Page last updated: 2024-08-05 15:05:46

EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor

A compound or agent that combines with cyclooxygenases (EC 1.14.99.1) and thereby prevents its substrate-enzyme combination with arachidonic acid and the formation of icosanoids, prostaglandins, and thromboxanes.

ChEBI ID: 35544

Members (39)

MemberDefinitionClass
2,3,6,8-tetrahydroxy-1-(3-methylbut-2-enyl)-5-(2-methylbut-3-en-2-yl)-9h-xanthen-9-oneA member of the class of xanthones that is 9H-xanthen-9-one substituted by hydroxy groups at positions 2, 3, 6 and 8, an isoprenyl group at position 1 and a 2-methylbut-3-en-2-yl group at position 5. It is isolated from the root barks of Cudrania tricuspidata and exhibits cytotoxicity towards human cancer cell lines.cudratricusxanthone A
6-methoxy-2-naphthylacetic acidA monocarboxylic acid consisting of 2-naphthylacetic acid having a methoxy substituent at the 6-position. The active metabolite of the prodrug nabumetone.(6-methoxy-2-naphthyl)acetic acid
aceclofenacA monocarboxylic acid that is the carboxymethyl ester of diclofenac. A non-steroidal anti-inflammatory drug related to diclofenac, it is used in the management of osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis.aceclofenac
acemetacinA carboxylic ester that is the carboxymethyl ester of indometacin. A non-steroidal anti-inflammatory drug, it is used in the treatment of rheumatoid arthritis, osteoarthritis, and low back pain, as well as for postoperative pain and inflammation. Its activity is due to both acemetacin and its major metabolite, indometacin.acemetacin
aiphanolA lignan that is (2R)-2,3-dihydro-1,4-benzodioxin-2-ylmethanol which is substituted by a 2-(3,5-dihydroxyphenyl)ethenyl group at position 6 and a 4-hydroxy-3,5-dimethoxyphenyl group at position 3. It is a stilbenolignan isolated from the seeds of Aiphanes aculeata and exhibits potent inhibitory efficacy against cyclooxygenase-1 and -2 (COX-1 and COX-2).aiphanol
ampiroxicamA benzothiazine that is the 1-[(ethoxycarbonyl)oxy]ethyl ether of piroxicam. A prodrug for piroxicam, it is used for the relief of pain and inflammation in musculoskeletal disorders such as rheumatoid arthritis and osteoarthritis.ampiroxicam
ampyroneA pyrazolone, a member of the class of pyrazoles that is antipyrine substituted at C-4 by an amino group. It is a metabolite of aminopyrine and of metamizole.4-aminoantipyrine
carprofenPropanoic acid in which one of the methylene hydrogens is substituted by a 6-chloro-9H-carbazol-2-yl group. A non-steroidal anti-inflammatory drug, it is no longer used in human medicine but is still used for treatment of arthritis in elderly dogs.carprofen
clonixinA pyridinemonocarboxylic acid that is nicotinic acid substituted at position 2 by a (2-methyl-3-chlorophenyl)amino group. Used (as its lysine salt) for treatment of renal colic, muscular pain and moderately severe migraine attacks.clonixin
diclofenacA monocarboxylic acid consisting of phenylacetic acid having a (2,6-dichlorophenyl)amino group at the 2-position.diclofenac
flufenamic acidAn aromatic amino acid consisting of anthranilic acid carrying an N-(trifluoromethyl)phenyl substituent. An analgesic and anti-inflammatory, it is used in rheumatic disorders.flufenamic acid
flunixinA pyridinemonocarboxylic acid that is nicotinic acid substituted at position 2 by a 2-methyl-3-(trifluoromethyl)phenylamino group. A relatively potent non-narcotic, nonsteroidal analgesic with anti-inflammatory, anti-endotoxic and anti-pyretic properties; used in veterinary medicine (usually as the meglumine salt) for treatment of horses, cattle and pigs.flunixin
flunixin meglumineAn organoammonium salt obtained by combining flunixin with one molar equivalent of 1-deoxy-1-(methylamino)-D-glucitol. A relatively potent non-narcotic, nonsteroidal analgesic with anti-inflammatory, anti-endotoxic and anti-pyretic properties; used in veterinary medicine for treatment of horses, cattle and pigs.flunixin meglumine
flurbiprofenA monocarboxylic acid that is a 2-fluoro-[1,1'-biphenyl-4-yl] moiety linked to C-2 of propionic acid. A non-steroidal anti-inflammatory, analgesic and antipyretic, it is used as a pre-operative anti-miotic as well as orally for arthritis or dental pain.flurbiprofen
