romidepsin [Ligand Id: 7006] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL343448 (Chromadax, Depsipeptide, FK-228, FK228, FR-901228, FR901228, Istodax, NSC-630176, Romidepsin, Romidepsina, Romidepsine) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885] | ||||||||
| ChEMBL | Inhibition of BRD4 (unknown origin) | B | 7.44 | pIC50 | 36 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4051-4055 [PMID:28765013] |
| Histone deacetylase in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5541] [UniProtKB: Q9XYC7] | ||||||||
| ChEMBL | Inhibition of HDAC1 in Plasmodium falciparum 3D7 nuclear extract using Ac-RGK(Ac)-AMC fluorogenic peptide as substrate preincubated for 1 hr followed by substrate addition measured after 10 min by fluorescence assay | B | 9.05 | pIC50 | 0.9 | nM | IC50 | J Med Chem (2017) 60: 4780-4804 [PMID:28241112] |
| histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547] | ||||||||
| ChEMBL | Binding affinity to HDAC1 (unknown origin) using Ac-LGKac-AMC as substrate assessed as inhibition constant(ki,1) | B | 9.06 | pKi | 0.88 | nM | Ki | J Med Chem (2023) 66: 11672-11700 [PMID:37651268] |
| ChEMBL | Binding affinity to HDAC1 (unknown origin) using Ac-LGKac-AMC as substrate assessed as inhibition constant | B | 10.7 | pKi | ~0.02 | nM | Ki | J Med Chem (2023) 66: 11672-11700 [PMID:37651268] |
| GtoPdb | - | - | 11.82 | pKi | 0 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of recombinant human HDAC1 after 60 mins by fluorescence assay | B | 5.98 | pIC50 | 1050 | nM | IC50 | J Med Chem (2015) 58: 7672-7680 [PMID:26331334] |
| ChEMBL | Inhibitory concentration against human Histone deacetylase 1 (C151S) | B | 6.55 | pIC50 | 280 | nM | IC50 | J Med Chem (2003) 46: 5097-5116 [PMID:14613312] |
| ChEMBL | Inhibition of recombinant human HDAC1 | B | 6.85 | pIC50 | 140 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 375-379 [PMID:26706171] |
| ChEMBL | Inhibitory concentration against human Histone deacetylase 1 | B | 7.44 | pIC50 | 36 | nM | IC50 | J Med Chem (2003) 46: 5097-5116 [PMID:14613312] |
| ChEMBL | Inhibition of HDAC1 by fluorimetric assay | B | 7.44 | pIC50 | 36 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6770-6772 [PMID:23021104] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 7.44 | pIC50 | 36 | nM | IC50 | Eur J Med Chem (2019) 183: 111691-111691 [PMID:31536895] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 7.44 | pIC50 | 36 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of human HDAC1 expressed in HEK293T cells by scintillation counting analysis | B | 7.44 | pIC50 | 36 | nM | IC50 | Bioorg Med Chem (2021) 52: 116510-116510 [PMID:34826681] |
| ChEMBL | Inhibition of human recombinant HDAC1 using ZMAL (Z-(Ac)Lys-AMC) as fluorogenic substrate preincubated for 5 mins followed by substrate addition and measured after 1 hr by fluorescence based analysis | B | 7.44 | pIC50 | 36 | nM | IC50 | Eur J Med Chem (2023) 245: 114920-114920 [PMID:36399875] |
| ChEMBL | Inhibition of human recombinant HDAC1 using fluorogenic HDAC substrate by fluorescence assay | B | 7.44 | pIC50 | 36 | nM | IC50 | Eur J Med Chem (2023) 261: 115835-115835 [PMID:37801827] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) incubated for 1 hr by fluor de lys substrate based fluorescence method | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem (2015) 23: 6785-6793 [PMID:26481659] |
| ChEMBL | Inhibition of HDAC1 in presence of DTT | B | 8.4 | pIC50 | 3.97 | nM | IC50 | J Med Chem (2007) 50: 5720-5726 [PMID:17958342] |
| ChEMBL | Inhibition of human HDAC1 expressed in human 293T cells using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay | B | 8.44 | pIC50 | 3.6 | nM | IC50 | Eur J Med Chem (2014) 76: 301-313 [PMID:24589486] |
| ChEMBL | Inhibition of human HDAC1 using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay | B | 8.44 | pIC50 | 3.6 | nM | IC50 | Eur J Med Chem (2013) 60: 295-304 [PMID:23313638] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) by fluorescence based assay | B | 8.44 | pIC50 | 3.6 | nM | IC50 | Eur J Med Chem (2024) 265: 116109-116109 [PMID:38183777] |
