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 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]