Page last updated: 2024-08-05 15:18:30

EC 3.5.4.4 (adenosine deaminase) inhibitor

An EC 3.5.4.* (non-peptide cyclic amidine C-N hydrolase) inhibitor that interferes with the action of adenosine deaminase (EC 3.5.4.4).

ChEBI ID: 50445

Members (6)

MemberDefinitionClass
(2R,3S)-EHNA hydrochlorideA hydrochloride salt obtained by reaction of (2R,3S)-EHNA with one equivalent of hydrochloric acid. Selective inhibitor of cGMP-stimulated phosphodiesterase (PDE2) (IC50 = 0.8 - 4 mM). Also a potent inhibitor of adenosine deaminase.(2R,3S)-EHNA hydrochloride
9-(2-hydroxy-3-nonyl)adenineEHNA of absolute configuration 2R,3S. Selective inhibitor of cGMP-stimulated phosphodiesterase (PDE2) (IC50 = 0.8 - 4 mM). Also a potent inhibitor of adenosine deaminase.(2R,3S)-EHNA
coformycinAn N-glycosyl in which (8R)-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol is attached to ribofuranose via a beta-N(3)-glycosidic bond. compound The parent of the class of coformycins.coformycin
dideoxyadenosineA purine 2',3'-dideoxyribonucleoside in which the nucleobase component is specified as adenine.2',3'-dideoxyadenosine
dipyridamoleA pyrimidopyrimidine that is 2,2',2'',2'''-(pyrimido[5,4-d]pyrimidine-2,6-diyldinitrilo)tetraethanol substituted by piperidin-1-yl groups at positions 4 and 8 respectively. A vasodilator agent, it inhibits the formation of blood clots.dipyridamole
pentostatinA member of the class of coformycins that is coformycin in which the hydroxy group at position 2' is replaced with a hydrogen. It is a drug used for the treatment of hairy cell leukaemia.pentostatin

Research

Studies (8,753)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19903,835 (43.81)18.7374
1990's2,497 (28.53)18.2507
2000's1,513 (17.29)29.6817
2010's750 (8.57)24.3611
2020's158 (1.81)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials994 (10.16%)5.53%
Reviews949 (9.70%)6.00%
Case Studies605 (6.18%)4.05%
Observational11 (0.11%)0.25%
Other7,229 (73.86%)84.16%

