20041717]
NAD-dependent histone deacetylase SIR2 in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3275] [UniProtKB: P06700]
ChEMBL In vitro inhibition of sirtuin 2 was evaluated using yeast whole cell lysates B 4.13 pIC50 74000 nM IC50 J Med Chem (2004) 47: 2635-2644 [PMID:15115404]
ChEMBL Inhibition of yeast Sir 2 protein B 4.22 pIC50 60000 nM IC50 Bioorg Med Chem Lett (2013) 23: 1351-1357 [PMID:23410798]
sirtuin 5/NAD-dependent protein deacylase sirtuin-5, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2163183] [GtoPdb: 2711] [UniProtKB: Q9NXA8]
ChEMBL Inhibition of human SIRT5 assessed as reduction in desuccinylase activity using KQTAR(SuK)STGGKA substrate B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (2015) 25: 1671-1674 [PMID:25818461]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 by [3H]hypoxanthine uptake F 5 pIC50 >10000 nM IC50 J Med Chem (2009) 52: 2185-2187 [PMID:19317450]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 assessed as growth inhibition after 24 hrs by measuring incorporation of [3H]-hypoxanthine by liquid scintillation counting method F 5 pIC50 >10000 nM IC50 J Med Chem (2017) 60: 4780-4804 [PMID:28241112]

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]