| ChEMBL | Inhibition of human recombinant C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells after 1 hr by HDAC-Glo1/2 luminescent assay | B | 8.62 | pIC50 | 2.4 | nM | IC50 | Medchemcomm (2019) 10: 538-542 [PMID:31057733] |
| ChEMBL | Inhibition of human HDAC1 expressed in 293T cells using Ac-KGLGK(Ac)-MCA as substrate incubated for 30 mins in presence of 0.1 mM DTT by fluorescence plate reader assay | B | 8.62 | pIC50 | 2.4 | nM | IC50 | Eur J Med Chem (2016) 121: 592-609 [PMID:27318982] |
| ChEMBL | Inhibition of HADC1 (unknown origin) | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2020) 63: 23-39 [PMID:31415174] |
| ChEMBL | Displacement of [3H]-acetylated histones from human HDAC1 transfected in HEK-293T cells incubated for 15 mins by scintillation counting method | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2022) 65: 3080-3097 [PMID:35148101] |
| ChEMBL | Inhibition of HDAC1 in human DU-145 cells assessed as increase in histone H3 acetylation after 24 hrs by immunofluorescence microscopy | B | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (2022) 65: 3388-3403 [PMID:35133171] |
| ChEMBL | Inhibition of human HDAC1 using fluorescent substrate Ac-KGLGK(Ac)-MCA after 30 mins by fluorescence plate reader in presence of 0.1 mM dithiothreitol | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem (2014) 22: 3850-3855 [PMID:24997578] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2023) 258: 115594-115594 [PMID:37429084] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2024) 269: 116324-116324 [PMID:38520762] |
| ChEMBL | Inhibition of HDAC1 by fluorimetric assay in presence of DTT | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6770-6772 [PMID:23021104] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) incubated for 30 mins in presence of BSA and DTT by fluorescence assay | B | 9.1 | pIC50 | 0.8 | nM | IC50 | ACS Med Chem Lett (2014) 5: 905-910 [PMID:25147612] |
| ChEMBL | Inhibition of human recombinant HDAC1 after 1 hr by luminescence assay | B | 9.51 | pIC50 | 0.31 | nM | IC50 | Medchemcomm (2012) 3: 976-981 [PMID:23997923] |
| ChEMBL | Inhibition of recombinant HDAC1 using Ac-Lys(Ac)-AMC as substrate after 30 mins by fluorescence analysis | B | 9.7 | pIC50 | 0.2 | nM | IC50 | ACS Med Chem Lett (2012) 3: 505-508 [PMID:24900500] |
| ChEMBL | Inhibition of Histone deacetylase 1 induced acetylated histone in mammalian cells. | B | 4.44 | pEC50 | 36000 | nM | EC50 | J Med Chem (2003) 46: 4826-4829 [PMID:14584932] |
| histone deacetylase 11/Histone deacetylase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3310] [GtoPdb: 2615] [UniProtKB: Q96DB2] | ||||||||
| 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 HDAC11 (unknown origin) incubated for 3 hrs in presence of BSA and DTT by fluorescence assay | B | 9.52 | pIC50 | 0.3 | nM | IC50 | ACS Med Chem Lett (2014) 5: 905-910 [PMID:25147612] |
| ChEMBL | Inhibition of HDAC11 (unknown origin) | B | 9.52 | pIC50 | 0.3 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of HDAC11 (unknown origin) | B | 9.52 | pIC50 | 0.3 | nM | IC50 | Eur J Med Chem (2024) 269: 116324-116324 [PMID:38520762] |
| histone deacetylase 1/Histone deacetylase 1/Nuclear receptor corepressor 2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3885590] [GtoPdb: 2658] [UniProtKB: Q13547, Q9Y618] | ||||||||
| GtoPdb | - | - | 11.82 | pKi | 0 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of recombinant human HDAC1/NCOR2 using Boc-L-Lys(epsilon-acetyl)-AMC as substrate by two-step fluorogenic assay | B | 5.17 | pIC50 | 6700 | nM | IC50 | J Nat Prod (2011) 74: 2031-2038 [PMID:21793558] |
| histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769] | ||||||||
| ChEMBL | Binding affinity to HDAC2 (unknown origin) using Ac-LGKac-AMC as substrate assessed as inhibition constant(ki,1) | B | 9.33 | pKi | 0.47 | nM | Ki | J Med Chem (2023) 66: 11672-11700 [PMID:37651268] |
