Roles > phosphodiesterase IV inhibitor
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phosphodiesterase IV inhibitor

An EC 3.1.4.53 (3',5'-cyclic-AMP phosphodiesterase) inhibitor that specifically blocks the action of phosphodiesterase IV.

ChEBI ID: 68844

Members (5)

MemberDefinitionClass
an2728A member of the class of benzoxaboroles that is 5-hydroxy-1,3-dihydro-2,1-benzoxaborole in which the phenolic hydrogen has been replaced by a 4-cyanophenyl group. A phosphodiesterase 4 inhibitor that is used for treatment of mild to moderate atopic dermatitis in children and adults.crisaborole
apremilastA member of the class of isoindoles that is isoindole-1,3-dione substituted at position 4 by an acetamido group and at position 1 by a 1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl group. Used for treatment of psoriatic arthritis.apremilast
etazolateA pyrazolopyridine that is 1H-pyrazolo[3,4-b]pyridine which is substituted at positions 1, 4, and 5 by ethyl, 2-isopropylidenehydrazino, and ethoxycarbonyl groups, respectively. A phosphodiesterase IV inhibitor with antidepressant and anxiolytic properties.etazolate
roflumilastA benzamide obtained by formal condensation of the carboxy group of 3-(cyclopropylmethoxy)-4-(difluoromethoxy)benzoic acid with the amino group of 3,5-dichloropyridin-4-amine. Used for treatment of bronchial asthma and chronic obstructive pulmonary disease.roflumilast
rp 73401A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of 3-(cyclopentyloxy)-4-methoxybenzoic acid with the primary amino group of 3,5-dichloropyridin-4-amine.piclamilast

Research

Studies (1,385)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199053 (3.83)18.7374
1990's25 (1.81)18.2507
2000's144 (10.40)29.6817
2010's673 (48.59)24.3611
2020's490 (35.38)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials209 (14.05%)5.53%
Reviews286 (19.22%)6.00%
Case Studies108 (7.26%)4.05%
Observational21 (1.41%)0.25%
Other864 (58.06%)84.16%

Protein Targets (99)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency28.183811
arylsulfatase AHomo sapiens (human)Potency4.256211
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency35.481311
Chain A, CruzipainTrypanosoma cruziPotency39.810711
Chain A, HADH2 proteinHomo sapiens (human)Potency27.867523
Chain B, HADH2 proteinHomo sapiens (human)Potency27.867523
CREB-binding proteinHomo sapiens (human)Potency5.441533
cytochrome P450 2C19 precursorHomo sapiens (human)Potency10.000011
cytochrome P450 2C9 precursorHomo sapiens (human)Potency31.622811
cytochrome P450 2C9, partialHomo sapiens (human)Potency6.741211
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency14.219124
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency1.509211
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency29.934911
EWS/FLI fusion proteinHomo sapiens (human)Potency23.324745
Fumarate hydrataseHomo sapiens (human)Potency37.221211
GVesicular stomatitis virusPotency6.741211
GABA theta subunitRattus norvegicus (Norway rat)Potency14.219112
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency14.219112
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency14.219112
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency14.219112
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency14.219112
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency14.219112
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency14.219112
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency14.219112
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency14.219112
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency14.219112
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency14.219112
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency14.219112
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency14.219112
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency14.219112
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency14.219112
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency14.219112
GLS proteinHomo sapiens (human)Potency10.000011
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency31.622813
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency6.741211
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency6.741212
Interferon betaHomo sapiens (human)Potency6.741211
mitogen-activated protein kinase 1Homo sapiens (human)Potency18.854112
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency7.943311
polyproteinZika virusPotency37.221211
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.810711
TDP1 proteinHomo sapiens (human)Potency26.608611
thioredoxin reductaseRattus norvegicus (Norway rat)Potency16.001422

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
3',5'-cyclic-AMP phosphodiesterase Sus scrofa (pig)IC500.001011
Adenosine receptor A1Homo sapiens (human)IC501.000011
Adenosine receptor A2aHomo sapiens (human)IC501.000011
Adenosine receptor A2bHomo sapiens (human)IC501.000011
Beta-2 adrenergic receptorCavia porcellus (domestic guinea pig)IC500.001011
Beta-lactamase Klebsiella pneumoniaeIC500.670011
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)IC502,803.050022
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)Ki60.000011
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)IC50929.0429221
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)Ki60.000011
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)IC5071,000.000011
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)Ki60.000011
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)IC504,724.2810221
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)IC500.04692731
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)Ki0.001166
cAMP-specific 3',5'-cyclic phosphodiesterase 4ARattus norvegicus (Norway rat)Ki0.026011
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC5019.79285785
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)Ki0.001077
cAMP-specific 3',5'-cyclic phosphodiesterase 4BRattus norvegicus (Norway rat)Ki0.026011
cAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)IC500.05062529
cAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)Ki0.001166
cAMP-specific 3',5'-cyclic phosphodiesterase 4CRattus norvegicus (Norway rat)Ki0.026011
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC5022.10834373
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)Ki0.001166
cAMP-specific 3',5'-cyclic phosphodiesterase 4D Rattus norvegicus (Norway rat)Ki0.026011
cAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)IC5080.4951120
Carboxylic ester hydrolase Rattus norvegicus (Norway rat)IC5010.000011
cGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC50249.5191221
cGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)IC5021,368.800033
cGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)Ki12.000011
cGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)IC502,746.1955322
cGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)Ki12.000011
cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC502,748.0906221
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC500.0006129
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC500.0019122
Chain A, cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC500.000418
Chain B, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC500.000414
Cytochrome P450 1A2Homo sapiens (human)IC5010.000011
Cytochrome P450 2C19Homo sapiens (human)IC5010.000011
Cytochrome P450 2C9 Homo sapiens (human)IC5010.000011
Cytochrome P450 2D6Homo sapiens (human)IC5010.000011
Cytochrome P450 3A4Homo sapiens (human)IC5010.000011
Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)IC5080.4951120
Endothelin-1 receptorSus scrofa (pig)IC500.001011
High affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7AHomo sapiens (human)IC501,015.365022
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)IC5080.4951120
Phosphodiesterase Trypanosoma bruceiKi3.162311
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)IC500.500222
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