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| ChEMBL ligand: CHEMBL98 (MK-0683, MK0683, NSC-701852, NSC-748799, NSC-759852, Suberoylanilide hydroxamic acid, Vorinostat, Zolinza) |
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| 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: Q13547, Q9P2K3] | ||||||||
| 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 | |