Protein Targets (191)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency27.594215
15-lipoxygenase, partialHomo sapiens (human)Potency12.589311
67.9K proteinVaccinia virusPotency16.989323
acetylcholinesteraseHomo sapiens (human)Potency43.648611
acid sphingomyelinaseHomo sapiens (human)Potency25.118911
activating transcription factor 6Homo sapiens (human)Potency15.603422
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency28.354019
Alpha-synucleinHomo sapiens (human)Potency3.548111
AR proteinHomo sapiens (human)Potency24.94371012
ATAD5 protein, partialHomo sapiens (human)Potency9.924423
Ataxin-2Homo sapiens (human)Potency29.595722
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency23.710111
Bloom syndrome protein isoform 1Homo sapiens (human)Potency17.039024
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency79.432811
caspase-1 isoform alpha precursorHomo sapiens (human)Potency4.496512
Caspase-7Homo sapiens (human)Potency3.981112
Cellular tumor antigen p53Homo sapiens (human)Potency21.131722
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency23.110316
Chain A, Beta-lactamaseEscherichia coli K-12Potency15.848911
Chain A, Breast cancer type 1 susceptibility proteinHomo sapiens (human)Potency27.829812
Chain A, Ferritin light chainEquus caballus (horse)Potency19.356923
Chain A, HADH2 proteinHomo sapiens (human)Potency23.110313
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency28.796822
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency28.244713
Chain B, HADH2 proteinHomo sapiens (human)Potency23.110313
chromobox protein homolog 1Homo sapiens (human)Potency70.504123
cytochrome P450 2C19 precursorHomo sapiens (human)Potency2.620012
cytochrome P450 2C9 precursorHomo sapiens (human)Potency6.477612
cytochrome P450 2C9, partialHomo sapiens (human)Potency2.454511
cytochrome P450 2D6Homo sapiens (human)Potency4.897511
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency11.294712
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency19.936926
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency8.709011
D(1A) dopamine receptorHomo sapiens (human)Potency8.043133
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency7.943312
DNA dC->dU-editing enzyme APOBEC-3F isoform aHomo sapiens (human)Potency22.387211
DNA polymerase III, partialBacillus subtilisPotency29.934911
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency79.432811
endonuclease IVEscherichia coliPotency7.943311
estrogen nuclear receptor alphaHomo sapiens (human)Potency22.6428810
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency25.156622
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency16.65261012
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency13.284516
EWS/FLI fusion proteinHomo sapiens (human)Potency24.995744
eyes absent homolog 2 isoform aHomo sapiens (human)Potency125.892011
farnesoid X nuclear receptorHomo sapiens (human)Potency18.047433
Fumarate hydrataseHomo sapiens (human)Potency37.221211
GVesicular stomatitis virusPotency2.454511
GABA theta subunitRattus norvegicus (Norway rat)Potency19.936913
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency19.936913
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency19.936913
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency19.936913
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency19.936913
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency19.936913
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency19.936913
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency19.936913
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency19.936913
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency19.936913
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency19.936913
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency19.936913
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency19.936913
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency19.936913
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency19.936913
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency19.936913
gemininHomo sapiens (human)Potency8.7293311
GLI family zinc finger 3Homo sapiens (human)Potency1.804622
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency20.154822
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency27.218812
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency34.451812
guanine nucleotide-binding protein G(i) subunit alpha-1 isoform 1Homo sapiens (human)Potency10.000011
heat shock protein beta-1Homo sapiens (human)Potency19.966622
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency9.846328
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency18.604913
Histone H2A.xCricetulus griseus (Chinese hamster)Potency27.663811
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency17.559412
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency2.454511
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency13.806222
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency25.118922
IDH1Homo sapiens (human)Potency11.215912
importin subunit beta-1 isoform 1Homo sapiens (human)Potency34.451812
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency2.454512
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency19.702012
Interferon betaHomo sapiens (human)Potency2.454511
isocitrate dehydrogenase 1, partialHomo sapiens (human)Potency44.668411
lamin isoform A-delta10Homo sapiens (human)Potency11.568814
lethal factor (plasmid)Bacillus anthracis str. A2012Potency14.597714
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency11.220222
Microtubule-associated protein tauHomo sapiens (human)Potency7.996017
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency15.848911
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency39.810711
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency11.220211
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Potency11.220211
neuropeptide S receptor isoform AHomo sapiens (human)Potency10.496133
NFKB1 protein, partialHomo sapiens (human)Potency11.220222
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency15.848911
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency17.281633
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency23.109311
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency21.313811
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency1.412511
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency24.709822
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency25.394312
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency13.975422
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency42.561511
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency18.623422
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency14.820033
polyproteinZika virusPotency37.221211
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency19.952611
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency31.622811
pregnane X nuclear receptorHomo sapiens (human)Potency20.335012
progesterone receptorHomo sapiens (human)Potency28.226222
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency89.716422
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency84.218022
RAR-related orphan receptor gammaMus musculus (house mouse)Potency47.960323
regulator of G-protein signaling 4Homo sapiens (human)Potency10.039612
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency26.603211
retinoid X nuclear receptor alphaHomo sapiens (human)Potency32.991122
RGS12Homo sapiens (human)Potency10.000011
serine-protein kinase ATM isoform aHomo sapiens (human)Potency31.622811
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency11.917311
Single-stranded DNA cytosine deaminaseHomo sapiens (human)Potency79.432813
SMAD family member 2Homo sapiens (human)Potency15.576433
SMAD family member 3Homo sapiens (human)Potency15.576433
Smad3Homo sapiens (human)Potency8.912511
snurportin-1Homo sapiens (human)Potency34.451812
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency31.622811
survival motor neuron protein isoform dHomo sapiens (human)Potency15.387814
TAR DNA-binding protein 43Homo sapiens (human)Potency17.488212
TDP1 proteinHomo sapiens (human)Potency17.1319221
thioredoxin reductaseRattus norvegicus (Norway rat)Potency36.953522
ThrombopoietinHomo sapiens (human)Potency10.000022
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency24.655822
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency33.997222
thyroid stimulating hormone receptorHomo sapiens (human)Potency21.245234
thyrotropin-releasing hormone receptorHomo sapiens (human)Potency11.987711
tumor susceptibility gene 101 proteinHomo sapiens (human)Potency35.398133
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency10.449034
USP1 protein, partialHomo sapiens (human)Potency34.607024
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency11.985611
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency20.063022
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency27.218812

