Page last updated: 2024-08-05 15:07:47

gastrointestinal drug

A drug used for its effects on the gastrointestinal system, e.g. controlling gastric acidity, regulating gastrointestinal motility and water flow, and improving digestion.

ChEBI ID: 55324

Members (17)

MemberDefinitionClass
16,16-dimethylprostaglandin e2A prostanoid that is prostaglandin E2 in which both of the hydrogens at position 16 have been replaced by methyl groups. A synthetic analogue of prostaglandin E2, it is a potent inhibitor of pancreatic function and growth of experimental tumors. It also protects the gastric mucosa, prevents ulceration, and promotes the healing of peptic ulcers.16,16-dimethylprostaglandin E2
alosetronA pyrido[4,3-b]indole compound having a 5-methyl-1H-imidazol-4-ylmethyl group at the 2-position.alosetron
alpha-methylene gamma-butyrolactoneA butan-4-olide having a methylene group at the 3-position.alpha-methylene gamma-butyrolactone
auraptenA member of the class of coumarins that is umbelliferone in which the phenolic hydrogen has been replaced by a geranyl group. Ii is isolated from several edible fruits and vegetables and exhibits a variety of therapeutic properties.auraptene
betazolePyrazole in which a hydrogen adjacent to one of the nitrogen atoms is substituted by a 2-aminoethyl group. It is a histamine H2-receptor agonist used clinically to test gastric secretory function.betazole
ceruletideA decapeptide comprising 5-oxoprolyl, glutamyl, aspartyl, O-sulfotyrosyl, threonyl, glycyl, tryptopyl, methionyl, aspartyl and phenylalaninamide residues in sequence. Found in the skins of certain Australian amphibians, it is an analogue of the gastrointestinal peptide hormone cholecystokinin and stimulates gastric, biliary, and pancreatic secretion. It is used in cases of paralysis of the intestine (paralytic ileus) and as a diagnostic aid in pancreatic malfunction.ceruletide
ceruletide diethylamineThe diethylamine salt of ceruletide.ceruletide diethylamine
cyproheptadineThe product resulting from the formal oxidative coupling of position 5 of 5H-dibenzo[a,d]cycloheptene with position 4 of 1-methylpiperidine resulting in the formation of a double bond between the two fragments. It is a sedating antihistamine with antimuscarinic and calcium-channel blocking actions. It is used (particularly as the hydrochloride sesquihydrate) for the relief of allergic conditions including rhinitis, conjunctivitis due to inhalant allergens and foods, urticaria and angioedema, and in pruritic skin disorders. Unlike other antihistamines, it is also a seratonin receptor antagonist, making it useful in conditions such as vascular headache and anorexia.cyproheptadine
dehydrocholic acidAn oxo-5beta-cholanic acid in which three oxo substituents are located at positions 3, 7 and 12 on the cholanic acid skeleton.3,7,12-trioxo-5beta-cholanic acid
devazepideAn indolecarboxamide obtained by formal condensation of the carboxy group of indole-2-carboxylic acid with the exocyclic amino group of (3S)-3-amino-1-methyl-5-phenyl-1,3-dihydro-1,4-benzodiazepin-2-one. A cholecystokinin antagonist used for treatment of gastrointestinal disorders.devazepide
eluxadolineAn amino acid amide obtained by the formal condensation of the carboxy group of 4-carbamoyl-2,6-dimethyl-L-phenylalanine with the secondary amino group of 2-methoxy-5-({[(1S)-1-(4-phenylimidazol-2-yl)ethyl]amino}methyl)benzoic acid. It has mixed opioid receptor activity and is used for treatment of irritable bowel syndrome with diarrhoea.eluxadoline
lactuloseA synthetic galactosylfructose disaccharide used in the treatment of constipation and hepatic encephalopathy.lactulose
metoclopramideA member of the class of benzamides resulting from the formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with the primary amino group of N,N-diethylethane-1,2-diamine.metoclopramide
proglumideA racemate composed of equal amounts of (R)- and (S)-proglumide. A non-selective CCK antagonist that was used primarily for treatment of stomach ulcers, but has been replaced by newer drugs.N(2)-benzoyl-N,N-dipropyl-alpha-glutamine; proglumide
rifaximinA semisynthetic member of the class of rifamycins and non-systemic gastrointestinal site-specific broad spectrum antibiotic. Used in the treatment of traveller's diarrhoea, hepatic encephalopathy and irritable bowel syndrome.rifaximin
sofalconeA member of the class of chalcones that is benzene in which the hydrogens at positions 1,2 and 5 are replaced by carboxymethoxy, (1E)-1-{4-[(3-methylbut-2-en-1-yl)oxy]phenyl}-3-oxoprop-1-en-3-yl, and (3-methylbut-2-en-1-yl)oxy groups, respectively. It is a gastrointestinal drug currently used for treatment of gastritis and gastric ulcers in Japan and South Korea.sofalcone
tegaserodtegaserod

