vorinostat [Ligand Id: 6852] 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: CHEMBL98 (MK-0683, MK0683, NSC-701852, NSC-748799, NSC-759852, Suberoylanilide hydroxamic acid, Vorinostat, Zolinza)
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • bromodomain containing 4/Bromodomain-containing protein 4 in Human [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
There should be some charts here, you may need to enable JavaScript!
  • DNA methyltransferase 1/DNA (cytosine-5)-methyltransferase 1 in Human [ChEMBL: CHEMBL1993] [GtoPdb: 2605] [UniProtKB: P26358]
There should be some charts here, you may need to enable JavaScript!
  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • heat shock protein 90 alpha family class A member 1/Heat shock protein HSP 90-alpha in Human [ChEMBL: CHEMBL3880] [GtoPdb: 2905] [UniProtKB: P07900]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • Histone deacetylase in Plasmodium falciparum [ChEMBL: CHEMBL5541] [UniProtKB: Q9XYC7]
  • Plasmodium falciparum histone deacetylase 1/Histone deacetylase in Plasmodium falciparum 3D7 [ChEMBL: CHEMBL1293190] [GtoPdb: 3072] [UniProtKB: Q7K6A1]
There should be some charts here, you may need to enable JavaScript!
  • histone deacetylase 1/Histone deacetylase 1 in Human [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547]
  • histone deacetylase 1/Histone deacetylase 1 in Mouse [ChEMBL: CHEMBL4001] [GtoPdb: 2658] [UniProtKB: O09106]
There should be some charts here, you may need to enable JavaScript!
  • histone deacetylase 10/Histone deacetylase 10 in Human [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8]
There should be some charts here, you may need to enable JavaScript!
  • histone deacetylase 11/Histone deacetylase 11 in Human [ChEMBL: CHEMBL3310] [GtoPdb: 2615] [UniProtKB: Q96DB2]
There should be some charts here, you may need to enable JavaScript!
  • histone deacetylase 2/Histone deacetylase 2 in Human [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769]
There should be some charts here, you may need to enable JavaScript!
  • histone deacetylase 3/Histone deacetylase 3 in Human [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • histone deacetylase 3/Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) in Human [ChEMBL: CHEMBL2111363] [GtoPdb: 2617] [UniProtKB: O15379Q9Y618]
There should be some charts here, you may need to enable JavaScript!
  • histone deacetylase 4/Histone deacetylase 4 in Human [ChEMBL: CHEMBL3524] [GtoPdb: 2659] [UniProtKB: P56524]
There should be some charts here, you may need to enable JavaScript!
  • histone deacetylase 5/Histone deacetylase 5 in Human [ChEMBL: CHEMBL2563] [GtoPdb: 2660] [UniProtKB: Q9UQL6]
There should be some charts here, you may need to enable JavaScript!
  • histone deacetylase 6/Histone deacetylase 6 in Human [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
There should be some charts here, you may need to enable JavaScript!
  • histone deacetylase 7/Histone deacetylase 7 in Human [ChEMBL: CHEMBL2716] [GtoPdb: 2661] [UniProtKB: Q8WUI4]
There should be some charts here, you may need to enable JavaScript!
  • Histone deacetylase 8 in Schistosoma mansoni [ChEMBL: CHEMBL3797017] [UniProtKB: A5H660]
  • histone deacetylase 8/Histone deacetylase 8 in Human [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41]
There should be some charts here, you may need to enable JavaScript!
  • histone deacetylase 9/Histone deacetylase 9 in Human [ChEMBL: CHEMBL4145] [GtoPdb: 2620] [UniProtKB: Q9UKV0]
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!
  • Histone deacetylase-like amidohydrolase in Alcaligenes sp. (strain DSM 11172) (Bordetella sp. (strain FB188)) [ChEMBL: CHEMBL6017] [UniProtKB: Q70I53]
There should be some charts here, you may need to enable JavaScript!
  • euchromatic histone lysine methyltransferase 2/Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 in Human [ChEMBL: CHEMBL6032] [GtoPdb: 2652] [UniProtKB: Q96KQ7]
There should be some charts here, you may need to enable JavaScript!
  • hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Human [ChEMBL: CHEMBL402] [GtoPdb: 639] [UniProtKB: P04035]
There should be some charts here, you may need to enable JavaScript!
  • Human immunodeficiency virus type 1 Tat protein in Human immunodeficiency virus type 1 group M subtype B (isolate HXB2)(HIV-1) [ChEMBL: CHEMBL4011] [UniProtKB: P04608]
There should be some charts here, you may need to enable JavaScript!
  • Leukotriene A4 hydrolase/Leukotriene A4 hydrolase in Human [ChEMBL: CHEMBL4618] [GtoPdb: 1395] [UniProtKB: P09960]
  • Leukotriene A4 hydrolase/Leukotriene A4 hydrolase in Mouse [ChEMBL: CHEMBL3738] [GtoPdb: 1395] [UniProtKB: P24527]
There should be some charts here, you may need to enable JavaScript!
  • lysine demethylase 4E/Lysine-specific demethylase 4D-like in Human [ChEMBL: CHEMBL1293226] [GtoPdb: 2679] [UniProtKB: B2RXH2]
There should be some charts here, you may need to enable JavaScript!
  • lysine demethylase 1A/Lysine-specific histone demethylase 1 in Human [ChEMBL: CHEMBL6136] [GtoPdb: 2669] [UniProtKB: O60341]
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!
  • sirtuin 5/NAD-dependent protein deacylase sirtuin-5, mitochondrial in Human [ChEMBL: CHEMBL2163183] [GtoPdb: 2711] [UniProtKB: Q9NXA8]
There should be some charts here, you may need to enable JavaScript!
  • MDM2 proto-oncogene/p53-binding protein Mdm-2 in Human [ChEMBL: CHEMBL5023] [GtoPdb: 3136] [UniProtKB: Q00987]
There should be some charts here, you may need to enable JavaScript!
  • phosphoinositide-3-kinase regulatory subunit 1/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha/p85-alpha in Human [ChEMBL: CHEMBL2111367] [GtoPdb: 25032153] [UniProtKB: P27986P42336]
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!
  • proteasome 20S subunit beta 5/Proteasome Macropain subunit MB1 in Human [ChEMBL: CHEMBL4662] [GtoPdb: 2406] [UniProtKB: P28074]
There should be some charts here, you may need to enable JavaScript!
  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
There should be some charts here, you may need to enable JavaScript!
  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
There should be some charts here, you may need to enable JavaScript!
  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
There should be some charts here, you may need to enable JavaScript!
  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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
Amyloid-beta A4 protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2487] [UniProtKB: P05067]
ChEMBL Inhibition of amyloid beta (1 to 42) (unknown origin) self aggregation after 24 hrs by thioflavin-T fluorescence method B 4.7 pIC50 >20000 nM IC50 Eur J Med Chem (2020) 192: 112193-112193 [PMID:32151835]
Apoptosis regulator BAX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5318] [UniProtKB: Q07812]
ChEMBL Binding affinity to recombinant human full length His-tagged BAX expressed in Escherichia coli BL21 (DE3) cells preincubated for 30 min followed by FITC-BIM addition and measured after 20 mins by fluorescence polarization assay B 5 pEC50 >10000 nM EC50 J Med Chem (2020) 63: 12083-12099 [PMID:33021789]
bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
ChEMBL Inhibition of recombinant BRD4 bromodomain 1 (unknown origin) using histone H4 peptide as substrate incubated for 1 hr under dark condition by HTRF assay B 4.3 pIC50 >50000 nM IC50 Medchemcomm (2014) 5: 342-351
ChEMBL Inhibition of His-tagged BRD4 bromodomain 1 (unknown origin) using [Lys (5,8,12,16) Ac] H4(1-21) as substrate by fluorescence based assay B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2021) 209: 112868-112868 [PMID:33077265]
ChEMBL Inhibition of His-tagged BRD4 bromodomain 2 (unknown origin) using [Lys (5,8,12,16) Ac] H4(1-21) as substrate by fluorescence based assay B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2021) 209: 112868-112868 [PMID:33077265]
ChEMBL Inhibition of BRD4 in human HL60 cells assessed as reduction in C-myc production after 24 hrs by ELISA B 6.13 pIC50 740 nM IC50 Bioorg Med Chem (2017) 25: 3677-3684 [PMID:28549889]
ChEMBL Inhibition of BRD4 (unknown origin) by ELISA B 7.37 pIC50 43.13 nM IC50 Bioorg Med Chem Lett (2021) 31: 127671-127671 [PMID:33229136]
ChEMBL Inhibition of BRD4 (unknown origin) B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2017) 27: 4051-4055 [PMID:28765013]
DNA methyltransferase 1/DNA (cytosine-5)-methyltransferase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1993] [GtoPdb: 2605] [UniProtKB: P26358]
ChEMBL Inhibition of human DNMT1 enzyme using polydeoxy-inosine polydeoxy-cytosine DNA as substrate incubated for 15 mins in presence of SAM by TR-FRET assay B 5 pIC50 >10000 nM IC50 J Med Chem (2021) 64: 3392-3426 [PMID:33661013]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of EGFR (unknown origin) B 6.05 pIC50 900 nM IC50 J Med Chem (2020) 63: 8977-9002 [PMID:32320239]
ChEMBL Inhibition of EGFR (unknown origin) B 7.92 pIC50 12 nM IC50 Eur J Med Chem (2021) 209: 112904-112904 [PMID:33077264]
histone deacetylase 1/HDAC1/REST corepressor 3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4296112] [GtoPdb: 2658] [UniProtKB: Q13547Q9P2K3]
ChEMBL Inhibition of HDAC1/CoREST3 in HEK293 whole cell extract using fluorescent acetylated histone peptide as substrate after 60 mins by fluorescence based assay B 8.52 pKi 3.04 nM Ki Bioorg Med Chem Lett (2018) 28: 1001-1004 [PMID:29496367]
GtoPdb - - 8.89 pKi 1.3 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
heat shock protein 90 alpha family class A member 1/Heat shock protein HSP 90-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3880] [GtoPdb: 2905] [UniProtKB: P07900]
ChEMBL Inhibition of FITC-geldanamycin binding to HSP90alpha (unknown origin) after 3 hrs by fluorescence polarization assay B 6 pIC50 >1000 nM IC50 Eur J Med Chem (2018) 150: 667-677 [PMID:29567459]
ChEMBL Inhibition of HSP90a (unknown origin) B 6 pIC50 >1000 nM IC50 Eur J Med Chem (2020) 190: 112086-112086 [PMID:32058238]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG by automated patch clamp assay B 4.52 pIC50 >30000 nM IC50 Bioorg Med Chem Lett (2011) 21: 4909-4912 [PMID:21742496]
ChEMBL Inhibition of human ERG by automated Q-patch assay B 4.52 pIC50 >30000 nM IC50 J Med Chem (2011) 54: 4752-4772 [PMID:21650221]
ChEMBL Inhibition of recombinant human ERG expressed in HEK293 cells at -80 mV holding potential measured for 9 mins by Qpatch clamp method B 4.52 pIC50 >30000 nM IC50 Bioorg Med Chem Lett (2017) 27: 4885-4888 [PMID:28947154]
ChEMBL Inhibition of human ERG B 6.49 pIC50 322 nM IC50 Eur J Med Chem (2020) 206: 112677-112677 [PMID:32823005]
Histone deacetylase in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5541] [UniProtKB: Q9XYC7]
ChEMBL Inhibition of Plasmodium falciparum HDAC1 B 6.89 pIC50 130 nM IC50 J Med Chem (2010) 53: 6100-6111 [PMID:20669972]
ChEMBL Inhibition of Plasmodium falciparum HDAC1 expressed in Drosophila melanogaster S2 cells B 7.23 pIC50 59 nM IC50 J Med Chem (2009) 52: 2185-2187 [PMID:19317450]
Plasmodium falciparum histone deacetylase 1/Histone deacetylase in Plasmodium falciparum 3D7 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293190] [GtoPdb: 3072] [UniProtKB: Q7K6A1]
ChEMBL Inhibition of Plasmodium falciparum 3D7 histone deacetylase infected in human erythrocytes assessed as alteration of histone H3 acetylation after 3.5 hrs by SDS-PAGE B 7 pIC50 100 nM IC50 Antimicrob Agents Chemother (2008) 52: 3467-3477 [PMID:18644969]
histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547]
ChEMBL Binding affinity to human HDAC1 assessed as dissociation constant B 6.74 pKd 182 nM Kd J Med Chem (2023) 66: 11672-11700 [PMID:37651268]
ChEMBL Inhibition of recombinant human HDAC1 using Boc-L-Lys(acetyl)-MCA as substrate by fluorogenic enzymatic assay B 7.4 pKd 40 nM Kd Bioorg Med Chem (2012) 20: 985-995 [PMID:22182579]
ChEMBL Inhibition of HDAC1 B 7.2 pKi 63 nM Ki Bioorg Med Chem Lett (2010) 20: 3314-3321 [PMID:20451378]
ChEMBL Competitive inhibition of HDAC1 using KI-104 as substrate by fluorescence assay B 7.22 pKi 60 nM Ki J Med Chem (2011) 54: 4694-4720 [PMID:21634430]
ChEMBL Inhibition of HDAC1 B 7.32 pKi 48 nM Ki J Med Chem (2008) 51: 2898-2906 [PMID:18412327]
ChEMBL Inhibition of human recombinant HDAC1 using Fluor de Lys as substrate after 2 hrs by fluorescence method B 7.92 pKi 12 nM Ki Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227]
ChEMBL Inhibition of human recombinant HDAC1 using Ac-Leu-Gly-Lys (Ac)-AMC substrate incubated for 30 mins by fluorescence assay B 8 pKi 10 nM Ki Medchemcomm (2014) 5: 1849-1855
ChEMBL Inhibition of recombinant human HDAC1 enzyme using flurogenic Ac-LeuGlyLys (Ac)-AMC as substrate after 15 to 30 mins B 8.1 pKi 8 nM Ki J Med Chem (2013) 56: 6512-6520 [PMID:23865683]
ChEMBL Inhibition of human recombinant HDAC1 using [Ac-Leu-Gly-Lys(Ac)-AMC substrate incubated for 15 to 30 mins B 8.1 pKi 8 nM Ki J Med Chem (2014) 57: 9644-9657 [PMID:25380299]
ChEMBL Inhibition of recombinant His-tagged human HDAC1 expressed in insect cells assessed as hydrolase activity using fluorogenic Ac-LGK-ac-AMC as substrate measured after 60 mins by fluorescence analysis B 8.19 pKi 6.4 nM Ki Medchemcomm (2016) 7: 464-470
ChEMBL Binding affinity to recombinant human HDAC1 expressed in baculovirus infected HEK293T cells using acetylLys(Ac)-AMC as substrate assessed as inhibition constant B 8.27 pKi 5.4 nM Ki J Med Chem (2023) 66: 11672-11700 [PMID:37651268]
ChEMBL Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in sf9 cells using acetyl-Lys(Ac)-AMC as substrate B 8.3 pKi 5 nM Ki J Med Chem (2020) 63: 12460-12484 [PMID:32608981]
ChEMBL Binding affinity to recombinant human HDAC1 assessed as inhibition constant B 8.72 pKi 1.9 nM Ki J Med Chem (2023) 66: 11672-11700 [PMID:37651268]
ChEMBL Inhibition of human HDAC1 B 8.89 pKi 1.3 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
GtoPdb - - 8.89 pKi 1.3 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of recombinant HDAC1 (unknown origin) incubated for 3 hrs by chemiluminescent assay B 4.48 pIC50 33000 nM IC50 Eur J Med Chem (2022) 244: 114807-114807 [PMID:36244186]
ChEMBL Inhibition of HDAC1 in human COLO205 cells assessed as induction of histone H3 acetylation B 5.66 pIC50 2200 nM IC50 Bioorg Med Chem Lett (2010) 20: 3314-3321 [PMID:20451378]
ChEMBL Inhibition of HDAC1 in presence of DTT B 6.11 pIC50 775 nM IC50 J Med Chem (2007) 50: 5720-5726 [PMID:17958342]
ChEMBL Inhibition of HDAC1 in human 293T cells after 16 hrs by fluorimetry B 6.22 pIC50 600 nM IC50 Bioorg Med Chem Lett (2009) 19: 336-340 [PMID:19084395]
ChEMBL Inhibition of human recombinant HDAC1 using modified Boc-Lys(Ac)-AMC MAL as substrate after 1 hr by fluorescent activity assay B 6.22 pIC50 600 nM IC50 ACS Med Chem Lett (2014) 5: 973-978 [PMID:25221651]
ChEMBL Inhibition of Histone deacetylase 1 (HDAC1) of HeLa nuclear extracts B 6.32 pIC50 480 nM IC50 Bioorg Med Chem Lett (2004) 14: 449-453 [PMID:14698179]
ChEMBL Inhibition of human recombinant HDAC1 by fluorimetry B 6.46 pIC50 350 nM IC50 J Med Chem (2009) 52: 2909-2922 [PMID:19419205]
ChEMBL Inhibition of HDAC1 (unknown origin) by fluorimetric assay B 6.46 pIC50 350 nM IC50 Bioorg Med Chem Lett (2016) 26: 154-159 [PMID:26611919]
ChEMBL Inhibition of human HDAC1 by fluorescence assay B 6.49 pIC50 320 nM IC50 J Med Chem (2013) 56: 427-436 [PMID:23252603]
ChEMBL Inhibition of full length His-tagged human recombinant HDAC1 expressed in baculovirus system using fluor de Lys as substrate by fluorometric analysis B 6.51 pIC50 310 nM IC50 Eur J Med Chem (2013) 66: 56-68 [PMID:23792316]
ChEMBL Inhibition of HDAC1 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay B 6.51 pIC50 310 nM IC50 Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503]
ChEMBL Inhibition of HDAC1 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay B 6.51 pIC50 310 nM IC50 J Med Chem (2014) 57: 8026-8034 [PMID:25238284]
ChEMBL Inhibition of HDAC1 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHKK(Ac)) as substrate by fluorescence assay B 6.51 pIC50 306 nM IC50 ACS Med Chem Lett (2013) 4: 779-783 [PMID:24015327]
ChEMBL Inhibition of C-terminal FLAG His tagged full length human recombinant HDAC1 (1 to 482 residues) expressed in baculovirus infected sf21 cells using RHKKAc as substrate in presence of ATP B 6.51 pIC50 306 nM IC50 J Med Chem (2017) 60: 8336-8357 [PMID:28953386]
ChEMBL Inhibition of HDAC1 (unknown origin) using Arg-His-Lys-Lys(Ac) as substrate after 2 hrs by fluorescence analysis B 6.51 pIC50 306 nM IC50 Bioorg Med Chem Lett (2018) 28: 1357-1362 [PMID:29545103]
ChEMBL Inhibition of HDAC1 (unknown origin) B 6.51 pIC50 306 nM IC50 Eur J Med Chem (2018) 158: 593-619 [PMID:30243158]
ChEMBL Inhibition of human HDAC1 using Arg-His-Lys-Lys (Ac) as substrate incubated for 2 hrs by fluorescence assay B 6.51 pIC50 306 nM IC50 Eur J Med Chem (2019) 184: 111755-111755 [PMID:31627059]
ChEMBL Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in sf21 cells preincubated with enzyme followed by fluorogenic Arg-His-Lys-Lys(Ac)-AMC substrate addition measured after 2 hrs by fluorescence assay B 6.51 pIC50 306 nM IC50 J Med Chem (2016) 59: 8233-8262 [PMID:27541357]
ChEMBL Inhibition of human recombinant HDAC1 using histone H3 substrate pre-incubated at room temperature for 15 mins before substrate addition by fluorimetric assay B 6.52 pIC50 300 nM IC50 J Med Chem (2014) 57: 6259-6265 [PMID:24972008]
ChEMBL Inhibition of HDAC1 by fluorescent activity assay B 6.54 pIC50 290 nM IC50 Bioorg Med Chem Lett (2011) 21: 5735-5738 [PMID:21875796]