| GtoPdb | - | - | 10.42 | pKi | 0.04 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC2 | B | 10.42 | pKi | 0.04 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of recombinant human HDAC2 enzyme using flurogenic Ac-LeuGlyLys (Ac)-AMC as substrate after 15 to 30 mins | B | 10.42 | pKi | 0.04 | nM | Ki | J Med Chem (2013) 56: 6512-6520 [PMID:23865683] |
| ChEMBL | Inhibition of recombinant human HDAC2 after 60 mins by fluorescence assay | B | 5.22 | pIC50 | 6070 | nM | IC50 | J Med Chem (2015) 58: 7672-7680 [PMID:26331334] |
| ChEMBL | Inhibitory concentration against human Histone deacetylase 2 | B | 7.33 | pIC50 | 47 | nM | IC50 | J Med Chem (2003) 46: 5097-5116 [PMID:14613312] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 7.33 | pIC50 | 47 | nM | IC50 | Eur J Med Chem (2019) 183: 111691-111691 [PMID:31536895] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 7.33 | pIC50 | 47 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 7.33 | pIC50 | 47 | nM | IC50 | Eur J Med Chem (2021) 216: 113332-113332 [PMID:33714914] |
| ChEMBL | Inhibition of human HDAC2 expressed in HEK293T cells by scintillation counting analysis | B | 7.33 | pIC50 | 47 | nM | IC50 | Bioorg Med Chem (2021) 52: 116510-116510 [PMID:34826681] |
| ChEMBL | Inhibition of human full length recombinant HDAC2 expressed in baculovirus infected Sf9 cells using RHKKAc as substrate preincubated for 10 mins followed by substrate addition and measured after 2 hrs by fluorescence based analysis | B | 7.33 | pIC50 | 47 | nM | IC50 | Eur J Med Chem (2023) 245: 114920-114920 [PMID:36399875] |
| ChEMBL | Inhibition of human recombinant HDAC2 using AMC-K(Ac)GL as substrate by fluorescence based assay | B | 7.33 | pIC50 | 47 | nM | IC50 | Eur J Med Chem (2023) 261: 115835-115835 [PMID:37801827] |
| ChEMBL | Inhibition of HDAC2 in human DU-145 cells assessed as increase in histone H3 acetylation after 24 hrs by immunofluorescence microscopy | B | 8.33 | pIC50 | 4.7 | nM | IC50 | J Med Chem (2022) 65: 3388-3403 [PMID:35133171] |
| ChEMBL | Inhibition of HADC2 (unknown origin) | B | 8.41 | pIC50 | 3.9 | nM | IC50 | J Med Chem (2020) 63: 23-39 [PMID:31415174] |
| ChEMBL | Displacement of [3H]-acetylated histones from human HDAC2 transfected in HEK-293T cells incubated for 15 mins by scintillation counting method | B | 8.41 | pIC50 | 3.9 | nM | IC50 | J Med Chem (2022) 65: 3080-3097 [PMID:35148101] |
| ChEMBL | Inhibition of recombinant HDAC2 using Ac-Lys(Ac)-AMC as substrate after 30 mins by fluorescence analysis | B | 9 | pIC50 | 1 | nM | IC50 | ACS Med Chem Lett (2012) 3: 505-508 [PMID:24900500] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2023) 258: 115594-115594 [PMID:37429084] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2024) 269: 116324-116324 [PMID:38520762] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) incubated for 30 mins in presence of BSA and DTT by fluorescence assay | B | 9 | pIC50 | 1 | nM | IC50 | ACS Med Chem Lett (2014) 5: 905-910 [PMID:25147612] |
| histone deacetylase 2/Histone deacetylase 2/Nuclear receptor corepressor 2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3885591] [GtoPdb: 2616] [UniProtKB: Q92769, Q9Y618] | ||||||||
| GtoPdb | - | - | 10.42 | pKi | 0.04 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of recombinant human HDAC2/NCOR2 using Boc-L-Lys(epsilon-acetyl)-AMC as substrate by two-step fluorogenic assay | B | 5.82 | pIC50 | 1500 | nM | IC50 | J Nat Prod (2011) 74: 2031-2038 [PMID:21793558] |
| histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379] | ||||||||
| ChEMBL | Binding affinity to HDAC3 (unknown origin) using Ac-LGKac-AMC as substrate assessed as inhibition constant(ki,1) | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (2023) 66: 11672-11700 [PMID:37651268] |