ibufenacA monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is replaced by a 4-isobutylphenyl group. Although it was shown to be effective in treatment of rheumatoid arthritis, the clinical use of ibufenac was discontinued due to hepatotoxic side-effects.ibufenac
indomethacinA member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis.indometacin
indoprofenA monocarboxylic acid that is propionic acid in which one of the hydrogens at position 2 is substituted by a 4-(1-oxo-1,3-dihydroisoindol-2-yl)phenyl group. Initially used as an anti-inflammatory and analgesic, it was withdrawn from the market due to causing severe gastrointestinal bleeding. It has been subsequently found to increase production of the survival motor neuron protein.indoprofen
ketoprofenAn oxo monocarboxylic acid that consists of propionic acid substituted by a 3-benzoylphenyl group at position 2.ketoprofen
lonazolacA monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is replaced by a 3-(4-chlorophenyl)-1-phenylpyrazol-4-yl group.lonazolac
loxoprofenA monocarboxylic acid that is propionic acid in which one of the hydrogens at position 2 is substituted by a 4-[(2-oxocyclopentyl)methyl]phenyl group. A prodrug that is rapidly converted into its active trans-alcohol metabolite following oral administration.loxoprofen
lysine clonixinateAn organoammonium salt obtained by combining clonixin with one molar equivalent of L-lysine. Used for treatment of renal colic, muscular pain and moderately severe migraine attacks.clonixin lysine salt
meclofenamate sodium anhydrousA hydrate that is the monohydrate of the sodium salt of meclofenamic acid. It is used for the treatment of dysmenorrhoea (painful periods), osteoarthritis and rheumatoid arthritis.sodium meclofenamate monohydrate
meclofenamic acidAn aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,6-dichloro-3-methylphenyl group. A non-steroidal anti-inflammatory drug, it is used as the sodium salt for the treatment of dysmenorrhoea (painful periods), osteoarthritis and rheumatoid arthritis.meclofenamic acid
mefenamic acidAn aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,3-dimethylphenyl group. Although classed as a non-steroidal anti-inflammatory drug, its anti-inflammatory properties are considered to be minor. It is used to relieve mild to moderate pain, including headaches, dental pain, osteoarthritis and rheumatoid arthritis.mefenamic acid
mobiflexA thienothiazine-derived monocarboxylic acid amide obtained by formal condensation of the carboxy group of 4-hydroxy-2-methylthieno[2,3-e][1,2]thiazine-3-carboxylic acid 1,1-dioxide with the amino group of 2-aminopyridine. Used for the treatment of pain and inflammation in osteoarthritis and rheumatoid arthritis. It is also indicated for short term treatment of acute musculoskeletal disorders including strains, sprains and other soft-tissue injuries.tenoxicam
naproxen-n-butyl nitrateA carboxylic ester obtained by formal condensation of the carboxy group of naproxen with the hydroxy group of 4-(nitrooxy)butanol. A cyclooxygenase-inhibiting nitric oxide donator that is metabolised to naproxen and a nitric oxide donating moiety, effective in treatment of osteoarthritis.naproxcinod
noramidopyrineA member of the class of pyrazoles that is antipyrine substituted at C-4 by a methylamino group. It is a metabolite of aminopyrine and of metamizole.4-(methylamino)antipyrine
oxamethacinA hydroxamic acid obtained by formal condensation of the carboxy group of indometacin with the amino group of hydroxylamine.oxametacin
piroxicamA monocarboxylic acid amide resulting from the formal condensation of the carboxy group of 4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxylic acid 1,1-dioxide with the exocyclic nitrogen of 2-aminopyridine. A non-steroidal anti-inflammatory drug of the oxicam class, it is used to relieve pain and works by preventing the production of endogenous prostaglandins involved in the mediation of pain, stiffness, tenderness and swelling.piroxicam
proglumetacinA carboxylic ester obtained by formal condensation of the carboxy group of indometacin with the hydroxy group of 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl N(2)-benzoyl-N,N-dipropyl-alpha-glutaminate. Used (as its dimaleate salt) to control pain and inflammation associated with musculoskeletal and joint disorders. Following oral administration, it is metabolised to indometacin and proglumide, a drug with antisecretory effects that helps prevent injury to the stomach lining.proglumetacin
