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

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ChEMBL ligand: CHEMBL2103863 (Abexinostat, CRA 024781, CRA-024781, CRA 24781, PCI 24781, PCI-24781, PZP115891, PZP-115891, S78454, S-78454)
  • histone deacetylase 1/Histone deacetylase 1 in Human [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547]
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  • histone deacetylase 10/Histone deacetylase 10 in Human [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8]
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  • histone deacetylase 11/Histone deacetylase 11 in Human [ChEMBL: CHEMBL3310] [GtoPdb: 2615] [UniProtKB: Q96DB2]
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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 3/Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) in Human [ChEMBL: CHEMBL2111363] [GtoPdb: 2617] [UniProtKB: O15379Q9Y618]
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  • histone deacetylase 4/Histone deacetylase 4 in Human [ChEMBL: CHEMBL3524] [GtoPdb: 2659] [UniProtKB: P56524]
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  • histone deacetylase 5/Histone deacetylase 5 in Human [ChEMBL: CHEMBL2563] [GtoPdb: 2660] [UniProtKB: Q9UQL6]
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  • histone deacetylase 6/Histone deacetylase 6 in Human [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
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  • histone deacetylase 7/Histone deacetylase 7 in Human [ChEMBL: CHEMBL2716] [GtoPdb: 2661] [UniProtKB: Q8WUI4]
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  • histone deacetylase 8/Histone deacetylase 8 in Human [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41]
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  • histone deacetylase 9/Histone deacetylase 9 in Human [ChEMBL: CHEMBL4145] [GtoPdb: 2620] [UniProtKB: Q9UKV0]
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  • Leukotriene A4 hydrolase/Leukotriene A4 hydrolase in Human [ChEMBL: CHEMBL4618] [GtoPdb: 1395] [UniProtKB: P09960]
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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]
ChEMBL Inhibition of human HDAC1 expressed in baculovirus infected sf9 cells using p53 residues 379-382 (RHKKAc) as substrate by fluorescence-based assay B 7.68 pIC50 21 nM IC50 J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
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 HDAC10 (unknown origin) B 7.28 pIC50 52 nM IC50 J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
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 11/Histone deacetylase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3310] [GtoPdb: 2615] [UniProtKB: Q96DB2]
ChEMBL Inhibition of human HDAC11 expressed in baculovirus infected sf9 cells using (Boc-Lys(trifluoroacetyl)-AMC) as substrate by fluorescence-based assay B 7.85 pIC50 14 nM IC50 J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
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]
ChEMBL Inhibition of human HDAC2 expressed in baculovirus infected sf9 cells using p53 residues 379-382 (RHKKAc) as substrate by fluorescence-based assay B 7.2 pIC50 63 nM IC50 J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
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 3/Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111363] [GtoPdb: 2617] [UniProtKB: O15379Q9Y618]
ChEMBL Inhibition of human HDAC3/NcoR2 expressed in sf9 cells using p53 residues 379-382 (RHKKAc) as substrate by fluorescence-based assay B 6.83 pIC50 148 nM IC50 J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
GtoPdb - - 8.09 pIC50 8.2 nM IC50 Mol Cancer Ther (2006) 5: 1309-17 [PMID:16731764]
histone deacetylase 4/Histone deacetylase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3524] [GtoPdb: 2659] [UniProtKB: P56524]
ChEMBL Inhibition of human HDAC4 expressed in baculovirus infected sf9 cells using (Boc-Lys(trifluoroacetyl)-AMC) as substrate by fluorescence-based assay B 7.22 pIC50 60 nM IC50 J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
histone deacetylase 5/Histone deacetylase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2563] [GtoPdb: 2660] [UniProtKB: Q9UQL6]
ChEMBL Inhibition of human HDAC5 expressed in baculovirus infected sf9 cells using (Boc-Lys(trifluoroacetyl)-AMC) as substrate by fluorescence-based assay B 7.32 pIC50 48 nM IC50 J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
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]
ChEMBL Inhibition of human HDAC6 expressed in baculovirus infected sf9 cells using p53 residues 379-382 (RHKKAc) as substrate by fluorescence-based assay B 7.92 pIC50 12 nM IC50 J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
histone deacetylase 7/Histone deacetylase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2716] [GtoPdb: 2661] [UniProtKB: Q8WUI4]
ChEMBL Inhibition of human HDAC7 expressed in baculovirus infected sf9 cells using (Boc-Lys(trifluoroacetyl)-AMC) as substrate by fluorescence-based assay B 6.46 pIC50 350 nM IC50 J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
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]
ChEMBL Inhibition of human HDAC8 expressed in baculovirus infected sf9 cells using p53 residues 379-382 (RHKAcKAc) as substrate by fluorescence-based assay B 6.43 pIC50 370 nM IC50 J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
histone deacetylase 9/Histone deacetylase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4145] [GtoPdb: 2620] [UniProtKB: Q9UKV0]
ChEMBL Inhibition of human HDAC9 expressed in baculovirus infected sf9 cells using (Boc-Lys(trifluoroacetyl)-AMC) as substrate by fluorescence-based assay B 6.77 pIC50 168 nM IC50 J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
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 32:

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]