dacinostat [Ligand Id: 7497] 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: CHEMBL356066 (Dacinostat, Laq-824, LAQ824, NVP-LAQ824) |
|---|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 |
|---|---|---|---|---|---|---|---|---|
| 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 | Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 with custom peptide substrate | B | 8.01 | pIC50 | 9.83 | nM | IC50 | HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators |
| 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 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]
