givinostat [Ligand Id: 7490] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1213492 (Givinostat) |
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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 human HDAC1 | B | 8.7 | pKi | 2 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC1 | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| GtoPdb | - | - | 8.7 | pKi | 2 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in sf9 cells using Fluor-de-lys as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence method | B | 6.88 | pIC50 | 133 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of recombinant human C-terminal His-tagged HDAC1 expressed in Sf9 insect cells using Fluor de Lys deacetylase or Fluor de Lys Green deacetylase as substrate by fluorescent microplate reader assay | B | 7.15 | pIC50 | 70 | nM | IC50 | ACS Med Chem Lett (2021) 12: 1810-1817 [PMID:34795871] |
| GtoPdb | - | - | 7.55 | pEC50 | 28 | nM | EC50 | Biochem J (2008) 409: 581-9 [PMID:17868033] |
| histone deacetylase 10/Histone deacetylase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8] | ||||||||
| ChEMBL | Inhibition of recombinant human HDAC10 (2 to 631 residues) expressed in baculovirus infected sf9 cells using Fluor-de-lys as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence method | B | 6.48 | pIC50 | 331 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| histone deacetylase 11/Histone deacetylase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3310] [GtoPdb: 2615] [UniProtKB: Q96DB2] | ||||||||
| ChEMBL | Inhibition of recombinant human HDAC11 expressed in baculovirus infected sf9 cells using Fluor-de-lys as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence method | B | 6.54 | pIC50 | 287 | 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] | ||||||||
| GtoPdb | - | - | 8.52 | pKi | 3 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC2 | B | 8.52 | pKi | 3 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC2 | B | 8.52 | pKi | 3 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| ChEMBL | Inhibition of human HDAC2 expressed in Sf9 cells using Fluor-de-lys as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence method | B | 6.53 | pIC50 | 293 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| GtoPdb | - | - | 7.25 | pEC50 | 56 | 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] | ||||||||
| GtoPdb | - | - | 8.52 | pKi | 3 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC3 | B | 8.52 | pKi | 3 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC3 | B | 8.52 | pKi | 3 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| GtoPdb | - | - | 7.68 | pEC50 | 21 | 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: O15379, Q9Y618] | ||||||||
| GtoPdb | - | - | 8.52 | pKi | 3 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human C-terminal His-tagged HDAC3 (1 to 428 residues)/human N-terminal GST-tagged NcoR2 (395 to 489 residues) expressed in sf9 cells using Fluor-de-lys as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence method | B | 6.87 | pIC50 | 136 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| GtoPdb | - | - | 7.68 | pEC50 | 21 | 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 human HDAC4 | B | 5.98 | pKi | 1050 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC4 | B | 5.98 | pKi | 1050 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| GtoPdb | - | - | 5.98 | pKi | 1050 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC4 expressed in baculovirus infected sf9 cells using Boc-L-Lys-MCA as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence method | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| GtoPdb | - | - | 7.28 | pEC50 | 52 | nM | EC50 | Biochem J (2008) 409: 581-9 [PMID:17868033] |
| histone deacetylase 5/Histone deacetylase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2563] [GtoPdb: 2660] [UniProtKB: Q9UQL6] | ||||||||
| GtoPdb | - | - | 6.22 | pKi | 600 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC5 | B | 6.22 | pKi | 600 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC5 | B | 6.22 | pKi | 600 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| ChEMBL | Inhibition of human HDAC5 using Boc-L-Lys-MCA as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence method | B | 6.27 | pIC50 | 532 | 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 human HDAC6 | B | 8.38 | pKi | 4.2 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC6 | 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 recombinant human HDAC6 using Fluor-de-lys as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence method | B | 6.51 | pIC50 | 312 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method | B | 7.36 | pIC50 | 44 | nM | IC50 | J Med Chem (2019) 62: 10711-10739 [PMID:31710483] |
| ChEMBL | Inhibition of recombinant human full length N-terminal GST-tagged HDAC6 expressed in Sf9 insect cells using Fluor de Lys deacetylase or Fluor de Lys Green deacetylase substrate by fluorescent microplate reader assay | B | 7.64 | pIC50 | 23 | nM | IC50 | ACS Med Chem Lett (2021) 12: 1810-1817 [PMID:34795871] |
| GtoPdb | - | - | 7.57 | pEC50 | 27 | nM | EC50 | Biochem J (2008) 409: 581-9 [PMID:17868033] |
| histone deacetylase 7/Histone deacetylase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2716] [GtoPdb: 2661] [UniProtKB: Q8WUI4] | ||||||||
| ChEMBL | Inhibition of human HDAC7 | B | 6.62 | pKi | 240 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC7 | B | 6.62 | pKi | 240 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| GtoPdb | - | - | 6.62 | pKi | 240 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human N-terminal GST-tagged HDAC7 (518 to end residues) expressed in baculovirus infected sf9 cells using Boc-L-Lys-MCA as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence method | B | 6.28 | pIC50 | 524 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| GtoPdb | - | - | 6.79 | pEC50 | 163 | nM | EC50 | Biochem J (2008) 409: 581-9 [PMID:17868033] |
| histone deacetylase 8/Histone deacetylase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41] | ||||||||
| ChEMBL | Activity of human HDAC8 | B | 7.41 | pKi | 39 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC8 | B | 7.41 | pKi | 39 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| GtoPdb | - | - | 7.41 | pKi | 39 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of recombinant human C-terminal His-tagged HDAC8 expressed in baculovirus infected sf9 cells using Fluor-de-lys as substrate by fluorometric method | B | 6.08 | pIC50 | 837 | 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 | B | 6.41 | pKi | 390 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC9 | B | 6.41 | pKi | 390 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| GtoPdb | - | - | 6.41 | pKi | 390 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of C-terminal His-tagged human HDAC9 (604 to 1066 residues) expressed in baculovirus infected sf9 cells using Boc-L-Lys-MCA as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence method | B | 6.29 | pIC50 | 512 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| Histone deacetylase HD1B in Zea mays (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3541] [UniProtKB: Q9ZTP8] | ||||||||
| ChEMBL | Inhibition of maize HD1B | B | 8.12 | pIC50 | 7.5 | nM | IC50 | 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 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]
