dacinostat [Ligand Id: 7497] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL356066 (Dacinostat, Laq-824, LAQ824, NVP-LAQ824) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG expressed in CHO cells by automated patch clamp electrophysiology assay | B | 4.91 | pIC50 | 12200 | nM | IC50 | J Med Chem (2010) 53: 2952-2963 [PMID:20205394] |
| ChEMBL | Inhibition of human ERG by automated patch clamp assay | B | 4.99 | pIC50 | 10300 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4909-4912 [PMID:21742496] |
| ChEMBL | Inhibition of human ERG by radioligand binding assay | B | 4.99 | pIC50 | 10300 | nM | IC50 | J Med Chem (2011) 54: 4752-4772 [PMID:21650221] |
| ChEMBL | Inhibition of human ERG by patch clamp assay | B | 4.99 | pIC50 | 10300 | nM | IC50 | J Med Chem (2011) 54: 4752-4772 [PMID:21650221] |
| ChEMBL | Inhibition of human ERG by manual patch clamp assay | B | 4.99 | pIC50 | 10300 | nM | IC50 | J Med Chem (2011) 54: 4752-4772 [PMID:21650221] |
| histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547] | ||||||||
| ChEMBL | Inhibition of human HDAC1 | B | 9.22 | pKi | 0.6 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| ChEMBL | Inhibition of human HDAC1 | B | 9.26 | pKi | 0.55 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| GtoPdb | - | - | 9.26 | pKi | 0.55 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of purified recombinant HDAC1 | B | 7.82 | pIC50 | 15 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4909-4912 [PMID:21742496] |
| ChEMBL | Inhibition of HDAC1 | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2011) 54: 4752-4772 [PMID:21650221] |
| ChEMBL | Inhibition of FLAG-tagged HDAC1 expressed in HEK293 cells by fluorescent assay | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2010) 53: 2952-2963 [PMID:20205394] |
| ChEMBL | Inhibition of human recombinant HDAC1 | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2007) 50: 5543-5546 [PMID:17941625] |
| ChEMBL | Inhibition of recombinant C-terminal FLAG-tagged HDAC1 expressed in baculovirus after 10 mins by fluorimetric analysis | B | 8.1 | pIC50 | 8 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5684-5688 [PMID:19699639] |
| ChEMBL | Inhibition of C-terminal FLAG-tagged full length recombinant human HDAC1 expressed in baculovirus infected Sf9 insect cells after 3 hrs by FDL assay | B | 8.3 | pIC50 | 5 | nM | IC50 | Medchemcomm (2017) 8: 767-770 [PMID:30108795] |
| ChEMBL | Inhibition of human HDAC1 by fluorimetric assay | B | 8.49 | pIC50 | 3.23 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
| ChEMBL | Inhibition of HDAC1 in HEK293 cells | B | 8.59 | pIC50 | 2.6 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1814-1819 [PMID:18308563] |
| histone deacetylase 10/Histone deacetylase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8] | ||||||||
| ChEMBL | Inhibition of human HDAC10 by fluorimetric assay | B | 8.08 | pIC50 | 8.41 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
| histone deacetylase 11/Histone deacetylase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3310] [GtoPdb: 2615] [UniProtKB: Q96DB2] | ||||||||
| ChEMBL | Inhibition of human HDAC11 by fluorimetric assay | B | 8.25 | pIC50 | 5.58 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
| histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769] | ||||||||
| GtoPdb | - | - | 8.85 | pKi | 1.4 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC2 | B | 8.85 | pKi | 1.4 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC2 | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| ChEMBL | Inhibition of human HDAC2 by fluorimetric assay | B | 7.8 | pIC50 | 15.7 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
| ChEMBL | Inhibition of recombinant C-terminal FLAG-tagged HDAC2 expressed in baculovirus after 10 mins by fluorimetric analysis | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5684-5688 [PMID:19699639] |
| ChEMBL | Inhibition of human recombinant HDAC2 | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2007) 50: 5543-5546 [PMID:17941625] |
| ChEMBL | Inhibition of C-terminal FLAG-tagged full length recombinant human HDAC2 expressed in baculovirus infected Sf9 insect cells after 3 hrs by FDL assay | B | 8.3 | pIC50 | 5 | nM | IC50 | Medchemcomm (2017) 8: 767-770 [PMID:30108795] |
| histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379] | ||||||||
| ChEMBL | Inhibition of human HDAC3 | B | 8.38 | pKi | 4.2 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC3 | B | 8.38 | pKi | 4.2 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| GtoPdb | - | - | 8.38 | pKi | 4.2 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC3 by fluorimetric assay | B | 7.98 | pIC50 | 10.5 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
| ChEMBL | Inhibition of human recombinant HDAC3 | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2007) 50: 5543-5546 [PMID:17941625] |
| ChEMBL | Inhibition of HDAC3 in HEK293 cells | B | 8.44 | pIC50 | 3.6 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1814-1819 [PMID:18308563] |
| ChEMBL | Inhibition of flag-tagged HDAC3 | B | 9.4 | pIC50 | 0.4 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 17335-17340 [PMID:17956988] |