salicinAn aryl beta-D-glucoside that is salicyl alcohol in which the phenolic hydrogen has been replaced by a beta-D-glucosyl residue.salicin
sulindacA monocarboxylic acid that is 1-benzylidene-1H-indene which is substituted at positions 2, 3, and 5 by methyl, carboxymethyl, and fluorine respectively, and in which the phenyl group of the benzylidene moiety is substituted at the para position by a methylsulfinyl group. It is a prodrug for the corresponding sulfide, a non-steroidal anti-inflammatory drug, used particularly in the treatment of acute and chronic inflammatory conditions.sulindac
suprofenAn aromatic ketone that is thiophene substituted at C-2 by a 4-(1-carboxyethyl)benzoyl group.suprofen
tepoxalinA hydroxamic acid obtained by formal condensation of the carboxy group of 3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)pyrazol-3-yl]propanoic acid with the amino group of N-methylhydroxylamine. It is used in veterinary medicine for the control of pain and inflammation caused by musculoskeletal disorders such as hip dysplasia and arthritis in dogs.tepoxalin
tofisopamAn organic sodium salt having loxoprofen(1-) as the counterion. The parent acid, loxoprofen, is a prodrug that is rapidly converted to its active trans-alcohol metabolite following oral administration.loxoprofen sodium
tolfenamic acidAn aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 3-chloro-2-methylphenyl group. Tolfenamic acid is used specifically for relieving the pain of migraine. It also shows anticancer activity.tolfenamic acid
tolmetinA monocarboxylic acid that is (1-methylpyrrol-2-yl)acetic acid substituted at position 5 on the pyrrole ring by a 4-methylbenzoyl group. Used in the form of its sodium salt dihydrate as a nonselective nonsteroidal anti-inflammatory drug.tolmetin
tolmetin sodiumAn organic sodium salt that is the dihydrate form of tolmetin sodium. Used as a nonselective nonsteroidal anti-inflammatory drug.tolmetin sodium dihydrate
tricinThe 3',5'-di-O-methyl ether of tricetin. Known commonly as tricin, it is a constituent of rice bran and has been found to potently inhibit colon cancer cell growth.3',5'-di-O-methyltricetin

Research

Studies (48,871)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199016,669 (34.11)18.7374
1990's11,224 (22.97)18.2507
2000's9,507 (19.45)29.6817
2010's9,046 (18.51)24.3611
2020's2,425 (4.96)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials7,574 (13.16%)5.53%
Reviews2,139 (3.72%)6.00%
Case Studies3,190 (5.54%)4.05%
Observational48 (0.08%)0.25%
Other44,606 (77.50%)84.16%

Protein Targets (319)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency23.407015
15-lipoxygenase, partialHomo sapiens (human)Potency19.952611
67.9K proteinVaccinia virusPotency14.280725
acetylcholinesteraseHomo sapiens (human)Potency43.648611
activating transcription factor 6Homo sapiens (human)Potency19.537628
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency24.036515
Alpha-synucleinHomo sapiens (human)Potency15.461812
AR proteinHomo sapiens (human)Potency19.27351060
aryl hydrocarbon receptorHomo sapiens (human)Potency20.9492213
arylsulfatase AHomo sapiens (human)Potency8.890114
ATAD5 protein, partialHomo sapiens (human)Potency17.757826
Ataxin-2Homo sapiens (human)Potency1.972412
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency11.796914
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency1.972424
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.004524
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency66.745813
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency17.572413
caspase-3Homo sapiens (human)Potency17.572413
Cellular tumor antigen p53Homo sapiens (human)Potency27.8304213
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency10.000022
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency22.582119
Chain A, Beta-lactamaseEscherichia coli K-12Potency8.568913
Chain A, CruzipainTrypanosoma cruziPotency31.823413
Chain A, Ferritin light chainEquus caballus (horse)Potency33.997212
Chain A, HADH2 proteinHomo sapiens (human)Potency39.810711
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency42.800012
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency8.7193110
