pracinostat [Ligand Id: 8365] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1851943 (Pracinostat, Sb939, SB 939, SB-939) |
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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 | 7.55 | pKi | 28 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| ChEMBL | Inhibition of recombinant human HDAC-1 expressed in baculovirus infected insect Sf9 cells using Fluor de Lys as substrate preincubated for 2 hrs followed by substrate addition measured after 10 mins by fluorescence assay | B | 7.8 | pKi | 16 | nM | Ki | Medchemcomm (2012) 3: 135-161 |
| ChEMBL | Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 end residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC substrate 3 measured after 30 mins by fluorescence based assay | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2018) 61: 1552-1575 [PMID:29360358] |
| GtoPdb | - | - | 7.31 | pIC50 | 49 | nM | IC50 | Mol Cancer Ther (2010) 9: 642-52 [PMID:20197387] |
| histone deacetylase 10/Histone deacetylase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8] | ||||||||
| ChEMBL | Inhibition of human HDAC10 | B | 7.64 | pKi | 23 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| 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 | 5.5 | pIC50 | 3162.28 | 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 | 5.8 | pIC50 | 1584.89 | nM | IC50 | J Med Chem (2019) 62: 4426-4443 [PMID:30964290] |
| ChEMBL | Inhibition of N-terminal FLAG-tagged human HDAC10 (2 to 631 residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC substrate 3 measured after 30 mins by fluorescence based assay | B | 7.09 | pIC50 | 82 | nM | IC50 | J Med Chem (2018) 61: 1552-1575 [PMID:29360358] |
| GtoPdb | - | - | 7.4 | pIC50 | 40 | nM | IC50 | Mol Cancer Ther (2010) 9: 642-52 [PMID:20197387] |
| histone deacetylase 11/Histone deacetylase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3310] [GtoPdb: 2615] [UniProtKB: Q96DB2] | ||||||||
| ChEMBL | Inhibition of human HDAC11 | B | 7.37 | pKi | 43 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| ChEMBL | Inhibition of human full length HDAC11 expressed in baculovirus infected Sf9 cells using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2018) 61: 1552-1575 [PMID:29360358] |
| histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769] | ||||||||
| ChEMBL | Inhibition of human HDAC2 | B | 7.57 | pKi | 27 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| ChEMBL | Inhibition of recombinant human HDAC-2 expressed in baculovirus infected insect Sf9 cells using Fluor de Lys as substrate preincubated for 2 hrs followed by substrate addition measured after 10 mins by fluorescence assay | B | 7.8 | pKi | 16 | nM | Ki | Medchemcomm (2012) 3: 135-161 |
| ChEMBL | Inhibition of HDAC2 (unknown origin) using fluorogenic HDAC substrate 3 incubated for 30 mins by fluorescence based assay | B | 6.54 | pIC50 | 290 | nM | IC50 | J Med Chem (2018) 61: 1552-1575 [PMID:29360358] |
| histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379] | ||||||||
| ChEMBL | Inhibition of human HDAC3 | B | 7.72 | pKi | 19 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| GtoPdb | - | - | 7.37 | pIC50 | 43 | nM | IC50 | Mol Cancer Ther (2010) 9: 642-52 [PMID:20197387] |
| 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 recombinant human C-terminal His-tagged HDAC3 (1 to 428 end residues)/N-terminal GST-tagged recombinant human NCoR2 (395 to 489 residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC substrate 3 measured after 30 mins by fluorescence based assay | B | 7.15 | pIC50 | 70 | nM | IC50 | J Med Chem (2018) 61: 1552-1575 [PMID:29360358] |
| GtoPdb | - | - | 7.37 | pIC50 | 43 | nM | IC50 | Mol Cancer Ther (2010) 9: 642-52 [PMID:20197387] |
| histone deacetylase 4/Histone deacetylase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3524] [GtoPdb: 2659] [UniProtKB: P56524] | ||||||||
| ChEMBL | Inhibition of human HDAC4 | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged and C-terminal His-tagged HDAC4 (627 to 1084 end residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2018) 61: 1552-1575 [PMID:29360358] |