Research

Studies (12,791)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19905,595 (43.74)18.7374
1990's3,175 (24.82)18.2507
2000's1,974 (15.43)29.6817
2010's1,538 (12.02)24.3611
2020's509 (3.98)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials1,847 (13.05%)5.53%
Reviews849 (6.00%)6.00%
Case Studies832 (5.88%)4.05%
Observational18 (0.13%)0.25%
Other10,602 (74.94%)84.16%

Protein Targets (291)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency26.108113
acetylcholinesteraseHomo sapiens (human)Potency27.939723
acid sphingomyelinaseHomo sapiens (human)Potency31.622811
activating transcription factor 6Homo sapiens (human)Potency22.712925
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency33.862015
alpha-galactosidaseHomo sapiens (human)Potency14.125411
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency15.848911
AR proteinHomo sapiens (human)Potency17.8426816
aryl hydrocarbon receptorHomo sapiens (human)Potency10.437522
ATAD5 protein, partialHomo sapiens (human)Potency23.099911
Ataxin-2Homo sapiens (human)Potency15.917922
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency12.115622
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency11.668111
Bloom syndrome protein isoform 1Homo sapiens (human)Potency26.093222
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency28.432612
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency11.883211
caspase-3Cricetulus griseus (Chinese hamster)Potency23.710111
caspase-3Homo sapiens (human)Potency11.883211
Caspase-7Cricetulus griseus (Chinese hamster)Potency23.710111
Cellular tumor antigen p53Homo sapiens (human)Potency19.595926
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency12.589311
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency31.832612
Chain A, Beta-lactamaseEscherichia coli K-12Potency7.943311
Chain A, CruzipainTrypanosoma cruziPotency22.024323
Chain A, HADH2 proteinHomo sapiens (human)Potency25.787722
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency56.234112
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency47.963413
Chain B, HADH2 proteinHomo sapiens (human)Potency25.787722
chaperonin GroELMethanococcus maripaludis S2Potency100.000011
chromobox protein homolog 1Homo sapiens (human)Potency60.036624
cytochrome P450 2C19 precursorHomo sapiens (human)Potency12.589312
cytochrome P450 2C9, partialHomo sapiens (human)Potency18.716513
cytochrome P450 2D6Homo sapiens (human)Potency12.198614
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency8.248215
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency39.810722
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency19.903223
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency17.902512
D(1A) dopamine receptorHomo sapiens (human)Potency4.497424
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency5.011911
DNA polymerase eta isoform 1Homo sapiens (human)Potency94.562612
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency45.192012
DNA polymerase kappa isoform 1Homo sapiens (human)Potency35.481311
endonuclease IVEscherichia coliPotency14.125411
estrogen nuclear receptor alphaHomo sapiens (human)Potency14.6288817
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency21.936036
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency16.4168618
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency24.254814
EWS/FLI fusion proteinHomo sapiens (human)Potency17.028844
farnesoid X nuclear receptorHomo sapiens (human)Potency22.745538
Fumarate hydrataseHomo sapiens (human)Potency28.430613
GVesicular stomatitis virusPotency18.716513
GABA theta subunitRattus norvegicus (Norway rat)Potency39.810711
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency39.810711
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency39.810711
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency39.810711
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency39.810711
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency39.810711
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency39.810711
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency39.810711
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency39.810711
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency39.810711
