Page last updated: 2024-08-05 15:24:31

EC 2.3.1.48 (histone acetyltransferase) inhibitor

An EC 2.3.1.* (acyltransferase transferring other than amino-acyl group) inhibitor that interferes with the function of histone acetyltransferase (EC 2.3.1.48).

ChEBI ID: 76395

Members (5)

MemberDefinitionClass
anacardic acidA hydroxybenzoic acid that is salicylic acid substituted by a pentadecyl group at position 6. It is a major component of cashew nut shell liquid and exhibits an extensive range of bioactivities.anacardic acid
cyclopentylidene-[4-(4-chlorophenyl)thiazol-2-yl]hydrazoneA member of the class of 1,3-thiazole bearing 2-cyclopentylidenehydrazino and 4-chlorophenyl substituents at positions 2 and 4 respectively.cyclopentylidene-[4-(4-chlorophenyl)thiazol-2-yl]hydrazone
hydrazinocurcuminA pyrazole obtained by cyclocodensation of the two carbonyl groups of curcumin with hydrazine.hydrazinocurcumin
pentamidineA diether consisting of pentane-1,5-diol in which both hydroxyl hydrogens have been replaced by 4-amidinophenyl groups. A trypanocidal drug that is used for treatment of cutaneous leishmaniasis and Chagas disease.pentamidine
procyanidin b3A proanthocyanidin consisting of two molecules of (+)-catechin joined by a bond between positions 4 and 8' in alpha-configuration. It can be found in red wine, in barley, in beer, in peach or in Jatropha macrantha, the Huanarpo Macho.procyanidin B3

Research

Studies (2,514)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-1990526 (20.92)18.7374
1990's840 (33.41)18.2507
2000's424 (16.87)29.6817
2010's573 (22.79)24.3611
2020's151 (6.01)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials137 (5.13%)5.53%
Reviews222 (8.31%)6.00%
Case Studies352 (13.17%)4.05%
Observational1 (0.04%)0.25%
Other1,960 (73.35%)84.16%

Protein Targets (85)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
EWS/FLI fusion proteinHomo sapiens (human)Potency11.190644
Interferon betaHomo sapiens (human)Potency20.821213
PPM1D proteinHomo sapiens (human)Potency20.821212