| histone deacetylase 5/Histone deacetylase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2563] [GtoPdb: 2660] [UniProtKB: Q9UQL6] | ||||||||
| ChEMBL | Inhibition of human HDAC5 | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| ChEMBL | Inhibition of HDAC5 (unknown origin) using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay | B | 5.29 | pIC50 | 5113 | nM | IC50 | J Med Chem (2018) 61: 1552-1575 [PMID:29360358] |
| GtoPdb | - | - | 7.33 | pIC50 | 47 | nM | IC50 | Mol Cancer Ther (2010) 9: 642-52 [PMID:20197387] |
| histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
| ChEMBL | Inhibition of human HDAC6 | B | 6.61 | pKi | 247 | 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 | 6.48 | pIC50 | 334 | nM | IC50 | HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators |
| ChEMBL | Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 with custom peptide substrate | B | 6.73 | pIC50 | 186.1 | nM | IC50 | HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 cells using fluorogenic HDAC substrate 3 measured after 30 mins by fluorescence based assay | B | 7.03 | pIC50 | 93 | nM | IC50 | J Med Chem (2018) 61: 1552-1575 [PMID:29360358] |
| histone deacetylase 7/Histone deacetylase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2716] [GtoPdb: 2661] [UniProtKB: Q8WUI4] | ||||||||
| ChEMBL | Inhibition of human HDAC7 | B | 6.97 | pKi | 107 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| ChEMBL | Inhibition of N-terminal GST-tagged human HDAC7 (518 to end residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2018) 61: 1552-1575 [PMID:29360358] |
| histone deacetylase 8/Histone deacetylase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41] | ||||||||
| ChEMBL | Inhibition of human HDAC8 | B | 7.32 | pKi | 48 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| ChEMBL | Inhibition of recombinant human HDAC-8 expressed in HEK293-F cells using Fluor de Lys as substrate preincubated for 2 hrs followed by substrate addition measured after 10 mins by fluorescence assay | B | 7.8 | pKi | 16 | nM | Ki | Medchemcomm (2012) 3: 135-161 |
| ChEMBL | Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 cells using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay | B | 5.55 | pIC50 | 2835 | nM | IC50 | J Med Chem (2018) 61: 1552-1575 [PMID:29360358] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) | B | 6.85 | pIC50 | 140 | nM | IC50 | Eur J Med Chem (2019) 164: 214-240 [PMID:30594678] |
| histone deacetylase 9/Histone deacetylase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4145] [GtoPdb: 2620] [UniProtKB: Q9UKV0] | ||||||||
| ChEMBL | Inhibition of human HDAC9 | B | 7.62 | pKi | 24 | nM | Ki | Bioorg Med Chem (2015) 23: 5151-5155 [PMID:25637120] |
| ChEMBL | Inhibition of C-terminal His-tagged human HDAC9 (604 to 1066 residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2018) 61: 1552-1575 [PMID:29360358] |
| 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] |
| Plasmodium berghei (target type: ORGANISM) [ChEMBL: CHEMBL612653] | ||||||||
| ChEMBL | Antimalarial activity against exo-erythrocytic form of Plasmodium berghei infected in human HepG2 cells | F | 6.82 | pIC50 | 150 | nM | IC50 | Eur J Med Chem (2014) 82: 204-213 [PMID:24904967] |
| ChEMBL | Antiplasmodial activity against exoerythrocytic-stage of Plasmodium berghei ANKA infected in human HepG2 cells after 53 hrs by DAPI staining-based method | F | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (2017) 60: 4780-4804 [PMID:28241112] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antimalarial activity against Plasmodium falciparum infected in human erythrocytes after 72 hrs | F | 7.1 | pIC50 | 80 | nM | IC50 | Eur J Med Chem (2014) 82: 204-213 [PMID:24904967] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum infected in human erythrocytes after 24 hrs by microbeta scintillation counting-based [3H]-hypoxanthine incorporation assay | F | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (2017) 60: 4780-4804 [PMID:28241112] |
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]