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency39.810711
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency39.810711
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency39.810711
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency39.810711
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency39.810711
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency39.810711
gemininHomo sapiens (human)Potency8.063926
GLI family zinc finger 3Homo sapiens (human)Potency2.757725
glp-1 receptor, partialHomo sapiens (human)Potency19.952611
glucocerebrosidaseHomo sapiens (human)Potency31.622811
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency16.221627
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency17.373113
heat shock protein beta-1Homo sapiens (human)Potency22.775926
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency16.6498110
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency24.905412
histone deacetylase 9 isoform 3Homo sapiens (human)Potency0.059611
Histone H2A.xCricetulus griseus (Chinese hamster)Potency55.562822
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency18.716513
huntingtin isoform 2Homo sapiens (human)Potency35.481311
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency26.832524
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency18.716516
Interferon betaHomo sapiens (human)Potency14.1130310
lamin isoform A-delta10Homo sapiens (human)Potency9.981515
lethal factor (plasmid)Bacillus anthracis str. A2012Potency8.171213
lethal(3)malignant brain tumor-like protein 1 isoform IHomo sapiens (human)Potency31.622811
LuciferasePhotinus pyralis (common eastern firefly)Potency35.064922
Microtubule-associated protein tauHomo sapiens (human)Potency9.834412
mitogen-activated protein kinase 1Homo sapiens (human)Potency39.810711
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.029823
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency11.662525
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency23.585424
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency10.602522
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency18.448637
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency79.432811
ParkinHomo sapiens (human)Potency44.668411
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency16.646926
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency10.789337
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency29.653937
phosphopantetheinyl transferaseBacillus subtilisPotency57.764024
PINK1Homo sapiens (human)Potency44.668411
polyproteinZika virusPotency28.430613
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency16.649815
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency10.693713
PPM1D proteinHomo sapiens (human)Potency10.662214
pregnane X nuclear receptorHomo sapiens (human)Potency16.798523
progesterone receptorHomo sapiens (human)Potency24.412723
RAR-related orphan receptor gammaMus musculus (house mouse)Potency23.263725
regulator of G-protein signaling 4Homo sapiens (human)Potency3.176313
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency17.388736
retinoid X nuclear receptor alphaHomo sapiens (human)Potency10.235724
serine-protein kinase ATM isoform aHomo sapiens (human)Potency22.387211
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency26.121611
SMAD family member 2Homo sapiens (human)Potency27.651034
SMAD family member 3Homo sapiens (human)Potency27.651034
Smad3Homo sapiens (human)Potency35.481311
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency29.359222
TAR DNA-binding protein 43Homo sapiens (human)Potency10.000011
TDP1 proteinHomo sapiens (human)Potency22.514528
thioredoxin reductaseRattus norvegicus (Norway rat)Potency70.794611
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency14.156627
thyroid stimulating hormone receptorHomo sapiens (human)Potency15.672046
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency5.011911
USP1 protein, partialHomo sapiens (human)Potency67.833412
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency15.774825
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency18.681312
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency40.397312
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency17.373113

