nexturastat A [Ligand Id: 7504] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2179618 (Nexturastat A) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547] | ||||||||
| ChEMBL | Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate | B | 5.52 | pIC50 | 3020 | nM | IC50 | J Med Chem (2012) 55: 9891-9899 [PMID:23009203] |
| ChEMBL | Inhibition Assay: HDAC inhibition assays were performed by Reaction Biology Corp. (Malvern, Pa.) using isolated human, recombinant full-length HDAC1 and -6 from a baculovirus expression system in Sf9 cells. An acetylated fluorogenic peptide, RHKKAc, derived from residues 379-382 of p53 was used as substrate. The reaction buffer was made up of 50 mM Tris-HCl pH 8.0, 127 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1 mg/mL BSA, and a final concentration of 1% DMSO. Compounds were delivered in DMSO and delivered to enzyme mixture with preincubation of 5-10 min followed by substrate addition and incubation for 2 h at 30° C. Trichostatin A and developer were added to quench the reaction and generate fluorescence, respectively. Dose-response curves were generated starting at 30 μM compound with three-fold serial dilutions to generate a 10-dose plot. | B | 5.52 | pIC50 | 3020 | nM | IC50 | US-9409858-B2. Selective histone deactylase 6 inhibitors (2016) |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 5.52 | pIC50 | 3020 | nM | IC50 | Bioorg Med Chem Lett (2021) 47: 128207-128207 [PMID:34146703] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 5.52 | pIC50 | 3020 | nM | IC50 | Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 5.52 | pIC50 | 3020 | nM | IC50 | J Med Chem (2022) 65: 12140-12162 [PMID:36073117] |
| GtoPdb | - | - | 5.52 | pIC50 | 3002 | nM | IC50 | J Med Chem (2012) 55: 9891-9 [PMID:23009203] |
| ChEMBL | Inhibition of recombinant full length C-terminal His/FLAG tagged human HDAC1 (1 to 482 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins followed by substrate addition and further incubated for 2 hrs by fluorescence assay | B | 5.54 | pIC50 | 2860 | nM | IC50 | J Med Chem (2019) 62: 8557-8577 [PMID:31414801] |
| ChEMBL | Inhibition of human recombinant HDAC1 using ZMAL (Z-Lys(Ac)-AMC) fluorogenic substrate incubated for 90 mins by fluorescence based assay | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (2020) 63: 10339-10351 [PMID:32803970] |
| ChEMBL | Inhibition of recombinant human HDAC1 expressed in HEK293T/17 cells 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 | 6.44 | pIC50 | 360 | nM | IC50 | J Med Chem (2019) 62: 8557-8577 [PMID:31414801] |
| ChEMBL | Inhibition of human HDAC1 expressed in HEK293/T17 cells pre-incubated for 10 mins before Ac-GAK(Ac)-AM substrate addition and measured after 30 mins by fluorescence-based assay | B | 6.82 | pIC50 | 151 | nM | IC50 | J Med Chem (2020) 63: 10246-10262 [PMID:32815366] |
| 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 | 6.82 | pIC50 | 151 | nM | IC50 | J Med Chem (2021) 64: 4810-4840 [PMID:33830764] |
| ChEMBL | Inhibition of full length recombinant human HDAC1 expressed in baculovirus infected Sf9 insect cells using RHKKAc fluorogenic peptide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence assay | B | 8.29 | pIC50 | 5.1 | nM | IC50 | J Med Chem (2021) 64: 4810-4840 [PMID:33830764] |
| histone deacetylase 10/Histone deacetylase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8] | ||||||||
| ChEMBL | Inhibition of HDAC10 | B | 5.12 | pIC50 | 7570 | nM | IC50 | J Med Chem (2012) 55: 9891-9899 [PMID:23009203] |
| ChEMBL | Inhibition of HDAC10 (unknown origin) | B | 5.12 | pIC50 | 7570 | nM | IC50 | Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929] |
| 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 | 6.3 | pIC50 | 501.19 | nM | IC50 | J Med Chem (2019) 62: 4426-4443 [PMID:30964290] |
| ChEMBL | Inhibition of tubastatin-Alexa647-tracer binding to recombinant GST-tagged HDAC10 (unknown origin) measured after 1 hr by TR-FRET assay | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2019) 62: 4426-4443 [PMID:30964290] |
| histone deacetylase 11/Histone deacetylase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3310] [GtoPdb: 2615] [UniProtKB: Q96DB2] | ||||||||
| ChEMBL | Inhibition of recombinant human HDAC11 expressed in HEK293T/17 cells using Boc-Lys(TFA)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence-based assay | B | 4.97 | pIC50 | 10600 | nM | IC50 | J Med Chem (2019) 62: 8557-8577 [PMID:31414801] |