ChEMBL Inhibition of HDAC1 by fluorometric assay B 6.57 pIC50 270 nM IC50 J Med Chem (2012) 55: 9562-9575 [PMID:23116147]
ChEMBL Inhibition of human recombinant HDAC1 using AMC-K(Ac)GL as substrate by fluorescence based assay B 6.59 pIC50 260 nM IC50 ACS Med Chem Lett (2020) 11: 977-983 [PMID:32435414]
ChEMBL Inhibition of full length human recombinant C-terminal FLAG-His-tagged HDAC1 (1 to 482 residues) expressed in sf21 cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay B 6.59 pIC50 260 nM IC50 Eur J Med Chem (2016) 112: 99-105 [PMID:26890116]
ChEMBL Inhibition of human HDAC-1 using RHKK(Ac) as substrate by fluorescence assay B 6.59 pIC50 260 nM IC50 J Med Chem (2014) 57: 2258-2274 [PMID:24588105]
ChEMBL Inhibition of human HDAC1 using RHKK(Ac) as substrate by fluorimetric analysis B 6.59 pIC50 258 nM IC50 Bioorg Med Chem Lett (2014) 24: 61-64 [PMID:24345446]
ChEMBL Inhibition of human HDAC1 using fluorogenic tetrapeptide RHKKAc as substrate B 6.59 pIC50 258 nM IC50 Eur J Med Chem (2014) 79: 251-259 [PMID:24742384]
ChEMBL Inhibition of HDAC1 (unknown origin) using fluorogenic tetrapeptide RHKK(Ac) substrate by fluorescence assay B 6.59 pIC50 258 nM IC50 J Med Chem (2014) 57: 8358-8377 [PMID:25233084]
ChEMBL Inhibition of human HDAC-1 using RHKK(Ac) as substrate B 6.59 pIC50 258 nM IC50 Eur J Med Chem (2014) 76: 53-60 [PMID:24565573]
ChEMBL Inhibition of human HDAC1 using RHKK(Ac) as substrate by fluorimetric analysis B 6.59 pIC50 258 nM IC50 Bioorg Med Chem Lett (2015) 25: 459-461 [PMID:25563890]
ChEMBL Inhibition of human HDAC1 by fluorimetric assay B 6.59 pIC50 258 nM IC50 J Med Chem (2010) 53: 8387-8399 [PMID:21073160]
ChEMBL Inhibition of Nanoluc-fused HDAC1 (unknown origin) expressed in HEK293 cells incubated for 2 hrs by NANOBRET assay B 6.62 pIC50 240 nM IC50 J Med Chem (2021) 64: 4810-4840 [PMID:33830764]
ChEMBL Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate B 6.62 pIC50 240 nM IC50 J Med Chem (2015) 58: 2809-2820 [PMID:25734520]
ChEMBL Inhibition of human recombinant HDAC1 using fluorogenic HDAC substrate-3 by fluorescence assay B 6.63 pIC50 236 nM IC50 Eur J Med Chem (2019) 164: 263-272 [PMID:30597327]
ChEMBL Inhibition of recombinant human HDAC1 B 6.66 pIC50 220 nM IC50 Bioorg Med Chem Lett (2016) 26: 375-379 [PMID:26706171]
ChEMBL Inhibition of HDAC1 (unknown origin) using fluorogenic substrate incubated for 30 mins by fluorescence plate reader B 6.66 pIC50 219.3 nM IC50 Eur J Med Chem (2022) 240: 114582-114582 [PMID:35834905]
ChEMBL Inhibition of full length His6-tagged GST-fused recombinant human HDAC1 expressed in High5 insect cells using Ac-Lys-Tyr-Lys (e-acetyl)-AMC as substrate after 24 hrs by fluorescence assay B 6.68 pIC50 210.98 nM IC50 Eur J Med Chem (2016) 112: 81-90 [PMID:26890114]
ChEMBL Inhibition of HDAC1 (unknown origin) using Boc-Lys (acetyl)-AMC as substrate preincubated for 30 mins before substrate addition measured after 20 mins by UV-vis spectrophotometer analysis B 6.69 pIC50 203.06 nM IC50 Bioorg Med Chem (2015) 23: 4728-4736 [PMID:26100440]
ChEMBL Inhibitory activity against human Histone deacetylase 1 B 6.7 pIC50 200 nM IC50 J Med Chem (2004) 47: 3409-3417 [PMID:15189037]
ChEMBL Inhibition of human HDAC1 B 6.7 pIC50 200 nM IC50 J Med Chem (2008) 51: 1505-1529 [PMID:18247554]
ChEMBL Inhibition of HDAC1 by in vitro deacetylation assay B 6.7 pIC50 200 nM IC50 Nat Chem Biol (2010) 6: 25-33 [PMID:19966789]
ChEMBL Inhibition of C-terminal His-tagged and C-terminal FLAG-tagged full length human recombinant HDAC1 expressed in baculovirus expression system using fluorogenic acetylated peptide as substrate preincubated with enzyme for 10 mins prior to substrate addition measured after 60 mins by fluorescence analysis B 6.71 pIC50 196 nM IC50 ACS Med Chem Lett (2013) 4: 132-136 [PMID:24900575]
ChEMBL Inhibition of full length recombinant human GST fused His6-tagged HDAC1 expressed in baculovirus infected High5 cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate measured after 24 hrs B 6.71 pIC50 195 nM IC50 Eur J Med Chem (2017) 128: 293-299 [PMID:28213282]
ChEMBL Inhibition of HDAC1 in human HeLa cell nuclear extract using Boc-Lys (Ac)-AMC as substrate after 60 mins by fluorometric analysis B 6.72 pIC50 190 nM IC50 J Med Chem (2015) 58: 9214-9227 [PMID:26555243]
ChEMBL Inhibition of human recombinant HDAC1 expressed in baculovirus infected High5 insect cells using Ac-Lys-Tyr-Lys(e-acetyl)-AMC as substrate incubated for 24 hrs measured after 30 mins by microplate reader based spectrophotometric analysis B 6.72 pIC50 190 nM IC50 Bioorg Med Chem (2020) 28: 115639-115639 [PMID:32773090]
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 6.72 pIC50 190 nM IC50 Eur J Med Chem (2018) 143: 320-333 [PMID:29202397]
ChEMBL Inhibition of recombinant human HDAC1 (482 residues) expressed in baculovirus infected insect cells preincubated with enzyme followed by flour de lys-green substrate addition measured after 1 hr by fluorescence assay B 6.72 pIC50 190 nM IC50 Bioorg Med Chem Lett (2017) 27: 4415-4420 [PMID:28818449]
ChEMBL Inhibition of HDAC1 (unknown origin) incubated for 60 mins using microplate reader analysis B 6.74 pIC50 180.3 nM IC50 J Med Chem (2022) 65: 1243-1264 [PMID:33586434]
ChEMBL Inhibition of human recombinant His6-tagged and GST-fuses HDAC1 expressed in insect High5 cells using Ac-Lys-Tyr-Lys(e-acetyl)-AMC as substrate after 24 hrs by fluorescence assay B 6.74 pIC50 180 nM IC50 Bioorg Med Chem Lett (2012) 22: 4540-4545 [PMID:22738629]
ChEMBL Inhibition of HDAC1 (unknown origin) B 6.74 pIC50 180 nM IC50 Bioorg Med Chem Lett (2021) 31: 127671-127671 [PMID:33229136]
ChEMBL Inhibition of HDAC1 (unknown origin) B 6.74 pIC50 180 nM IC50 Bioorg Med Chem Lett (2021) 38: 127829-127829 [PMID:33685790]
ChEMBL Inhibition of HDAC1 (unknown origin) B 6.74 pIC50 180 nM IC50 Medchemcomm (2014) 5: 342-351
ChEMBL Inhibition of HDAC1 in human HeLa cell nuclear extract using Bos-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition incubated for 30 mins B 6.75 pIC50 178 nM IC50 Eur J Med Chem (2021) 209: 112904-112904 [PMID:33077264]
ChEMBL Inhibition of HDAC1 B 6.77 pIC50 170 nM IC50 Eur J Med Chem (2010) 45: 4331-4338 [PMID:20637529]
ChEMBL Inhibition of recombinant human HDAC1 using Z-(Ac)-Lys-AMC as substrate incubated for 40 mins by fluorescence based assay B 6.79 pIC50 162.7 nM IC50 Eur J Med Chem (2021) 218: 113392-113392 [PMID:33831778]
ChEMBL Inhibition of HDAC 1 in human HeLa nuclear extract using HDAC substrate-3 measured after 60 mins by fluorometric analysis B 6.82 pIC50 150 nM IC50 J Med Chem (2017) 60: 3484-3497 [PMID:28368585]
ChEMBL Inhibition of recombinant HDAC1 (unknown origin) using fluorogenic substrate Boc-Lys (acetyl)-AMC after 20 mins by homogeneous fluorescence release assay B 6.82 pIC50 150 nM IC50 Eur J Med Chem (2015) 96: 1-13 [PMID:25874326]
ChEMBL Inhibition of recombinant HDAC1 (unknown origin) incubated for 10 mins using Boc-Lys(acetyl)-AMC fluorogenic substrate by homogeneous fluorescence release assay B 6.82 pIC50 150 nM IC50 Bioorg Med Chem (2015) 23: 3457-3471 [PMID:25953722]
ChEMBL Inhibition of HDAC1 (unknown origin) using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins and measured after 30 mins by fluorescence assay B 6.85 pIC50 142 nM IC50 Eur J Med Chem (2019) 168: 515-526 [PMID:30851694]
ChEMBL Inhibition of HDAC1 (unknown origin) B 6.85 pIC50 142 nM IC50 Eur J Med Chem (2018) 144: 398-409 [PMID:29288941]
ChEMBL Inhibition of HDAC1 (unknown origin) using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay B 6.85 pIC50 142 nM IC50 J Nat Prod (2019) 82: 1442-1450 [PMID:31120744]
ChEMBL Inhibition of human recombinant HDAC1 using Tosyl-Gly-ProLys(Ac)-AMC as substrate measured after 60 mins by fluorescence assay B 6.85 pIC50 140 nM IC50 J Med Chem (2021) 64: 10403-10417 [PMID:34185525]
ChEMBL Inhibition of recombinant C-terminal FLAG-tagged HDAC1 expressed in baculovirus after 10 mins by fluorimetric analysis B 6.85 pIC50 140 nM IC50 Bioorg Med Chem Lett (2009) 19: 5684-5688 [PMID:19699639]
ChEMBL Inhibition of human HDAC1 B 6.85 pIC50 140 nM IC50 J Med Chem (2008) 51: 7417-7427 [PMID:19007204]
ChEMBL Inhibition of HDAC1 (unknown origin) B 6.86 pIC50 138.5 nM IC50 Eur J Med Chem (2021) 226: 113870-113870 [PMID:34610548]
ChEMBL Inhibition of recombinant human HDAC1 using Boc-Lys(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence-based assay B 6.87 pIC50 136 nM IC50 Eur J Med Chem (2016) 109: 350-359 [PMID:26814680]
ChEMBL Inhibition of human recombinant HDAC1 using fluorogenic substrate measured after 30 mins B 6.88 pIC50 132 nM IC50 Bioorg Med Chem (2023) 79: 117154-117154 [PMID:36645952]
ChEMBL Inhibition of human recombinant HDAC1 using fluorogenic substrate measured after 30 mins B 6.88 pIC50 131.58 nM IC50 Bioorg Med Chem (2023) 79: 117154-117154 [PMID:36645952]
ChEMBL Inhibition of human recombinant HDAC1 after 60 mins by fluorimetric assay B 6.88 pIC50 131 nM IC50 Eur J Med Chem (2014) 86: 639-652 [PMID:25218912]
ChEMBL Inhibition of human recombinant HDAC1 incubated for 10 mins prior to substrate addition measured after 60 mins by spectrophotometric analysis B 6.88 pIC50 131 nM IC50 Bioorg Med Chem Lett (2013) 23: 3295-3299 [PMID:23601706]
ChEMBL Inhibition of C-terminal 6His/FLAG tagged human recombinant HDAC1 (1 to 482 residues) purified as tubulin complex expressed in Sf9 insect cells using Z-Lys(Ac)-AMC as fluorogenic substrate preincubated for 60 mins followed by substrate addition and measured after 90 mins by microplate reader analysis B 6.89 pIC50 128 nM IC50 J Med Chem (2023) 66: 13821-13837 [PMID:37782298]
ChEMBL Inhibition of HDAC activity measured by HDAC Fluorescent Activity Assay (mean of two experiments) F 6.9 pIC50 125 nM IC50 Bioorg Med Chem Lett (2007) 17: 370-375 [PMID:17095213]
ChEMBL Inhibition of HDAC activity measured by HDAC Fluorescent Activity Assay (mean of two experiments) F 6.9 pIC50 125 nM IC50 Bioorg Med Chem Lett (2007) 17: 363-369 [PMID:17107790]
ChEMBL Inhibition of HDAC1 (unknown origin) expressed in HEK293 cells cotransfected with nano-luciferase incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition by NanoBRET assay B 6.91 pIC50 122 nM IC50 J Med Chem (2019) 62: 8557-8577 [PMID:31414801]
ChEMBL Inhibition of HDAC1 B 6.92 pIC50 121 nM IC50 Bioorg Med Chem Lett (2010) 20: 3314-3321 [PMID:20451378]
ChEMBL Inhibition of human recombinant HDAC1 using ZMAL (Z-Lys(Ac)-AMC) fluorogenic substrate incubated for 90 mins by fluorescence based assay B 6.92 pIC50 120 nM IC50 J Med Chem (2020) 63: 10339-10351 [PMID:32803970]
ChEMBL Inhibition of human recombinant HDAC1 expressed in High5 insect cells using Ac-Lys-Tyr-Lys(-acetyl)-AMC as substrate after 24 hrs by fluorescence assay B 6.92 pIC50 120 nM IC50 Bioorg Med Chem (2013) 21: 3240-3244 [PMID:23602523]
ChEMBL Inhibition of human recombinant HDAC1 assessed as fluorescence using fluorogenic substrate ZMAL incubated for 90 min by microplate reader B 6.92 pIC50 120 nM IC50 J Med Chem (2021) 64: 14620-14646 [PMID:34582215]
ChEMBL Inhibition of recombinant HDAC1 by fluorimetric assay B 6.92 pIC50 120 nM IC50 Bioorg Med Chem Lett (2009) 19: 1403-1408 [PMID:19181524]
ChEMBL Inhibition of full length C-terminal 6His/FLAG-tagged human recombinant HDAC1 (1 to 482 residues) purified as tubulin complex expressed in Sf9 cells using ZMAL as fluorogenic substrate incubated for 90 mins by microplate reader analysis B 6.92 pIC50 120 nM IC50 J Med Chem (2023) 66: 14787-14814 [PMID:37902787]
ChEMBL Inhibition of HDAC1 (unknown origin) B 6.92 pIC50 120 nM IC50 Bioorg Med Chem Lett (2015) 25: 4457-4460 [PMID:26376355]
ChEMBL Inhibition of human recombinant HDAC1 expressed in baculovirus infected insect High5 cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate by fluorescence assay B 6.92 pIC50 120 nM IC50 Bioorg Med Chem Lett (2011) 21: 4844-4846 [PMID:21745740]
ChEMBL Inhibition of human recombinant HDAC1 after 15 mins by fluorimetric assay B 6.92 pIC50 120 nM IC50 J Med Chem (2010) 53: 4654-4667 [PMID:20491440]
ChEMBL Inhibition of human recombinant HDAC1 using ZMAL (Z-(Ac)Lys-AMC fluorogenic substrate incubated for 90 mins by fluorescence method B 6.92 pIC50 119.5 nM IC50 ACS Med Chem Lett (2019) 10: 671-676 [PMID:30996816]
ChEMBL Inhibition of full length GST-tagged human HDAC1 using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay B 6.92 pIC50 119 nM IC50 Bioorg Med Chem Lett (2014) 24: 5450-5454 [PMID:25454270]
ChEMBL Inhibition of full length recombinant HDAC1 using Fluor de Lys as substrate by fluorescence assay B 6.92 pIC50 119 nM IC50 J Med Chem (2011) 54: 4694-4720 [PMID:21634430]
ChEMBL Inhibition of full length FLAG-tagged recombinant HDAC1 (unknown origin) transfected in human HeLa cells assessed as deacetylation of [3H]-acetylated histones after 2 hrs by scintillation counting analysis B 6.92 pIC50 119 nM IC50 J Med Chem (2013) 56: 7201-7211 [PMID:23964961]
ChEMBL Inhibition of human HDAC1 using (Z-(Ac)Lys-AMC) as substrate after 90 mins by fluorescence analysis B 6.92 pIC50 119 nM IC50 J Med Chem (2016) 59: 1545-1555 [PMID:26653328]
ChEMBL Ex vivo inhibition of human HDAC1 in human Caco-2 cells by fluorometric cellular activity assay B 6.92 pIC50 119 nM IC50 J Med Chem (2010) 53: 1937-1950 [PMID:20143840]
ChEMBL Inhibition of recombinant human HDAC1 using Cbz-(Ac)Lys-AMC as substrate preincubated for 90 mins followed by trypsin addition measured after 20 mins by fluorescence assay B 6.93 pIC50 117 nM IC50 J Med Chem (2016) 59: 2423-2435 [PMID:26937828]
ChEMBL Inhibition of recombinant C-terminal His/FLAG-tagged human HDAC1 expressed in baculovirus expression system using fluorogenic ZMAL as substrate incubated for 90 mins by fluorescence assay B 6.93 pIC50 117 nM IC50 J Med Chem (2019) 62: 1138-1166 [PMID:30645113]
ChEMBL Inhibition of recombinant human full length C-terminal His/FLAG-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells using ZMAL as substrate incubated for 90 mins by fluorescence assay B 6.95 pIC50 111 nM IC50 J Med Chem (2019) 62: 11260-11279 [PMID:31762274]
ChEMBL Inhibition of recombinant human FLAG/His-tagged HDAC1 expressed in baculovirus expression system using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay B 6.96 pIC50 110 nM IC50 Eur J Med Chem (2018) 158: 620-706 [PMID:30245394]
ChEMBL Inhibition of HDAC1 by fluorometric assay B 6.96 pIC50 110 nM IC50 Bioorg Med Chem Lett (2012) 22: 6200-6204 [PMID:22932316]
ChEMBL Inhibition of HDAC1 (unknown origin) using RHKK(Ac) (379 to 382) p53 peptide as substrate by fluorescence assay B 6.96 pIC50 110 nM IC50 J Med Chem (2014) 57: 4009-4022 [PMID:24766560]
ChEMBL Inhibition of C-terminal His/FLAG-tagged full length recombinant human HDAC1 expressed in baculovirus expression system assessed as release of 7-amino-4-methylcoumarin by fluorogenic assay B 6.96 pIC50 110 nM IC50 Eur J Med Chem (2016) 122: 92-101 [PMID:27344487]
ChEMBL Inhibition of HDAC1 (unknown origin) B 6.96 pIC50 110 nM IC50 Eur J Med Chem (2016) 121: 451-483 [PMID:27318122]
ChEMBL Inhibition of recombinant human full length HDAC1 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis B 6.96 pIC50 110 nM IC50 Eur J Med Chem (2017) 134: 13-23 [PMID:28395150]
ChEMBL Inhibition of human HDAC1 using Boc-Lys (acetyl)-AMC as substrate pretreated with compound for 1 hrs followed by substrate addition measured after 1 hrs by microplate reader analysis B 6.97 pIC50 106.13 nM IC50 Eur J Med Chem (2022) 243: 114705-114705 [PMID:36215854]
ChEMBL Inhibition of HDAC1 (unknown origin) using substrate after 30 mins by fluorometric analysis B 6.97 pIC50 106 nM IC50 Eur J Med Chem (2017) 133: 11-23 [PMID:28371677]
ChEMBL Inhibition of C-terminal 6His tagged human recombinant full length HDAC1 (1 to 482 residues) using Z- Lys(Ac)-AMC as fluorogenic substrate incubated for 90 mins followed by trypsin addition and measured after 30 min by microplate reader analysis B 6.99 pIC50 102.8 nM IC50 ACS Med Chem Lett (2023) 14: 1863-1868 [PMID:38116436]
ChEMBL Inhibition of HDAC1 (unknown origin) using Boc-Lys(Ac)-AMC or Boc-Lys(Tfa)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 2 hrs by fluorescence assay B 6.99 pIC50 102 nM IC50 Bioorg Med Chem (2023) 85: 117242-117242 [PMID:37079967]
ChEMBL Inhibition of recombinant human HDAC1 using fluorogenic substrate by fluorescence assay B 6.99 pIC50 101.98 nM IC50 Eur J Med Chem (2017) 125: 1268-1278 [PMID:27886544]
ChEMBL Inhibition of recombinant full length C-terminal FLAG/His-tagged human HDAC1 expressed in baculovirus infected Sf9 cells using Z-Lys(Ac)-AMC as substrate incubated for 90 mins followed by trypsin addition and measured after 30 mins by fluorescence based assay B 7 pIC50 101 nM IC50 Medchemcomm (2019) 10: 1109-1115 [PMID:31391882]
ChEMBL Inhibition of human recombinant C-terminal FLAG-tagged HDAC1 expressed in baculovirus by fluorimetry B 7 pIC50 100 nM IC50 Bioorg Med Chem Lett (2009) 19: 336-340 [PMID:19084395]
ChEMBL Inhibition of recombinant human HDAC1 expressed in baculovirus infected High5 insect cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate after 24 hrs by fluorescence assay B 7 pIC50 100 nM IC50 Bioorg Med Chem (2018) 26: 4706-4715 [PMID:30115492]
ChEMBL Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using Z-Lys(Ac)-AMC as fluorogenic substrate incubated for 90 mins by microplate reader analysis B 7 pIC50 99 nM IC50 J Med Chem (2022) 65: 15457-15472 [PMID:36351184]
ChEMBL Inhibition of recombinant human His-tagged HDAC1 (482 residues) expressed in baculovirus infected insect cells using Boc Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay B 7.01 pIC50 98.13 nM IC50 Eur J Med Chem (2018) 158: 620-706 [PMID:30245394]