| GtoPdb | - | - | 9.82 | pKi | 0.15 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC3 | B | 9.82 | pKi | 0.15 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of recombinant human HDAC3 after 60 mins by fluorescence assay | B | 7.21 | pIC50 | 62 | nM | IC50 | J Med Chem (2015) 58: 7672-7680 [PMID:26331334] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) incubated for 30 mins in presence of BSA and DTT by fluorescence assay | B | 8.89 | pIC50 | 1.3 | nM | IC50 | ACS Med Chem Lett (2014) 5: 905-910 [PMID:25147612] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2024) 269: 116324-116324 [PMID:38520762] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2023) 258: 115594-115594 [PMID:37429084] |
| ChEMBL | Inhibition of HDAC3 in human DU-145 cells assessed as increase in histone H3 acetylation after 24 hrs by immunofluorescence microscopy | B | 9.05 | pIC50 | 0.9 | nM | IC50 | J Med Chem (2022) 65: 3388-3403 [PMID:35133171] |
| histone deacetylase 3/Histone deacetylase 3/NCoR1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038484] [GtoPdb: 2617] [UniProtKB: O15379, O75376] | ||||||||
| GtoPdb | - | - | 9.82 | pKi | 0.15 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of GST-tagged recombinant human HDAC3/NcoR1 enzyme using flurogenic Ac-LeuGlyLys (Ac)-AMC as substrate after 15 to 30 mins | B | 9.82 | pKi | 0.15 | nM | Ki | J Med Chem (2013) 56: 6512-6520 [PMID:23865683] |
| histone deacetylase 3/Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111363] [GtoPdb: 2617] [UniProtKB: O15379, Q9Y618] | ||||||||
| ChEMBL | Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from human HDAC3/NcoR2 by fluorescence polarization assay | B | 7.6 | pKi | 24.9 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2809-2812 [PMID:18430569] |
| GtoPdb | - | - | 9.82 | pKi | 0.15 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from human HDAC3/NcoR2 by fluorescence polarization assay | B | 6.83 | pIC50 | 146.9 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 2809-2812 [PMID:18430569] |
| ChEMBL | Inhibition of recombinant human HDAC3/N-CoR2 using Boc-L-Lys(epsilon-trifluoroacetyl)-AMC as substrate by two-step fluorogenic assay in presence of 1 mM H2O2 (Rvb = 0.018 uM) | B | 7.39 | pIC50 | 41 | nM | IC50 | J Nat Prod (2011) 74: 2031-2038 [PMID:21793558] |
| ChEMBL | Inhibition of recombinant human HDAC3/N-CoR2 using Boc-L-Lys(epsilon-trifluoroacetyl)-AMC as substrate by two-step fluorogenic assay in presence of 0.4 mM H2O2 (Rvb = 0.018 uM) | B | 7.41 | pIC50 | 39 | nM | IC50 | J Nat Prod (2011) 74: 2031-2038 [PMID:21793558] |
| ChEMBL | Inhibition of recombinant human HDAC3/N-CoR2 using Boc-L-Lys(epsilon-trifluoroacetyl)-AMC as substrate by two-step fluorogenic assay in presence of 0.2 mM H2O2 (Rvb = 0.018 uM) | B | 7.7 | pIC50 | 20 | nM | IC50 | J Nat Prod (2011) 74: 2031-2038 [PMID:21793558] |
| ChEMBL | Inhibition of recombinant human HDAC3/NCOR2 using Boc-L-Lys(epsilon-trifluoroacetyl)-AMC as substrate by two-step fluorogenic assay | B | 7.74 | pIC50 | 18 | nM | IC50 | J Nat Prod (2011) 74: 2031-2038 [PMID:21793558] |
| ChEMBL | Inhibition of recombinant HDAC3/NCoR2 using Ac-Lys(Ac)-AMC as substrate after 30 mins by fluorescence analysis | B | 8.52 | pIC50 | 3 | nM | IC50 | ACS Med Chem Lett (2012) 3: 505-508 [PMID:24900500] |
| histone deacetylase 4/Histone deacetylase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3524] [GtoPdb: 2659] [UniProtKB: P56524] | ||||||||
| ChEMBL | Inhibition of human HDAC4 | B | 7.69 | pKi | 20.5 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of recombinant human HDAC4 enzyme using Ac-LeuGlyLys (tfa)-AMC as substrate after 15 to 30 mins | B | 7.69 | pKi | 20.5 | nM | Ki | J Med Chem (2013) 56: 6512-6520 [PMID:23865683] |
| GtoPdb | - | - | 7.69 | pKi | 20.5 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of recombinant human HDAC4 using Boc-L-Lys(epsilon-trifluoroacetyl)-AMC as substrate by two-step fluorogenic assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Nat Prod (2011) 74: 2031-2038 [PMID:21793558] |
| ChEMBL | Inhibition of recombinant human HDAC4 after 60 mins by fluorescence assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 7672-7680 [PMID:26331334] |
