Page last updated: 2024-08-05 14:59:51

EC 4.6.1.2 (guanylate cyclase) inhibitor

An EC 4.6.* (P-O lyase) inhibitor that interferes with the action of enzyme guanylate cyclase (EC 4.6.1.2).

ChEBI ID: 78678

Members (3)

MemberDefinitionClass
1h-(1,2,4)oxadiazolo(4,3-a)quinoxalin-1-oneA member of the class of oxadiazoloquinoxalines that is 1H-[1,2,4]oxadiazolo[4,3-a]quinoxaline substituted at position 1 by an oxo group.1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one
6-anilino-5,8-quinolinedioneA quinolone that is quinoline-5,8-dione in which the hydrogen at position 6 is replaced by an anilino group.6-anilino-5,8-quinolinedione
methylene blueAn organic chloride salt having 3,7-bis(dimethylamino)phenothiazin-5-ium as the counterion. A commonly used dye that also exhibits antioxidant, antimalarial, antidepressant and cardioprotective properties.methylene blue

Research

Studies (11,410)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19902,670 (23.40)18.7374
1990's1,730 (15.16)18.2507
2000's2,340 (20.51)29.6817
2010's3,157 (27.67)24.3611
2020's1,513 (13.26)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials394 (3.22%)5.53%
Reviews374 (3.06%)6.00%
Case Studies834 (6.82%)4.05%
Observational18 (0.15%)0.25%
Other10,605 (86.75%)84.16%

Protein Targets (174)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency30.300112
acetylcholinesteraseHomo sapiens (human)Potency3.376648
activating transcription factor 6Homo sapiens (human)Potency0.436411
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency18.364413
Alpha-synucleinHomo sapiens (human)Potency15.848911
AR proteinHomo sapiens (human)Potency3.3117711
aryl hydrocarbon receptorHomo sapiens (human)Potency4.995724
arylsulfatase AHomo sapiens (human)Potency37.933011
ATAD5 protein, partialHomo sapiens (human)Potency0.730511
Ataxin-2Homo sapiens (human)Potency14.960111
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency29.632222
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency14.960111
Bloom syndrome protein isoform 1Homo sapiens (human)Potency31.622811
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency39.810711
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency10.870711
caspase-3Homo sapiens (human)Potency10.870711
Cellular tumor antigen p53Homo sapiens (human)Potency11.989523
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency32.059413
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency23.735822
Chain A, Ferritin light chainEquus caballus (horse)Potency35.638323
Chain A, HADH2 proteinHomo sapiens (human)Potency25.564823
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency44.668411
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency31.099022
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency22.334211
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency24.078126
Chain B, HADH2 proteinHomo sapiens (human)Potency25.564823
chaperonin-containing TCP-1 beta subunit homologHomo sapiens (human)Potency22.387211
chromobox protein homolog 1Homo sapiens (human)Potency0.005311
cytochrome P450 2C9 precursorHomo sapiens (human)Potency39.810711
cytochrome P450 2C9, partialHomo sapiens (human)Potency0.691811
cytochrome P450 2D6Homo sapiens (human)Potency0.389011
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency10.000023
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency0.489711
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency4.935412
DNA dC->dU-editing enzyme APOBEC-3G isoform 1Homo sapiens (human)Potency23.715011
DNA polymerase betaHomo sapiens (human)Potency25.118911
DNA polymerase eta isoform 1Homo sapiens (human)Potency56.234111
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency14.125411
estrogen nuclear receptor alphaHomo sapiens (human)Potency30.7609815
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency11.883211
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency2.9580713
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency37.541913
farnesoid X nuclear receptorHomo sapiens (human)Potency15.142212
flap endonuclease 1Homo sapiens (human)Potency17.782811
Fumarate hydrataseHomo sapiens (human)Potency17.782811
GVesicular stomatitis virusPotency0.691811
GABA theta subunitRattus norvegicus (Norway rat)Potency10.000012
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency10.000012
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency10.000012
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency10.000012
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency10.000012
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency10.000012
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency10.000012
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency10.000012
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency10.000012
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency10.000012
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency10.000012
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency10.000012
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency10.000012
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency10.000012
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency10.000012
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency10.000012
gemininHomo sapiens (human)Potency18.716233
GLI family zinc finger 3Homo sapiens (human)Potency0.732324
glp-1 receptor, partialHomo sapiens (human)Potency6.309611
GLS proteinHomo sapiens (human)Potency7.079511
glucocerebrosidaseHomo sapiens (human)Potency7.079511
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency13.806222
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency28.577612
Glycoprotein hormones alpha chainHomo sapiens (human)Potency0.501211
Guanine nucleotide-binding protein GHomo sapiens (human)Potency10.000011
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency7.079511
heat shock protein beta-1Homo sapiens (human)Potency58.292922
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency39.810713
histone deacetylase 9 isoform 3Homo sapiens (human)Potency12.306624
Histone H2A.xCricetulus griseus (Chinese hamster)Potency11.530124
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency24.068212
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency0.691811
huntingtin isoform 2Homo sapiens (human)Potency12.589311
hypothetical protein, conservedTrypanosoma bruceiPotency19.952611
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency42.270723
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency12.589322
IDH1Homo sapiens (human)Potency7.307811
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency0.691812
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency1.790112
Interferon betaHomo sapiens (human)Potency17.931335
isocitrate dehydrogenase 1, partialHomo sapiens (human)Potency52.119411
lethal factor (plasmid)Bacillus anthracis str. A2012Potency7.943311
LuciferasePhotinus pyralis (common eastern firefly)Potency17.494323
luciferasePhoturis pensylvanica (Pennsylania firefly)Potency10.000011
luteinizing hormone receptorHomo sapiens (human)Potency84.921411
M-phase phosphoprotein 8Homo sapiens (human)Potency44.668411
Microtubule-associated protein tauHomo sapiens (human)Potency16.168025
mitogen-activated protein kinase 1Homo sapiens (human)Potency11.464222
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.035511
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency2.818411
neuropeptide S receptor isoform AHomo sapiens (human)Potency3.182433
NFKB1 protein, partialHomo sapiens (human)Potency5.623422
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency2.575624
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency11.582111
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency54.941011
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency3.814622
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency0.662536
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency19.952611
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency56.234111
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency43.641211
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency36.719511
phosphoglycerate kinaseTrypanosoma brucei brucei TREU927Potency17.782811
phosphopantetheinyl transferaseBacillus subtilisPotency71.811234
plasminogen precursorMus musculus (house mouse)Potency2.238711
polyproteinZika virusPotency17.782811
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency8.912511
PPM1D proteinHomo sapiens (human)Potency18.556912
pregnane X nuclear receptorHomo sapiens (human)Potency1.886822
progesterone receptorHomo sapiens (human)Potency51.040612
pyruvate kinase PKM isoform aHomo sapiens (human)Potency39.810722
RAR-related orphan receptor gammaMus musculus (house mouse)Potency11.823023
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency19.706037
retinoid X nuclear receptor alphaHomo sapiens (human)Potency32.785923
serine-protein kinase ATM isoform aHomo sapiens (human)Potency13.025844
SMAD family member 2Homo sapiens (human)Potency6.740011
SMAD family member 3Homo sapiens (human)Potency6.740011
Smad3Homo sapiens (human)Potency10.000011
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.810711
survival motor neuron protein isoform dHomo sapiens (human)Potency10.819614
T cell receptor, partialHomo sapiens (human)Potency6.284111
TAR DNA-binding protein 43Homo sapiens (human)Potency15.848911
TDP1 proteinHomo sapiens (human)Potency4.599028
thioredoxin glutathione reductaseSchistosoma mansoniPotency31.622811
thioredoxin reductaseRattus norvegicus (Norway rat)Potency26.407622
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency18.207924
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency42.239522
thyroid stimulating hormone receptorHomo sapiens (human)Potency11.5759510
TSHR proteinHomo sapiens (human)Potency15.503522
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency2.238711
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency2.238711
USP1 protein, partialHomo sapiens (human)Potency3.358711
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency8.196624
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency69.621912
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency28.577612
VprHuman immunodeficiency virus 1Potency39.810711