ChEMBL Inhibition of HDAC1 in human HeLa cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence based analysis B 7.01 pIC50 98.13 nM IC50 Bioorg Med Chem (2021) 52: 116510-116510 [PMID:34826681]
ChEMBL Inhibition of HDAC1 after 30 mins by Fluor de Lys fluorescence assay B 7.02 pIC50 96 nM IC50 Bioorg Med Chem Lett (2011) 21: 6139-6142 [PMID:21889343]
ChEMBL Inhibition of HDAC1 after 17 hrs B 7.02 pIC50 96 nM IC50 J Med Chem (2008) 51: 4370-4373 [PMID:18642892]
ChEMBL Inhibition of human recombinant HDAC1 B 7.02 pIC50 96 nM IC50 Bioorg Med Chem Lett (2009) 19: 3023-3026 [PMID:19419863]
ChEMBL Inhibition of HDAC1 using Fluor-de-Lys as substrate compound pretreated for 30 mins before substrate addition by fluorescence assay B 7.02 pIC50 96 nM IC50 Bioorg Med Chem Lett (2012) 22: 7084-7086 [PMID:23089527]
ChEMBL Inhibition of HDAC1 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs B 7.02 pIC50 96 nM IC50 J Med Chem (2010) 53: 1347-1356 [PMID:20055418]
ChEMBL Inhibition of HDAC1 (unknown origin) using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method B 7.03 pIC50 93.6 nM IC50 Eur J Med Chem (2021) 225: 113799-113799 [PMID:34500130]
ChEMBL Inhibition of recombinant His6-tagged GST-fused human HDAC1 expressed in baculovirus infected insect High5 cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate after 24 hrs B 7.03 pIC50 93.34 nM IC50 Bioorg Med Chem (2015) 23: 5881-5890 [PMID:26211462]
ChEMBL Inhibition of human recombinant full length HDAC1 using (Ac)-Lys-Tyr-Lys(-acetyl)-AMC substrate after 30 mins B 7.03 pIC50 93.34 nM IC50 Bioorg Med Chem (2014) 22: 6146-6155 [PMID:25261927]
ChEMBL Inhibition of HDAC1 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition by fluorescence assay B 7.04 pIC50 91 nM IC50 Medchemcomm (2015) 6: 1816-1825
ChEMBL Inhibition of human recombinant HDAC1 expressed in baculovirus infected insect high5 cells using Ac-Lys-Tyr-Lys (epsilon-acetyl)-AMC as substrate after 3 to 24 hrs by fluorescence assay B 7.05 pIC50 90 nM IC50 Bioorg Med Chem (2013) 21: 6981-6995 [PMID:24095018]
ChEMBL Inhibition of recombinant HDAC1 (unknown origin) using Fluor-de-Lys-SIRT1 as substrate by fluorescence assay B 7.05 pIC50 90 nM IC50 J Nat Prod (2014) 77: 49-56 [PMID:24328302]
ChEMBL Inhibition of recombinant his-tagged human HDAC1 using Ac-LeuGlyLys (Ac) AMC substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence based microplate reader analysis B 7.05 pIC50 89 nM IC50 J Med Chem (2022) 65: 12200-12218 [PMID:36097406]
ChEMBL Inhibition of recombinant human full length C-terminal Flag/His-tagged HDAC1 expressed in baculovirus infected Sf9 cells using ZMAL as substrate incubated for 90 mins by fluorometric method B 7.05 pIC50 89 nM IC50 Bioorg Med Chem (2019) 27: 115039-115039 [PMID:31420257]
ChEMBL Inhibition of recombinant human HDAC1 after 60 mins by fluorescence assay B 7.05 pIC50 88.5 nM IC50 J Med Chem (2015) 58: 7672-7680 [PMID:26331334]
ChEMBL Inhibition of recombinant full length C-terminal His/Flag-tagged human HDAC1 (1 to 482 residues) using Z-Lys(Ac)-AMC as substrate preincubated for 90 mins followed by trypsin addition and measured after 30 mins by fluorescence based microplate reader analysis B 7.06 pIC50 88 nM IC50 J Med Chem (2022) 65: 16860-16878 [PMID:36473103]
ChEMBL Inhibition of HDAC1 (unknown origin) measured after 30 mins by fluorescence microplate reader assay B 7.06 pIC50 87.9 nM IC50 J Med Chem (2021) 64: 15280-15296 [PMID:34624191]
ChEMBL Inhibition of HDAC1 (unknown origin) using (FAM)-labeled acetylated peptide as substrate measured after 17 hrs by fluorescence assay B 7.06 pIC50 87.4 nM IC50 Eur J Med Chem (2018) 158: 620-706 [PMID:30245394]
ChEMBL Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay B 7.07 pIC50 85 nM IC50 Bioorg Med Chem (2018) 26: 1418-1425 [PMID:29500130]
ChEMBL Inhibition of HDAC1 (unknown origin) using Boc-Lys(Ac)-pNA as substrate preincubated for 20 mins followed by substrate addition and further incubated for 90 mins by fluorescence assay B 7.09 pIC50 82 nM IC50 J Med Chem (2020) 63: 6959-6978 [PMID:32551649]
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 7.09 pIC50 81 nM IC50 J Med Chem (2018) 61: 1552-1575 [PMID:29360358]
ChEMBL Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using fluorometric substrate measured after 60 mins by FRET assay B 7.1 pIC50 80 nM IC50 J Med Chem (2021) 64: 4020-4033 [PMID:33745280]
ChEMBL Inhibition of human recombinant HDAC1 using fluorogenic p53 (379-382 residues) (RHKK(Ac)AMC) as substrate B 7.11 pIC50 77 nM IC50 Eur J Med Chem (2023) 247: 115022-115022 [PMID:36549114]
ChEMBL Inhibition of purified recombinant HDAC1 B 7.11 pIC50 77 nM IC50 Bioorg Med Chem Lett (2011) 21: 4909-4912 [PMID:21742496]
ChEMBL Inhibition of recombinant human HDAC1 using Cbz-Lys(TFAc)-AMC as substrate by fluorometric analysis B 7.12 pIC50 76 nM IC50 Bioorg Med Chem Lett (2010) 20: 7067-7070 [PMID:20947351]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.12 pIC50 76 nM IC50 Eur J Med Chem (2021) 209: 112887-112887 [PMID:33035922]
ChEMBL Inhibition of HDAC1 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated with enzyme for 5 mins prior to substrate addition measured after 30 mins by fluorescence assay B 7.12 pIC50 76 nM IC50 ACS Med Chem Lett (2013) 4: 235-238 [PMID:23493449]
ChEMBL Inhibition of HDAC1 (unknown origin) preincubated for 5 mins followed by substrate addition and measured after 30 mins by multimode microplate reader analysis B 7.12 pIC50 75 nM IC50 J Med Chem (2022) 65: 12838-12859 [PMID:36153841]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.14 pIC50 73 nM IC50 J Med Chem (2021) 64: 26-41 [PMID:33346659]
ChEMBL Inhibition of HDAC1 (unknown origin) pre-incubated for 5 mins before fluorogenic substrate Boc-Lys (acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC addition and measured after 30 mins by fluorescence based assay B 7.14 pIC50 71.8 nM IC50 J Med Chem (2020) 63: 4701-4715 [PMID:32267687]
ChEMBL Inhibition of C-terminal 6His/FLAG-tagged human recombinant full-length HDAC1 (1 to 482(end) residues) using Boc-Lys-(Ac)-AMC as substrate incubated for 10 mins followed by substrate addition measured after 1 hr by fluorescence based analysis B 7.15 pIC50 70.65 nM IC50 J Med Chem (2023) 66: 11761-11791 [PMID:37585683]
ChEMBL Inhibition of HDAC1 in human HeLa cell nuclear extract using Boc-Lys(Ac)-AMC or Boc-Lys(triflouroacetyl)-AMC as substrate incubated for 30 mins and measured by fluorescence assay B 7.15 pIC50 70 nM IC50 Eur J Med Chem (2022) 241: 114634-114634 [PMID:35939996]
ChEMBL Inhibition of full length recombinant C-terminal GST-tagged human HDAC1 expressed in baculovirus infected Sf9 insect cells incubated for 50 mins by Glo- luminescence assay B 7.15 pIC50 70 nM IC50 J Med Chem (2022) 65: 12346-12366 [PMID:36053318]
ChEMBL Inhibition of human recombinant full-length HDAC1 (1 to 482 residues) expressed in baculovirus using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay B 7.16 pIC50 69 nM IC50 Eur J Med Chem (2017) 141: 596-602 [PMID:29102179]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.16 pIC50 69 nM IC50 Bioorg Med Chem Lett (2020) 30: 127128-127128 [PMID:32247729]
ChEMBL Inhibition of recombinant HDAC1 using Ac-Lys(Ac)-AMC as substrate after 30 mins by fluorescence analysis B 7.16 pIC50 69 nM IC50 ACS Med Chem Lett (2012) 3: 505-508 [PMID:24900500]
ChEMBL Inhibition of human recombinant HDAC1 B 7.17 pIC50 68.1 nM IC50 Eur J Med Chem (2009) 44: 1067-1085 [PMID:18672316]
ChEMBL Inhibition of HDAC1 B 7.17 pIC50 68 nM IC50 J Med Chem (2008) 51: 3437-3448 [PMID:18494463]
ChEMBL Inhibition of HDAC1 in human HeLa cells using BOC-K(Ac)-AMC as substrate measured after 30 mins by fluorescence based microtiter plate reader assay B 7.18 pIC50 66 nM IC50 J Med Chem (2022) 65: 11187-11213 [PMID:35926141]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.18 pIC50 65.4 nM IC50 Eur J Med Chem (2015) 89: 628-637 [PMID:25462271]
ChEMBL Inhibition of human HDAC1 using H3(1-21)K9 after 60 mins by fluorescence assay B 7.19 pIC50 65.2 nM IC50 J Nat Prod (2017) 80: 201-204 [PMID:28026946]
ChEMBL Inhibition of human HDAC1 after 30 mins by microplate reader analysis B 7.19 pIC50 65 nM IC50 Bioorg Med Chem Lett (2020) 30: 127023-127023 [PMID:32067866]
ChEMBL Inhibition of full-length recombinant human HDAC1 (1 to 482 residues) expressed in baculovirus infected insect cells using Ac-Leu-Gly-Lys(Tfa)-AMC as substrate incubated for 30 mins by fluorescence based analysis B 7.19 pIC50 64 nM IC50 J Med Chem (2023) 66: 5950-5964 [PMID:37037787]
ChEMBL Inhibition of C-terminal FLAG/His-tagged full length recombinant human HDAC1 expressed in baculovirus infected Sf9 insect cells using KI 177 as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay B 7.2 pIC50 63.5 nM IC50 Eur J Med Chem (2018) 143: 792-805 [PMID:29223096]
ChEMBL Inhibition of HDAC1 using KI-177 as substrate incubated 30 mins before substrate addition measured after 30 mins post substrate addition by fluorescence assay B 7.2 pIC50 62.9 nM IC50 Eur J Med Chem (2011) 46: 4042-4049 [PMID:21712146]
ChEMBL Inhibition of human HDAC1 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay B 7.21 pIC50 61 nM IC50 J Med Chem (2011) 54: 2165-2182 [PMID:21417297]
ChEMBL Inhibition of recombinant HDAC1 (unknown origin) measured after 30 mins by fluorescence assay B 7.21 pIC50 61 nM IC50 Eur J Med Chem (2019) 180: 171-190 [PMID:31306905]
ChEMBL Inhibition of HDAC1 (unknown origin) using FAM-RHKK(Ac)-NH2/FAM-RHKK(trifluoroacetyl)-NH2 as substrate preincubated for 15 mins followed by substrate addition and measured after 3 hrs by microfluidic chip based fluorescence assay B 7.22 pIC50 60.7 nM IC50 Bioorg Med Chem (2022) 56: 116599-116599 [PMID:35041998]
ChEMBL Inhibition of HDAC1 (unknown origin) using Boc-Lys(Ac)-AMC as substrate incubated for 30 mins by fluorescence based analysis B 7.22 pIC50 60 nM IC50 J Med Chem (2023) 66: 14150-14174 [PMID:37796543]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.23 pIC50 59 nM IC50 Bioorg Med Chem Lett (2017) 27: 3289-3293 [PMID:28648462]
ChEMBL Inhibition of human recombinant full length HDAC1 using fluorogenic substrate 3 after 30 mins by fluorescence assay B 7.25 pIC50 56 nM IC50 J Med Chem (2018) 61: 7245-7260 [PMID:30045621]
ChEMBL Inhibition of full-length recombinant human C-terminal GST tagged HDAC1 expressed in Sf9 insect cells using aminoluciferin peptide substrate preincubated for 3 hrs followed by substrate addition and measured after 30 mins by HDAC-Glo I/II chemiluminescence assay B 7.26 pIC50 55 nM IC50 J Med Chem (2023) 66: 15171-15188 [PMID:37847303]
ChEMBL Inhibition of HDAC1 (unknown origin) by fluorescence based assay B 7.26 pIC50 54.6 nM IC50 Eur J Med Chem (2021) 209: 112868-112868 [PMID:33077265]
ChEMBL Inhibition of HDAC1 (unknown origin) preincubated for 120 mins B 7.27 pIC50 53.78 nM IC50 Bioorg Med Chem Lett (2022) 70: 128797-128797 [PMID:35580726]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.28 pIC50 52 nM IC50 Bioorg Med Chem (2023) 92: 117437-117437 [PMID:37563016]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.28 pIC50 52 nM IC50 Bioorg Med Chem Lett (2013) 23: 3346-3348 [PMID:23591111]
ChEMBL Inhibition of HDAC1 (unknown origin) preincubated for 90 mins B 7.29 pIC50 51.75 nM IC50 Bioorg Med Chem Lett (2022) 70: 128797-128797 [PMID:35580726]
ChEMBL Inhibition of recombinant full length human HDAC1 (1 to 482 amino acids) expressed in Baculovirus infected insect Sf9 cells incubated for 30 mins measured by fluorescence assay B 7.29 pIC50 51 nM IC50 Medchemcomm (2014) 5: 1887-1891
ChEMBL Inhibition of HDAC1 in human HeLa nuclear extract B 7.29 pIC50 51 nM IC50 J Med Chem (2023) 66: 7698-7729 [PMID:37276138]
ChEMBL Inhibition of human recombinant HDAC1 B 7.3 pIC50 50 nM IC50 J Med Chem (2023) 66: 7698-7729 [PMID:37276138]
ChEMBL Inhibition of HDAC1 in human HeLa nuclear extract using Boc-Lys(Ac)-AMC as substrate measured after 2 hrs by fluorescence based assay B 7.3 pIC50 50 nM IC50 J Med Chem (2018) 61: 1552-1575 [PMID:29360358]
ChEMBL Inhibition of human recombinant HDAC1 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate by measuring fluorescence intensity incubated for 30 mins by microplate reader assay B 7.31 pIC50 49 nM IC50 Eur J Med Chem (2021) 217: 113363-113363 [PMID:33744687]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.32 pIC50 48 nM IC50 Eur J Med Chem (2020) 185: 111725-111725 [PMID:31655430]
ChEMBL Inhibition of HDAC1 B 7.32 pIC50 48 nM IC50 J Med Chem (2008) 51: 7053-7056 [PMID:18942826]
ChEMBL Inhibition of human HDAC 1 B 7.32 pIC50 48 nM IC50 Bioorg Med Chem Lett (2007) 17: 3969-3971 [PMID:17507219]
ChEMBL Inhibition of HDAC1 (unknown origin) preincubated for 60 mins B 7.32 pIC50 47.95 nM IC50 Bioorg Med Chem Lett (2022) 70: 128797-128797 [PMID:35580726]
ChEMBL Inhibition of human recombinant HDAC1 after 15 mins by fluorogenic assay B 7.32 pIC50 47.4 nM IC50 J Med Chem (2015) 58: 4550-4572 [PMID:25993269]
ChEMBL Inhibition of full length recombinant FLAG/His-tagged C-terminal human HDAC1 expressed in baculovirus infected Sf9 insect cells using ZMAL (Z-Lys(Ac)-AMC) as substrate incubated for 90 mins by fluorescence based assay B 7.33 pIC50 47 nM IC50 ACS Med Chem Lett (2019) 10: 1336-1340 [PMID:31531206]
ChEMBL Inhibition of HDAC1 (unknown origin) using Ac-LeuGlyLys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay B 7.34 pIC50 46 nM IC50 ACS Med Chem Lett (2019) 10: 1122-1127 [PMID:31413795]
ChEMBL Inhibition of HDAC1 (unknown origin) using Ac-LeuGlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and further incubated for incubated for 1 hrs by fluorescence microtiter plate reader assay B 7.34 pIC50 45.5 nM IC50 Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929]
ChEMBL Inhibition of C-terminal FLAG/His-tagged recombinant human HDAC1 expressed in baculovirus infected Sf9 insect cells using Z-(Ac)Lys-AMC as substrate measured after 90 mins by fluorescence assay B 7.35 pIC50 45 nM IC50 J Med Chem (2017) 60: 5493-5506 [PMID:28574690]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.35 pIC50 45 nM IC50 Bioorg Med Chem Lett (2017) 27: 4885-4888 [PMID:28947154]
ChEMBL Inhibition of recombinant full length human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using Z-(Ac)Lys-AMC as substrate measured after 90 mins by fluorescence assay B 7.35 pIC50 45 nM IC50 J Med Chem (2017) 60: 5334-5348 [PMID:28581289]
ChEMBL Inhibition of recombinant human full length HDAC1 expressed in baculovirus infected Sf9 insect cells using biotinylated lysine 9 acetylated histone H3 (1 to 21 residues) as substrate incubated for 5 mins followed by substrate addition measured after 60 mins by HTRF assay B 7.36 pIC50 44 nM IC50 ACS Med Chem Lett (2017) 8: 830-834 [PMID:28835797]
ChEMBL Inhibition of human recombinant HDAC1 using fluorogenic HDAC substrate incubated for 30 mins by fluorescence assay B 7.36 pIC50 44 nM IC50 Eur J Med Chem (2020) 187: 111970-111970 [PMID:31881454]
ChEMBL Inhibition of human HDAC1 incubated for 30 mins by SpectraMax M2 microplate reader analysis B 7.36 pIC50 44 nM IC50 Eur J Med Chem (2021) 209: 112904-112904 [PMID:33077264]
ChEMBL Inhibition of human HDAC1 expressed in Escherichia coli using fluorogenic substrate treated for 5 mins before substrate addition measured after 30 mins by fluorescence assay B 7.36 pIC50 44 nM IC50 Eur J Med Chem (2011) 46: 5387-5397 [PMID:21924799]
ChEMBL Inhibition of full length human C-terminal His-tagged/C-terminal Flag-tagged HDAC1 using fluorogenic acetylated peptide as substrate incubated for 30 mins by fluorescence plate reader assay B 7.36 pIC50 43.9 nM IC50 J Med Chem (2021) 64: 3392-3426 [PMID:33661013]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.36 pIC50 43.76 nM IC50 Bioorg Med Chem Lett (2022) 70: 128797-128797 [PMID:35580726]
ChEMBL Inhibition of recombinant HDAC1 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based micro plate reader analysis B 7.36 pIC50 43.76 nM IC50 J Med Chem (2020) 63: 5501-5525 [PMID:32321249]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.37 pIC50 43 nM IC50 Eur J Med Chem (2016) 108: 274-286 [PMID:26689485]
ChEMBL Inhibition of HDAC1 (unknown origin) preincubated for 30 mins B 7.37 pIC50 42.82 nM IC50 Bioorg Med Chem Lett (2022) 70: 128797-128797 [PMID:35580726]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.37 pIC50 42.5 nM IC50 J Med Chem (2019) 62: 3171-3183 [PMID:30418766]
ChEMBL Inhibition of HDAC1 (unknown origin) using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay B 7.38 pIC50 42 nM IC50 Bioorg Med Chem Lett (2019) 29: 2638-2645 [PMID:31400938]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.38 pIC50 42 nM IC50 Eur J Med Chem (2018) 158: 620-706 [PMID:30245394]
ChEMBL Inhibition of human recombinant HDAC1 using fluorogenic HDAC substrate preincubated for 30 mins followed by substrate addition and measured after 15 mins by fluorogenic assay B 7.38 pIC50 42 nM IC50 Bioorg Med Chem (2020) 28: 115345-115345 [PMID:32061484]
ChEMBL Inhibition of human recombinant HDAC1 after 30 mins by fluorescence assay B 7.38 pIC50 42 nM IC50 J Med Chem (2013) 56: 5782-5796 [PMID:23786452]
ChEMBL Inhibition of human full-length recombinant HDAC1 preincubated for 5 mins followed by HDAC substrate addition and further incubated for 45 mins by fluorescence microplate reader assay B 7.39 pIC50 41 nM IC50 Eur J Med Chem (2021) 222: 113569-113569 [PMID:34111829]
ChEMBL Inhibition of HDAC1 in human HeLa cells nuclear extract using Fluor-de-Lys as substrate after 30 mins by spectrophotometry B 7.39 pIC50 41 nM IC50 ACS Med Chem Lett (2011) 2: 703-707 [PMID:21984958]