| ChEMBL | Inhibition of human recombinant HDAC4 after 1 hr by luminescence assay | B | 5.06 | pIC50 | 8670 | nM | IC50 | Medchemcomm (2012) 3: 976-981 [PMID:23997923] |
| ChEMBL | Inhibition of human recombinant C-terminal GST-tagged HDAC4 (101 to 1084 residues) expressed in baculovirus infected Sf9 insect cells after 1 hr by HDAC-Glo1/2 luminescent assay | B | 5.35 | pIC50 | 4462 | nM | IC50 | Medchemcomm (2019) 10: 538-542 [PMID:31057733] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) | B | 6.19 | pIC50 | 647 | nM | IC50 | Eur J Med Chem (2024) 269: 116324-116324 [PMID:38520762] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) | B | 6.19 | pIC50 | 647 | nM | IC50 | Eur J Med Chem (2023) 258: 115594-115594 [PMID:37429084] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) incubated for 30 mins in presence of BSA and DTT by fluorescence assay | B | 6.19 | pIC50 | 647 | nM | IC50 | ACS Med Chem Lett (2014) 5: 905-910 [PMID:25147612] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) | B | 6.19 | pIC50 | 647 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of human recombinant HDAC4 using AMC-K(TFA)GL as substrate by fluorescence based analysis | B | 6.29 | pIC50 | 510 | nM | IC50 | Eur J Med Chem (2023) 261: 115835-115835 [PMID:37801827] |
| ChEMBL | Inhibition of Histone deacetylase 4 in mammalian cells. | B | 6.29 | pIC50 | 510 | nM | IC50 | J Med Chem (2003) 46: 4826-4829 [PMID:14584932] |
| ChEMBL | Inhibition of HDAC4 by fluorimetric assay | B | 6.29 | pIC50 | 510 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6770-6772 [PMID:23021104] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) | B | 6.29 | pIC50 | 510 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of human HDAC4 expressed in HEK293T cells by scintillation counting analysis | B | 6.29 | pIC50 | 510 | nM | IC50 | Bioorg Med Chem (2021) 52: 116510-116510 [PMID:34826681] |
| ChEMBL | Inhibition of human recombinant HDAC4 using Boc-Lys(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence based analysis | B | 6.29 | pIC50 | 510 | nM | IC50 | Eur J Med Chem (2023) 245: 114920-114920 [PMID:36399875] |
| ChEMBL | Inhibitory concentration against human Histone deacetylase 4 | B | 6.29 | pIC50 | 510 | nM | IC50 | J Med Chem (2003) 46: 5097-5116 [PMID:14613312] |
| histone deacetylase 5/Histone deacetylase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2563] [GtoPdb: 2660] [UniProtKB: Q9UQL6] | ||||||||
| ChEMBL | Inhibition of human HDAC5 | B | 6.26 | pKi | 550 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of recombinant human HDAC5 enzyme using Ac-LeuGlyLys (tfa)-AMC as substrate after 15 to 30 mins | B | 6.26 | pKi | 550 | nM | Ki | J Med Chem (2013) 56: 6512-6520 [PMID:23865683] |
| GtoPdb | - | - | 6.26 | pKi | 550 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of recombinant human HDAC5 after 60 mins by fluorescence assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 7672-7680 [PMID:26331334] |
| ChEMBL | Inhibition of HDAC5 (unknown origin) | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of HDAC5 (unknown origin) | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2024) 269: 116324-116324 [PMID:38520762] |
| histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
| ChEMBL | Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from human HDAC6 by fluorescence polarization assay | B | 6.52 | pKi | 300.1 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2809-2812 [PMID:18430569] |
| ChEMBL | Inhibition of recombinant human HDAC6 enzyme using flurogenic Ac-LeuGlyLys (Ac)-AMC as substrate after 15 to 30 mins | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2013) 56: 6512-6520 [PMID:23865683] |
| GtoPdb | - | - | 8.02 | pKi | 9.5 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC6 | B | 8.02 | pKi | 9.5 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibitory concentration against human Histone deacetylase 6 | B | 4.85 | pIC50 | 14000 | nM | IC50 | J Med Chem (2003) 46: 5097-5116 [PMID:14613312] |