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency19.101218
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency0.229012
Chain B, HADH2 proteinHomo sapiens (human)Potency39.810711
chromobox protein homolog 1Homo sapiens (human)Potency64.7760211
cytochrome P450 2C19 precursorHomo sapiens (human)Potency8.736814
cytochrome P450 2C9 precursorHomo sapiens (human)Potency12.2506112
cytochrome P450 2C9, partialHomo sapiens (human)Potency16.8423115
cytochrome P450 2D6Homo sapiens (human)Potency9.382213
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency20.483912
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency16.0977220
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency12.668817
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency34.456417
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency10.637616
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency69.485013
DNA polymerase kappa isoform 1Homo sapiens (human)Potency7.519311
endonuclease IVEscherichia coliPotency17.782811
Endothelin receptor type BRattus norvegicus (Norway rat)Potency15.848911
Endothelin-1 receptorRattus norvegicus (Norway rat)Potency15.848911
estrogen nuclear receptor alphaHomo sapiens (human)Potency17.46501272
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency18.9103216
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency39.4387629
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency18.2447113
EWS/FLI fusion proteinHomo sapiens (human)Potency21.3869416
farnesoid X nuclear receptorHomo sapiens (human)Potency21.5657410
flap endonuclease 1Homo sapiens (human)Potency5.972811
GVesicular stomatitis virusPotency16.8423115
GABA theta subunitRattus norvegicus (Norway rat)Potency16.0977110
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency16.0977110
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency16.0977110
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency16.0977110
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency16.0977110
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency16.0977110
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency16.0977110
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency16.0977110
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency16.0977110
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency16.0977110
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency16.0977110
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency16.0977110
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency16.0977110
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency16.0977110
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency16.0977110
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency16.0977110
gemininHomo sapiens (human)Potency11.6249219
GLI family zinc finger 3Homo sapiens (human)Potency17.7769212
glp-1 receptor, partialHomo sapiens (human)Potency20.895422
GLS proteinHomo sapiens (human)Potency23.273929
glucocerebrosidaseHomo sapiens (human)Potency11.057613
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency15.3246419
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency15.690614
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency13.554612
Guanine nucleotide-binding protein GHomo sapiens (human)Potency16.531112
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency28.115214
heat shock protein beta-1Homo sapiens (human)Potency25.577616
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency13.2702238
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency26.388216
histone deacetylase 9 isoform 3Homo sapiens (human)Potency33.0412212
Histone H2A.xCricetulus griseus (Chinese hamster)Potency74.465723
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency41.490412
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency16.8423115
huntingtin isoform 2Homo sapiens (human)Potency6.694323
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency21.937528
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency7.6401222
IDH1Homo sapiens (human)Potency15.364412
importin subunit beta-1 isoform 1Homo sapiens (human)Potency13.554612
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency16.8423130
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency5.011911
Integrin alpha-IIbHomo sapiens (human)Potency10.000011
Integrin beta-3Homo sapiens (human)Potency10.000011