ChEMBL Inhibition of recombinant human HDAC1 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry B 7.39 pIC50 41 nM IC50 ACS Med Chem Lett (2011) 2: 703-707 [PMID:21984958]
ChEMBL Inhibition of full length human recombinant HDAC1 expressed in baculovirus expression system using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay B 7.4 pIC50 40 nM IC50 J Med Chem (2018) 61: 6056-6074 [PMID:29940115]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.4 pIC50 40 nM IC50 Eur J Med Chem (2021) 219: 113419-113419 [PMID:33845233]
ChEMBL Inhibition of full-length recombinant human HDAC1 (1 to 482 residues) expressed in baculovirus infected insect cells using Ac-Leu-Gly-Lys(Ac)-AMC as substrate incubated for 30 mins by fluorescence based assay B 7.4 pIC50 40 nM IC50 J Med Chem (2023) 66: 1239-1253 [PMID:36622852]
ChEMBL Inhibition of recombinant human HDAC1 using Boc-Lys-(acetyl)-AMC as substrate incubated for 0.5 hr and measured after 20 mins by fluorescence assay B 7.4 pIC50 40 nM IC50 Eur J Med Chem (2022) 233: 114228-114228 [PMID:35245830]
ChEMBL Inhibition of HDAC1 (unknown origin) preincubated for 5 mins B 7.4 pIC50 39.91 nM IC50 Bioorg Med Chem Lett (2022) 70: 128797-128797 [PMID:35580726]
ChEMBL Inhibition of HDAC1 (unknown origin) in using Boc-Lys(acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay B 7.4 pIC50 39.8 nM IC50 J Med Chem (2020) 63: 12083-12099 [PMID:33021789]
ChEMBL Inhibition of His-tagged HDAC1 (unknown origin) expressed in Escherichia coli BL21(DE3) after 60 mins by MALDI mass spectrometry B 7.42 pIC50 38 nM IC50 Eur J Med Chem (2015) 96: 340-359 [PMID:25899338]
ChEMBL Inhibition of human HDAC1 preincubated for 15 mins followed by substrate addition by fluorescence-based assay B 7.42 pIC50 38 nM IC50 Eur J Med Chem (2021) 218: 113383-113383 [PMID:33799069]
ChEMBL Inhibition of HDAC1 in human HeLa cell nuclear extract using Fluor de Lys as substrate after 15 mins by fluorometric analysis B 7.42 pIC50 38 nM IC50 J Med Chem (2012) 55: 1465-1477 [PMID:22260166]
ChEMBL Inhibition of HDAC1 (unknown origin) at 10 uM after 60 mins by SAMDI spectrophotometric analysis relative to control B 7.42 pIC50 38 nM IC50 J Med Chem (2013) 56: 3492-3506 [PMID:23547652]
ChEMBL Inhibition of HDAC1 (unknown origin) expressed in Escherichia coli BL21 (DE3) using GRKacFGC as substrate after 60 mins by SAMDI mass spectrometric analysis B 7.42 pIC50 38 nM IC50 J Med Chem (2013) 56: 9969-9981 [PMID:24304348]
ChEMBL Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using Boc-Lys (Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay B 7.42 pIC50 38 nM IC50 Eur J Med Chem (2020) 188: 111991-111991 [PMID:31883490]
ChEMBL Inhibition of full length human recombinant HDAC1 expressed in baculovirus using Ac-Leu-GlyLys(Ac)-AMC as substrate after 30 mins by fluorescence assay B 7.42 pIC50 38 nM IC50 J Med Chem (2015) 58: 4325-4338 [PMID:25906087]
ChEMBL Inhibition of HDAC1 in human HeLa cells using Fluor-de-Lys as substrate after 15 mins by fluorescence assay B 7.42 pIC50 38 nM IC50 Bioorg Med Chem Lett (2013) 23: 3283-3287 [PMID:23622981]
ChEMBL Inhibition of recombinant human HDAC1 using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay B 7.42 pIC50 37.7 nM IC50 Bioorg Med Chem Lett (2020) 30: 127638-127638 [PMID:33132117]
ChEMBL Inhibition of full length recombinant human C-terminal FLAG-tagged HDAC1 expressed in sf9 cells preincubated for 5 mins followed by biotinylated H3K9-Ac substrate addition and measured after 60 mins by HTRF assay B 7.46 pIC50 35 nM IC50 Bioorg Med Chem Lett (2019) 29: 349-352 [PMID:30594434]
ChEMBL Inhibition of HDAC1 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay B 7.46 pIC50 34.6 nM IC50 J Med Chem (2014) 57: 3324-3341 [PMID:24694055]
ChEMBL Inhibition of human recombinant HDAC1 using Boc-L-Lys (Ac)-AMC as substrate preincubated with compound for 3 hrs measured after 35 mins by spectrofluorometric analysis B 7.47 pIC50 34 nM IC50 Bioorg Med Chem Lett (2012) 22: 5025-5030 [PMID:22771007]
ChEMBL Inhibition of human recombinant HDAC1 using MAZ1600 as fluorogenic substrate measured every 5 mins by optimized homogenous fluorescence based assay B 7.47 pIC50 34 nM IC50 J Med Chem (2015) 58: 4812-4821 [PMID:25974739]
ChEMBL Inhibition of human recombinant HDAC1 expressed in Escherichia coli BL21(DE3) cells using KL177 as substrate preincubated for 5 followed by substrate addition and measured after 30 mins by fluorescence based assay B 7.47 pIC50 33.5 nM IC50 ACS Med Chem Lett (2020) 11: 713-719 [PMID:32435375]
ChEMBL Inhibition of recombinant HDAC1 expressed in HEK293 cells B 7.48 pIC50 33 nM IC50 J Med Chem (2008) 51: 3985-4001 [PMID:18558669]
ChEMBL Inhibition of HDAC1 (unknown origin) by ELISA-based assay B 7.48 pIC50 33 nM IC50 Bioorg Med Chem Lett (2017) 27: 3254-3258 [PMID:28648461]
ChEMBL Inhibition of HADC1 (unknown origin) B 7.48 pIC50 33 nM IC50 J Med Chem (2020) 63: 23-39 [PMID:31415174]
ChEMBL Inhibition of human recombinant HDAC1 using ZMAL (Z-(Ac)Lys-AMC) as fluorogenic substrate incubated for 120 mins by microplate reader assay B 7.48 pIC50 33 nM IC50 J Med Chem (2021) 64: 9960-9988 [PMID:34251197]
ChEMBL Inhibition of HDAC1 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA B 7.48 pIC50 33 nM IC50 ACS Med Chem Lett (2017) 8: 281-286 [PMID:28337317]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.48 pIC50 33 nM IC50 J Med Chem (2022) 65: 3080-3097 [PMID:35148101]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.48 pIC50 33 nM IC50 Bioorg Med Chem Lett (2021) 47: 128207-128207 [PMID:34146703]
ChEMBL Inhibition of HDAC1 in human HeLa-S3 cell lysates preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 40 mins by fluorimetric method B 7.48 pIC50 33 nM IC50 Eur J Med Chem (2018) 143: 1790-1806 [PMID:29150330]
ChEMBL Inhibition of full length his6/FLAG-tagged human recombinant HDAC1(1 to 482 residues) expressed in Sf9 insect cells B 7.48 pIC50 33 nM IC50 J Med Chem (2022) 65: 14764-14791 [PMID:36306372]
ChEMBL Inhibition of recombinant human His-tagged HDAC1 expressed in insect cells using Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured after 30 mins by fluorescence assay B 7.49 pIC50 32.33 nM IC50 Eur J Med Chem (2020) 205: 112648-112648 [PMID:32791401]
ChEMBL Inhibition of recombinant C-terminal His/FLAG-tagged HDAC1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr B 7.49 pIC50 32 nM IC50 J Med Chem (2019) 62: 6992-7014 [PMID:31117517]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.51 pIC50 31 nM IC50 Bioorg Med Chem Lett (2017) 27: 744-749 [PMID:28131715]
ChEMBL Inhibition of recombinant human HDAC1 using Ac-GAK(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence-based assay B 7.51 pIC50 31 nM IC50 J Med Chem (2021) 64: 4810-4840 [PMID:33830764]
ChEMBL Inhibition of HDAC1 in human HeLa cells after 72 hrs by ELISA B 7.51 pIC50 31 nM IC50 Eur J Med Chem (2018) 146: 79-92 [PMID:29396364]
ChEMBL Inhibition of recombinant human full length HDAC1 expressed in baculovirus infected Sf9 insect cells using p53 (379 to 382 residues) derived RHKKAc as substrate preincubated for 5 to 10 mins followed by substrate addition measured after 2 hrs by fluorescence assay B 7.51 pIC50 31 nM IC50 ACS Med Chem Lett (2017) 8: 1031-1036 [PMID:29057046]
ChEMBL Inhibition of HDAC1 in HEK293 cells B 7.52 pIC50 30 nM IC50 Bioorg Med Chem Lett (2008) 18: 1814-1819 [PMID:18308563]
ChEMBL Inhibition of human HDAC1 pre-incubated for 30 mins before substrate addition and measured after 30 mins by HDAC-Glo I/II assay B 7.52 pIC50 30 nM IC50 Bioorg Med Chem (2014) 22: 3720-3731 [PMID:24864038]
ChEMBL Inhibition of human recombinant full length HDAC1 using (Ac)Arg-Gly-Lys(Ac) as substrate after 60 mins by fluorescence assay B 7.52 pIC50 30 nM IC50 J Med Chem (2013) 56: 9934-9954 [PMID:24261862]
ChEMBL Inhibition of human recombinant HDAC1 using Boc-lys(Ac)-AMC as substrate preincubated for 20 mins with substrate measured after 60 mins by fluorescence analysis B 7.52 pIC50 30 nM IC50 J Med Chem (2012) 55: 1731-1750 [PMID:22280363]
ChEMBL Inhibition of human recombinant HDAC1 using fluor de Lys as substrate by fluorometric analysis B 7.52 pIC50 30 nM IC50 J Med Chem (2010) 53: 8663-8678 [PMID:21080647]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.52 pIC50 30 nM IC50 J Med Chem (2021) 64: 3392-3426 [PMID:33661013]
ChEMBL Inhibition of human C-terminal FLAG-tagged HDAC1 in HEK293 cells B 7.52 pIC50 30 nM IC50 J Med Chem (2009) 52: 3453-3456 [PMID:19441846]
ChEMBL Inhibition of HDAC1 (unknown origin) by colorimetric method B 7.52 pIC50 30 nM IC50 Eur J Med Chem (2022) 240: 114602-114602 [PMID:35858522]
ChEMBL Inhibition of human recombinant C-terminally flag tagged HDAC1 B 7.52 pIC50 30 nM IC50 Bioorg Med Chem Lett (2008) 18: 5528-5532 [PMID:18809328]
ChEMBL Inhibition of HDAC1 B 7.52 pIC50 30 nM IC50 J Med Chem (2008) 51: 2350-2353 [PMID:18370373]
ChEMBL Inhibition of HDAC1 B 7.52 pIC50 30 nM IC50 Bioorg Med Chem Lett (2008) 18: 726-731 [PMID:18060775]
ChEMBL Inhibition of recombinant human HDAC1 expressed in baculovirus expression system using Ac-Leu-Gly-Lys (Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence microtiter plate reader assay B 7.54 pIC50 29 nM IC50 J Med Chem (2022) 65: 2434-2457 [PMID:35043615]
ChEMBL Inhibition of human recombinant HDAC1 using Boc-L-Lys (Ac)-AMC as substrate preincubated with compound for 5 mins measured after 35 mins by spectrofluorometric analysis B 7.54 pIC50 29 nM IC50 Bioorg Med Chem Lett (2012) 22: 5025-5030 [PMID:22771007]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.54 pIC50 29 nM IC50 Bioorg Med Chem Lett (2023) 94: 129462-129462 [PMID:37652098]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.57 pIC50 27 nM IC50 J Med Chem (2018) 61: 3166-3192 [PMID:29518312]
ChEMBL Inhibition of HDAC1 (mean IC50) B 7.57 pIC50 27 nM IC50 Bioorg Med Chem Lett (2006) 16: 5948-5952 [PMID:16987657]
ChEMBL Inhibition of HDAC1 by fluorogenic enzyme assay B 7.57 pIC50 27 nM IC50 Bioorg Med Chem Lett (2009) 19: 3651-3656 [PMID:19457659]
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 7.59 pIC50 26 nM IC50 J Med Chem (2017) 60: 7965-7983 [PMID:28885834]
ChEMBL Inhibition of recombinant full length human C-terminal His/flag-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells after 30 mins by fluorescence assay B 7.59 pIC50 26 nM IC50 ACS Med Chem Lett (2018) 9: 34-38 [PMID:29348808]
ChEMBL Inhibition of HDAC1 (unknown origin) incubated for 30 mins by microplate reader assay B 7.59 pIC50 25.8 nM IC50 Eur J Med Chem (2022) 229: 114058-114058 [PMID:34954595]
ChEMBL Inhibition of recombinant HDAC1 (unknown origin) expressed in baculovirus expression system using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition by fluorescence based protease coupled assay B 7.6 pIC50 25 nM IC50 Medchemcomm (2019) 10: 1828-1837 [PMID:32180916]
ChEMBL Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using fluor de lys SIRT1 as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay B 7.6 pIC50 25 nM IC50 Eur J Med Chem (2020) 192: 112193-112193 [PMID:32151835]
ChEMBL Inhibition of HDAC1 (unknown origin) using fluorimetric substrate incubated for 30 mins by fluorogenic assay B 7.6 pIC50 25 nM IC50 Eur J Med Chem (2022) 227: 113946-113946 [PMID:34775332]
ChEMBL Inhibition of full-length recombinant human HDAC1 expressed in Baculovirus expression system using Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubated for 30 mins by fluorescence based microtiter plate reader assay B 7.62 pIC50 24 nM IC50 J Med Chem (2022) 65: 4818-4831 [PMID:35238576]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.64 pIC50 23.04 nM IC50 Bioorg Med Chem Lett (2023) 88: 129305-129305 [PMID:37116762]
ChEMBL Inhibition of purified human HDAC1 using Ac-Leu-Gly-(e-Ac)Lys-AMC by fluorometric HDAC assay B 7.64 pIC50 23 nM IC50 Bioorg Med Chem Lett (2022) 55: 128441-128441 [PMID:34767912]
ChEMBL Inhibition of recombinant full length human HDAC1 (1 to 482) expressed in baculovirus infected insect Sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay B 7.64 pIC50 23 nM IC50 ACS Med Chem Lett (2015) 6: 239-243 [PMID:25815139]
ChEMBL Inhibition of human HDAC1 pre-incubated for 5 mins before substrate addition and measured after 30 mins by fluorescence based assay B 7.64 pIC50 22.7 nM IC50 J Med Chem (2021) 64: 1116-1126 [PMID:33356256]
ChEMBL Inhibition of recombinant human FLAG/His-tagged HDAC1 expressed in baculovirus expression system using Boc-l-Lys(Ac)-AMC as substrate preincubated up to 3 hrs and measured after 35 mins by fluorescence assay B 7.65 pIC50 22.4 nM IC50 Eur J Med Chem (2018) 158: 620-706 [PMID:30245394]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.65 pIC50 22.4 nM IC50 Medchemcomm (2014) 5: 1829-1833
ChEMBL Inhibition of human recombinant HDAC1 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins B 7.65 pIC50 22.37 nM IC50 J Med Chem (2011) 54: 4350-4364 [PMID:21548582]
ChEMBL Inhibition of human recombinant HDAC1 using Boc-Lys(Ac)-AMC as substrate incubated for 1 hrs in presence of illumination with 550 nm light by fluorescence based assay B 7.66 pIC50 22 nM IC50 J Med Chem (2023) 66: 1909-1927 [PMID:36654474]
ChEMBL Inhibition of HDAC1 B 7.68 pIC50 21 nM IC50 J Med Chem (2008) 51: 1505-1529 [PMID:18247554]
ChEMBL Inhibition of human recombinant HDAC1 expressed in HEK293 cells B 7.68 pIC50 21 nM IC50 J Med Chem (2010) 53: 8546-8555 [PMID:21080629]
ChEMBL Inhibition of human recombinant HDAC1 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 30 mins followed by substrate addition and measured after 15 to 30 mins B 7.68 pIC50 21 nM IC50 J Med Chem (2018) 61: 3779-3798 [PMID:29039662]
ChEMBL Inhibition of HDAC1 (unknown origin) using trypsin and LGK(Ac)-AMC as substrates incubated for 1 hr and measured by fluorescence assay B 7.68 pIC50 21 nM IC50 Eur J Med Chem (2022) 236: 114326-114326 [PMID:35390714]
ChEMBL Fluorescent Activity Assay: The HDAC activity was performed using the HDAC fluorescent activity assay kit (BIOMOL, Plymouth Meeting, Pa., USA) according to the manufacturer's instructions. Briefly, recombinant proteins of HDAC1 or HDAC6 were incubated with test compounds, and HDAC reaction was initiated by addition of Fluor-de-Lys substrate. Samples were incubated for 10 min at room temperature, followed by adding developer to stop the reaction. Fluorescence was measured by fluorometric reader with excitation at 360 nm and emission at 460 nm. The HDAC activity was expressed as arbitrary fluorescence units (AFU). B 7.68 pIC50 20.9 nM IC50 US-9115116-B2. Dual action inhibitors against histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme a reductase (2015)
ChEMBL Inhibition of recombinant HDAC1 (unknown origin) after 10 mins by fluorimetric analysis B 7.68 pIC50 20.9 nM IC50 J Med Chem (2013) 56: 3645-3655 [PMID:23570542]
ChEMBL Fluorescent Activity Assay: The HDAC activity was performed using the HDAC fluorescent activity assay kit (BIOMOL, Plymouth Meeting, Pa., USA) according to the manufacturer's instructions. Briefly, recombinant proteins of HDAC1 or HDAC6 were incubated with test compounds, and HDAC reaction was initiated by addition of Fluor-de-Lys substrate. Samples were incubated for 10 min at room temperature, followed by adding developer to stop the reaction. Fluorescence was measured by fluorometric reader with excitation at 360 nm and emission at 460 nm. The HDAC activity was expressed as arbitrary fluorescence units (AFU). B 7.68 pIC50 20.9 nM IC50 US-9353061-B2. 3,5,N-trihydroxy-alkanamide and derivatives: method for making same and use thereof (2016)
ChEMBL Inhibition of human recombinant HDAC1 expressed in HEK293 cells B 7.7 pIC50 20 nM IC50 J Med Chem (2009) 52: 2265-2279 [PMID:19301902]
ChEMBL Inhibition of recombinant full length HDAC1 (unknown origin) using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay B 7.7 pIC50 20 nM IC50 Eur J Med Chem (2019) 178: 116-130 [PMID:31177073]
ChEMBL Inhibition of HDAC1 (unknown origin) using Ac-peptide as a substrate pretreated for 15 mins followed by substrate addition B 7.7 pIC50 20 nM IC50 Eur J Med Chem (2021) 225: 113824-113824 [PMID:34509167]
ChEMBL Inhibition of recombinant HDAC1 in HeLa cells B 7.7 pIC50 20 nM IC50 J Med Chem (2007) 50: 4405-4418 [PMID:17691763]
ChEMBL Inhibition of recombinant full length C-terminal FLAG/His-tagged human HDAC1 expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay B 7.72 pIC50 19 nM IC50 Eur J Med Chem (2019) 182: 111672-111672 [PMID:31505452]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.72 pIC50 19 nM IC50 J Med Chem (2023) 66: 4802-4826 [PMID:36934335]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.73 pIC50 18.55 nM IC50 Eur J Med Chem (2020) 205: 112679-112679 [PMID:32791404]
ChEMBL Inhibition of recombinant human HDAC1 using Ac-LGK(Ac)-AMC as substrate preincubated for 30 mins followed by substrate addition and measured after 90 mins by fluorescence based assay B 7.74 pIC50 18 nM IC50 J Med Chem (2021) 64: 2186-2204 [PMID:33570940]
ChEMBL Inhibition of HDAC1 (unknown origin) using trypsin and Ac-peptide as substrates B 7.76 pIC50 17.39 nM IC50 Eur J Med Chem (2022) 230: 114115-114115 [PMID:35033824]
ChEMBL Inhibition of HDAC1 (unknown origin) assessed as release of fluorogenic AMC preincubated for 15 mins followed by addition of trypsin and substrate measured after 60 mins Spectra max microplate reader analysis B 7.77 pIC50 17 nM IC50 J Med Chem (2023) 66: 4802-4826 [PMID:36934335]
ChEMBL Inhibition of HDAC1 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay B 7.77 pIC50 17 nM IC50 J Med Chem (2020) 63: 3678-3700 [PMID:32153186]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.77 pIC50 17 nM IC50 J Med Chem (2022) 65: 16541-16569 [PMID:36449947]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.8 pIC50 16 nM IC50 Eur J Med Chem (2021) 213: 113173-113173 [PMID:33493830]
