FNDR-20123 [Ligand Id: 11797] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4090165
  • histone deacetylase 1/Histone deacetylase 1 in Human [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547]
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  • histone deacetylase 2/Histone deacetylase 2 in Human [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769]
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  • histone deacetylase 3/Histone deacetylase 3 in Human [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379]
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  • histone deacetylase 6/Histone deacetylase 6 in Human [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
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  • Plasmodium falciparum histone deacetylase 1 in Plasmodium falciparum TM90C2B [GtoPdb: 3072]
  • Plasmodium falciparum histone deacetylase 1 in Plasmodium falciparum [GtoPdb: 3072]
  • Plasmodium falciparum histone deacetylase 1 in Plasmodium falciparum K1 [GtoPdb: 3072]
  • Plasmodium falciparum histone deacetylase 1 in Plasmodium falciparum NF54 [GtoPdb: 3072]
  • Plasmodium falciparum histone deacetylase 1 in Plasmodium falciparum 3D7 [GtoPdb: 3072] [UniProtKB: Q7K6A1]
  • Plasmodium falciparum histone deacetylase 1 in Plasmodium falciparum 7G8 [GtoPdb: 3072]
  • Plasmodium falciparum histone deacetylase 1 in Plasmodium falciparum Dd2 [GtoPdb: 3072]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547]
ChEMBL Inhibition of recombinant human HDAC1 using Boc-Lys (Ac)-AMC substrate by fluorescence assay B 7.6 pIC50 25 nM IC50 Eur J Med Chem (2017) 135: 174-195 [PMID:28453994]
histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769]
ChEMBL Inhibition of recombinant human HDAC2 using Boc-Lys (Ac)-AMC substrate by fluorescence assay B 7.54 pIC50 29 nM IC50 Eur J Med Chem (2017) 135: 174-195 [PMID:28453994]
histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379]
ChEMBL Inhibition of recombinant human HDAC3 using Boc-Lys (Ac)-AMC substrate by fluorescence assay B 8.7 pIC50 2 nM IC50 Eur J Med Chem (2017) 135: 174-195 [PMID:28453994]
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
ChEMBL Inhibition of recombinant human HDAC8 using Boc-Lys (Ac)-AMC substrate by fluorescence assay B 6.55 pIC50 280 nM IC50 Eur J Med Chem (2017) 135: 174-195 [PMID:28453994]
ChEMBL Inhibition of recombinant human HDAC6 using Boc-Lys (Ac)-AMC substrate by fluorescence assay B 7.96 pIC50 11 nM IC50 Eur J Med Chem (2017) 135: 174-195 [PMID:28453994]
Plasmodium falciparum histone deacetylase 1 in Plasmodium falciparum TM90C2B [GtoPdb: 3072]
GtoPdb Parasite growth inhibition assay - 7.88 pIC50 13.26 nM IC50 Malar J (2020) 19: 365 [PMID:33046062]
Plasmodium falciparum histone deacetylase 1 in Plasmodium falciparum [GtoPdb: 3072]
GtoPdb Parasite dual gamete formation assay (DGFA) - 6.72 pIC50 190 nM IC50 Malar J (2020) 19: 365 [PMID:33046062]
Plasmodium falciparum histone deacetylase 1 in Plasmodium falciparum K1 [GtoPdb: 3072]
GtoPdb Parasite growth inhibition assay - 7.72 pIC50 19.05 nM IC50 Malar J (2020) 19: 365 [PMID:33046062]
Plasmodium falciparum histone deacetylase 1 in Plasmodium falciparum NF54 [GtoPdb: 3072]
GtoPdb Parasite growth inhibition assay - 7.6 pIC50 25.27 nM IC50 Malar J (2020) 19: 365 [PMID:33046062]
Plasmodium falciparum histone deacetylase 1 in Plasmodium falciparum 3D7 [GtoPdb: 3072] [UniProtKB: Q7K6A1]
GtoPdb Parasite growth inhibition assay - 7.39 pIC50 41 nM IC50 Malar J (2020) 19: 365 [PMID:33046062]
Plasmodium falciparum histone deacetylase 1 in Plasmodium falciparum 7G8 [GtoPdb: 3072]
GtoPdb Parasite growth inhibition assay - 7.84 pIC50 14.36 nM IC50 Malar J (2020) 19: 365 [PMID:33046062]
Plasmodium falciparum histone deacetylase 1 in Plasmodium falciparum Dd2 [GtoPdb: 3072]
GtoPdb Parasite growth inhibition assay - 7.76 pIC50 17.5 nM IC50 Malar J (2020) 19: 365 [PMID:33046062]

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]