Interferon betaHomo sapiens (human)Potency20.2062218
interleukin 8Homo sapiens (human)Potency66.824211
lamin isoform A-delta10Homo sapiens (human)Potency3.7420110
LuciferasePhotinus pyralis (common eastern firefly)Potency29.0254331
luciferasePhoturis pensylvanica (Pennsylania firefly)Potency14.125411
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency0.588924
M-phase phosphoprotein 8Homo sapiens (human)Potency0.794311
Microtubule-associated protein tauHomo sapiens (human)Potency25.783816
mitogen-activated protein kinase 1Homo sapiens (human)Potency4.476122
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency3.162311
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency27.142415
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency0.588912
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Potency0.588912
neuropeptide S receptor isoform AHomo sapiens (human)Potency8.716912
NFKB1 protein, partialHomo sapiens (human)Potency0.010022
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency4.447614
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency0.089111
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency38.3975317
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency32.642711
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency30.557718
Nuclear receptor ROR-gammaHomo sapiens (human)Potency9.439211
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency20.3381212
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency0.100011
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency33.2618318
P53Homo sapiens (human)Potency10.000011
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency23.119313
ParkinHomo sapiens (human)Potency13.952012
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency15.827526
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency64.592313
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency17.6875532
Peroxisome proliferator-activated receptor alphaHomo sapiens (human)Potency31.832612
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency18.4906520
phosphopantetheinyl transferaseBacillus subtilisPotency50.068528
plasminogen precursorMus musculus (house mouse)Potency4.466811
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency31.622811
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency11.034412
PPM1D proteinHomo sapiens (human)Potency37.025912
pregnane X nuclear receptorHomo sapiens (human)Potency31.8724210
progesterone receptorHomo sapiens (human)Potency24.1577214
pyruvate kinaseLeishmania mexicana mexicanaPotency15.848922
pyruvate kinase PKM isoform aHomo sapiens (human)Potency39.810723
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency50.118711
RAR-related orphan receptor gammaMus musculus (house mouse)Potency28.5482223
ras-related protein Rab-9AHomo sapiens (human)Potency3.312912
regulator of G-protein signaling 4Homo sapiens (human)Potency19.298412
relaxin receptor 1 isoform 1Homo sapiens (human)Potency12.589311
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency30.1486318
retinoid X nuclear receptor alphaHomo sapiens (human)Potency17.8870425
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency4.645111
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency28.307212
SMAD family member 2Homo sapiens (human)Potency19.2201224
SMAD family member 3Homo sapiens (human)Potency19.2201224
snurportin-1Homo sapiens (human)Potency13.554612
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency16.102417
survival motor neuron protein isoform dHomo sapiens (human)Potency10.775014
TAR DNA-binding protein 43Homo sapiens (human)Potency18.187617
TDP1 proteinHomo sapiens (human)Potency19.1109229
thioredoxin glutathione reductaseSchistosoma mansoniPotency69.621912
thioredoxin reductaseRattus norvegicus (Norway rat)Potency33.130848
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency25.1261321
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency31.354012
thyroid stimulating hormone receptorHomo sapiens (human)Potency13.800046
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency10.637616
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency4.466811
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency4.466811
USP1 protein, partialHomo sapiens (human)Potency55.527812
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency23.679926