| ChEMBL | Inhibition of recombinant human HDAC6 using Boc-L-Lys(epsilon-acetyl)-AMC as substrate by two-step fluorogenic assay | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Nat Prod (2011) 74: 2031-2038 [PMID:21793558] |
| ChEMBL | Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from human HDAC6 by fluorescence polarization assay | B | 5.8 | pIC50 | 1595 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 2809-2812 [PMID:18430569] |
| ChEMBL | Inhibition of human HDAC6 expressed in HEK293T cells by scintillation counting analysis | B | 5.85 | pIC50 | 1400 | nM | IC50 | Bioorg Med Chem (2021) 52: 116510-116510 [PMID:34826681] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 5.85 | pIC50 | 1400 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of human recombinant HDAC6 using fluorogenic HDAC substrate incubated for 30 mins by fluorescence assay | B | 5.85 | pIC50 | 1400 | nM | IC50 | Eur J Med Chem (2023) 245: 114920-114920 [PMID:36399875] |
| ChEMBL | Inhibition of recombinant human HDAC6 after 60 mins by fluorescence assay | B | 5.91 | pIC50 | 1220 | nM | IC50 | J Med Chem (2015) 58: 7672-7680 [PMID:26331334] |
| ChEMBL | Inhibition of HADC6 (unknown origin) | B | 6.1 | pIC50 | 790 | nM | IC50 | J Med Chem (2020) 63: 23-39 [PMID:31415174] |
| ChEMBL | Inhibition of HDAC6 in presence of DTT | B | 6.1 | pIC50 | 787 | nM | IC50 | J Med Chem (2007) 50: 5720-5726 [PMID:17958342] |
| ChEMBL | Inhibition of human recombinant HDAC6 after 1 hr by luminescence assay | B | 6.17 | pIC50 | 670 | nM | IC50 | Medchemcomm (2012) 3: 976-981 [PMID:23997923] |
| ChEMBL | Inhibition of HDAC6 by fluorimetric assay in presence of DTT | B | 6.21 | pIC50 | 620 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6770-6772 [PMID:23021104] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) incubated for 1 hr by fluor de lys substrate based fluorescence method | B | 6.55 | pIC50 | 281 | nM | IC50 | Bioorg Med Chem (2015) 23: 6785-6793 [PMID:26481659] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 6.65 | pIC50 | 226 | nM | IC50 | Eur J Med Chem (2024) 269: 116324-116324 [PMID:38520762] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 6.65 | pIC50 | 226 | nM | IC50 | Eur J Med Chem (2023) 258: 115594-115594 [PMID:37429084] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 6.65 | pIC50 | 226 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of recombinant HDAC6 using Ac-Lys(Ac)-AMC as substrate after 30 mins by fluorescence analysis | B | 6.7 | pIC50 | 200 | nM | IC50 | ACS Med Chem Lett (2012) 3: 505-508 [PMID:24900500] |
| ChEMBL | Inhibition of HDAC6 in human DU-145 cells assessed as increase in histone H3 acetylation after 24 hrs by immunofluorescence microscopy | B | 6.74 | pIC50 | 180 | nM | IC50 | J Med Chem (2022) 65: 3388-3403 [PMID:35133171] |
| ChEMBL | Inhibition of recombinant human HDAC6 | B | 7.1 | pIC50 | 80 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 375-379 [PMID:26706171] |
| ChEMBL | Inhibition of human recombinant C-terminal FLAG-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells after 1 hr by HDAC-Glo1/2 luminescent assay | B | 8.04 | pIC50 | 9.1 | nM | IC50 | Medchemcomm (2019) 10: 538-542 [PMID:31057733] |
| ChEMBL | Inhibition of human recombinant HDAC6 using RHKKAc-AMC as substrate by fluorescence based assay | B | 8.85 | pIC50 | 1.4 | nM | IC50 | Eur J Med Chem (2023) 261: 115835-115835 [PMID:37801827] |
| histone deacetylase 6/Histone deacetylase 6 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2878] [GtoPdb: 2618] [UniProtKB: Q9Z2V5] | ||||||||
| ChEMBL | Displacement of [3H]-acetylated histones from mouse HDAC6 transfected in HEK-293T cells incubated for 15 mins by scintillation counting method | B | 6.1 | pIC50 | 790 | nM | IC50 | J Med Chem (2022) 65: 3080-3097 [PMID:35148101] |
| ChEMBL | Inhibition of mouse HDAC6 using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay | B | 6.41 | pIC50 | 390 | nM | IC50 | Eur J Med Chem (2013) 60: 295-304 [PMID:23313638] |