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC500.500011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC500.500011
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC500.500011
Amine oxidase [flavin-containing] AHomo sapiens (human)IC500.070011
Amyloid-beta precursor proteinHomo sapiens (human)IC500.500011
Apoptotic peptidase activating factor 1Homo sapiens (human)IC5057.750022
caspase-3 isoform a preproproteinHomo sapiens (human)IC5017.000011
caspase-9 isoform alpha precursorHomo sapiens (human)IC5017.000011
Chain E, Fibrin beta chainHomo sapiens (human)IC5046.265522
CruzipainTrypanosoma cruziIC5070.000022
Dihydrolipoyl dehydrogenase Plasmodium falciparum (malaria parasite P. falciparum)IC501,000.000011
Dihydrolipoyl dehydrogenase, mitochondrialSus scrofa (pig)IC501,000.000011
Glutathione reductasePlasmodium falciparum 3D7IC506.400011
Glutathione reductase, mitochondrialHomo sapiens (human)IC5016.200022
Guanylate cyclase soluble subunit alpha-1Homo sapiens (human)IC501.000011
Guanylate cyclase soluble subunit alpha-2Homo sapiens (human)IC501.000011
Guanylate cyclase soluble subunit beta-1Homo sapiens (human)IC501.000011
Guanylate cyclase soluble subunit beta-2Homo sapiens (human)IC501.000011
integrase, partialHuman immunodeficiency virus 1IC5019.240522
lens epithelium-derived growth factor p75Homo sapiens (human)IC5019.240522
Microtubule-associated protein tauHomo sapiens (human)IC509.425044
neutrophil cytosol factor 1Homo sapiens (human)IC500.390011
Thioredoxin reductase 1, cytoplasmicHomo sapiens (human)IC5030.000011
Translation factor GUF1, mitochondrialSaccharomyces cerevisiae S288CIC50300.000011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Microtubule-associated protein tauHomo sapiens (human)EC500.360022
POsterior SegregationCaenorhabditis elegansEC50186.681011
recombinase AMycobacterium tuberculosis H37RvEC5078.650022
Sodium-dependent noradrenaline transporter Homo sapiens (human)EC50113.886011
Zinc finger protein mex-5Caenorhabditis elegansEC50113.886011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
AlbuminBos taurus (cattle)Kdiss2.900011
Caspase 6, apoptosis-related cysteine peptidaseHomo sapiens (human)AC501.600011
Dihydrolipoyl dehydrogenase Plasmodium falciparum (malaria parasite P. falciparum)Km49.000011
Dihydrolipoyl dehydrogenase, mitochondrialSus scrofa (pig)Km28.000011
DNA repair protein RAD52 homolog isoform aHomo sapiens (human)AC500.936011
Glutathione reductase, mitochondrialHomo sapiens (human)Km6.300011
protein AF-9 isoform aHomo sapiens (human)AC504.080011
replicative DNA helicaseMycobacterium tuberculosis H37RvAC5058.180022
Thioredoxin reductase 1, cytoplasmicHomo sapiens (human)Km95.000011