ChEMBL Inhibition of C-terminal His-tagged and C-terminal FLAG-tagged human HDAC1 expressed in baculovirus expression system using Ac-peptide substrate incubated for 15 mins by fluorescence based assay B 7.8 pIC50 16 nM IC50 Eur J Med Chem (2017) 140: 392-402 [PMID:28987602]
ChEMBL Inhibition of recombinant human HDAC1 expressed in baculovirus infection system using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence assay B 7.8 pIC50 16 nM IC50 Bioorg Med Chem (2022) 53: 116524-116524 [PMID:34847495]
ChEMBL Inhibition of HDAC1 (unknown origin) using Boc-Lys (Ac)-AMC as substrate measured after 60 mins by ELISA B 7.82 pIC50 15 nM IC50 Bioorg Med Chem Lett (2019) 29: 15-21 [PMID:30455152]
ChEMBL Inhibition of HDAC1 (unknown origin) assessed as release of 7-amino-4-methylcoumarin incubated in room temperature for 15 min measured by Spectra max microtitre plate reader B 7.84 pIC50 14.6 nM IC50 J Med Chem (2021) 64: 16573-16597 [PMID:34783558]
ChEMBL Inhibition of recombinant human full length HDAC1 using fluorogenic substrate 3 after 30 mins by fluorescence assay B 7.84 pIC50 14.4 nM IC50 ACS Med Chem Lett (2018) 9: 312-317 [PMID:29670692]
ChEMBL Inhibition of C-terminal FLAG tagged recombinant human HDAC1 expressed in Sf9 cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition by fluorescence based analysis B 7.84 pIC50 14.38 nM IC50 Eur J Med Chem (2023) 254: 115367-115367 [PMID:37086699]
ChEMBL Inhibition of HDAC1 (unknown origin) using Ac-peptide as substrate pretreated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay B 7.84 pIC50 14.3 nM IC50 Bioorg Med Chem (2018) 26: 3958-3966 [PMID:29954683]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.85 pIC50 14.15 nM IC50 Bioorg Med Chem Lett (2020) 30: 127610-127610 [PMID:33045329]
ChEMBL Inhibition of human C-terminal Flag tagged HDAC1 (1 to 482 residues) expressed in SF9 cells using Ac-peptide substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by microplate reader method B 7.85 pIC50 14.15 nM IC50 Eur J Med Chem (2020) 204: 112651-112651 [PMID:32738414]
ChEMBL Inhibition of HDAC1 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition by fluorescence assay B 7.85 pIC50 14 nM IC50 Eur J Med Chem (2021) 220: 113453-113453 [PMID:33957387]
ChEMBL Inhibition of human recombinant HDAC1 by microplate reader assay B 7.85 pIC50 14 nM IC50 Medchemcomm (2015) 6: 613-618 [PMID:26005563]
ChEMBL Inhibition of human recombinant HDAC1 using Boc-Lys(Ac)-AMC as substrate incubated for 1 hrs in presence of illumination with 420 nm light by fluorescence based assay B 7.85 pIC50 14 nM IC50 J Med Chem (2023) 66: 1909-1927 [PMID:36654474]
ChEMBL Inhibition of human recombinant HDAC1 using fluorogenic Boc-Lys (aetyl)-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 2 hrs by measuring fluorescence intensity using multimode microplate reader B 7.88 pIC50 13.2 nM IC50 J Med Chem (2023) 66: 10791-10807 [PMID:37498552]
ChEMBL Inhibition of HDAC1 (unknown origin) using Boc-Lys(Ac)-AMC as substrate by fluorescence assay B 7.89 pIC50 13 nM IC50 Bioorg Med Chem Lett (2014) 24: 4768-4772 [PMID:25182565]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.89 pIC50 13 nM IC50 Bioorg Med Chem Lett (2022) 64: 128663-128663 [PMID:35272009]
ChEMBL Inhibition of recombinant human C-terminal His/FLAG-tagged HDAC1 (1 to end residues) expressed in sf9 insect cells using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay B 7.89 pIC50 13 nM IC50 Eur J Med Chem (2020) 192: 112189-112189 [PMID:32151834]
ChEMBL Inhibition of HDAC1 (unknown origin) measured by fluorescence based assay B 7.89 pIC50 13 nM IC50 Bioorg Med Chem (2022) 73: 117028-117028 [PMID:36182802]
ChEMBL Inhibition of human recombinant HDAC1 using Boc-Lys(Ac)-AMC as substrate incubated for 1 hrs in presence of illumination with 380 nm light by fluorescence based assay B 7.89 pIC50 13 nM IC50 J Med Chem (2023) 66: 1909-1927 [PMID:36654474]
ChEMBL Inhibition of human recombinant HDAC1 expressed in human HEK293 cells using Ac-NH-GGK(Ac)-AMC as substrate after 180 mins by fluorescence assay B 7.89 pIC50 13 nM IC50 Medchemcomm (2012) 3: 829-835
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.92 pIC50 12 nM IC50 Eur J Med Chem (2021) 209: 112904-112904 [PMID:33077264]
ChEMBL Inhibition of HDAC-1 (unknown origin) expressed in Escherichia coli BL21 (DE3) in HeLa nuclear extract using KI177 as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by Bradford reagent method B 7.92 pIC50 12 nM IC50 Eur J Med Chem (2021) 209: 112904-112904 [PMID:33077264]
ChEMBL Inhibition of recombinant human C-terminal His/FLAG-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by addition of substrate and trypsin measured by flourescence assay B 7.92 pIC50 12 nM IC50 Eur J Med Chem (2021) 224: 113672-113672 [PMID:34237620]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2022) 72: 128846-128846 [PMID:35697181]
ChEMBL Inhibition of HDAC1 (unknown origin) using acetylated peptide substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence analysis B 7.95 pIC50 11.34 nM IC50 Bioorg Med Chem (2017) 25: 4100-4109 [PMID:28601509]
ChEMBL Inhibition of HDAC1 (unknown origin) preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay B 7.95 pIC50 11.11 nM IC50 Eur J Med Chem (2017) 134: 281-292 [PMID:28419930]
ChEMBL Inhibition of recombinant human full length C-terminal His/FLAG tagged HDAC1 (1 to 482 residues) expressed in baculovirus-infected Sf9 cells using Ac-peptide as substrate incubated for 4 hrs B 7.96 pIC50 11 nM IC50 J Med Chem (2022) 65: 4156-4181 [PMID:35175762]
ChEMBL Inhibition of HDAC1 B 7.96 pIC50 11 nM IC50 Bioorg Med Chem (2010) 18: 4103-4110 [PMID:20472442]
ChEMBL Inhibition of full length C-terminal His/FLAG-tagged human recombinant HDAC1 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay B 7.96 pIC50 11 nM IC50 J Med Chem (2016) 59: 5488-5504 [PMID:27186676]
ChEMBL Inhibition of recombinant full length HDAC1 (unknown origin) using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay B 7.96 pIC50 11 nM IC50 J Med Chem (2019) 62: 1577-1592 [PMID:30629434]
ChEMBL Inhibition of human recombinant HDAC1 using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis B 7.96 pIC50 11 nM IC50 J Med Chem (2016) 59: 1455-1470 [PMID:26443078]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.96 pIC50 11 nM IC50 Bioorg Med Chem Lett (2023) 94: 129466-129466 [PMID:37660833]
ChEMBL Inhibition of human recombinant HDAC1 using Boc-Lys(Ac)-AMC as substrate incubated for 1 hrs in presence of illumination with 365 nm light by fluorescence based assay B 7.96 pIC50 11 nM IC50 J Med Chem (2023) 66: 1909-1927 [PMID:36654474]
ChEMBL Inhibition of HDAC1 (unknown origin) B 7.96 pIC50 11 nM IC50 Bioorg Med Chem Lett (2021) 49: 128286-128286 [PMID:34314844]
ChEMBL Inhibition of HDAC1 (unknown origin) using acetylated peptide substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence analysis B 7.97 pIC50 10.8 nM IC50 Bioorg Med Chem (2017) 25: 27-37 [PMID:27769671]
ChEMBL Inhibition of HDAC1 (unknown origin) using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorescence plate reader assay B 7.97 pIC50 10.68 nM IC50 Eur J Med Chem (2022) 227: 113893-113893 [PMID:34656899]
ChEMBL Inhibition of HDAC1 (unknown origin) B 8 pIC50 10 nM IC50 Eur J Med Chem (2019) 183: 111691-111691 [PMID:31536895]
ChEMBL Inhibition of HDAC1 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence assay B 8 pIC50 10 nM IC50 Eur J Med Chem (2018) 158: 620-706 [PMID:30245394]
ChEMBL Inhibition of recombinant human HDAC1 after 30 mins by fluorescence assay B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2017) 27: 4051-4055 [PMID:28765013]
ChEMBL Inhibition of recombinant human GST-fused HDAC1 expressed in HEK293 cells Fluor-de-lys as substrate measured after 60 mins by fluorescence assay B 8 pIC50 10 nM IC50 Eur J Med Chem (2018) 158: 620-706 [PMID:30245394]
ChEMBL Inhibition of C-terminal FLAG/His-tagged human recombinant HDAC1 (1 to 482 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in 7-amino-4-methylcoumarin release using fluorogenic HDAC substrate 3 measured every 5 mins by fluorescence based analysis B 8 pIC50 10 nM IC50 Bioorg Med Chem (2021) 42: 116251-116251 [PMID:34116381]
ChEMBL Inhibition of HDAC1 (unknown origin) B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2023) 94: 129466-129466 [PMID:37660833]
ChEMBL Inhibition of HDAC1 in human Jurkat cells extract after 30 mins by immunoprecipitation assay B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2016) 26: 3122-3126 [PMID:27177826]
ChEMBL Inhibition of human recombinant full-length HDAC1 using fluorophore conjugated substrate by fluorescence assay B 8.01 pIC50 9.7 nM IC50 J Med Chem (2011) 54: 5576-5582 [PMID:21721525]
ChEMBL Inhibition of HDAC1 (unknown origin) using Ac-Leu-GlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence analysis B 8.05 pIC50 9 nM IC50 Bioorg Med Chem (2017) 25: 4123-4132 [PMID:28629630]
ChEMBL Inhibition of human recombinant HDAC1 after 30 mins by fluorometric assay B 8.05 pIC50 8.9 nM IC50 J Med Chem (2012) 55: 3777-3791 [PMID:22439863]
ChEMBL Inhibition of human recombinant HDAC1 using acetyllysine tripeptide coupled with 7-amino-4-methylcoumarin as substrate by fluorescence assay B 8.15 pIC50 7 nM IC50 Bioorg Med Chem Lett (2016) 26: 1265-1271 [PMID:26804233]
ChEMBL Inhibition of human KDAC1 B 8.15 pIC50 7 nM IC50 J Med Chem (2016) 59: 1613-1633 [PMID:26681404]
ChEMBL Inhibition of HDAC1 (unknown origin) using fluorogenic substrate incubated for 30 mins by fluorescence based assay B 8.28 pIC50 5.2 nM IC50 J Med Chem (2022) 65: 3667-3683 [PMID:35152694]
ChEMBL Inhibition of HDAC1 (unknown origin) after 60 mins by fluorescence assay B 8.3 pIC50 5 nM IC50 J Med Chem (2013) 56: 4816-4820 [PMID:23672185]
ChEMBL Inhibition of HDAC1 (unknown origin) using Fluor de lys as substrate by fluorescence based analysis B 8.37 pIC50 4.24 nM IC50 Eur J Med Chem (2020) 187: 111950-111950 [PMID:31865013]
ChEMBL Inhibition of HDAC1 (unknown origin) using fluorogenic peptide RHKKAc-AMC as substrate by fluorescence-based assay B 8.37 pIC50 4.24 nM IC50 Bioorg Med Chem Lett (2023) 81: 129148-129148 [PMID:36690041]
ChEMBL Inhibition of HDAC1 (unknown origin) using Fluor de Lys substrate by fluorescence assay relative to control B 8.4 pIC50 4 nM IC50 Eur J Med Chem (2019) 168: 110-122 [PMID:30802729]
ChEMBL Inhibition of HDAC1 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay B 8.4 pIC50 4 nM IC50 J Med Chem (2013) 56: 1772-1776 [PMID:23368884]
ChEMBL Inhibition of human recombinant HDAC1 using Boc-Lys(Ac)-AMC as substrate incubated for 1 hrs in dark by fluorescence based assay B 8.52 pIC50 3 nM IC50 J Med Chem (2023) 66: 1909-1927 [PMID:36654474]
ChEMBL Inhibition of recombinant human HDAC1 B 8.7 pIC50 2 nM IC50 J Med Chem (2023) 66: 11672-11700 [PMID:37651268]
ChEMBL Inhibition of HDAC1 in human HeLa cells nuclear extract incubated for 30 mins by multiplate reader analysis B 9.07 pIC50 0.85 nM IC50 J Med Chem (2023) 66: 5753-5773 [PMID:37057760]
histone deacetylase 1/Histone deacetylase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4001] [GtoPdb: 2658] [UniProtKB: O09106]
ChEMBL Binding affinity towards HDAC1 (Histone deacetylase 1) in mouse A20 cells, expressed as binding constant (pKi) B 7.17 pKi 67.61 nM Ki J Med Chem (2002) 45: 1778-1784 [PMID:11960489]
ChEMBL Inhibition of mouse HDAC1 B 6.95 pIC50 112.2 nM IC50 J Med Chem (2004) 47: 1351-1359 [PMID:14998325]
ChEMBL In vitro for anti-HDAC1 (Histone deacetylase 1) activity in mouse A20 cells B 6.95 pIC50 112 nM IC50 J Med Chem (2002) 45: 1778-1784 [PMID:11960489]
ChEMBL Inhibition of mouse Histone deacetylase 1 (HDAC1) receptor B 6.95 pIC50 112 nM IC50 J Med Chem (2004) 47: 1351-1359 [PMID:14998325]
ChEMBL Inhibition of mouse HDAC1 B 6.95 pIC50 112 nM IC50 J Med Chem (2006) 49: 6046-6056 [PMID:17004718]
ChEMBL Inhibition of mouse liver HDAC1 B 6.95 pIC50 112 nM IC50 J Med Chem (2008) 51: 1505-1529 [PMID:18247554]
histone deacetylase 10/Histone deacetylase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8]
ChEMBL Competitive inhibition of HDAC10 using KI-104 as substrate by fluorescence assay B 7.22 pKi 60 nM Ki J Med Chem (2011) 54: 4694-4720 [PMID:21634430]
GtoPdb - - 7.3 pKi 50 nM Ki Bioorg Med Chem Lett (2010) 20: 3314-21 [PMID:20451378]
ChEMBL Inhibition of HDAC10 B 7.3 pKi 50 nM Ki Bioorg Med Chem Lett (2010) 20: 3314-3321 [PMID:20451378]
ChEMBL Inhibition of human recombinant HDAC10 using Ac-Arg-His-Lys(Ac)-Lys(Ac)-AMC substrate incubated for 15 to 30 mins B 7.4 pKi 40 nM Ki J Med Chem (2014) 57: 9644-9657 [PMID:25380299]
ChEMBL Inhibition of human recombinant HDAC10 using Ac-Arg-His-Lys (Ac)-Lys (Ac)-AMC substrate incubated for 30 mins by fluorescence assay B 7.4 pKi 40 nM Ki Medchemcomm (2014) 5: 1849-1855
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 5.9 pIC50 1258.93 nM IC50 J Med Chem (2019) 62: 4426-4443 [PMID:30964290]
ChEMBL Inhibition of HDAC 10 in human HeLa nuclear extract measured after 60 mins by fluorometric analysis B 6.01 pIC50 982 nM IC50 J Med Chem (2017) 60: 3484-3497 [PMID:28368585]
ChEMBL Inhibition of recombinant human HDAC10 after 60 mins by fluorescence assay B 6.16 pIC50 686 nM IC50 J Med Chem (2015) 58: 7672-7680 [PMID:26331334]
ChEMBL Inhibition of human recombinant HDAC10 after 60 mins by fluorimetric assay B 6.16 pIC50 686 nM IC50 Eur J Med Chem (2014) 86: 639-652 [PMID:25218912]
ChEMBL Inhibition of human HDAC10 using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay B 6.34 pIC50 460 nM IC50 Eur J Med Chem (2016) 112: 99-105 [PMID:26890116]
ChEMBL Inhibition of human HDAC-10 using RHKK(Ac) as substrate by fluorescence assay B 6.34 pIC50 456 nM IC50 J Med Chem (2014) 57: 2258-2274 [PMID:24588105]
ChEMBL Inhibition of HDAC10 (unknown origin) using fluorogenic tetrapeptide RHKK(Ac) substrate by fluorescence assay B 6.34 pIC50 456 nM IC50 J Med Chem (2014) 57: 8358-8377 [PMID:25233084]
ChEMBL Inhibition of human HDAC10 by fluorimetric assay B 6.34 pIC50 456 nM IC50 J Med Chem (2010) 53: 8387-8399 [PMID:21073160]
ChEMBL Inhibition of human HDAC-10 using RHKK(Ac) as substrate B 6.34 pIC50 456 nM IC50 Eur J Med Chem (2014) 76: 53-60 [PMID:24565573]
ChEMBL Inhibition of human HDAC10 using RHKK(Ac) as substrate by fluorimetric analysis B 6.34 pIC50 456 nM IC50 Bioorg Med Chem Lett (2014) 24: 61-64 [PMID:24345446]
ChEMBL Inhibition of human HDAC10 using RHKK(Ac) as substrate by fluorimetric analysis B 6.34 pIC50 456 nM IC50 Bioorg Med Chem Lett (2015) 25: 459-461 [PMID:25563890]
ChEMBL Inhibition of human HDAC10 using fluorogenic tetrapeptide RHKKAc as substrate B 6.34 pIC50 456 nM IC50 Eur J Med Chem (2014) 79: 251-259 [PMID:24742384]
ChEMBL Inhibition of HDAC10 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHKK(Ac)) as substrate by fluorescence assay B 6.36 pIC50 432 nM IC50 ACS Med Chem Lett (2013) 4: 779-783 [PMID:24015327]
ChEMBL Inhibition of HDAC10 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay B 6.37 pIC50 430 nM IC50 Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503]
ChEMBL Inhibition of HDAC10 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay B 6.37 pIC50 430 nM IC50 J Med Chem (2014) 57: 8026-8034 [PMID:25238284]
ChEMBL Inhibition of HDAC10 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay B 6.56 pIC50 278 nM IC50 J Med Chem (2020) 63: 3678-3700 [PMID:32153186]
ChEMBL Inhibition of HDAC10 (unknown origin) B 6.62 pIC50 238.1 nM IC50 Bioorg Med Chem Lett (2022) 70: 128797-128797 [PMID:35580726]
ChEMBL Inhibition of HDAC10 B 6.68 pIC50 210 nM IC50 Eur J Med Chem (2010) 45: 4331-4338 [PMID:20637529]
ChEMBL Inhibition of recombinant N-terminal FLAG-tagged human HDAC10 (2 to 631 residues) expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay B 6.68 pIC50 208 nM IC50 Eur J Med Chem (2019) 178: 116-130 [PMID:31177073]
ChEMBL Inhibition of HDAC10 by in vitro deacetylation assay B 6.7 pIC50 200 nM IC50 Nat Chem Biol (2010) 6: 25-33 [PMID:19966789]
ChEMBL Inhibition of tubastatin-Alexa647-tracer binding to recombinant GST-tagged HDAC10 (unknown origin) measured after 1 hr by TR-FRET assay B 6.7 pIC50 199.53 nM IC50 J Med Chem (2019) 62: 4426-4443 [PMID:30964290]
ChEMBL Inhibition of human recombinant HDAC10 using fluorogenic p53 (379-382 residues) (RHKK(Ac)AMC) as substrate B 6.7 pIC50 198 nM IC50 Eur J Med Chem (2023) 247: 115022-115022 [PMID:36549114]
ChEMBL Inhibition of recombinant HDAC10 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis B 6.77 pIC50 170 nM IC50 J Med Chem (2016) 59: 1455-1470 [PMID:26443078]
ChEMBL Inhibition of recombinant full length N-terminal FLAG-tagged human HDAC10 expressed in baculovirus infected sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay B 6.77 pIC50 170 nM IC50 J Med Chem (2019) 62: 1577-1592 [PMID:30629434]
ChEMBL Inhibition of HDAC10 (unknown origin) incubated for 1 hr by TR-FRET analysis B 6.8 pIC50 159 nM IC50 Eur J Med Chem (2020) 187: 111950-111950 [PMID:31865013]
ChEMBL Inhibition of human HDAC10 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay B 6.82 pIC50 150 nM IC50 J Med Chem (2011) 54: 2165-2182 [PMID:21417297]
ChEMBL Inhibition of HDAC10 (unknown origin) B 6.84 pIC50 144.6 nM IC50 J Med Chem (2023) 66: 5753-5773 [PMID:37057760]
ChEMBL Inhibition of recombinant his-tagged human HDAC10 using Ac-ArgHisLys (Ac) Lys (Ac)-AMC substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence based microplate reader analysis B 7 pIC50 100 nM IC50 J Med Chem (2022) 65: 12200-12218 [PMID:36097406]
