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, PZP-115891, PZP115891, S-78454, S78454) |
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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: O15379, Q9Y618] | ||||||||
| 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 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]