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency15.8461524
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency42.806719
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency15.690614
VprHuman immunodeficiency virus 1Potency12.589311

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
3',5'-cyclic-AMP phosphodiesterase Sus scrofa (pig)IC501,000.000011
Acid-sensing ion channel 1Rattus norvegicus (Norway rat)IC50596.557012
Acid-sensing ion channel 3Rattus norvegicus (Norway rat)IC50322.978012
Adenosine receptor A1Rattus norvegicus (Norway rat)IC50164.000011
Adenosine receptor A2aRattus norvegicus (Norway rat)IC50164.000011
AlbuminHomo sapiens (human)Ki221,583,216,666.666616
Aldo-keto reductase family 1 member B1Bos taurus (cattle)IC503.431023
Aldo-keto reductase family 1 member B1Homo sapiens (human)IC5072.384337
Aldo-keto reductase family 1 member B10Homo sapiens (human)IC5017.285046
Aldo-keto reductase family 1 member C1Homo sapiens (human)IC5044.2250510
Aldo-keto reductase family 1 member C1Homo sapiens (human)Ki0.810011
Aldo-keto reductase family 1 member C2 Homo sapiens (human)IC5022.16061116
Aldo-keto reductase family 1 member C2 Homo sapiens (human)Ki0.220011
Aldo-keto reductase family 1 member C3Homo sapiens (human)IC501.94671520
Aldo-keto reductase family 1 member C3Homo sapiens (human)Ki0.986346
Aldo-keto reductase family 1 member C4Homo sapiens (human)IC5094.250038
Amyloid-beta precursor proteinHomo sapiens (human)IC50305.000011
Androgen receptorHomo sapiens (human)IC5051.633333
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50123.428617
ATP-dependent translocase ABCB1Homo sapiens (human)IC5030.000012
Beta-lactamaseEscherichia coli K-12IC50350.000011
Bifunctional epoxide hydrolase 2Homo sapiens (human)IC501.000011
Bile salt export pumpHomo sapiens (human)IC50177.9432519
Bile salt export pumpRattus norvegicus (Norway rat)IC5087.500011
C-X-C chemokine receptor type 1Homo sapiens (human)IC505.006022
C-X-C chemokine receptor type 3Homo sapiens (human)IC500.050011
Calcium/calmodulin-dependent protein kinase type II subunit alphaRattus norvegicus (Norway rat)Ki5.100011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50153.400025
Carbonic anhydrase 1Homo sapiens (human)IC50666.625038
Carbonic anhydrase 2Homo sapiens (human)IC50666.625038
Carbonic anhydrase 4Bos taurus (cattle)IC50100.000024
Carbonic anhydrase 9Homo sapiens (human)IC50100.000022
Caspase-1Homo sapiens (human)IC5015.2460110
Caspase-3Homo sapiens (human)IC5015.2460110
Caspase-4Homo sapiens (human)IC5015.2460110
Caspase-5Homo sapiens (human)IC5015.2460110
Caspase-9Homo sapiens (human)IC5015.2460110
Chain A, membrane-associated prostaglandin E synthase-2Macaca fascicularis (crab-eating macaque)IC501,000.000011
cysteine protease ATG4B isoform aHomo sapiens (human)IC508.170011
Cytochrome c oxidase subunit 2Homo sapiens (human)IC5018.885046
Cytochrome P450 2C9 Homo sapiens (human)IC5050.000015
Cytochrome P450 2C9 Homo sapiens (human)Ki163,388,500,012.175034
Cytochrome P450 2J2Homo sapiens (human)IC5050.000015
Cytochrome P450 3A4Homo sapiens (human)IC501,000.000011
Cytochrome P450 3A4Homo sapiens (human)Ki1,640.000013
Cytosolic phospholipase A2 gammaHomo sapiens (human)IC50100.000011
Dehydrogenase/reductase SDR family member 9Homo sapiens (human)IC5014.000011
Dihydrofolate reductaseHomo sapiens (human)Ki116.000012
Dihydroorotate dehydrogenase (quinone), mitochondrialHomo sapiens (human)IC5010.500012
Epidermal growth factor receptorHomo sapiens (human)IC5010.000013
Fatty acid-binding protein, intestinalHomo sapiens (human)Ki33.950028
Fatty acid-binding protein, liverRattus norvegicus (Norway rat)Ki53.088128
Fatty-acid amide hydrolase 1Rattus norvegicus (Norway rat)IC5027.150022
Indoleamine 2,3-dioxygenase 1Mus musculus (house mouse)IC500.082012
Interleukin-8Homo sapiens (human)IC500.287014
Lactoylglutathione lyaseHomo sapiens (human)Ki279.6154313
Malate dehydrogenase, cytoplasmicHomo sapiens (human)IC50225.000011
Mitogen-activated protein kinase 1Homo sapiens (human)IC504.535512
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC50500.000012
Multidrug resistance-associated protein 1 Homo sapiens (human)IC5012.300022
Multidrug resistance-associated protein 4Homo sapiens (human)IC5096.257117
Myc proto-oncogene proteinHomo sapiens (human)IC50403.000011
