Roles > EC 2.1.1.6 (catechol O-methyltransferase) inhibitor
Page last updated: 2024-08-05 15:45:06

EC 2.1.1.6 (catechol O-methyltransferase) inhibitor

An EC 2.1.1.* (methyltransferase) inhibitor that interferes with the action of catechol O-methyltransferase (EC 2.1.1.6).

ChEBI ID: 48406

Members (2)

MemberDefinitionClass
entacaponeA monocarboxylic acid amide that is N,N-diethylprop-2-enamide in which the hydrogen at position 2 is substituted by a cyano group and the hydrogen at the 3E position is substituted by a 3,4-dihydroxy-5-nitrophenyl group.entacapone
tolcaponeBenzophenone substituted on one of the phenyl rings at C-3 and C-4 by hydroxy groups and at C-5 by a nitro group, and on the other phenyl ring by a methyl group at C-4. It is an inhibitor of catechol O-methyltransferase.tolcapone

Research

Studies (745)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19900 (0.00)18.7374
1990's192 (25.77)18.2507
2000's250 (33.56)29.6817
2010's213 (28.59)24.3611
2020's90 (12.08)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials194 (21.18%)5.53%
Reviews154 (16.81%)6.00%
Case Studies35 (3.82%)4.05%
Observational2 (0.22%)0.25%
Other531 (57.97%)84.16%

Protein Targets (67)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
AR proteinHomo sapiens (human)Potency25.3720817
aryl hydrocarbon receptorHomo sapiens (human)Potency14.960111
Ataxin-2Homo sapiens (human)Potency25.360212
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency17.782811
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency23.864623
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency48.557711
caspase-3Homo sapiens (human)Potency48.557711
Cellular tumor antigen p53Homo sapiens (human)Potency36.699124
cytochrome P450 2C9, partialHomo sapiens (human)Potency2.769312
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency9.771711
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency49.219412
DNA polymerase kappa isoform 1Homo sapiens (human)Potency6.701611
estrogen nuclear receptor alphaHomo sapiens (human)Potency32.4732919
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency14.315824
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency31.1887615
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency7.079511
EWS/FLI fusion proteinHomo sapiens (human)Potency36.209344
farnesoid X nuclear receptorHomo sapiens (human)Potency19.165824
GVesicular stomatitis virusPotency2.769312
GLI family zinc finger 3Homo sapiens (human)Potency29.656424
GLS proteinHomo sapiens (human)Potency31.622811
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency31.786124
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency36.031112
heat shock protein beta-1Homo sapiens (human)Potency20.780022
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency35.481311
histone deacetylase 9 isoform 3Homo sapiens (human)Potency25.156622
Histone H2A.xCricetulus griseus (Chinese hamster)Potency64.019226
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency100.000011
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency2.769312
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency18.910123
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency2.769314
Interferon betaHomo sapiens (human)Potency18.754125
lamin isoform A-delta10Homo sapiens (human)Potency0.044711
LuciferasePhotinus pyralis (common eastern firefly)Potency43.376323
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency20.223225
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency35.125938
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency16.672634
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency10.638424
phosphopantetheinyl transferaseBacillus subtilisPotency25.118911
PPM1D proteinHomo sapiens (human)Potency29.410712
pregnane X nuclear receptorHomo sapiens (human)Potency30.398812
progesterone receptorHomo sapiens (human)Potency21.520612
RAR-related orphan receptor gammaMus musculus (house mouse)Potency26.094526
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency32.277433
retinoid X nuclear receptor alphaHomo sapiens (human)Potency15.619224
SMAD family member 2Homo sapiens (human)Potency15.564726
SMAD family member 3Homo sapiens (human)Potency15.564726
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency25.118911
TDP1 proteinHomo sapiens (human)Potency31.676822
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency37.679326
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency2.702225
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency50.118711
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency36.031112

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Adenosine receptor A2aHomo sapiens (human)IC501.625012
Alpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)IC503.000011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC5060.050012
Bile salt export pumpHomo sapiens (human)IC5056.044045
Bile salt export pumpRattus norvegicus (Norway rat)IC5047.200011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000011
Catechol O-methyltransferaseHomo sapiens (human)IC500.115045
Catechol O-methyltransferaseRattus norvegicus (Norway rat)IC500.870634
Genome polyproteinDengue virus 2 Thailand/16681/84IC500.640055
Krueppel-like factor 10Homo sapiens (human)IC5050.000022
Multidrug resistance-associated protein 4Homo sapiens (human)IC5011.750012
TransthyretinHomo sapiens (human)IC5016.600022

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Genome polyproteinDengue virus 2 Thailand/16681/84EC507.100011
TransthyretinHomo sapiens (human)Kd0.203366

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
UDP-glucuronosyltransferase 1A9Homo sapiens (human)Km38.000012
UDP-glucuronosyltransferase 2B15Homo sapiens (human)Km375.500012