| histone deacetylase 4/Histone deacetylase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3524] [GtoPdb: 2659] [UniProtKB: P56524] | ||||||||
| ChEMBL | Inhibition of human HDAC4 | B | 5.65 | pKi | 2250 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC4 | B | 5.65 | pKi | 2250 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| GtoPdb | - | - | 5.65 | pKi | 2250 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human recombinant N-terminal FLAG-tagged HDAC4 (612-1034) expressed in baculovirus after 10 mins by fluorimetric analysis | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5684-5688 [PMID:19699639] |
| ChEMBL | Inhibition of wild type HDAC4 expressed in Escherichia coli | B | 6.38 | pIC50 | 420 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1814-1819 [PMID:18308563] |
| ChEMBL | Inhibition of human HDAC4 by fluorimetric assay | B | 8.24 | pIC50 | 5.82 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
| ChEMBL | Inhibition of HDAC4 H976Y mutant expressed in Escherichia coli | B | 8.36 | pIC50 | 4.4 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1814-1819 [PMID:18308563] |
| ChEMBL | Inhibition of flag-tagged HDAC4 by pull-down assay | B | 8.4 | pIC50 | 4 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 17335-17340 [PMID:17956988] |
| ChEMBL | Inhibition of flag-tagged HDAC4 expressed in HEK293 cells by Biomol assay | B | 8.52 | pIC50 | 3 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 17335-17340 [PMID:17956988] |
| ChEMBL | Inhibition of HDAC4 catalytic domain expressed in HEK293 cells by Biomol assay | B | 8.6 | pIC50 | 2.5 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 17335-17340 [PMID:17956988] |
| ChEMBL | Inhibition of flag-tagged HDAC4 | 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 by Biomol assay | B | 9 | pIC50 | 1 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 17335-17340 [PMID:17956988] |
| histone deacetylase 5/Histone deacetylase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2563] [GtoPdb: 2660] [UniProtKB: Q9UQL6] | ||||||||
| ChEMBL | Inhibition of human HDAC5 | B | 6.38 | pKi | 420 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC5 | B | 6.38 | pKi | 420 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| GtoPdb | - | - | 6.38 | pKi | 420 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human recombinant N-terminal FLAG-tagged HDAC5 (620-1122) expressed in baculovirus after 10 mins by fluorimetric analysis | B | 6.72 | pIC50 | 190 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5684-5688 [PMID:19699639] |
| ChEMBL | Inhibition of human HDAC5 by fluorimetric assay | B | 8.25 | pIC50 | 5.58 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
| histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
| GtoPdb | - | - | 8.02 | pKi | 9.5 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC6 | B | 8.02 | pKi | 9.5 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC6 | B | 8.02 | pKi | 9.5 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| ChEMBL | Inhibition of HDAC6 in HEK293 cells | B | 8.08 | pIC50 | 8.3 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1814-1819 [PMID:18308563] |
| ChEMBL | Inhibition of human HDAC6 by fluorimetric assay | B | 8.23 | pIC50 | 5.93 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
| histone deacetylase 7/Histone deacetylase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2716] [GtoPdb: 2661] [UniProtKB: Q8WUI4] | ||||||||
| GtoPdb | - | - | 5.02 | pKi | 9500 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC7 | B | 5.02 | pKi | 9500 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC7 | B | 5.02 | pKi | 9500 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| ChEMBL | Inhibition of human recombinant N-terminal FLAG-tagged HDAC7 (438-915) expressed in baculovirus after 10 mins by fluorimetric analysis | B | 5.65 | pIC50 | 2240 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5684-5688 [PMID:19699639] |
| ChEMBL | Inhibition of human HDAC7 by fluorimetric assay | B | 8.21 | pIC50 | 6.11 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
| histone deacetylase 8/Histone deacetylase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41] | ||||||||
| ChEMBL | Activity of human HDAC8 | B | 6.47 | pKi | 340 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC8 | B | 6.47 | pKi | 340 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| GtoPdb | - | - | 6.47 | pKi | 340 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human recombinant HDAC8 | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2007) 50: 5543-5546 [PMID:17941625] |
| ChEMBL | Inhibition of human HDAC8 by fluorimetric assay | B | 8.42 | pIC50 | 3.84 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
| histone deacetylase 9/Histone deacetylase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4145] [GtoPdb: 2620] [UniProtKB: Q9UKV0] | ||||||||
| ChEMBL | Inhibition of human HDAC9 | B | 5.05 | pKi | 9000 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC9 | B | 5.05 | pKi | 9000 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| GtoPdb | - | - | 5.05 | pKi | 9000 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC9 by fluorimetric assay | B | 8.08 | pIC50 | 8.24 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
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]