| ChEMBL | Inhibition of human HDAC11 expressed in HEK293/T17 cells pre-incubated for 10 mins before Boc-Lys(TFA)-AM substrate addition and measured after 30 mins by fluorescence-based assay | B | 4.97 | pIC50 | 10600 | nM | IC50 | J Med Chem (2020) 63: 10246-10262 [PMID:32815366] |
| ChEMBL | Inhibition of HDAC11 | B | 5.29 | pIC50 | 5140 | nM | IC50 | J Med Chem (2012) 55: 9891-9899 [PMID:23009203] |
| ChEMBL | Inhibition of HDAC11 (unknown origin) | B | 5.29 | pIC50 | 5140 | nM | IC50 | Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929] |
| 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] |
| histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769] | ||||||||
| 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 | 5.9 | pKi | 1250 | nM | Ki | Bioorg Med Chem (2019) 27: 115036-115036 [PMID:31431326] |
| ChEMBL | Inhibition of HDAC2 | B | 5.16 | pIC50 | 6920 | nM | IC50 | J Med Chem (2012) 55: 9891-9899 [PMID:23009203] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 5.16 | pIC50 | 6920 | nM | IC50 | Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 5.16 | pIC50 | 6920 | nM | IC50 | J Med Chem (2022) 65: 12140-12162 [PMID:36073117] |
| ChEMBL | Inhibition of human HDAC2 expressed in HEK293/T17 cells pre-incubated for 10 mins before Ac-GAK(Ac)-AM substrate addition and measured after 30 mins by fluorescence-based assay | B | 6.56 | pIC50 | 276 | nM | IC50 | J Med Chem (2020) 63: 10246-10262 [PMID:32815366] |
| histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379] | ||||||||
| ChEMBL | Inhibition of HDAC3 | B | 5.18 | pIC50 | 6680 | nM | IC50 | J Med Chem (2012) 55: 9891-9899 [PMID:23009203] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) | B | 5.18 | pIC50 | 6680 | nM | IC50 | Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) | B | 5.22 | pIC50 | 6080 | nM | IC50 | J Med Chem (2022) 65: 12140-12162 [PMID:36073117] |
| ChEMBL | Inhibition of human HDAC3 expressed in HEK293/T17 cells pre-incubated for 10 mins before Ac-GAK(Ac)-AM substrate addition and measured after 30 mins by fluorescence-based assay | B | 5.85 | pIC50 | 1420 | nM | IC50 | J Med Chem (2020) 63: 10246-10262 [PMID:32815366] |
| ChEMBL | Inhibition of full length human recombinant HDAC3 expressed in Sf9 baculovirus system using FAM-labeled acetylated peptide as substrate by measuring fluorescence intensity by EMSA method | B | 6.62 | pIC50 | 238 | nM | IC50 | J Med Chem (2022) 65: 3193-3217 [PMID:35119267] |
| histone deacetylase 4/Histone deacetylase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3524] [GtoPdb: 2659] [UniProtKB: P56524] | ||||||||
| ChEMBL | Inhibition of C-terminal His-tagged/N-terminal GST-tagged recombinant human HDAC4 (627 to 1084 residues) expressed in Baculovirus infected insect cells using Boc-Lys(TFa)-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 | 5.12 | pKi | 7570 | nM | Ki | Bioorg Med Chem (2019) 27: 115036-115036 [PMID:31431326] |
| ChEMBL | Inhibition of recombinant human HDAC4 expressed in HEK293T/17 cells using Boc-Lys(TFA)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence-based assay | B | 4.83 | pIC50 | 14800 | nM | IC50 | J Med Chem (2019) 62: 8557-8577 [PMID:31414801] |
| ChEMBL | Inhibition of human HDAC4 expressed in HEK293/T17 cells pre-incubated for 10 mins before Boc-Lys(TFA)-AM substrate addition and measured after 30 mins by fluorescence-based assay | B | 4.83 | pIC50 | 14800 | nM | IC50 | J Med Chem (2020) 63: 10246-10262 [PMID:32815366] |
| ChEMBL | Inhibition of HDAC4 | B | 5.03 | pIC50 | 9390 | nM | IC50 | J Med Chem (2012) 55: 9891-9899 [PMID:23009203] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) | B | 5.03 | pIC50 | 9390 | nM | IC50 | Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929] |
| histone deacetylase 5/Histone deacetylase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2563] [GtoPdb: 2660] [UniProtKB: Q9UQL6] | ||||||||
| ChEMBL | Inhibition of HDAC5 | B | 4.93 | pIC50 | 11700 | nM | IC50 | J Med Chem (2012) 55: 9891-9899 [PMID:23009203] |
| ChEMBL | Inhibition of HDAC5 (unknown origin) | B | 4.93 | pIC50 | 11700 | nM | IC50 | Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929] |
| ChEMBL | Inhibition of recombinant human HDAC5 expressed in HEK293T/17 cells using Boc-Lys(TFA)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence-based assay | B | 5.18 | pIC50 | 6620 | nM | IC50 | J Med Chem (2019) 62: 8557-8577 [PMID:31414801] |