| ChEMBL | Inhibition of mouse HDAC6 expressed in human 293T cells using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay | B | 6.41 | pIC50 | 390 | nM | IC50 | Eur J Med Chem (2014) 76: 301-313 [PMID:24589486] |
| ChEMBL | Inhibition of mouse HDAC6 using fluorescent substrate Ac-KGLGK(Ac)-MCA after 30 mins by fluorescence plate reader in presence of 0.1 mM dithiothreitol | B | 9.2 | pIC50 | 0.63 | nM | IC50 | Bioorg Med Chem (2014) 22: 3850-3855 [PMID:24997578] |
| histone deacetylase 7/Histone deacetylase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2716] [GtoPdb: 2661] [UniProtKB: Q8WUI4] | ||||||||
| GtoPdb | - | - | 5.9 | pKi | 1250 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC7 | B | 5.9 | pKi | 1250 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of recombinant human HDAC7 enzyme using Ac-LeuGlyLys (tfa)-AMC as substrate after 15 to 30 mins | B | 5.9 | pKi | 1250 | nM | Ki | J Med Chem (2013) 56: 6512-6520 [PMID:23865683] |
| ChEMBL | Inhibition of recombinant human HDAC7 using Boc-L-Lys(epsilon-trifluoroacetyl)-AMC as substrate by two-step fluorogenic assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Nat Prod (2011) 74: 2031-2038 [PMID:21793558] |
| ChEMBL | Inhibition of recombinant human HDAC7 after 60 mins by fluorescence assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 7672-7680 [PMID:26331334] |
| ChEMBL | Inhibition of HDAC7 (unknown origin) | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of HDAC7 (unknown origin) | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2024) 269: 116324-116324 [PMID:38520762] |
| histone deacetylase 8/Histone deacetylase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41] | ||||||||
| GtoPdb | - | - | 9.82 | pKi | 0.15 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Activity of human HDAC8 | B | 9.82 | pKi | 0.15 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of recombinant human HDAC8 enzyme using Ac-LeuGlyLys (tfa)-AMC as substrate after 15 to 30 mins | B | 9.82 | pKi | 0.15 | nM | Ki | J Med Chem (2013) 56: 6512-6520 [PMID:23865683] |
| ChEMBL | Inhibition of recombinant human HDAC8 using Boc-L-Lys(epsilon-trifluoroacetyl)-AMC as substrate by two-step fluorogenic assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Nat Prod (2011) 74: 2031-2038 [PMID:21793558] |
| ChEMBL | Inhibition of recombinant human HDAC8 after 60 mins by fluorescence assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 7672-7680 [PMID:26331334] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2024) 269: 116324-116324 [PMID:38520762] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2023) 258: 115594-115594 [PMID:37429084] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) incubated for 1 hr by fluor de lys substrate based fluorescence method | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem (2015) 23: 6785-6793 [PMID:26481659] |
| ChEMBL | Inhibition of HDAC8 in human DU-145 cells assessed as increase in histone H3 acetylation after 24 hrs by immunofluorescence microscopy | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2022) 65: 3388-3403 [PMID:35133171] |
| histone deacetylase 9/Histone deacetylase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4145] [GtoPdb: 2620] [UniProtKB: Q9UKV0] | ||||||||
| ChEMBL | Inhibition of human HDAC9 | B | 5.96 | pKi | 1100 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of recombinant human HDAC9 enzyme using Ac-LeuGlyLys (tfa)-AMC as substrate after 15 to 30 mins | B | 5.96 | pKi | 1100 | nM | Ki | J Med Chem (2013) 56: 6512-6520 [PMID:23865683] |
| GtoPdb | - | - | 5.96 | pKi | 1100 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of recombinant human HDAC9 using Boc-L-Lys(epsilon-trifluoroacetyl)-AMC as substrate by two-step fluorogenic assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Nat Prod (2011) 74: 2031-2038 [PMID:21793558] |
| ChEMBL | Inhibition of recombinant human HDAC9 after 60 mins by fluorescence assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 7672-7680 [PMID:26331334] |
