apicidin [Ligand Id: 7495] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL430060 (Acipidin)
There should be some charts here, you may need to enable JavaScript!
  • Histone deacetylase in Cryptosporidium parvum [ChEMBL: CHEMBL4740] [UniProtKB: Q7YY07]
  • Histone deacetylase in Plasmodium falciparum [ChEMBL: CHEMBL5541] [UniProtKB: Q9XYC7]
There should be some charts here, you may need to enable JavaScript!
  • histone deacetylase 1/Histone deacetylase 1 in Human [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547]
There should be some charts here, you may need to enable JavaScript!
  • histone deacetylase 2/Histone deacetylase 2 in Human [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769]
There should be some charts here, you may need to enable JavaScript!
  • histone deacetylase 3/Histone deacetylase 3 in Human [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379]
There should be some charts here, you may need to enable JavaScript!
  • histone deacetylase 3/Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) in Human [ChEMBL: CHEMBL2111363] [GtoPdb: 2617] [UniProtKB: O15379Q9Y618]
There should be some charts here, you may need to enable JavaScript!
  • histone deacetylase 4/Histone deacetylase 4 in Human [ChEMBL: CHEMBL3524] [GtoPdb: 2659] [UniProtKB: P56524]
There should be some charts here, you may need to enable JavaScript!
  • histone deacetylase 6/Histone deacetylase 6 in Human [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
There should be some charts here, you may need to enable JavaScript!
  • histone deacetylase 8/Histone deacetylase 8 in Human [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41]
There should be some charts here, you may need to enable JavaScript!
  • Histone deacetylase-like amidohydrolase in Alcaligenes sp. (strain DSM 11172) (Bordetella sp. (strain FB188)) [ChEMBL: CHEMBL6017] [UniProtKB: Q70I53]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Coagulation factor III in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4081] [UniProtKB: P13726]
ChEMBL Inhibition of TNF-alpha-induced tissue factor activity in HUVEC preincubated for 4 hrs assessed after 4 hrs of TNFalpha challenge by one stage clotting assay B 6.7 pIC50 200 nM IC50 J. Biol. Chem. (2007) 282: 28408-28418 [PMID:17675290]
ChEMBL Inhibition of LPS-induced tissue factor activity in HUVEC preincubated for 4 hrs assessed after 4 hrs of LPS challenge by one stage clotting assay B 6.82 pIC50 150 nM IC50 J. Biol. Chem. (2007) 282: 28408-28418 [PMID:17675290]
Histone deacetylase in Cryptosporidium parvum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4740] [UniProtKB: Q7YY07]
ChEMBL Binding affinity towards HDAC enzyme derived from Eimeria tenella protozoa B 8.1 pKi 8 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 113-117 [PMID:11206439]
ChEMBL Tested for Histone deacetylase enzyme inhibition assay using Eimeria tenella extract B 9 pIC50 1 nM IC50 J. Med. Chem. (2000) 43: 4919-4922 [PMID:11124001]
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 9 pIC50 1 nM IC50 J. Med. Chem. (2009) 52: 2185-2187 [PMID:19317450]
histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547]
ChEMBL Inhibition of human HDAC1 B 10.4 pKi 0.04 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
GtoPdb - - 10.4 pKi 0.04 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of HDAC1 (mean IC50) B 7.36 pIC50 44 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 5948-5952 [PMID:16987657]
ChEMBL Inhibition of HDAC1 B 7.36 pIC50 44 nM IC50 J. Med. Chem. (2008) 51: 2350-2353 [PMID:18370373]
ChEMBL Inhibition of human recombinant C-terminally flag tagged HDAC1 B 7.36 pIC50 44 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 5528-5532 [PMID:18809328]
ChEMBL Inhibition of C-terminal FLAG tagged HDAC1 B 7.36 pIC50 44 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 3081-3084 [PMID:19410459]
ChEMBL Inhibition of HDAC1 in human NIH3T3 cells by radiometric histone deacetylation assay B 7.36 pIC50 44 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 3651-3656 [PMID:19457659]