MyeloperoxidaseHomo sapiens (human)IC501.595022
NACHT, LRR and PYD domains-containing protein 3 Mus musculus (house mouse)IC5025.000011
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)IC500.004011
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)IC500.004011
Nicotinate phosphoribosyltransferaseHomo sapiens (human)Ki0.000113
Nitric oxide synthase, inducibleMus musculus (house mouse)IC5024.350055
P2Y purinoceptor 12Rattus norvegicus (Norway rat)IC500.490012
phospholipase A2 precursorHomo sapiens (human)IC507.740011
Phospholipase A2, major isoenzymeSus scrofa (pig)IC501,000.000011
Polyunsaturated fatty acid 5-lipoxygenaseRattus norvegicus (Norway rat)IC50316.50001113
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50301.995011
Procathepsin LHomo sapiens (human)IC5011.800011
Prostaglandin D2 receptor Mus musculus (house mouse)IC5010.000011
Prostaglandin D2 receptor Mus musculus (house mouse)Ki10.000022
Prostaglandin D2 receptor 2Homo sapiens (human)Ki4.025022
Prostaglandin E synthaseHomo sapiens (human)IC5060.300022
Prostaglandin E2 receptor EP1 subtypeMus musculus (house mouse)Ki10.000022
Prostaglandin E2 receptor EP2 subtypeMus musculus (house mouse)Ki10.000022
Prostaglandin E2 receptor EP3 subtypeMus musculus (house mouse)Ki10.000022
Prostaglandin E2 receptor EP4 subtypeMus musculus (house mouse)Ki10.000022
Prostaglandin G/H synthase 1Homo sapiens (human)IC506.28427296
Prostaglandin G/H synthase 1Mus musculus (house mouse)IC500.011022
Prostaglandin G/H synthase 1Ovis aries (sheep)IC502.649789129
Prostaglandin G/H synthase 1Ovis aries (sheep)Ki4.450022
Prostaglandin G/H synthase 1 Bos taurus (cattle)IC5018.05851317
Prostaglandin G/H synthase 1 Rattus norvegicus (Norway rat)IC500.86291315
Prostaglandin G/H synthase 2Homo sapiens (human)IC509.4709120164
Prostaglandin G/H synthase 2Mus musculus (house mouse)IC501.03742135
Prostaglandin G/H synthase 2Ovis aries (sheep)IC5063.17252933
Prostaglandin G/H synthase 2Homo sapiens (human)Ki1.500011
Prostaglandin G/H synthase 2Ovis aries (sheep)Ki9.860011
Prostaglandin G/H synthase 2 Bos taurus (cattle)IC5012.4535711
Prostaglandin G/H synthase 2 Rattus norvegicus (Norway rat)IC500.91451214
Prostaglandin-H2 D-isomeraseMus musculus (house mouse)IC501.100022
Pyruvate kinase PKMHomo sapiens (human)IC5021.000011
Retinoic acid receptor RXR-alphaHomo sapiens (human)IC5082.900011
Rho-associated protein kinase 2Rattus norvegicus (Norway rat)IC507.700012
Seed linoleate 13S-lipoxygenase-1Glycine max (soybean)IC50130.000011
Serum paraoxonase/arylesterase 1Homo sapiens (human)Ki4,471.000013
SialidaseClostridium perfringensIC500.245011
SialidaseClostridium perfringensKi0.174822
Sigma intracellular receptor 2Rattus norvegicus (Norway rat)IC500.490011
Sodium- and chloride-dependent betaine transporterRattus norvegicus (Norway rat)IC500.350012
Sodium- and chloride-dependent GABA transporter 1Rattus norvegicus (Norway rat)IC500.350012
Sodium- and chloride-dependent GABA transporter 2Rattus norvegicus (Norway rat)IC500.350012
Sodium- and chloride-dependent GABA transporter 3Rattus norvegicus (Norway rat)IC500.350012
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC5014.000011
Solute carrier family 22 member 11Homo sapiens (human)Ki107.800011
Solute carrier family 22 member 6Homo sapiens (human)IC505.283326
Solute carrier family 22 member 6Rattus norvegicus (Norway rat)IC500.500011
Solute carrier family 22 member 6Homo sapiens (human)Ki19.800011
Solute carrier family 22 member 6Rattus norvegicus (Norway rat)Ki22.066723
Solute carrier family 22 member 7Rattus norvegicus (Norway rat)Ki1.840011
Solute carrier family 22 member 8Homo sapiens (human)Ki592.707524
Solute carrier organic anion transporter family member 1A3Rattus norvegicus (Norway rat)Ki1,450.000012
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)IC5012.000011
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)Ki11.000011
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)IC5041.000011
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)Ki38.000011
Solute carrier organic anion transporter family member 2B1 Homo sapiens (human)IC50140.000011
Solute carrier organic anion transporter family member 2B1 Homo sapiens (human)Ki130.000011
Substance-P receptorCavia porcellus (domestic guinea pig)IC505.700011
Thromboxane-A synthase Homo sapiens (human)IC5050.050022