ChEMBL Inhibition of HDAC10 (unknown origin) by fluorescence assay B 7.01 pIC50 97 nM IC50 Eur J Med Chem (2019) 164: 263-272 [PMID:30597327]
ChEMBL Inhibition of HDAC10 (unknown origin) using (FAM)-labeled acetylated peptide as substrate measured after 17 hrs by fluorescence assay B 7.04 pIC50 91.8 nM IC50 Eur J Med Chem (2018) 158: 620-706 [PMID:30245394]
ChEMBL Inhibition of HDAC10 (unknown origin) B 7.06 pIC50 88 nM IC50 Eur J Med Chem (2021) 209: 112887-112887 [PMID:33035922]
ChEMBL Inhibition of HDAC10 (unknown origin) using Ac-ArgThr- Lys(Ac)Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay B 7.1 pIC50 80 nM IC50 ACS Med Chem Lett (2019) 10: 1122-1127 [PMID:31413795]
ChEMBL Inhibition of human recombinant HDAC10 B 7.1 pIC50 80 nM IC50 J Med Chem (2023) 66: 7698-7729 [PMID:37276138]
ChEMBL Inhibition of HDAC10 (unknown origin) B 7.11 pIC50 77 nM IC50 Eur J Med Chem (2016) 121: 451-483 [PMID:27318122]
ChEMBL Inhibition of recombinant human N-terminal FLAG-tagged HDAC10 (2 to 631 residues) expressed in baculovirus infected using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay B 7.11 pIC50 77 nM IC50 Eur J Med Chem (2018) 158: 620-706 [PMID:30245394]
ChEMBL Inhibition of human recombinant HDAC10 B 7.14 pIC50 72 nM IC50 Bioorg Med Chem Lett (2009) 19: 3023-3026 [PMID:19419863]
ChEMBL Inhibition of N-terminal GST-tagged human HDAC10 (1 to 481 residues) using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay B 7.14 pIC50 72 nM IC50 Bioorg Med Chem Lett (2014) 24: 5450-5454 [PMID:25454270]
ChEMBL Inhibition of HDAC10 after 17 hrs B 7.14 pIC50 72 nM IC50 J Med Chem (2008) 51: 4370-4373 [PMID:18642892]
ChEMBL Inhibition of HDAC10 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs B 7.14 pIC50 72 nM IC50 J Med Chem (2010) 53: 1347-1356 [PMID:20055418]
ChEMBL Inhibition of recombinant HDAC10 (unknown origin) using Fluor-de-Lys-SIRT1 as substrate by fluorescence assay B 7.15 pIC50 70 nM IC50 J Nat Prod (2014) 77: 49-56 [PMID:24328302]
ChEMBL Inhibition of HDAC10 (unknown origin) B 7.16 pIC50 68.4 nM IC50 J Med Chem (2019) 62: 3171-3183 [PMID:30418766]
ChEMBL Inhibition of HDAC10 (unknown origin) B 7.19 pIC50 64 nM IC50 Eur J Med Chem (2016) 108: 274-286 [PMID:26689485]
ChEMBL Inhibition of recombinant human HDAC10 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry B 7.24 pIC50 58 nM IC50 ACS Med Chem Lett (2011) 2: 703-707 [PMID:21984958]
ChEMBL Inhibition of recombinant human C-terminal His-tagged HDAC10 expressed in baculovirus infected Sf9 insect cells using Ac-Arg-His-Lys(Ac)-Lys(Ac)-AMC as substrate measured after 30 mins by fluorescence assay B 7.24 pIC50 57.25 nM IC50 Eur J Med Chem (2020) 205: 112648-112648 [PMID:32791401]
ChEMBL Inhibition of human recombinant HDAC10 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate by measuring fluorescence intensity incubated for 30 mins by microplate reader assay B 7.3 pIC50 50 nM IC50 Eur J Med Chem (2021) 217: 113363-113363 [PMID:33744687]
ChEMBL Inhibition of recombinant HDAC10 (unknown origin) using Ac-peptide-AMC as substrate incubated for 240 mins by microplate reader analysis B 7.32 pIC50 47.5 nM IC50 J Med Chem (2022) 65: 1243-1264 [PMID:33586434]
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 7.57 pIC50 27 nM IC50 J Med Chem (2018) 61: 1552-1575 [PMID:29360358]
histone deacetylase 11/Histone deacetylase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3310] [GtoPdb: 2615] [UniProtKB: Q96DB2]
ChEMBL Inhibition of human recombinant HDAC11 using Ac-Leu-Gly-Lys (Ac)-AMC substrate incubated for 30 mins by fluorescence assay B 7.22 pKi 60 nM Ki Medchemcomm (2014) 5: 1849-1855
GtoPdb - - 7.44 pKi 36 nM Ki Bioorg Med Chem Lett (2010) 20: 3314-21 [PMID:20451378]
ChEMBL Inhibition of HDAC11 B 7.44 pKi 36 nM Ki Bioorg Med Chem Lett (2010) 20: 3314-3321 [PMID:20451378]
ChEMBL Competitive inhibition of HDAC11 using KI-104 as substrate by fluorescence assay B 7.51 pKi 31 nM Ki J Med Chem (2011) 54: 4694-4720 [PMID:21634430]
ChEMBL Inhibition of recombinant human HDAC11 enzyme using Ac-LeuGlyLys(Ac)-AMC as substrate after 15 to 30 mins B 7.89 pKi 13 nM Ki J Med Chem (2013) 56: 6512-6520 [PMID:23865683]
ChEMBL Inhibition of human recombinant HDAC11 using [Ac-Leu-Gly-Lys(Ac)-AMC substrate incubated for 15 to 30 mins B 7.89 pKi 13 nM Ki J Med Chem (2014) 57: 9644-9657 [PMID:25380299]
ChEMBL Inhibition of recombinant his-tagged human HDAC11 using Ac-LeuGlyLys (Ac) AMC substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence based microplate reader analysis B 4 pIC50 >100000 nM IC50 J Med Chem (2022) 65: 12200-12218 [PMID:36097406]
ChEMBL Inhibition of human recombinant HDAC11 using fluorogenic HDAC substrate class 2A by fluorescence assay B 4.13 pIC50 73770 nM IC50 Eur J Med Chem (2019) 164: 263-272 [PMID:30597327]
ChEMBL Inhibition of HDAC11 (unknown origin) using Ac-LeuGlyLys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay B 4.4 pIC50 40000 nM IC50 ACS Med Chem Lett (2019) 10: 1122-1127 [PMID:31413795]
ChEMBL Inhibition of HDAC11 (unknown origin) B 4.46 pIC50 34500 nM IC50 Eur J Med Chem (2021) 209: 112904-112904 [PMID:33077264]
ChEMBL Inhibition of recombinant human HDAC11 using Boc-Lys(TFA)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence-based assay B 4.9 pIC50 12542 nM IC50 Eur J Med Chem (2016) 109: 350-359 [PMID:26814680]
ChEMBL Inhibition of HDAC11 (unknown origin) B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2022) 70: 128797-128797 [PMID:35580726]
ChEMBL Inhibition of recombinant human HDAC11 after 60 mins by fluorescence assay B 5 pIC50 >10000 nM IC50 J Med Chem (2015) 58: 7672-7680 [PMID:26331334]
ChEMBL Inhibition of recombinant HDAC11 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis B 5 pIC50 >10000 nM IC50 J Med Chem (2016) 59: 1455-1470 [PMID:26443078]
ChEMBL Inhibition of HDAC 11 in human HeLa nuclear extract using fluorogenic HDAC class 2A substrate measured after 60 mins by fluorometric analysis B 5 pIC50 >10000 nM IC50 J Med Chem (2017) 60: 3484-3497 [PMID:28368585]
ChEMBL Inhibition of HDAC11 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay B 5 pIC50 >10000 nM IC50 J Med Chem (2020) 63: 3678-3700 [PMID:32153186]
ChEMBL Inhibition of recombinant full length human HDAC11 expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2019) 178: 116-130 [PMID:31177073]
ChEMBL Inhibition of HDAC11 (unknown origin) by fluorescence based assay B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2021) 209: 112868-112868 [PMID:33077265]
ChEMBL Inhibition of recombinant human full length HDAC11 expressed in baculovirus infected Sf9 cells measured after 60 mins by FRET assay B 5 pIC50 >10000 nM IC50 J Med Chem (2021) 64: 4020-4033 [PMID:33745280]
ChEMBL Inhibition of HDAC11 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition by fluorescence based microplate reader analysis B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2021) 220: 113453-113453 [PMID:33957387]
ChEMBL Inhibition of HDAC11 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2023) 66: 5753-5773 [PMID:37057760]
ChEMBL Inhibition of HDAC11 (unknown origin) B 5.06 pIC50 8700 nM IC50 Eur J Med Chem (2016) 121: 451-483 [PMID:27318122]
ChEMBL Inhibition of recombinant full-length human HDAC11 expressed in baculovirus infected Sf9 insect cells using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay B 5.06 pIC50 8700 nM IC50 Eur J Med Chem (2018) 158: 620-706 [PMID:30245394]
ChEMBL Inhibition of human recombinant HDAC11 after 60 mins by fluorimetric assay B 5.23 pIC50 5840 nM IC50 Eur J Med Chem (2014) 86: 639-652 [PMID:25218912]
ChEMBL Inhibition of HDAC11 (unknown origin) measured by fluorescence based assay B 5.3 pIC50 >5000 nM IC50 Bioorg Med Chem (2022) 73: 117028-117028 [PMID:36182802]
ChEMBL Inhibition of HDAC11 (unknown origin) using Ac-ETDKrnyr-AMC as substrate incubated for 30 mins by fluorescence based analysis B 5.3 pIC50 >5000 nM IC50 J Med Chem (2023) 66: 14150-14174 [PMID:37796543]
ChEMBL Inhibition of recombinant human HDAC11 measured after 30 mins by fluorescence microplate reader assay B 5.3 pIC50 >5000 nM IC50 J Med Chem (2021) 64: 15280-15296 [PMID:34624191]
ChEMBL Inhibition of recombinant full length human HDAC11 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 17 hrs by electrophoretic mobility shift assay B 6 pIC50 >1000 nM IC50 ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464]
ChEMBL Inhibition of recombinant full length N-terminal GST-tagged human HDAC11 expressed in baculovirus expression system using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay B 6 pIC50 >1000 nM IC50 J Med Chem (2019) 62: 1577-1592 [PMID:30629434]
ChEMBL Inhibition of recombinant full length HDAC11 (unknown origin) expressed in insect Sf9 cells by EMSA analysis B 6 pIC50 >1000 nM IC50 J Med Chem (2021) 64: 8486-8509 [PMID:34101461]
ChEMBL Inhibition of full length human recombinant HDAC11 expressed in Sf9 baculovirus system using FAM-labeled acetylated peptide as substrate by measuring fluorescence intensity by EMSA method B 6 pIC50 >1000 nM IC50 J Med Chem (2022) 65: 3193-3217 [PMID:35119267]
ChEMBL Inhibition of HDAC11 (unknown origin) B 6 pIC50 >1000 nM IC50 Bioorg Med Chem Lett (2021) 49: 128286-128286 [PMID:34314844]
ChEMBL Inhibition of recombinant human N-terminal His-tagged HDAC11 expressed in baculovirus infected Sf9 insect cells using Ac-Arg-His-Lys(Ac)-Lys(Ac)-AMC as substrate measured after 30 mins by fluorescence assay B 6 pIC50 >1000 nM IC50 Eur J Med Chem (2020) 205: 112648-112648 [PMID:32791401]
ChEMBL Inhibition of HDAC11 (unknown origin) using Fluor de lys as substrate by fluorescence based analysis B 6.02 pIC50 952 nM IC50 Eur J Med Chem (2020) 187: 111950-111950 [PMID:31865013]
ChEMBL Inhibition of human HDAC11 by fluorescence assay B 6.32 pIC50 480 nM IC50 J Med Chem (2013) 56: 427-436 [PMID:23252603]
ChEMBL Inhibition of His-tagged human HDAC11 expressed in Sf9 cells using Ac-Arg-Gly-Lys(Ac)-AMC as substrate by fluorometric assay B 6.43 pIC50 370 nM IC50 Bioorg Med Chem Lett (2016) 26: 2434-2437 [PMID:27055940]
ChEMBL Inhibition of human HDAC11 using fluorogenic tetrapeptide RHKKAc as substrate B 6.44 pIC50 362 nM IC50 Eur J Med Chem (2014) 79: 251-259 [PMID:24742384]
ChEMBL Inhibition of human HDAC11 using RHKK(Ac) as substrate by fluorimetric analysis B 6.44 pIC50 362 nM IC50 Bioorg Med Chem Lett (2014) 24: 61-64 [PMID:24345446]
ChEMBL Inhibition of HDAC11 (unknown origin) using fluorogenic tetrapeptide RHKK(Ac) substrate by fluorescence assay B 6.44 pIC50 362 nM IC50 J Med Chem (2014) 57: 8358-8377 [PMID:25233084]
ChEMBL Inhibition of human HDAC11 using RHKK(Ac) as substrate by fluorimetric analysis B 6.44 pIC50 362 nM IC50 Bioorg Med Chem Lett (2015) 25: 459-461 [PMID:25563890]
ChEMBL Inhibition of human HDAC-11 using RHKK(Ac) as substrate B 6.44 pIC50 362 nM IC50 Eur J Med Chem (2014) 76: 53-60 [PMID:24565573]
ChEMBL Inhibition of human HDAC-11 using RHKK(Ac) as substrate by fluorescence assay B 6.44 pIC50 362 nM IC50 J Med Chem (2014) 57: 2258-2274 [PMID:24588105]
ChEMBL Inhibition of human HDAC11 by fluorimetric assay B 6.44 pIC50 362 nM IC50 J Med Chem (2010) 53: 8387-8399 [PMID:21073160]
ChEMBL Inhibition of human recombinant N-terminal His-tagged HDAC11 (1 to 347 residues) using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay B 6.44 pIC50 360 nM IC50 Eur J Med Chem (2016) 112: 99-105 [PMID:26890116]
ChEMBL Inhibition of HDAC11 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay B 6.7 pIC50 200 nM IC50 Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503]
ChEMBL Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated for 3 hrs followed by substrate addition after 30 mins by fluorometric method B 6.7 pIC50 200 nM IC50 Bioorg Med Chem Lett (2017) 27: 2943-2945 [PMID:28501514]
ChEMBL Inhibition of HDAC11 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHKK(Ac)) as substrate by fluorescence assay B 6.7 pIC50 200 nM IC50 ACS Med Chem Lett (2013) 4: 779-783 [PMID:24015327]
ChEMBL Inhibition of HDAC11 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay B 6.7 pIC50 200 nM IC50 J Med Chem (2014) 57: 8026-8034 [PMID:25238284]
ChEMBL Inhibition of recombinant human HDAC11 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry B 6.88 pIC50 133 nM IC50 ACS Med Chem Lett (2011) 2: 703-707 [PMID:21984958]
ChEMBL Inhibition of HDAC11 (unknown origin) B 6.96 pIC50 109 nM IC50 Eur J Med Chem (2021) 209: 112887-112887 [PMID:33035922]
ChEMBL Inhibition of human HDAC11 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay B 7 pIC50 100 nM IC50 J Med Chem (2011) 54: 2165-2182 [PMID:21417297]
ChEMBL Inhibition of recombinant HDAC11 (unknown origin) using Fluor-de-Lys-SIRT1 as substrate by fluorescence assay B 7.05 pIC50 90 nM IC50 J Nat Prod (2014) 77: 49-56 [PMID:24328302]
ChEMBL Inhibition of HDAC11 (unknown origin) B 7.21 pIC50 61.16 nM IC50 Bioorg Med Chem Lett (2023) 88: 129305-129305 [PMID:37116762]
ChEMBL Inhibition of HDAC11 (unknown origin) B 7.29 pIC50 51.3 nM IC50 J Med Chem (2019) 62: 3171-3183 [PMID:30418766]
ChEMBL Inhibition of full length human recombinant HDAC11 expressed in baculovirus infected insect S9 cells after 30 mins by fluorescence assay B 7.46 pIC50 34.5 nM IC50 J Med Chem (2015) 58: 4325-4338 [PMID:25906087]
ChEMBL Inhibition of human recombinant HDAC11 B 7.52 pIC50 30 nM IC50 J Med Chem (2023) 66: 7698-7729 [PMID:37276138]
ChEMBL Inhibition of human recombinant HDAC11 using fluorogenic class IIa (Bos-Lys(trifluoroacetyl)-AMC) as substrate B 8 pIC50 10 nM IC50 Eur J Med Chem (2023) 247: 115022-115022 [PMID:36549114]
histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769]
ChEMBL Binding affinity to C-terminal His-tagged human HDAC2 (2 to 488 residues) in transfected in baculovirus infected Sf9 cells assessed as dissociation constant B 6.79 pKd 163 nM Kd J Med Chem (2023) 66: 11672-11700 [PMID:37651268]
ChEMBL Inhibition of C-terminal GST-tagged recombinant human HDAC2 (1 to 488 residues) expressed in Baculovirus infected insect cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubation for 90 mins measured after 15 mins by microplate reader based fluorescence assay B 7 pKi 100 nM Ki Bioorg Med Chem (2019) 27: 115036-115036 [PMID:31431326]
ChEMBL Inhibition of recombinant human HDAC2 B 7.05 pKi 90 nM Ki Bioorg Med Chem (2020) 28: 115108-115108 [PMID:31787463]
ChEMBL Competitive inhibition of HDAC2 using KI-104 as substrate by fluorescence assay B 7.38 pKi 42 nM Ki J Med Chem (2011) 54: 4694-4720 [PMID:21634430]
ChEMBL Inhibition of HDAC2 B 7.4 pKi 40 nM Ki Bioorg Med Chem Lett (2010) 20: 3314-3321 [PMID:20451378]
ChEMBL Binding affinity to recombinant human HDAC2 assessed as inhibition constant B 7.82 pKi 15 nM Ki J Med Chem (2023) 66: 11672-11700 [PMID:37651268]
ChEMBL Inhibition of full-length recombinant human C-terminal GST tagged HDAC2 expressed in Sf9 insect cells assessed as inhibition constant using Ac-LGK(Ac)-AMC substrate and measured for 60 mins at 2 mins interval by fluorescence analysis B 7.89 pKi 13 nM Ki J Med Chem (2023) 66: 15171-15188 [PMID:37847303]
ChEMBL Inhibition of human recombinant HDAC2 using Ac-Leu-Gly-Lys (Ac)-AMC substrate incubated for 30 mins by fluorescence assay B 8.1 pKi 8 nM Ki Medchemcomm (2014) 5: 1849-1855
ChEMBL Inhibition of human recombinant HDAC2 using [Ac-Leu-Gly-Lys(Ac)-AMC substrate incubated for 15 to 30 mins B 8.15 pKi 7 nM Ki J Med Chem (2014) 57: 9644-9657 [PMID:25380299]
ChEMBL Inhibition of recombinant human HDAC2 enzyme using flurogenic Ac-LeuGlyLys (Ac)-AMC as substrate after 15 to 30 mins B 8.15 pKi 7 nM Ki J Med Chem (2013) 56: 6512-6520 [PMID:23865683]
ChEMBL Inhibition of His-tagged recombinant human HDAC2 expressed in insect cells assessed as hydrolase activity using fluorogenic AC-LGK-ac-AMC as substrate measured after 60 mins by fluorescence analysis B 8.38 pKi 4.2 nM Ki Medchemcomm (2016) 7: 464-470
ChEMBL Inhibition of human HDAC2 B 8.8 pKi 1.6 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
GtoPdb - - 8.8 pKi 1.6 nM Ki Nat Chem Biol (2010) 6: 238-243 [PMID:20139990]
ChEMBL Inhibition of recombinant HDAC2 (unknown origin) incubated for 3 hrs by chemiluminescent assay B 4.02 pIC50 96000 nM IC50 Eur J Med Chem (2022) 244: 114807-114807 [PMID:36244186]
ChEMBL Inhibition of human HDAC2 using RHKK(Ac) as substrate by fluorimetric analysis B 6.04 pIC50 921 nM IC50 Bioorg Med Chem Lett (2014) 24: 61-64 [PMID:24345446]
ChEMBL Inhibition of human HDAC2 using RHKK(Ac) as substrate by fluorimetric analysis B 6.04 pIC50 921 nM IC50 Bioorg Med Chem Lett (2015) 25: 459-461 [PMID:25563890]
ChEMBL Inhibition of human HDAC-2 using RHKK(Ac) as substrate B 6.04 pIC50 921 nM IC50 Eur J Med Chem (2014) 76: 53-60 [PMID:24565573]
ChEMBL Inhibition of HDAC2 (unknown origin) using fluorogenic tetrapeptide RHKK(Ac) substrate by fluorescence assay B 6.04 pIC50 921 nM IC50 J Med Chem (2014) 57: 8358-8377 [PMID:25233084]
ChEMBL Inhibition of human HDAC2 by fluorimetric assay B 6.04 pIC50 921 nM IC50 J Med Chem (2010) 53: 8387-8399 [PMID:21073160]
ChEMBL Inhibition of HDAC2 (unknown origin) B 6.04 pIC50 920 nM IC50 Eur J Med Chem (2021) 209: 112904-112904 [PMID:33077264]
ChEMBL Inhibition of human HDAC2 by fluorescence assay B 6.04 pIC50 920 nM IC50 J Med Chem (2013) 56: 427-436 [PMID:23252603]
ChEMBL Inhibition of human recombinant HDAC2 using AMC-K(Ac)GL as substrate by fluorescence based assay B 6.04 pIC50 920 nM IC50 ACS Med Chem Lett (2020) 11: 977-983 [PMID:32435414]
ChEMBL Inhibition of human recombinant full length HDAC2 using (Ac)Arg-Gly-Lys(Ac) as substrate after 60 mins by fluorescence assay B 6.04 pIC50 920 nM IC50 J Med Chem (2013) 56: 9934-9954 [PMID:24261862]
ChEMBL Inhibition of human HDAC-2 using RHKK(Ac) as substrate by fluorescence assay B 6.04 pIC50 920 nM IC50 J Med Chem (2014) 57: 2258-2274 [PMID:24588105]