| ChEMBL | Inhibition of human HDAC5 expressed in HEK293/T17 cells pre-incubated for 10 mins before Boc-Lys(TFA)-AM substrate addition and measured after 30 mins by fluorescence-based assay | B | 5.18 | pIC50 | 6620 | nM | IC50 | J Med Chem (2020) 63: 10246-10262 [PMID:32815366] |
| histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
| ChEMBL | Inhibition of N-terminal GST-tagged recombinant human HDAC6 (1 to 1215 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 | 7.52 | pKi | 30 | nM | Ki | Bioorg Med Chem (2019) 27: 115036-115036 [PMID:31431326] |
| ChEMBL | Inhibition of full length recombinant human HDAC6 expressed in baculovirus infected Sf9 insect cells using RHKKAc fluorogenic peptide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence assay | B | 5.66 | pIC50 | 2186 | nM | IC50 | J Med Chem (2021) 64: 4810-4840 [PMID:33830764] |
| ChEMBL | Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 with custom peptide substrate | B | 7.22 | pIC50 | 60.71 | nM | IC50 | HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators |
| ChEMBL | Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 with custom peptide substrate | B | 7.49 | pIC50 | 32.28 | nM | IC50 | HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators |
| ChEMBL | Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method | B | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (2019) 62: 10711-10739 [PMID:31710483] |
| ChEMBL | Inhibition of N-terminal GST-tagged full length human recombinant HDAC6 expressed in baculovirus infected Sf9 cells using ZMAL (Z-Lys(Ac)-AMC) fluorogenic substrate incubated for 90 mins by fluorescence based assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2021) 211: 113065-113065 [PMID:33360801] |
| ChEMBL | Inhibition of human recombinant HDAC6 using ZMAL (Z-Lys(Ac)-AMC) fluorogenic substrate incubated for 90 mins by fluorescence based assay | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2020) 63: 10339-10351 [PMID:32803970] |
| ChEMBL | Inhibition of full length human recombinant HDAC6 expressed in Sf9 baculovirus system using FAM-labeled acetylated peptide as substrate by measuring fluorescence intensity by EMSA method | B | 7.91 | pIC50 | 12.4 | nM | IC50 | J Med Chem (2022) 65: 3193-3217 [PMID:35119267] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) preincubated for 10 mins followed by Ac-Leu-GlyLys(Ac)-AMC substrate addition measured after 30 mins by fluorescence based assay | B | 8.28 | pIC50 | 5.2 | nM | IC50 | Bioorg Med Chem (2018) 26: 747-757 [PMID:29317150] |
| ChEMBL | Inhibition of human recombinant HDAC6 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate | B | 8.3 | pIC50 | 5.02 | nM | IC50 | J Med Chem (2012) 55: 9891-9899 [PMID:23009203] |
| ChEMBL | Inhibition Assay: HDAC inhibition assays were performed by Reaction Biology Corp. (Malvern, Pa.) using isolated human, recombinant full-length HDAC1 and -6 from a baculovirus expression system in Sf9 cells. An acetylated fluorogenic peptide, RHKKAc, derived from residues 379-382 of p53 was used as substrate. The reaction buffer was made up of 50 mM Tris-HCl pH 8.0, 127 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1 mg/mL BSA, and a final concentration of 1% DMSO. Compounds were delivered in DMSO and delivered to enzyme mixture with preincubation of 5-10 min followed by substrate addition and incubation for 2 h at 30° C. Trichostatin A and developer were added to quench the reaction and generate fluorescence, respectively. Dose-response curves were generated starting at 30 μM compound with three-fold serial dilutions to generate a 10-dose plot. | B | 8.3 | pIC50 | 5.02 | nM | IC50 | US-9409858-B2. Selective histone deactylase 6 inhibitors (2016) |
| GtoPdb | - | - | 8.3 | pIC50 | 5.02 | nM | IC50 | J Med Chem (2012) 55: 9891-9 [PMID:23009203] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2021) 47: 128207-128207 [PMID:34146703] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2022) 65: 12140-12162 [PMID:36073117] |
| ChEMBL | Inhibition of recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins followed by substrate addition and further incubated for 2 hrs by fluorescence assay | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2019) 62: 8557-8577 [PMID:31414801] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 8.3 | pIC50 | 5 | nM | IC50 | Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929] |
| ChEMBL | Inhibition of recombinant human HDAC6 expressed in HEK293T/17 cells 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 | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2019) 62: 8557-8577 [PMID:31414801] |