Transcription factor SOX-18Mus musculus (house mouse)IC50191.500024
Transcriptional enhancer factor TEF-3Homo sapiens (human)IC5054.000011
Transient receptor potential cation channel subfamily M member 2Homo sapiens (human)IC5088.000023
TransthyretinHomo sapiens (human)IC502.900011
UDP-glucuronosyltransferase 1-6Homo sapiens (human)IC50131.000013
UDP-glucuronosyltransferase 1-6Homo sapiens (human)Ki23.000011
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)IC50131.000013
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)Ki52.000011
UDP-glucuronosyltransferase 1A10Homo sapiens (human)Ki28.000011
UDP-glucuronosyltransferase 1A4Homo sapiens (human)IC50131.000013
UDP-glucuronosyltransferase 1A7Homo sapiens (human)Ki19.000011
UDP-glucuronosyltransferase 1A9Homo sapiens (human)Ki11.000011
UDP-glucuronosyltransferase 2B10 Homo sapiens (human)IC50131.000013
UDP-glucuronosyltransferase 2B7Homo sapiens (human)IC50131.000013
Uracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)IC5028.800022

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 2AMus musculus (house mouse)EC505.336011
Acid-sensing ion channel 5Rattus norvegicus (Norway rat)EC502,600.000011
AlbuminHomo sapiens (human)Kd41.051633
Androgen receptorHomo sapiens (human)EC5033.500122
cell division cycle 42 (GTP binding protein, 25kDa), partialHomo sapiens (human)EC5030.000024
Chain A, PROTEIN (TRANSTHYRETIN)Homo sapiens (human)Kd0.030011
Chain B, PROTEIN (TRANSTHYRETIN)Homo sapiens (human)Kd0.030011
Complement C5Homo sapiens (human)Kd0.575012
Estrogen receptorMus musculus (house mouse)EC501.518012
Estrogen receptor betaMus musculus (house mouse)EC501.518012
Glycine receptor subunit alpha-1Homo sapiens (human)EC500.380011
glycogen synthase kinase-3 beta isoform 1Homo sapiens (human)EC50300.000013
GTP-binding protein (rab7)Canis lupus familiaris (dog)EC5030.000012
Leukotriene B4 receptor 1Homo sapiens (human)EC500.070011
Leukotriene B4 receptor 2Homo sapiens (human)EC500.070011
mu-type opioid receptor isoform MOR-1Homo sapiens (human)EC5092.590011
nuclear factor NF-kappa-B p105 subunit isoform 1Homo sapiens (human)EC501.518011
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)EC5036.325022
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)Kd100.000011
Polyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)EC500.070011
Potassium channel subfamily K member 18Homo sapiens (human)EC50287.000022
Potassium channel subfamily K member 2Homo sapiens (human)EC50100.000011
Prostaglandin D2 receptor 2Homo sapiens (human)EC500.389012
Prostaglandin G/H synthase 2Homo sapiens (human)Kd1.020011
Rac1 proteinHomo sapiens (human)EC5030.000024
ras protein, partialHomo sapiens (human)EC5022.594324
Ras-related protein Rab-2ACanis lupus familiaris (dog)EC5030.000012
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusKd220.000011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)EC5030.000014
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)EC5022.594224
Taste receptor type 2 member 16Homo sapiens (human)EC501,400.000022
transcription factor p65 isoform 1Homo sapiens (human)EC501.518011
Transcriptional enhancer factor TEF-3Homo sapiens (human)Kd76.666733
Transient receptor potential cation channel subfamily A member 1Homo sapiens (human)EC5051.178929
TransthyretinHomo sapiens (human)Kd0.486726

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Caspase-1Homo sapiens (human)ID5030.000011
Cytochrome P450 2C9 Homo sapiens (human)Km1.700011
glycogen synthase kinase-3 alphaHomo sapiens (human)AC50300.000011
Polyunsaturated fatty acid 5-lipoxygenaseRattus norvegicus (Norway rat)ID5025.000011
Prostaglandin G/H synthase 1Ovis aries (sheep)Kinact3.900011
Prostaglandin G/H synthase 1 Bos taurus (cattle)ID500.430011
Prostaglandin G/H synthase 2Mus musculus (house mouse)Activity0.250011
Prostaglandin G/H synthase 2 Bos taurus (cattle)ID500.430011
Solute carrier family 22 member 7Rattus norvegicus (Norway rat)Km0.366011
Survival motor neuron proteinHomo sapiens (human)Activity1.000011
Taste receptor type 2 member 16Homo sapiens (human)Activity70.000022
TransthyretinHomo sapiens (human)Kd10.220022
TransthyretinHomo sapiens (human)Kd23.690022
UDP-glucuronosyltransferase 1A3Homo sapiens (human)Km202.500014
UDP-glucuronosyltransferase 1A9Homo sapiens (human)Km16.000011
UDP-glucuronosyltransferase 2B7Homo sapiens (human)Km48.400015