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ChEMBL ligand: CHEMBL235191 (Tacedinaline, GOE-5549, CI-994, PD-123654) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547] | ||||||||
GtoPdb | - | - | 7.3 | pKi | 50 | nM | Ki | Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibition of human HDAC1 | B | 7.3 | pKi | 50 | nM | Ki | Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibition of HDAC1 (unknown origin) by fluorimetric assay | B | 4.74 | pIC50 | 18220 | nM | IC50 | Bioorg. Med. Chem. Lett. (2016) 26: 154-159 [PMID:26611919] |
ChEMBL | Inhibition of human recombinant HDAC1 using Fluor de Lys as substrate by fluorometric assay | B | 5.79 | pIC50 | 1620 | nM | IC50 | Eur J Med Chem (2017) 134: 1-12 [PMID:28391133] |
ChEMBL | Inhibition of human recombinant HDAC1 using Fluor de Lys-Green as substrate preincubated for 5 mins followed by substrate addition and measured after 1 hr by fluorescence assay | B | 5.79 | pIC50 | 1620 | nM | IC50 | Eur J Med Chem (2018) 143: 320-333 [PMID:29202397] |
ChEMBL | Inhibition of human recombinant HDAC1 (1 to 482 residues) expressed in Baculovirus using Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2017) 60: 7965-7983 [PMID:28885834] |
ChEMBL | Inhibition of human recombinant full length HDAC1 using fluorogenic substrate 3 after 30 mins by fluorescence assay | B | 5.96 | pIC50 | 1090 | nM | IC50 | J Med Chem (2018) 61: 7245-7260 [PMID:30045621] |
ChEMBL | Inhibition of human recombinant HDAC1 | B | 6.05 | pIC50 | 900 | nM | IC50 | J. Med. Chem. (2007) 50: 5543-5546 [PMID:17941625] |
GtoPdb | - | - | 6.24 | pIC50 | 570 | nM | IC50 | Bioorg. Med. Chem. Lett. (2008) 18: 973-8 [PMID:18182289] |
ChEMBL | Inhibition of HDAC1 | B | 6.24 | pIC50 | 570 | nM | IC50 | Bioorg. Med. Chem. Lett. (2008) 18: 973-978 [PMID:18182289] |
ChEMBL | Inhibition of human recombinant HDAC1 (1 to 482 residues) expressed in Baculovirus using Ac-Leu-Gly-Lys(Ac)-AMC as substrate after 3 hrs by fluorescence assay | B | 7.22 | pIC50 | 60 | nM | IC50 | J Med Chem (2017) 60: 7965-7983 [PMID:28885834] |
histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769] | ||||||||
ChEMBL | Inhibition of human HDAC2 | B | 6.72 | pKi | 190 | nM | Ki | Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990] |
GtoPdb | - | - | 6.82 | pKi | 150 | nM | Ki | Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibition of HDAC2 (unknown origin) by fluorimetric assay | B | 5.41 | pIC50 | 3850 | nM | IC50 | Bioorg. Med. Chem. Lett. (2016) 26: 154-159 [PMID:26611919] |
ChEMBL | Inhibition of human recombinant HDAC2 using Fluor de Lys green as substrate by fluorometric assay | B | 5.92 | pIC50 | 1200 | nM | IC50 | Eur J Med Chem (2017) 134: 1-12 [PMID:28391133] |
ChEMBL | Inhibition of human recombinant HDAC2 using Fluor de Lys-Green as substrate preincubated for 5 mins followed by substrate addition and measured after 1 hr by fluorescence assay | B | 5.92 | pIC50 | 1200 | nM | IC50 | Eur J Med Chem (2018) 143: 320-333 [PMID:29202397] |
ChEMBL | Inhibition of human recombinant HDAC2 | B | 6.05 | pIC50 | 900 | nM | IC50 | J. Med. Chem. (2007) 50: 5543-5546 [PMID:17941625] |
histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379] | ||||||||
ChEMBL | Inhibition of human HDAC3 | B | 6.26 | pKi | 550 | nM | Ki | Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990] |
GtoPdb | - | - | 6.26 | pKi | 550 | nM | Ki | Nat. Chem. Biol. (2010) 6: 238-243 [PMID:20139990] |
ChEMBL | Inhibition of HDAC3 (unknown origin) by fluorimetric assay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg. Med. Chem. Lett. (2016) 26: 154-159 [PMID:26611919] |
ChEMBL | Inhibition of human recombinant HDAC3 | B | 5.92 | pIC50 | 1200 | nM | IC50 | J. Med. Chem. (2007) 50: 5543-5546 [PMID:17941625] |
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
ChEMBL | Inhibition of HDAC6 (unknown origin) by fluorimetric assay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg. Med. Chem. Lett. (2016) 26: 154-159 [PMID:26611919] |
ChEMBL | Inhibition of human recombinant HDAC6 using Fluor de Lys as substrate after 60 mins by fluorometric assay | B | 4.4 | pIC50 | >40000 | nM | IC50 | Eur J Med Chem (2017) 134: 1-12 [PMID:28391133] |
ChEMBL | Inhibition of human recombinant HDAC6 using Fluor de Lys-Green as substrate preincubated for 5 mins followed by substrate addition and measured after 1 hr by fluorescence assay | B | 4.4 | pIC50 | >40000 | nM | IC50 | Eur J Med Chem (2018) 143: 320-333 [PMID:29202397] |
histone deacetylase 8/Histone deacetylase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41] | ||||||||
ChEMBL | Inhibition of human recombinant HDAC8 | B | 4.7 | pIC50 | >20000 | nM | IC50 | J. Med. Chem. (2007) 50: 5543-5546 [PMID:17941625] |
Nicotinamide phosphoribosyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1744525] [UniProtKB: P43490] | ||||||||
ChEMBL | Inhibition of human recombinant NAMPT using NAM as substrate preincubated for 5 mins followed by substrate addition measured after 15 mins by fluorescence assay | B | 5.7 | pIC50 | >2000 | nM | IC50 | J Med Chem (2017) 60: 7965-7983 [PMID:28885834] |
ChEMBL data shown on this page come from version 27:
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]