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
3',5'-cyclic-AMP phosphodiesterase Sus scrofa (pig)IC505.835022
90-kda heat shock protein beta HSP90 beta, partialHomo sapiens (human)IC5021.068211
Adenosine deaminaseHomo sapiens (human)Ki0.02911118
Adenosine deaminase Bos taurus (cattle)Ki90,920.0030811
Adenosine deaminase Plasmodium falciparum (malaria parasite P. falciparum)Ki0.001835
Adenosine receptor A1Rattus norvegicus (Norway rat)Ki0.455011
AMP deaminase 3Homo sapiens (human)Ki3.000011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000011
ATP-dependent translocase ABCB1Homo sapiens (human)IC5026.900033
Bile salt export pumpHomo sapiens (human)IC5068.500012
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC506.400011
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)IC5072.500022
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)Ki200.000011
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)IC5072.500022
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)Ki200.000011
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)IC5072.500022
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)Ki200.000011
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)Ki1.000011
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)IC500.500011
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)Ki200.000011
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC500.500011
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)Ki200.000011
cAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)IC500.500011
cAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)Ki200.000011
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC502.100024
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)Ki200.000011
cAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)Ki0.600011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000011
cGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC502.5975810
cGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)Ki1.900022
cGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)IC5012.725024
cGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)Ki200.000011
cGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)IC5043.000011
cGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)Ki200.000011
cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC501.970846
cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)Ki200.000011
Cone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha'Homo sapiens (human)Ki0.125011
Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)Ki0.400011
Equilibrative nucleoside transporter 1Homo sapiens (human)IC500.053733
Equilibrative nucleoside transporter 1Homo sapiens (human)Ki0.008433
Exopolyphosphatase PRUNE1Homo sapiens (human)IC500.780011
heat shock protein HSP 90-alpha isoform 2Homo sapiens (human)IC5021.068211
High affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7AHomo sapiens (human)Ki0.600011
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)IC502.633313
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC5026.000011
Multidrug and toxin extrusion protein 2Homo sapiens (human)IC5074.000011
Multidrug resistance-associated protein 4Homo sapiens (human)IC505.150022
Multidrug resistance-associated protein 5Homo sapiens (human)IC5030.000011
Phosphodiesterase Sus scrofa (pig)IC5072.000022
Polyunsaturated fatty acid lipoxygenase ALOX15Oryctolagus cuniculus (rabbit)IC506.956011
Retinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)Ki0.125011
Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit deltaHomo sapiens (human)Ki0.125011
Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)Ki0.125011
Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alphaHomo sapiens (human)Ki0.125011
Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit betaHomo sapiens (human)Ki0.125011
Solute carrier family 22 member 1 Homo sapiens (human)IC5081.000011
Solute carrier family 22 member 2Homo sapiens (human)IC502.600011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
NPYLR7BAedes aegypti (yellow fever mosquito)EC502.760012

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Adenosine deaminase Bos taurus (cattle)Km45.000011
Deoxycytidine kinaseHomo sapiens (human)Km220.000011
kelch-like ECH-associated protein 1Homo sapiens (human)AC504.030011
kelch-like ECH-associated protein 1Homo sapiens (human)Max_Activity_Concentration_uM 50.000011
LANAHuman gammaherpesvirus 8AC508.726522
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)AC504.030011
Reverse transcriptase/RNaseH Human immunodeficiency virus 1ED506.400011