ChEMBL Inhibition of HDAC1 in HEK293 cells B 7.64 pIC50 23 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 1814-1819 [PMID:18308563]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.66 pIC50 22 nM IC50 Bioorg Med Chem Lett (2017) 27: 3289-3293 [PMID:28648462]
ChEMBL Inhibition of human recombinant HDAC1 after 30 mins by fluorimetric assay B 7.66 pIC50 22 nM IC50 J. Med. Chem. (2009) 52: 7836-7846 [PMID:19705846]
ChEMBL Inhibition of HDAC1 in human HeLa cells nuclear extract using Fluor-de-Lys as substrate after 30 mins by spectrophotometry B 7.66 pIC50 22 nM IC50 ACS Med. Chem. Lett. (2011) 2: 703-707 [PMID:21984958]
ChEMBL Inhibition of HDAC1 B 7.89 pIC50 13 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 2549-2554 [PMID:18381239]
ChEMBL Inhibition of human recombinant HDAC1 using Ac-Lys(Ac)-7-amino-4-methylcoumarin as substrate after 30 mins by trypsin-coupled fluorogenic assay B 7.96 pIC50 11 nM IC50 ACS Med. Chem. Lett. (2012) 3: 749-753 [PMID:24900543]
ChEMBL Inhibition of HDAC1 B 9.15 pIC50 0.7 nM IC50 Bioorg. Med. Chem. (2010) 18: 4103-4110 [PMID:20472442]
histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769]
GtoPdb - - 9.92 pKi 0.12 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human HDAC2 B 9.92 pKi 0.12 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of recombinant HDAC2 using Ac-Lys(Ac)-AMC as substrate after 30 mins by fluorescence analysis B 7.46 pIC50 35 nM IC50 ACS Med. Chem. Lett. (2012) 3: 505-508 [PMID:24900500]
ChEMBL Inhibition of HDAC2 (unknown origin) B 7.46 pIC50 35 nM IC50 Bioorg Med Chem Lett (2017) 27: 3289-3293 [PMID:28648462]
ChEMBL Inhibition of human recombinant HDAC2 using Ac-Lys(Ac)-7-amino-4-methylcoumarin as substrate after 30 mins by trypsin-coupled fluorogenic assay B 7.47 pIC50 34 nM IC50 ACS Med. Chem. Lett. (2012) 3: 749-753 [PMID:24900543]
ChEMBL Inhibition of HDAC2 B 9 pIC50 1 nM IC50 Bioorg. Med. Chem. (2010) 18: 4103-4110 [PMID:20472442]
GtoPdb - - 6.92 pEC50 120 nM EC50 Biochem. J. (2008) 409: 581-9 [PMID:17868033]
histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379]
ChEMBL Inhibition of human HDAC3 B 9.59 pKi 0.26 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
GtoPdb - - 9.59 pKi 0.26 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human recombinant HDAC3 after 30 mins by fluorimetric assay B 7.54 pIC50 29 nM IC50 J. Med. Chem. (2009) 52: 7836-7846 [PMID:19705846]
ChEMBL Inhibition of HDAC3 (unknown origin) B 7.54 pIC50 29 nM IC50 Bioorg Med Chem Lett (2017) 27: 3289-3293 [PMID:28648462]
ChEMBL Inhibition of HDAC3 in HEK293 cells B 8.01 pIC50 9.7 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 1814-1819 [PMID:18308563]
ChEMBL Inhibition of flag-tagged HDAC3 B 8.6 pIC50 2.5 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 17335-17340 [PMID:17956988]
ChEMBL Inhibition of HDAC3 B 9.22 pIC50 0.6 nM IC50 Bioorg. Med. Chem. (2010) 18: 4103-4110 [PMID:20472442]
GtoPdb - - 7.37 pEC50 43 nM EC50 Biochem. J. (2008) 409: 581-9 [PMID:17868033]
GtoPdb - - 7.52 pEC50 30 nM EC50 Biochem. J. (2008) 409: 581-9 [PMID:17868033]
histone deacetylase 3/Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111363] [GtoPdb: 2617] [UniProtKB: O15379Q9Y618]
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 8.82 pKi 1.5 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 2809-2812 [PMID:18430569]
GtoPdb - - 9.59 pKi 0.26 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of HDAC3-NCoR2 in human HeLa cells nuclear extract using Fluor-de-Lys as substrate after 30 mins by spectrophotometry B 7.54 pIC50 29 nM IC50 ACS Med. Chem. Lett. (2011) 2: 703-707 [PMID:21984958]
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 7.8 pIC50 15.8 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 2809-2812 [PMID:18430569]
ChEMBL Inhibition of human recombinant HDAC3/NCoR2 using Ac-Lys(Ac)-7-amino-4-methylcoumarin as substrate after 30 mins by trypsin-coupled fluorogenic assay B 7.89 pIC50 13 nM IC50 ACS Med. Chem. Lett. (2012) 3: 749-753 [PMID:24900543]
GtoPdb - - 7.37 pEC50 43 nM EC50 Biochem. J. (2008) 409: 581-9 [PMID:17868033]
GtoPdb - - 7.52 pEC50 30 nM EC50 Biochem. J. (2008) 409: 581-9 [PMID:17868033]
