abexinostat [Ligand Id: 8366] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2103863 (Abexinostat, PZP-115891, CRA-024781, PCI-24781, CRA 024781, S78454, CRA 24781, PCI 24781, PZP115891, S-78454)
  • histone deacetylase 1/Histone deacetylase 1 in Human [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547]
  • 8.08
1 CHEMBL2103863_lig_chart_1 Histone deacetylase 1 Human
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  • histone deacetylase 10/Histone deacetylase 10 in Human [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8]
  • 7.66
2 CHEMBL2103863_lig_chart_2 Histone deacetylase 10 Human
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  • histone deacetylase 2/Histone deacetylase 2 in Human [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769]
  • 7.71
3 CHEMBL2103863_lig_chart_3 Histone deacetylase 2 Human
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  • histone deacetylase 3/Histone deacetylase 3 in Human [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379]
  • 8.04
4 CHEMBL2103863_lig_chart_4 Histone deacetylase 3 Human
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  • histone deacetylase 6/Histone deacetylase 6 in Human [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
  • 7.73
5 CHEMBL2103863_lig_chart_5 Histone deacetylase 6 Human
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  • histone deacetylase 8/Histone deacetylase 8 in Human [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41]
  • 6.55
6 CHEMBL2103863_lig_chart_6 Histone deacetylase 8 Human
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  • Leukotriene A4 hydrolase/Leukotriene A4 hydrolase in Human [ChEMBL: CHEMBL4618] [GtoPdb: 1395] [UniProtKB: P09960]
  • This target only has 0 pki data point
  • 0
7 CHEMBL2103863_lig_chart_7 Leukotriene A4 hydrolase Human
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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 HDAC1 (unknown origin) B 8 pKi 10 nM Ki Eur J Med Chem (2017) 135: 174-195 [PMID:28453994]
ChEMBL Inhibition of human HDAC1 B 8.15 pKi 7 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
GtoPdb - - 8.15 pIC50 7 nM IC50 Mol Cancer Ther (2006) 5: 1309-17 [PMID:16731764]
histone deacetylase 10/Histone deacetylase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8]
ChEMBL Inhibition of human HDAC10 B 7.62 pKi 24 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
ChEMBL Inhibition of HDAC10 (unknown origin) B 7.7 pKi 20 nM Ki Eur J Med Chem (2017) 135: 174-195 [PMID:28453994]
ChEMBL Inhibition of dye-labeled tracer binding to HDAC10 (unknown origin) transfected in human HeLa cells measured after 2 hrs by nano-luciferase reporter gene-based BRET assay B 8.1 pIC50 7.94 nM IC50 J Med Chem (2019) 62: 4426-4443 [PMID:30964290]
ChEMBL Inhibition of tubastatin-Alexa647-tracer binding to recombinant GST-tagged HDAC10 (unknown origin) measured after 1 hr by TR-FRET assay B 8.4 pIC50 3.98 nM IC50 J Med Chem (2019) 62: 4426-4443 [PMID:30964290]
histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769]
ChEMBL Inhibition of HDAC2 (unknown origin) B 7.7 pKi 20 nM Ki Eur J Med Chem (2017) 135: 174-195 [PMID:28453994]
ChEMBL Inhibition of human HDAC2 B 7.72 pKi 19 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379]
ChEMBL Inhibition of HDAC3 (unknown origin) B 8 pKi 10 nM Ki Eur J Med Chem (2017) 135: 174-195 [PMID:28453994]
ChEMBL Inhibition of human HDAC3 B 8.09 pKi 8.2 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
GtoPdb - - 8.09 pIC50 8.2 nM IC50 Mol Cancer Ther (2006) 5: 1309-17 [PMID:16731764]
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
ChEMBL Inhibition of HDAC6 (unknown origin) B 7.7 pKi 20 nM Ki Eur J Med Chem (2017) 135: 174-195 [PMID:28453994]
ChEMBL Inhibition of human HDAC6 B 7.77 pKi 17 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
histone deacetylase 8/Histone deacetylase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41]
ChEMBL Inhibition of human HDAC8 B 6.55 pKi 280 nM Ki Bioorg. Med. Chem. (2015) 23: 5151-5155 [PMID:25637120]
ChEMBL Inhibition of HDAC8 (unknown origin) B 6.55 pKi 280 nM Ki Eur J Med Chem (2017) 135: 174-195 [PMID:28453994]
Leukotriene A4 hydrolase/Leukotriene A4 hydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4618] [GtoPdb: 1395] [UniProtKB: P09960]
ChEMBL Inhibition of recombinant human LTA4H Epoxide Hydrolase expressed in Escherichia coli BL21 (DE3) pLysS preincubated for 10 mins followed by addition of LTA4 as substrate measured after 15 mins by reverse-phase HPLC analysis B 5 pIC50 >10000 nM IC50 J Med Chem (2017) 60: 1817-1828 [PMID:28218840]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]