ChEMBL Inhibition of HDAC2 by fluorometric assay B 6.11 pIC50 780 nM IC50 J Med Chem (2012) 55: 9562-9575 [PMID:23116147]
ChEMBL Inhibition of recombinant human HDAC2 after 60 mins by fluorescence assay B 6.12 pIC50 760 nM IC50 J Med Chem (2015) 58: 7672-7680 [PMID:26331334]
ChEMBL Inhibition of HDAC2 (unknown origin) by fluorimetric assay B 6.26 pIC50 550 nM IC50 Bioorg Med Chem Lett (2016) 26: 154-159 [PMID:26611919]
ChEMBL Inhibition of C-terminal His-tagged full length human recombinant HDAC2 expressed in baculovirus expression system using fluorogenic acetylated peptide as substrate preincubated with enzyme for 10 mins prior to substrate addition measured after 60 mins by fluorescence analysis B 6.27 pIC50 537 nM IC50 ACS Med Chem Lett (2013) 4: 132-136 [PMID:24900575]
ChEMBL Inhibition of HDAC 2 in human HeLa nuclear extract using HDAC substrate-3 measured after 60 mins by fluorometric analysis B 6.34 pIC50 454 nM IC50 J Med Chem (2017) 60: 3484-3497 [PMID:28368585]
ChEMBL Inhibition of HDAC2 (unknown origin) using fluorogenic HDAC substrate-3 by fluorescence assay B 6.39 pIC50 411 nM IC50 Eur J Med Chem (2019) 164: 263-272 [PMID:30597327]
ChEMBL Inhibition of HDAC2 (unknown origin) using RHKK(Ac) (379 to 382) p53 peptide as substrate by fluorescence assay B 6.39 pIC50 410 nM IC50 J Med Chem (2014) 57: 4009-4022 [PMID:24766560]
ChEMBL Inhibition of HDAC2 by in vitro deacetylation assay B 6.4 pIC50 400 nM IC50 Nat Chem Biol (2010) 6: 25-33 [PMID:19966789]
ChEMBL Inhibition of HDAC2 B 6.41 pIC50 390 nM IC50 Eur J Med Chem (2010) 45: 4331-4338 [PMID:20637529]
ChEMBL Inhibition of HDAC2 (unknown origin) B 6.44 pIC50 362 nM IC50 Eur J Med Chem (2021) 209: 112887-112887 [PMID:33035922]
ChEMBL Inhibition of recombinant human HDAC2 using fluorogenic substrate by fluorescence assay B 6.48 pIC50 332.65 nM IC50 Eur J Med Chem (2017) 125: 1268-1278 [PMID:27886544]
ChEMBL Inhibition of HDAC2 (unknown origin) B 6.49 pIC50 322 nM IC50 J Med Chem (2023) 66: 5753-5773 [PMID:37057760]
ChEMBL Inhibition of human recombinant HDAC2 B 6.55 pIC50 282 nM IC50 Bioorg Med Chem Lett (2009) 19: 3023-3026 [PMID:19419863]
ChEMBL Inhibition of HDAC2 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs B 6.55 pIC50 282 nM IC50 J Med Chem (2010) 53: 1347-1356 [PMID:20055418]
ChEMBL Inhibition of HDAC2 after 17 hrs B 6.55 pIC50 282 nM IC50 J Med Chem (2008) 51: 4370-4373 [PMID:18642892]
ChEMBL Inhibition of recombinant HDAC2 (unknown origin) incubated for 10 mins using Boc-Lys(acetyl)-AMC fluorogenic substrate by homogeneous fluorescence release assay B 6.55 pIC50 280 nM IC50 Bioorg Med Chem (2015) 23: 3457-3471 [PMID:25953722]
ChEMBL Inhibition of recombinant HDAC2 (unknown origin) using fluorogenic substrate Boc-Lys (acetyl)-AMC after 20 mins by homogeneous fluorescence release assay B 6.55 pIC50 280 nM IC50 Eur J Med Chem (2015) 96: 1-13 [PMID:25874326]
ChEMBL Inhibition of human recombinant HDAC2 using Boc-L-Lys (Ac)-AMC as substrate preincubated with compound for 24 hrs measured after 35 mins by spectrofluorometric analysis B 6.59 pIC50 260 nM IC50 Bioorg Med Chem Lett (2012) 22: 5025-5030 [PMID:22771007]
ChEMBL Inhibition of HDAC2 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated with enzyme for 5 mins prior to substrate addition measured after 30 mins by fluorescence assay B 6.59 pIC50 256 nM IC50 ACS Med Chem Lett (2013) 4: 235-238 [PMID:23493449]
ChEMBL Inhibition of human recombinant HDAC2 by fluorimetry B 6.6 pIC50 250 nM IC50 J Med Chem (2009) 52: 2909-2922 [PMID:19419205]
ChEMBL Inhibition of human recombinant HDAC2 using Tosyl-Gly-ProLys(Ac)-AMC as substrate measured after 60 mins by fluorescence assay B 6.62 pIC50 240 nM IC50 J Med Chem (2021) 64: 10403-10417 [PMID:34185525]
ChEMBL Inhibition of human HDAC2 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay B 6.62 pIC50 240 nM IC50 J Med Chem (2011) 54: 2165-2182 [PMID:21417297]
ChEMBL Inhibition of HDAC2 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay B 6.62 pIC50 240 nM IC50 J Med Chem (2014) 57: 8026-8034 [PMID:25238284]
ChEMBL Inhibition of HDAC2 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay B 6.62 pIC50 240 nM IC50 Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503]
ChEMBL Inhibition of HDAC2 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHKK(Ac)) as substrate by fluorescence assay B 6.63 pIC50 232 nM IC50 ACS Med Chem Lett (2013) 4: 779-783 [PMID:24015327]
ChEMBL Inhibition of recombinant human full length C-terminal His- tagged HDAC2 (1 to 488 residues) expressed in Sf9 insect cells using fluorometric substrate measured after 60 mins by FRET assay B 6.64 pIC50 230 nM IC50 J Med Chem (2021) 64: 4020-4033 [PMID:33745280]
ChEMBL Inhibition of HDAC2 (unknown origin) using fluorogenic Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence-based assay B 6.66 pIC50 220 nM IC50 J Med Chem (2018) 61: 5304-5322 [PMID:29787262]
ChEMBL Inhibition of HDAC2 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay B 6.66 pIC50 220 nM IC50 J Med Chem (2019) 62: 3898-3923 [PMID:30901208]
ChEMBL Inhibition of HDAC2 (unknown origin) using fluorogenic HDAC substrate 3 incubated for 30 mins by fluorescence based assay B 6.66 pIC50 220 nM IC50 J Med Chem (2018) 61: 1552-1575 [PMID:29360358]
ChEMBL Inhibition of full length recombinant human HDAC2 expressed in baculovirus infected Sf9 insect cells using KI 177 as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay B 6.67 pIC50 214 nM IC50 Eur J Med Chem (2018) 143: 792-805 [PMID:29223096]
ChEMBL Inhibition of HDAC2 (unknown origin) using (FAM)-labeled acetylated peptide as substrate measured after 17 hrs by fluorescence assay B 6.67 pIC50 213 nM IC50 Eur J Med Chem (2018) 158: 620-706 [PMID:30245394]
ChEMBL Inhibition of HDAC2 after 10 mins by fluorometric assay B 6.68 pIC50 210 nM IC50 Bioorg Med Chem (2010) 18: 4119-4137 [PMID:20452225]
ChEMBL Inhibition of recombinant C-terminal FLAG-tagged HDAC2 expressed in baculovirus after 10 mins by fluorimetric analysis B 6.7 pIC50 200 nM IC50 Bioorg Med Chem Lett (2009) 19: 5684-5688 [PMID:19699639]
ChEMBL Inhibition of recombinant human full-length HDAC2 expressed in baculovirus expression system using Boc-l-Lys(Ac)-AMC as substrate preincubated up to 24 hrs and measured after 60 mins by fluorescence assay B 6.7 pIC50 200 nM IC50 Eur J Med Chem (2018) 158: 620-706 [PMID:30245394]
ChEMBL Inhibition of HDAC2 (unknown origin) measured after 30 mins by fluorescence microplate reader assay B 6.7 pIC50 200 nM IC50 J Med Chem (2021) 64: 15280-15296 [PMID:34624191]
ChEMBL Inhibition of full length human HDAC2 using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method B 6.7 pIC50 >200 nM IC50 Eur J Med Chem (2021) 225: 113799-113799 [PMID:34500130]
ChEMBL Inhibition of full length human recombinant C-terminal FLAG-tagged HDAC2 expressed in baculovirus infected Sf9 insect cells using Boc-Lys(epsilon-Ac)-AMC as substrate measured after 90 mins by fluorescence assay B 6.7 pIC50 200 nM IC50 J Med Chem (2017) 60: 5493-5506 [PMID:28574690]
ChEMBL Inhibition of human recombinant HDAC2 using Boc-L-Lys (Ac)-AMC as substrate preincubated with compound for 5 mins measured after 35 mins by spectrofluorometric analysis B 6.7 pIC50 200 nM IC50 Bioorg Med Chem Lett (2012) 22: 5025-5030 [PMID:22771007]
ChEMBL Inhibition of HDAC2 (unknown origin) B 6.71 pIC50 197 nM IC50 Eur J Med Chem (2013) 64: 273-284 [PMID:23644210]
ChEMBL Inhibition of HDAC2 (unknown origin) B 6.71 pIC50 197 nM IC50 Eur J Med Chem (2016) 108: 53-67 [PMID:26629860]
ChEMBL Inhibition of HDAC2 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition by fluorescence assay B 6.71 pIC50 193 nM IC50 Medchemcomm (2015) 6: 1816-1825
ChEMBL Inhibition of HDAC2 in human HeLa cells using BOC-K(Ac)-AMC as substrate measured after 30 mins by fluorescence based microtiter plate reader assay B 6.73 pIC50 188 nM IC50 J Med Chem (2022) 65: 11187-11213 [PMID:35926141]
ChEMBL Inhibition of HDAC2 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay B 6.73 pIC50 184.7 nM IC50 J Med Chem (2014) 57: 3324-3341 [PMID:24694055]
ChEMBL Inhibition of recombinant human full length C-terminal Flag-tagged HDAC2 expressed in baculovirus infected Sf9 cells using ZMAL as substrate incubated for 90 mins by fluorometric method B 6.74 pIC50 183 nM IC50 Bioorg Med Chem (2019) 27: 115039-115039 [PMID:31420257]
ChEMBL Inhibition of human recombinant HDAC2 after 60 mins by fluorimetric assay B 6.74 pIC50 182 nM IC50 Eur J Med Chem (2014) 86: 639-652 [PMID:25218912]
ChEMBL Inhibition of recombinant human HDAC2 preincubated with enzyme followed by flour de lys-green substrate addition measured after 1 hr by fluorescence assay B 6.74 pIC50 180 nM IC50 Bioorg Med Chem Lett (2017) 27: 4415-4420 [PMID:28818449]
ChEMBL Inhibition of HDAC2 in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 30 mins by fluorescence assay B 6.74 pIC50 180 nM IC50 Eur J Med Chem (2018) 158: 620-706 [PMID:30245394]
ChEMBL Inhibition of recombinant HDAC2 using Ac-Lys(Ac)-AMC as substrate after 30 mins by fluorescence analysis B 6.74 pIC50 180 nM IC50 ACS Med Chem Lett (2012) 3: 505-508 [PMID:24900500]
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 6.74 pIC50 180 nM IC50 Eur J Med Chem (2018) 143: 320-333 [PMID:29202397]
ChEMBL Inhibition of HDAC2 (unknown origin) B 6.75 pIC50 178 nM IC50 Bioorg Med Chem Lett (2020) 30: 127128-127128 [PMID:32247729]
ChEMBL Inhibition of human HDAC2 assessed as target activity using fluorogenic substrate ZMAL for 90 min by microplate reader at 355nm B 6.75 pIC50 178 nM IC50 J Med Chem (2021) 64: 14620-14646 [PMID:34582215]
ChEMBL Inhibition of HDAC2 (unknown origin) pre-incubated for 5 mins before fluorogenic substrate Boc-Lys (acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC addition and measured after 30 mins by fluorescence based assay B 6.75 pIC50 176 nM IC50 J Med Chem (2020) 63: 4701-4715 [PMID:32267687]
ChEMBL Inhibition of HDAC2 (unknown origin) B 6.76 pIC50 174.6 nM IC50 Eur J Med Chem (2015) 89: 628-637 [PMID:25462271]
ChEMBL Inhibition of recombinant C-terminal His-tagged full length human HDAC2 expressed in baculovirus infected insect Sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay B 6.76 pIC50 174 nM IC50 ACS Med Chem Lett (2015) 6: 239-243 [PMID:25815139]
ChEMBL Inhibition of recombinant HDAC2 (unknown origin) measured after 30 mins by fluorescence assay B 6.76 pIC50 173 nM IC50 Eur J Med Chem (2019) 180: 171-190 [PMID:31306905]
ChEMBL Inhibition of HDAC2 (unknown origin) B 6.77 pIC50 170 nM IC50 Eur J Med Chem (2021) 219: 113419-113419 [PMID:33845233]
ChEMBL Inhibition of HDAC2 (unknown origin) B 6.77 pIC50 170 nM IC50 J Med Chem (2021) 64: 3392-3426 [PMID:33661013]
ChEMBL Inhibition of HDAC2 B 6.77 pIC50 170 nM IC50 Bioorg Med Chem Lett (2008) 18: 726-731 [PMID:18060775]
ChEMBL Inhibition of C-terminal GST-tagged full-length recombinant human HDAC2 expressed in baculovirus infected Sf9 insect cells using Ac-Leu-Gly-Lys(Ac)-AMC as substrate incubated for 30 mins by fluorescence based assay B 6.77 pIC50 168 nM IC50 J Med Chem (2023) 66: 1239-1253 [PMID:36622852]
ChEMBL Inhibition of HDAC2 (unknown origin) incubated for 30 mins by microplate reader assay B 6.78 pIC50 167 nM IC50 Eur J Med Chem (2022) 229: 114058-114058 [PMID:34954595]
ChEMBL Inhibition of recombinant human HDAC2 expressed in baculovirus infected Sf9 cells using Boc-Lys(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay B 6.78 pIC50 166 nM IC50 Eur J Med Chem (2020) 188: 111991-111991 [PMID:31883490]
ChEMBL Inhibition of HDAC2 B 6.79 pIC50 164 nM IC50 J Med Chem (2008) 51: 3437-3448 [PMID:18494463]
ChEMBL Inhibition of human recombinant HDAC2 using fluorogenic substrate measured after 30 mins B 6.79 pIC50 164 nM IC50 Bioorg Med Chem (2023) 79: 117154-117154 [PMID:36645952]
ChEMBL Inhibition of full length C-terminal 6x-His tagged human HDAC2 using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay B 6.79 pIC50 164 nM IC50 Bioorg Med Chem Lett (2014) 24: 5450-5454 [PMID:25454270]
ChEMBL Inhibition of human recombinant HDAC2 B 6.79 pIC50 163.6 nM IC50 Eur J Med Chem (2009) 44: 1067-1085 [PMID:18672316]
ChEMBL Inhibition of HDAC2 (unknown origin) B 6.8 pIC50 160 nM IC50 Bioorg Med Chem Lett (2022) 71: 128821-128821 [PMID:35643262]
ChEMBL Inhibition of full length C-terminal FLAG-tagged human recombinant HDAC2 (1 to 488 residues) expressed in Sf9 cells using ZMAL as fluorogenic substrate incubated for 90 mins by microplate reader analysis B 6.8 pIC50 160 nM IC50 J Med Chem (2023) 66: 14787-14814 [PMID:37902787]
ChEMBL Inhibition of C-terminal 6His-tagged human recombinant HDAC2 (1 to 488 residues) expressed in Sf9 insect cells using Z-Lys(Ac)-AMC as fluorogenic substrate preincubated for 60 mins followed by substrate addition and measured after 90 mins by microplate reader analysis B 6.8 pIC50 158 nM IC50 J Med Chem (2023) 66: 13821-13837 [PMID:37782298]
ChEMBL Inhibition of HDAC2 (unknown origin) B 6.81 pIC50 156 nM IC50 J Med Chem (2019) 62: 3171-3183 [PMID:30418766]
ChEMBL Inhibition of HDAC2 (unknown origin) preincubated for 60 mins B 6.81 pIC50 154.6 nM IC50 Bioorg Med Chem Lett (2022) 70: 128797-128797 [PMID:35580726]
ChEMBL Inhibition of HDAC2 (unknown origin) after 30 mins by fluorescence assay B 6.82 pIC50 153.1 nM IC50 J Med Chem (2018) 61: 7245-7260 [PMID:30045621]
ChEMBL Inhibition of human HDAC2 after 40 mins by fluorescence analysis B 6.82 pIC50 150 nM IC50 Bioorg Med Chem Lett (2015) 25: 4457-4460 [PMID:26376355]
ChEMBL Inhibition of recombinant HDAC2 (unknown origin) 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 6.83 pIC50 149 nM IC50 J Med Chem (2017) 60: 7965-7983 [PMID:28885834]
ChEMBL Inhibition of C-terminal flag tagged human recombinant full length HDAC2 (1 to 488 residues) using Z- Lys(Ac)-AMC as fluorogenic substrate incubated for 90 mins followed by trypsin addition and measured after 30 min by microplate reader analysis B 6.83 pIC50 147.2 nM IC50 ACS Med Chem Lett (2023) 14: 1863-1868 [PMID:38116436]
ChEMBL Inhibition of recombinant human full length C-terminal FLAG-tagged HDAC2 expressed in baculovirus infected Sf9 insect cells using Boc-Lys(epsilon-acetyl)-AMC as substrate incubated for 90 mins by fluorescence assay B 6.84 pIC50 146 nM IC50 J Med Chem (2019) 62: 11260-11279 [PMID:31762274]
ChEMBL Inhibition of HDAC2 (unknown origin) B 6.85 pIC50 140 nM IC50 Eur J Med Chem (2016) 121: 451-483 [PMID:27318122]
ChEMBL Inhibition of recombinant human full-length HDAC2 expressed in baculovirus expression system using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay B 6.85 pIC50 140 nM IC50 Eur J Med Chem (2018) 158: 620-706 [PMID:30245394]
ChEMBL Inhibition of HDAC2 (unknown origin) B 6.85 pIC50 140 nM IC50 Bioorg Med Chem Lett (2017) 27: 3289-3293 [PMID:28648462]
ChEMBL Inhibition of HDAC2 (unknown origin) preincubated for 90 mins B 6.86 pIC50 137.2 nM IC50 Bioorg Med Chem Lett (2022) 70: 128797-128797 [PMID:35580726]
ChEMBL Inhibition of recombinant human HDAC2 using Boc-Lys(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence-based assay B 6.87 pIC50 135 nM IC50 Eur J Med Chem (2016) 109: 350-359 [PMID:26814680]
ChEMBL Inhibition of HDAC2 (unknown origin) in using Boc-Lys(acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay B 6.89 pIC50 128.9 nM IC50 J Med Chem (2020) 63: 12083-12099 [PMID:33021789]
ChEMBL Inhibition of HDAC2 (unknown origin) preincubated for 120 mins B 6.91 pIC50 123.7 nM IC50 Bioorg Med Chem Lett (2022) 70: 128797-128797 [PMID:35580726]
ChEMBL Inhibition of HDAC2 (unknown origin) B 6.92 pIC50 120.75 nM IC50 Bioorg Med Chem Lett (2023) 88: 129305-129305 [PMID:37116762]
ChEMBL Inhibition of full length human recombinant HDAC2 expressed in baculovirus infected insect S9 cells using Ac-Leu-GlyLys(Ac)-AMC as substrate after 30 mins by fluorescence assay B 6.92 pIC50 120.5 nM IC50 J Med Chem (2015) 58: 4325-4338 [PMID:25906087]
ChEMBL Inhibition of full length recombinant human HDAC2 expressed in baculovirus expression system assessed as release of 7-amino-4-methylcoumarin by fluorogenic assay B 6.92 pIC50 120 nM IC50 Eur J Med Chem (2016) 122: 92-101 [PMID:27344487]
ChEMBL Inhibition of HDAC2 (unknown origin) using Ac-LeuGlyLys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay B 6.92 pIC50 120 nM IC50 ACS Med Chem Lett (2019) 10: 1122-1127 [PMID:31413795]
ChEMBL Inhibition of recombinant human full length HDAC2 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis B 6.92 pIC50 120 nM IC50 Eur J Med Chem (2017) 134: 13-23 [PMID:28395150]
ChEMBL Inhibition of HDAC2 (unknown origin) B 6.93 pIC50 118 nM IC50 Eur J Med Chem (2016) 108: 274-286 [PMID:26689485]
ChEMBL Inhibition of human HDAC2 using Boc-Lys (acetyl)-AMC as substrate pretreated with compound for 1 hrs followed by substrate addition measured after 1 hrs by microplate reader analysis B 6.93 pIC50 116.27 nM IC50 Eur J Med Chem (2022) 243: 114705-114705 [PMID:36215854]
ChEMBL Inhibition of full length recombinant his-tagged human HDAC2 using Ac-LeuGlyLys (Ac) AMC substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence based microplate reader analysis B 6.94 pIC50 114 nM IC50 J Med Chem (2022) 65: 12200-12218 [PMID:36097406]
ChEMBL Inhibition of HDAC2 (unknown origin) using Ac-LeuGlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and further incubated for incubated for 1 hrs by fluorescence microtiter plate reader assay B 6.95 pIC50 112.5 nM IC50 Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929]
ChEMBL Inhibition of recombinant HDAC2 (unknown origin) using Fluor-de-Lys-SIRT1 as substrate by fluorescence assay B 6.96 pIC50 110 nM IC50 J Nat Prod (2014) 77: 49-56 [PMID:24328302]