histone deacetylase 4/Histone deacetylase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3524] [GtoPdb: 2659] [UniProtKB: P56524]
ChEMBL Inhibition of wild type HDAC4 expressed in Escherichia coli B 5.06 pIC50 8700 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 1814-1819 [PMID:18308563]
ChEMBL Inhibition of flag-tagged HDAC4 by pull-down assay B 8.62 pIC50 2.4 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 17335-17340 [PMID:17956988]
ChEMBL Inhibition of flag-tagged HDAC4 by Biomol assay B 8.92 pIC50 1.2 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 17335-17340 [PMID:17956988]
ChEMBL Inhibition of flag-tagged HDAC4 B 9 pIC50 1 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 17335-17340 [PMID:17956988]
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 6.91 pKi 123.4 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 2809-2812 [PMID:18430569]
ChEMBL Inhibition of HDAC6 in human HeLa cells nuclear extract using Fluor-de-Lys as substrate after 30 mins by spectrophotometry B 5 pIC50 >10000 nM IC50 ACS Med. Chem. Lett. (2011) 2: 703-707 [PMID:21984958]
ChEMBL Inhibition of HDAC6 (unknown origin) B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2017) 27: 3289-3293 [PMID:28648462]
ChEMBL Inhibition of human recombinant HDAC6 after 30 mins by fluorimetric assay B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2009) 52: 7836-7846 [PMID:19705846]
ChEMBL Inhibition of human recombinant HDAC6 using Ac-Lys(Ac)-7-amino-4-methylcoumarin as substrate after 30 mins by trypsin-coupled fluorogenic assay B 5 pIC50 >10000 nM IC50 ACS Med. Chem. Lett. (2012) 3: 749-753 [PMID:24900543]
ChEMBL Inhibition of HDAC6 B 5.02 pIC50 9600 nM IC50 Bioorg. Med. Chem. (2010) 18: 4103-4110 [PMID:20472442]
ChEMBL Inhibition of HDAC6 in HEK293 cells B 5.37 pIC50 4300 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 1814-1819 [PMID:18308563]
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 6.18 pIC50 665.1 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 2809-2812 [PMID:18430569]
histone deacetylase 8/Histone deacetylase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41]
ChEMBL Activity of human HDAC8 B 7.31 pKi 49 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
GtoPdb - - 7.31 pKi 49 nM Ki Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of human recombinant HDAC8 after 30 mins by fluorimetric assay B 6.12 pIC50 760 nM IC50 J. Med. Chem. (2009) 52: 7836-7846 [PMID:19705846]
ChEMBL Inhibition of HDAC8 (unknown origin) B 6.12 pIC50 760 nM IC50 Bioorg Med Chem Lett (2017) 27: 3289-3293 [PMID:28648462]
ChEMBL Inhibition of HDAC8 in human HeLa cells nuclear extract using Arg-His-Lys(Ac)-Lys(Ac)-AMC as substrate after 30 mins by spectrophotometry B 6.12 pIC50 755 nM IC50 ACS Med. Chem. Lett. (2011) 2: 703-707 [PMID:21984958]
ChEMBL Inhibition of human recombinant HDAC8 using Arg-His-Lys(Ac)-Lys(Ac)-AMC as substrate after 30 mins by trypsin-coupled fluorogenic assay B 6.12 pIC50 750 nM IC50 ACS Med. Chem. Lett. (2012) 3: 749-753 [PMID:24900543]
ChEMBL Inhibition of HDAC8 B 6.52 pIC50 300 nM IC50 Bioorg. Med. Chem. (2010) 18: 4103-4110 [PMID:20472442]
GtoPdb - - 6.24 pEC50 575 nM EC50 Biochem. J. (2008) 409: 581-9 [PMID:17868033]
Histone deacetylase-like amidohydrolase in Alcaligenes sp. (strain DSM 11172) (Bordetella sp. (strain FB188)) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6017] [UniProtKB: Q70I53]
ChEMBL Displacement of Atto700-HA from Bordetella / Alcaligenes strain FB188 HDAH by fluorescence anisotropy B 5.04 pKi 9200 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 3651-3656 [PMID:19457659]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 assessed as parasite growth inhibition after 48 hrs by light microscopic analysis F 6.7 pIC50 200 nM IC50 J. Nat. Prod. (2013) 76: 2136-2140 [PMID:24195442]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 by [3H]hypoxanthine uptake F 7.48 pIC50 33 nM IC50 J. Med. Chem. (2009) 52: 2185-2187 [PMID:19317450]

ChEMBL data shown on this page come from version 25:

A.P. Bento, A. Gaulton, A. Hersey, et al. (2014). The ChEMBL bioactivity database: an update. Nucl. Acids Res. Database Issue. 42 D1083-D1090. [PMID:24214965]