| ChEMBL | Inhibition of human N-terminal tagged human HDAC6 expressed in HEK293T/17 using Ac-Gly-Ala-[Ac-Lys]-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 15 mins by fluorescence assay | B | 8.42 | pIC50 | 3.8 | nM | IC50 | J Med Chem (2019) 62: 7042-7057 [PMID:31271281] |
| ChEMBL | Inhibition of recombinant human HDAC6 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 | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2021) 64: 4810-4840 [PMID:33830764] |
| ChEMBL | Inhibition of human HDAC6 expressed in HEK293/T17 cells using pre-incubated for 10 mins before Ac-GAK(Ac)-AM substrate addition and measured after 30 mins by fluorescence-based assay | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2020) 63: 10246-10262 [PMID:32815366] |
| GtoPdb | - | - | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2020) 63: 10246-10262 [PMID:32815366] |
| histone deacetylase 7/Histone deacetylase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2716] [GtoPdb: 2661] [UniProtKB: Q8WUI4] | ||||||||
| ChEMBL | Inhibition of HDAC7 | B | 5.35 | pIC50 | 4460 | nM | IC50 | J Med Chem (2012) 55: 9891-9899 [PMID:23009203] |
| ChEMBL | Inhibition of HDAC7 (unknown origin) | B | 5.35 | pIC50 | 4460 | nM | IC50 | Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929] |
| ChEMBL | Inhibition of recombinant human HDAC7 expressed in HEK293T/17 cells using Boc-Lys(TFA)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence-based assay | B | 5.61 | pIC50 | 2430 | nM | IC50 | J Med Chem (2019) 62: 8557-8577 [PMID:31414801] |
| ChEMBL | Inhibition of human HDAC7 expressed in HEK293/T17 cells pre-incubated for 10 mins before Boc-Lys(TFA)-AM substrate addition and measured after 30 mins by fluorescence-based assay | B | 5.61 | pIC50 | 2430 | nM | IC50 | J Med Chem (2020) 63: 10246-10262 [PMID:32815366] |
| histone deacetylase 8/Histone deacetylase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41] | ||||||||
| ChEMBL | Inhibition of C-terminal His-fusion tagged/N-terminal Strep-2 tagged recombinant human HDAC8 (1 to 377 residues) expressed in insect cells using Boc-Lys(TFa)-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 | 4.89 | pKi | 12800 | nM | Ki | Bioorg Med Chem (2019) 27: 115036-115036 [PMID:31431326] |
| ChEMBL | Inhibition of recombinant human HDAC8 expressed in HEK293T/17 cells using Boc-Lys(TFA)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence-based assay | B | 5.81 | pIC50 | 1540 | nM | IC50 | J Med Chem (2019) 62: 8557-8577 [PMID:31414801] |
| ChEMBL | Inhibition of full length human recombinant HDAC8 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 human HDAC8 expressed in HEK293/T17 cells pre-incubated for 10 mins before Boc-Lys(TFA)-AM substrate addition and measured after 30 mins by fluorescence-based assay | B | 6.01 | pIC50 | 988 | nM | IC50 | J Med Chem (2020) 63: 10246-10262 [PMID:32815366] |
| ChEMBL | Inhibition of recombinant human HDAC8 using Boc-Lys(TFA)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence-based assay | B | 6.01 | pIC50 | 988 | nM | IC50 | J Med Chem (2021) 64: 4810-4840 [PMID:33830764] |
| ChEMBL | Inhibition of HDAC8 | B | 6.02 | pIC50 | 954 | nM | IC50 | J Med Chem (2012) 55: 9891-9899 [PMID:23009203] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) | B | 6.02 | pIC50 | 954 | nM | IC50 | Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929] |
| histone deacetylase 9/Histone deacetylase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4145] [GtoPdb: 2620] [UniProtKB: Q9UKV0] | ||||||||
| ChEMBL | Inhibition of HDAC9 | B | 5.17 | pIC50 | 6720 | nM | IC50 | J Med Chem (2012) 55: 9891-9899 [PMID:23009203] |
| ChEMBL | Inhibition of HDAC9 (unknown origin) | B | 5.17 | pIC50 | 6720 | nM | IC50 | Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929] |
| ChEMBL | Inhibition of recombinant human HDAC9 expressed in HEK293T/17 cells using Boc-Lys(TFA)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence-based assay | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (2019) 62: 8557-8577 [PMID:31414801] |
| ChEMBL | Inhibition of human HDAC9 expressed in HEK293/T17 cells pre-incubated for 10 mins before Boc-Lys(TFA)-AM substrate addition and measured after 30 mins by fluorescence-based assay | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (2020) 63: 10246-10262 [PMID:32815366] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