ChEMBL Inhibition of recombinant human full length C-terminal GST-fusion tagged HDAC2 expressed in baculovirus infected insect cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 90 mins by fluorimetry B 6.97 pIC50 107 nM IC50 Eur J Med Chem (2021) 211: 113095-113095 [PMID:33360560]
ChEMBL Fluorescent Activity Assay: The HDAC activity was performed using the HDAC fluorescent activity assay kit (BIOMOL, Plymouth Meeting, Pa., USA) according to the manufacturer's instructions. Briefly, recombinant proteins of HDAC1 or HDAC6 were incubated with test compounds, and HDAC reaction was initiated by addition of Fluor-de-Lys substrate. Samples were incubated for 10 min at room temperature, followed by adding developer to stop the reaction. Fluorescence was measured by fluorometric reader with excitation at 360 nm and emission at 460 nm. The HDAC activity was expressed as arbitrary fluorescence units (AFU). B 7 pIC50 100.9 nM IC50 US-9353061-B2. 3,5,N-trihydroxy-alkanamide and derivatives: method for making same and use thereof (2016)
ChEMBL Fluorescent Activity Assay: The HDAC activity was performed using the HDAC fluorescent activity assay kit (BIOMOL, Plymouth Meeting, Pa., USA) according to the manufacturer's instructions. Briefly, recombinant proteins of HDAC1 or HDAC6 were incubated with test compounds, and HDAC reaction was initiated by addition of Fluor-de-Lys substrate. Samples were incubated for 10 min at room temperature, followed by adding developer to stop the reaction. Fluorescence was measured by fluorometric reader with excitation at 360 nm and emission at 460 nm. The HDAC activity was expressed as arbitrary fluorescence units (AFU). B 7 pIC50 100.9 nM IC50 US-9115116-B2. Dual action inhibitors against histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme a reductase (2015)
ChEMBL Inhibition of recombinant HDAC2 (unknown origin) after 10 mins by fluorimetric analysis B 7 pIC50 100.9 nM IC50 J Med Chem (2013) 56: 3645-3655 [PMID:23570542]
ChEMBL Inhibition of HDAC2 in human HeLa cells using KI-104 as substrate after 40 mins by fluorescence analysis B 7 pIC50 100 nM IC50 Eur J Med Chem (2014) 79: 251-259 [PMID:24742384]
ChEMBL Inhibition of human recombinant HDAC2 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins B 7 pIC50 100 nM IC50 J Med Chem (2011) 54: 4350-4364 [PMID:21548582]
ChEMBL Inhibition of HDAC2 in human HeLa cells B 7 pIC50 100 nM IC50 Eur J Med Chem (2009) 44: 1900-1912 [PMID:19084294]
ChEMBL Inhibition of human recombinant HDAC2 using Fluor de Lys Green as substrate incubated for 30 mins by fluorescence assay B 7 pIC50 100 nM IC50 Eur J Med Chem (2016) 112: 99-105 [PMID:26890116]
ChEMBL Inhibition of HDAC2 (unknown origin) preincubated for 30 mins B 7.01 pIC50 98.47 nM IC50 Bioorg Med Chem Lett (2022) 70: 128797-128797 [PMID:35580726]
ChEMBL Inhibition of HADC2 (unknown origin) B 7.02 pIC50 96 nM IC50 J Med Chem (2020) 63: 23-39 [PMID:31415174]
ChEMBL Inhibition of full length C-terminal his6-tagged human recombinant HDAC2 (1 to 488 residues) B 7.02 pIC50 96 nM IC50 J Med Chem (2022) 65: 14764-14791 [PMID:36306372]
ChEMBL Inhibition of HDAC2 in human HeLa-S3 cell lysates preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 40 mins by fluorimetric method B 7.02 pIC50 96 nM IC50 Eur J Med Chem (2018) 143: 1790-1806 [PMID:29150330]
ChEMBL Inhibition of HDAC2 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA B 7.02 pIC50 96 nM IC50 ACS Med Chem Lett (2017) 8: 281-286 [PMID:28337317]
ChEMBL Inhibition of HDAC2 (unknown origin) by ELISA-based assay B 7.02 pIC50 96 nM IC50 Bioorg Med Chem Lett (2017) 27: 3254-3258 [PMID:28648461]
ChEMBL Inhibition of full length human C-terminal His-tagged HDAC2 using fluorogenic acetylated peptide as substrate incubated for 30 mins by fluorescence plate reader assay B 7.03 pIC50 93.6 nM IC50 J Med Chem (2021) 64: 3392-3426 [PMID:33661013]
ChEMBL Inhibition of HDAC2 (unknown origin) preincubated for 5 mins B 7.03 pIC50 93.22 nM IC50 Bioorg Med Chem Lett (2022) 70: 128797-128797 [PMID:35580726]
ChEMBL Inhibition of human recombinant full-length C-terminal GST-tagged HDAC2 expressed in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay B 7.04 pIC50 91.6 nM IC50 Eur J Med Chem (2017) 141: 596-602 [PMID:29102179]
ChEMBL Inhibition of recombinant human C-terminal His-tagged HDAC2 (1 to 488 residues) expressed in Sf9 insect cells using fluor de lys SIRT1 as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay B 7.04 pIC50 91 nM IC50 Eur J Med Chem (2020) 192: 112193-112193 [PMID:32151835]
ChEMBL Inhibition of HDAC2 (unknown origin) B 7.05 pIC50 90 nM IC50 Bioorg Med Chem Lett (2013) 23: 3346-3348 [PMID:23591111]
ChEMBL Inhibition of HDAC2 (unknown origin) B 7.05 pIC50 89.23 nM IC50 Bioorg Med Chem Lett (2022) 70: 128797-128797 [PMID:35580726]
ChEMBL Inhibition of recombinant human HDAC2 expressed in baculovirus expression system using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based micro plate reader analysis B 7.05 pIC50 89.23 nM IC50 J Med Chem (2020) 63: 5501-5525 [PMID:32321249]
ChEMBL Inhibition of human recombinant HDAC2 after 30 mins by fluorescence assay B 7.07 pIC50 85.8 nM IC50 J Nat Prod (2013) 76: 2026-2033 [PMID:24164245]
ChEMBL Inhibition of C-terminal FLAG tagged HDAC2 B 7.09 pIC50 82 nM IC50 Bioorg Med Chem Lett (2009) 19: 3081-3084 [PMID:19410459]
ChEMBL Inhibition of HDAC2 B 7.09 pIC50 82 nM IC50 J Med Chem (2008) 51: 2350-2353 [PMID:18370373]
ChEMBL Inhibition of human C-terminal FLAG-tagged HDAC2 in HEK293 cells B 7.09 pIC50 82 nM IC50 J Med Chem (2009) 52: 3453-3456 [PMID:19441846]
ChEMBL Inhibition of HDAC2 B 7.09 pIC50 82 nM IC50 Bioorg Med Chem Lett (2008) 18: 5528-5532 [PMID:18809328]
ChEMBL Inhibition of human full-length C-terminal FLAG-tagged HDAC2 expressed in baculovirus infected Sf9 insect cells using Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured after 30 mins by fluorescence assay B 7.09 pIC50 81.28 nM IC50 Eur J Med Chem (2020) 205: 112648-112648 [PMID:32791401]
ChEMBL Inhibition of C-terminal GST-tagged human recombinant HDAC2 expressed in Sf9 cells after 30 mins by microtiter plate reader analysis B 7.09 pIC50 81 nM IC50 Bioorg Med Chem (2016) 24: 1446-1454 [PMID:26907204]
ChEMBL Inhibition of HDAC2 in human HeLa cells after 72 hrs by ELISA B 7.09 pIC50 81 nM IC50 Eur J Med Chem (2018) 146: 79-92 [PMID:29396364]
ChEMBL Inhibition of human recombinant HDAC2 preincubated for 1 hr with substrate by protease coupled end-point assay B 7.12 pIC50 76 nM IC50 Bioorg Med Chem Lett (2010) 20: 3142-3145 [PMID:20392638]
ChEMBL Inhibition of Histone deacetylase 2 (HDAC2) activity of HeLa nuclear extracts B 7.14 pIC50 73 nM IC50 Bioorg Med Chem Lett (2004) 14: 449-453 [PMID:14698179]
ChEMBL Inhibition of human recombinant HDAC2 preincubated for 24 hrs followed by 1 hr reaction with substrate by protease coupled end-point assay B 7.14 pIC50 72 nM IC50 Bioorg Med Chem Lett (2010) 20: 3142-3145 [PMID:20392638]
ChEMBL Inhibition of recombinant human C-terminal His-tagged HDAC2 (1 to end residues) expressed in sf9 insect cells using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay B 7.15 pIC50 70 nM IC50 Eur J Med Chem (2020) 192: 112189-112189 [PMID:32151834]
ChEMBL Inhibition of full length HDAC2 assessed as 7-amino-4-methylcoumarin release from fluorophore conjugated substrate after 5 mins by fluorescence assay B 7.18 pIC50 66 nM IC50 Bioorg Med Chem Lett (2011) 21: 2601-2605 [PMID:21334896]
ChEMBL Inhibition of recombinant human HDAC2 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry B 7.18 pIC50 66 nM IC50 ACS Med Chem Lett (2011) 2: 703-707 [PMID:21984958]
ChEMBL Inhibition of HDAC2 (unknown origin) B 7.25 pIC50 56 nM IC50 Medchemcomm (2014) 5: 1829-1833
ChEMBL Inhibition of HDAC2 in human HeLa nuclear extract B 7.26 pIC50 55 nM IC50 J Med Chem (2023) 66: 7698-7729 [PMID:37276138]
ChEMBL Inhibition of human recombinant HDAC2 using MAZ1600 as fluorogenic substrate measured every 5 mins by optimized homogenous fluorescence based assay B 7.28 pIC50 52 nM IC50 J Med Chem (2015) 58: 4812-4821 [PMID:25974739]
ChEMBL Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay B 7.29 pIC50 51 nM IC50 Eur J Med Chem (2019) 182: 111672-111672 [PMID:31505452]
ChEMBL Inhibition of HDAC2 in HeLa cell lysates B 7.3 pIC50 >=50 nM IC50 Bioorg Med Chem Lett (2007) 17: 6261-6265 [PMID:17892933]
ChEMBL Inhibition of HDAC2 (unknown origin) using Boc-Lys(Ac)-AMC or Boc-Lys(Tfa)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 1 hr by fluorescence assay B 7.32 pIC50 48 nM IC50 Bioorg Med Chem (2023) 85: 117242-117242 [PMID:37079967]
ChEMBL Inhibition of HDAC2 (unknown origin) B 7.4 pIC50 40 nM IC50 ACS Med Chem Lett (2018) 9: 34-38 [PMID:29348808]
ChEMBL Inhibition of full-length recombinant human C-terminal GST tagged HDAC2 expressed in Sf9 insect cells using aminoluciferin peptide substrate preincubated for 3 hrs followed by substrate addition and measured after 30 mins by HDAC-Glo I/II chemiluminescence assay B 7.42 pIC50 38 nM IC50 J Med Chem (2023) 66: 15171-15188 [PMID:37847303]
ChEMBL Inhibition of HDAC2 B 7.44 pIC50 36 nM IC50 Bioorg Med Chem (2010) 18: 4103-4110 [PMID:20472442]
ChEMBL Inhibition of human full-length recombinant HDAC2 preincubated for 5 mins followed by HDAC substrate addition and further incubated for 45 mins by fluorescence microplate reader assay B 7.46 pIC50 35 nM IC50 Eur J Med Chem (2021) 222: 113569-113569 [PMID:34111829]
ChEMBL Inhibition of recombinant full length human HDAC2 expressed in baculovirus expression system using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay B 7.46 pIC50 35 nM IC50 J Med Chem (2019) 62: 1577-1592 [PMID:30629434]
ChEMBL Inhibition of HDAC2 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay B 7.46 pIC50 35 nM IC50 J Med Chem (2020) 63: 3678-3700 [PMID:32153186]
ChEMBL Inhibition of recombinant HDAC2 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis B 7.46 pIC50 35 nM IC50 J Med Chem (2016) 59: 1455-1470 [PMID:26443078]
ChEMBL Inhibition of HDAC2 (unknown origin) B 7.48 pIC50 33 nM IC50 J Med Chem (2022) 65: 3080-3097 [PMID:35148101]
ChEMBL Inhibition of HDAC2 (unknown origin) B 7.48 pIC50 33 nM IC50 Bioorg Med Chem Lett (2020) 30: 127537-127537 [PMID:32916298]
ChEMBL Inhibition of human recombinant HDAC2 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 30 mins followed by substrate addition and measured after 15 to 30 mins B 7.49 pIC50 32 nM IC50 J Med Chem (2018) 61: 3779-3798 [PMID:29039662]
ChEMBL Inhibition of human recombinant HDAC2 B 7.49 pIC50 32 nM IC50 J Med Chem (2023) 66: 7698-7729 [PMID:37276138]
ChEMBL Inhibition of full length recombinant human C-terminal His-tagged HDAC2 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay B 7.51 pIC50 31 nM IC50 Bioorg Med Chem (2018) 26: 1418-1425 [PMID:29500130]
ChEMBL Inhibition of recombinant full length human HDAC2 expressed in sf9 insect cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay B 7.54 pIC50 29 nM IC50 Eur J Med Chem (2019) 178: 116-130 [PMID:31177073]
ChEMBL Inhibition of human HDAC2 pre-incubated for 30 mins before substrate addition and measured after 30 mins by HDAC-Glo I/II assay B 7.55 pIC50 28 nM IC50 Bioorg Med Chem (2014) 22: 3720-3731 [PMID:24864038]
ChEMBL Inhibition of C-terminal His-tagged full length human HDAC2 expressed in baculovirus expression system using Ac-peptide substrate incubated for 15 mins by fluorescence based assay B 7.55 pIC50 28 nM IC50 Eur J Med Chem (2017) 140: 392-402 [PMID:28987602]
ChEMBL Inhibition of HDAC2 (unknown origin) by colorimetric method B 7.55 pIC50 28 nM IC50 Eur J Med Chem (2022) 240: 114602-114602 [PMID:35858522]
ChEMBL Inhibition of HDAC2 (unknown origin) B 7.57 pIC50 27 nM IC50 Eur J Med Chem (2021) 218: 113392-113392 [PMID:33831778]
ChEMBL Inhibition of HDAC2 (unknown origin) using Ac-peptide as a substrate pretreated for 15 mins followed by substrate addition B 7.59 pIC50 26 nM IC50 Eur J Med Chem (2021) 225: 113824-113824 [PMID:34509167]
ChEMBL Inhibition of human recombinant HDAC2 using fluor de Lys as substrate by fluorometric analysis B 7.62 pIC50 24 nM IC50 J Med Chem (2010) 53: 8663-8678 [PMID:21080647]
ChEMBL Inhibition of recombinant human full length C-terminal His tagged HDAC2 (1 to 488 residues) expressed in baculovirus-infected Sf9 insect cells using Ac-peptide as substrate incubated for 4 hrs B 7.62 pIC50 23.8 nM IC50 J Med Chem (2022) 65: 4156-4181 [PMID:35175762]
ChEMBL Inhibition of HDAC2 (unknown origin) using trypsin and Ac-peptide as substrates B 7.67 pIC50 21.61 nM IC50 Eur J Med Chem (2022) 230: 114115-114115 [PMID:35033824]
ChEMBL Inhibition of HDAC2 (unknown origin) assessed as release of fluorogenic AMC preincubated for 15 mins followed by addition of trypsin and substrate measured after 60 mins Spectra max microplate reader analysis B 7.7 pIC50 20 nM IC50 J Med Chem (2023) 66: 4802-4826 [PMID:36934335]
ChEMBL Inhibition of human recombinant HDAC2 using fluorogenic p53 (379-382 residues) (RHKK(Ac)AMC) as substrate B 7.7 pIC50 20 nM IC50 Eur J Med Chem (2023) 247: 115022-115022 [PMID:36549114]
ChEMBL Inhibition of HDAC2 (unknown origin) using Boc-Lys-(acetyl)-AMC as substrate incubated for 0.5 hr and measured after 20 mins by fluorescence assay B 7.72 pIC50 19 nM IC50 Eur J Med Chem (2022) 233: 114228-114228 [PMID:35245830]
ChEMBL Inhibition of HDAC2 (unknown origin) B 7.73 pIC50 18.55 nM IC50 Eur J Med Chem (2020) 205: 112679-112679 [PMID:32791404]
ChEMBL Inhibition of C-terminal 6His-tagged human recombinant HDAC2 (1 to 488 residues) expressed in Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition by fluorescence based analysis B 7.73 pIC50 18.42 nM IC50 Eur J Med Chem (2023) 254: 115367-115367 [PMID:37086699]
ChEMBL Inhibition of HDAC2 (unknown origin) after 60 mins by fluorescence assay B 7.74 pIC50 18 nM IC50 J Med Chem (2013) 56: 4816-4820 [PMID:23672185]
ChEMBL Inhibition of HDAC2 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition by fluorescence based microplate reader analysis B 7.74 pIC50 18 nM IC50 Eur J Med Chem (2021) 220: 113453-113453 [PMID:33957387]
ChEMBL Inhibition of HDAC2 (unknown origin) using Ac-Leu-GlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence analysis B 7.77 pIC50 17 nM IC50 Bioorg Med Chem (2017) 25: 4123-4132 [PMID:28629630]
ChEMBL Inhibition of human recombinant full-length HDAC2 using fluorophore conjugated substrate by fluorescence assay B 7.8 pIC50 16 nM IC50 J Med Chem (2011) 54: 5576-5582 [PMID:21721525]
ChEMBL Inhibition of HDAC2 (unknown origin) B 7.82 pIC50 15 nM IC50 Bioorg Med Chem Lett (2022) 72: 128846-128846 [PMID:35697181]
ChEMBL Inhibition of HDAC2 (unknown origin) B 7.82 pIC50 15 nM IC50 Bioorg Med Chem Lett (2022) 64: 128663-128663 [PMID:35272009]
ChEMBL Inhibition of human recombinant HDAC2 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate by measuring fluorescence intensity incubated for 30 mins by microplate reader assay B 7.82 pIC50 15 nM IC50 Eur J Med Chem (2021) 217: 113363-113363 [PMID:33744687]
ChEMBL Inhibition of HDAC6 (unknown origin) B 7.89 pIC50 13 nM IC50 Eur J Med Chem (2021) 213: 113173-113173 [PMID:33493830]
ChEMBL Inhibition of C-terminal 6XHis-tagged human recombinant full length HDAC2 (1 to 488 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in 7-amino-4-methylcoumarin release measured every 5 mins by fluorescence based analysis B 7.89 pIC50 13 nM IC50 Bioorg Med Chem (2021) 42: 116251-116251 [PMID:34116381]
ChEMBL Inhibition of HDAC2 (unknown origin) B 7.92 pIC50 12 nM IC50 Eur J Med Chem (2021) 224: 113672-113672 [PMID:34237620]
ChEMBL Inhibition of human HDAC2 incubated for 30 mins by SpectraMax M2 microplate reader analysis B 7.92 pIC50 12 nM IC50 Eur J Med Chem (2021) 209: 112904-112904 [PMID:33077264]
ChEMBL Inhibition of HDAC2 (unknown origin) using fluorogenic peptide RHKKAc-AMC as substrate by fluorescence-based assay B 7.93 pIC50 11.7 nM IC50 Bioorg Med Chem Lett (2023) 81: 129148-129148 [PMID:36690041]
ChEMBL Inhibition of HDAC2 (unknown origin) using Fluor de lys as substrate by fluorescence based analysis B 7.93 pIC50 11.7 nM IC50 Eur J Med Chem (2020) 187: 111950-111950 [PMID:31865013]
ChEMBL Inhibition of HDAC2 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay B 7.96 pIC50 11 nM IC50 J Med Chem (2013) 56: 1772-1776 [PMID:23368884]
ChEMBL Inhibition of HDAC2 (unknown origin) B 7.96 pIC50 11 nM IC50 J Med Chem (2022) 65: 16541-16569 [PMID:36449947]
ChEMBL Inhibition of HDAC2 (unknown origin) using fluorogenic substrate incubated for 30 mins by fluorescence based assay B 7.96 pIC50 11 nM IC50 J Med Chem (2022) 65: 3667-3683 [PMID:35152694]
ChEMBL Inhibition of human recombinant HDAC2 using acetyllysine tripeptide coupled with 7-amino-4-methylcoumarin as substrate by fluorescence assay B 7.99 pIC50 10.2 nM IC50 Bioorg Med Chem Lett (2016) 26: 1265-1271 [PMID:26804233]
ChEMBL Inhibition of HDAC2 (unknown origin)-mediated deacetylation preincubated for 5 mins prior to substrate addition measured after 30 mins by fluorescence assay B 8 pIC50 10 nM IC50 J Med Chem (2013) 56: 7997-8007 [PMID:24074025]
ChEMBL Inhibition of recombinant human HDAC2 B 8.7 pIC50 2 nM IC50 J Med Chem (2023) 66: 11672-11700 [PMID:37651268]
ChEMBL Inhibition of human recombinant HDAC2 after 30 mins by fluorometric assay B 8.77 pIC50 1.7 nM IC50 J Med Chem (2012) 55: 3777-3791 [PMID:22439863]
histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379]
ChEMBL Competitive inhibition of HDAC3 using KI-104 as substrate by fluorescence assay B 7.44 pKi 36 nM Ki J Med Chem (2011) 54: 4694-4720 [PMID:21634430]
ChEMBL Inhibition of HDAC3 B 7.54 pKi 29 nM Ki