| ChEMBL | Inhibition of HDAC9 (unknown origin) | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of HDAC9 (unknown origin) | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2024) 269: 116324-116324 [PMID:38520762] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336] | ||||||||
| ChEMBL | Inhibition of full length wild type PI3Kalpha (unknown origin) | B | 4.24 | pIC50 | 57100 | nM | IC50 | Eur J Med Chem (2024) 265: 116109-116109 [PMID:38183777] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against synchronous ring-stage Plasmodium falciparum Dd2 infected in human erythrocytes assessed as parasitic growth inhibition measured after 48 hrs by [3H]hypoxanthine incorporation assay | F | 6.89 | pIC50 | 130 | nM | IC50 | Eur J Med Chem (2024) 277: 116782-116782 [PMID:39208744] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum infected in human erythrocytes preincubated for 48 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting assay | F | 7.05 | pIC50 | 90 | nM | IC50 | J Med Chem (2017) 60: 4780-4804 [PMID:28241112] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 48 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting method | F | 7.05 | pIC50 | 90 | nM | IC50 | Eur J Med Chem (2018) 158: 801-813 [PMID:30245402] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum Dd2 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 48 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting method | F | 7.05 | pIC50 | 90 | nM | IC50 | Eur J Med Chem (2018) 158: 801-813 [PMID:30245402] |
| ChEMBL | Antiplasmodial activity against synchronous ring-stage Plasmodium falciparum 3D7 infected in human erythrocytes assessed as parasitic growth inhibition measured after 48 hrs by [3H]hypoxanthine incorporation assay | F | 7.05 | pIC50 | 90 | nM | IC50 | Eur J Med Chem (2024) 277: 116782-116782 [PMID:39208744] |
| histone deacetylase 10/Polyamine deacetylase HDAC10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8] | ||||||||
| ChEMBL | Inhibition of recombinant human HDAC10 after 60 mins by fluorescence assay | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2015) 58: 7672-7680 [PMID:26331334] |
| ChEMBL | Inhibition of HDAC10 (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of HDAC10 (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2024) 269: 116324-116324 [PMID:38520762] |
| ChEMBL | Inhibition of HDAC10 (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2023) 258: 115594-115594 [PMID:37429084] |
| ChEMBL | Inhibition of HDAC10 (unknown origin) incubated for 30 mins in presence of BSA and DTT by fluorescence assay | B | 9.05 | pIC50 | 0.9 | nM | IC50 | ACS Med Chem Lett (2014) 5: 905-910 [PMID:25147612] |
| Protein Tat in Human immunodeficiency virus type 1 group M subtype B (isolate HXB2)(HIV-1) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4011] [UniProtKB: P04608] | ||||||||
| ChEMBL | Activation of Tat-mediated HIV1 transcription in J-Lat 10.6 cells harboring LTR driven GFP reporter co-expressing CMV driven RFP reporter assessed as LTR-driven gene expression incubated for 48 hr by FACSCalibur flow cytometry | B | 6.66 | pEC50 | 220 | nM | EC50 | J Med Chem (2019) 62: 5148-5175 [PMID:30973727] |
| p21 (RAC1) activated kinase 1/Serine/threonine-protein kinase PAK 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4600] [GtoPdb: 2133] [UniProtKB: Q13153] | ||||||||
| ChEMBL | Inhibition of PAK1 in estrogen-stimulated human MCF7 cells incubated for 48 hrs by immunoblot analysis | B | 9 | pIC50 | <1 | nM | IC50 | Eur J Med Chem (2017) 142: 229-243 [PMID:28814374] |
| p21 (RAC1) activated kinase 1/Serine/threonine-protein kinase PAK 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295682] [GtoPdb: 2133] [UniProtKB: O88643] | ||||||||
| ChEMBL | Inhibition of PAK1 in v-Ha-RAS-transformed mouse NIH/3T3 cells incubated for 48 hrs by immunoblot analysis | B | 9 | pIC50 | <1 | nM | IC50 | Eur J Med Chem (2017) 142: 229-243 [PMID:28814374] |
ChEMBL data shown on this page come from version 36:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