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
10 kDa chaperonin Escherichia coliIC50175.000022
10 kDa heat shock protein, mitochondrialHomo sapiens (human)IC50175.000022
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC501.639011
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.468011
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC503.278011
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki1.717011
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC503.278011
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki1.717011
60 kDa chaperonin Escherichia coliIC50175.000022
60 kDa heat shock protein, mitochondrialHomo sapiens (human)IC50175.000022
AcrosinSus scrofa (pig)Ki2.300011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC502.214011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki2.196011
Alpha-2A adrenergic receptorHomo sapiens (human)IC501.375011
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.516011
Alpha-synucleinHomo sapiens (human)IC50126.800011
Amiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)Ki0.290011
Amine oxidase [flavin-containing] AHomo sapiens (human)IC505.065823
Amine oxidase [flavin-containing] BHomo sapiens (human)IC500.262512
Amyloid-beta precursor proteinHomo sapiens (human)IC506.292033
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC5015.721511
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki12.880211
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000011
Aurora kinase BHomo sapiens (human)IC50100.000011
Bile salt export pumpHomo sapiens (human)IC50422.666733
Calcium/calmodulin-dependent protein kinase type II subunit alphaHomo sapiens (human)IC503.645044
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000011
Coagulation factor XHomo sapiens (human)IC5010.400011
Cytochrome P450 1A2Homo sapiens (human)IC5075.000033
Cytochrome P450 2C19Homo sapiens (human)IC5075.000033
Cytochrome P450 2C9 Homo sapiens (human)IC5075.000033
Cytochrome P450 2D6Homo sapiens (human)IC5019.866733
Cytochrome P450 3A4Homo sapiens (human)IC5075.000033
D(3) dopamine receptorHomo sapiens (human)IC503.998011
D(3) dopamine receptorHomo sapiens (human)Ki1.358011
Diamine acetyltransferase 1Homo sapiens (human)Ki2.000011
Glutamate receptor ionotropic, NMDA 1Homo sapiens (human)IC500.720011
Glutamate receptor ionotropic, NMDA 2AHomo sapiens (human)IC500.720011
Glyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)IC5050.000011
Histone acetyltransferase KAT2BHomo sapiens (human)IC5019.450044
Histone acetyltransferase KAT5Homo sapiens (human)IC5064.000011
Histone acetyltransferase KAT8Homo sapiens (human)IC5043.000011
Histone acetyltransferase KAT8Homo sapiens (human)Ki64.000011
Histone acetyltransferase p300Homo sapiens (human)IC507.412544
Matrix metalloproteinase-9Homo sapiens (human)IC5019.400011
Microtubule-associated protein tauHomo sapiens (human)IC5034.000011
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC501.703333
Multidrug and toxin extrusion protein 2Homo sapiens (human)IC506.550022
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000011
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC501.425011
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.507011
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC501.580011
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.220011
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC502.885011
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki2.073011
Nuclear factor NF-kappa-B p100 subunit Homo sapiens (human)IC5029.800011
Nuclear factor NF-kappa-B p105 subunitHomo sapiens (human)IC5029.800011
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)IC5015.721511
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)Ki12.880211
PlasminogenHomo sapiens (human)IC5028.400035
Polyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)IC500.161855
Polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)IC507.300011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC5015.805444
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki12.880211
Probable linoleate 9S-lipoxygenase 5Solanum tuberosum (potato)IC5043.000011
Prostaglandin G/H synthase 2Homo sapiens (human)IC509.700011
Protein arginine N-methyltransferase 1Homo sapiens (human)IC5081.000022
Protein arginine N-methyltransferase 5Homo sapiens (human)IC50582.000011
Protein S100-BHomo sapiens (human)IC50100.000011
Protein tyrosine phosphatase type IVA 1Homo sapiens (human)IC500.300011
Protein tyrosine phosphatase type IVA 2Homo sapiens (human)IC500.300011
Protein tyrosine phosphatase type IVA 3Homo sapiens (human)IC5035.833333
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC508.920022
Seed linoleate 13S-lipoxygenase-1Glycine max (soybean)IC5051.900011
Signal transducer and activator of transcription 3Homo sapiens (human)IC5016.200011
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC509.700011
Sodium-dependent dopamine transporter Homo sapiens (human)IC503.159011
Sodium-dependent dopamine transporter Homo sapiens (human)Ki2.510011
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC502.214011
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki2.196011
Solute carrier family 22 member 1 Homo sapiens (human)IC5022.100011
Solute carrier family 22 member 2Homo sapiens (human)IC501.200011
Solute carrier family 22 member 3Homo sapiens (human)IC509.500011
Sucrase-isomaltase, intestinalRattus norvegicus (Norway rat)IC50430.000011
SUMO-activating enzyme subunit 1Homo sapiens (human)IC502.200011
Suppressor of tumorigenicity 14 proteinHomo sapiens (human)Ki1.160011
Transcription factor p65Homo sapiens (human)IC5029.800011
Trypsin-1Homo sapiens (human)IC5043.333313
Urokinase-type plasminogen activatorHomo sapiens (human)IC5043.333313

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Peroxisome proliferator-activated receptor alphaHomo sapiens (human)EC503.500011
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)EC5017.000011
Protein kinase C delta typeHomo sapiens (human)EC5014.970011
Protein kinase C epsilon typeHomo sapiens (human)EC5018.810011
Protein kinase C theta typeHomo sapiens (human)EC507.250011
Protein S100-BHomo sapiens (human)Kd1.000011
Protein S100-BRattus norvegicus (Norway rat)Kd47.000022
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2EC503.980011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Amyloid-beta precursor proteinHomo sapiens (human)DC501.470011
Histone acetyltransferase KAT8Homo sapiens (human)K0.5205.000033
Histone acetyltransferase KAT8Homo sapiens (human)Km1.766733
Histone acetyltransferase p300Homo sapiens (human)INH8.500011
Microtubule-associated protein tauHomo sapiens (human)DC5017.000011
Peroxisome proliferator-activated receptor deltaHomo sapiens (human)Emax68.000011
Plasma kallikreinHomo sapiens (human)K0.5514.000011