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC503.961022
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.070011
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC503.961022
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki0.070011
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)IC507.800011
5-hydroxytryptamine receptor 1DHomo sapiens (human)Ki0.100011
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)IC507.800011
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC501.838012
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC506.601622
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.192656
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.001611
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC500.246513
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC506.601622
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.118324
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC501.192712
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC506.601622
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.340134
5-hydroxytryptamine receptor 2C Mus musculus (house mouse)Ki0.011011
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)IC500.880022
5-hydroxytryptamine receptor 3AHomo sapiens (human)Ki2.502755
5-hydroxytryptamine receptor 3AMus musculus (house mouse)Ki0.200012
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Ki0.422478
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)IC500.880022
5-hydroxytryptamine receptor 3BMus musculus (house mouse)Ki0.200012
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)Ki0.422478
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC501.192712
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki3.749823
5-hydroxytryptamine receptor 4Homo sapiens (human)Ki0.009455
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)Ki0.080011
5-hydroxytryptamine receptor 6Homo sapiens (human)IC500.281011
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.130011
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)IC5094.800012
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki0.092033
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki0.050111
6-phosphogluconate dehydrogenase, decarboxylatingHomo sapiens (human)Ki2,111.300011
AcetylcholinesteraseHomo sapiens (human)IC5020.000011
Acyl carrier protein, mitochondrialHomo sapiens (human)IC5014.500022
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC500.564011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki0.559011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC5020.300022
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC5020.300022
Alpha-1D adrenergic receptorHomo sapiens (human)IC500.107011
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC5020.300022
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.053011
Alpha-2A adrenergic receptorHomo sapiens (human)IC501.502012
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC507.700011
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.563012
Alpha-2B adrenergic receptorHomo sapiens (human)IC500.038011
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC507.700011
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.017011
Alpha-2C adrenergic receptorHomo sapiens (human)IC501.275011
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC507.700011
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.185011
Amine oxidase [flavin-containing] AMus musculus (house mouse)IC500.000011
Amine oxidase [flavin-containing] BMus musculus (house mouse)IC500.300022
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC5017.049111
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki13.967911
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC5099.000012
Beta-secretase 1Homo sapiens (human)IC50345.100011
Bile salt export pumpHomo sapiens (human)IC5080.000034
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC5074.200012
Cholecystokinin receptor type ACavia porcellus (domestic guinea pig)IC50400.135012
Cholecystokinin receptor type AHomo sapiens (human)IC500.000233
Cholecystokinin receptor type ARattus norvegicus (Norway rat)IC5019.23161213
Cholecystokinin receptor type AHomo sapiens (human)Ki0.000922
Cholecystokinin receptor type ARattus norvegicus (Norway rat)Ki0.000422
Collagenase 3Homo sapiens (human)Ki0.001811
Complex I intermediate-associated protein 30, mitochondrialHomo sapiens (human)IC5014.500022
Cytochrome c oxidase subunit NDUFA4Homo sapiens (human)IC5014.500022
Cytochrome P450 1A2Homo sapiens (human)IC505.302422
Cytochrome P450 2B6Homo sapiens (human)IC5010.000011
Cytochrome P450 2C19Homo sapiens (human)IC5010.000011
Cytochrome P450 2C9 Homo sapiens (human)IC5010.000011
Cytochrome P450 2D6Homo sapiens (human)IC505.400022
Cytochrome P450 2D6Homo sapiens (human)Ki0.960011
Cytochrome P450 3A4Homo sapiens (human)IC500.600033
Cytochrome P450 3A4Homo sapiens (human)Ki0.055011
DRattus norvegicus (Norway rat)Ki0.173723
D(1A) dopamine receptorHomo sapiens (human)IC500.158011
D(1A) dopamine receptorHomo sapiens (human)Ki0.079011
D(1B) dopamine receptorRattus norvegicus (Norway rat)Ki0.173723
D(2) dopamine receptorHomo sapiens (human)IC500.145512
D(2) dopamine receptorRattus norvegicus (Norway rat)IC500.527055
D(2) dopamine receptorBos taurus (cattle)Ki0.080011
D(2) dopamine receptorHomo sapiens (human)Ki0.069723
D(2) dopamine receptorMus musculus (house mouse)Ki0.112011
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.162246
D(3) dopamine receptorHomo sapiens (human)IC500.124012
D(3) dopamine receptorHomo sapiens (human)Ki0.037023
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki0.173723
D(4) dopamine receptorRattus norvegicus (Norway rat)Ki0.173723
Delta-type opioid receptorRattus norvegicus (Norway rat)Ki0.001311
Endothelin receptor type BHomo sapiens (human)Ki0.050122
Endothelin receptor type BRattus norvegicus (Norway rat)Ki0.050111
Gastrin/cholecystokinin type B receptorHomo sapiens (human)IC500.245011
Gastrin/cholecystokinin type B receptorRattus norvegicus (Norway rat)IC500.000811
Gastrin/cholecystokinin type B receptorHomo sapiens (human)Ki0.056033
Gastrin/cholecystokinin type B receptorRattus norvegicus (Norway rat)Ki0.269211
Glycogen phosphorylase, brain formHomo sapiens (human)Ki0.004011
Glycogen phosphorylase, muscle formHomo sapiens (human)Ki0.004011
Histamine H1 receptorHomo sapiens (human)IC500.003711
Histamine H1 receptorHomo sapiens (human)Ki0.000411
Histamine H2 receptorHomo sapiens (human)IC500.198011
Histamine H2 receptorRattus norvegicus (Norway rat)IC502,500.000011
Histamine H2 receptorHomo sapiens (human)Ki0.195011
Histone-lysine N-methyltransferase SETD7Homo sapiens (human)IC508.133333
Histone-lysine N-methyltransferase SETD7Homo sapiens (human)Ki15.000011
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)Ki0.055011
LactoperoxidaseBos taurus (cattle)IC505.000011
Melatonin receptor type 1AHomo sapiens (human)Ki1.900011
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki0.000911
Multidrug resistance-associated protein 4Homo sapiens (human)IC5081.600012
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC500.016011
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki0.004022
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki0.004011
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC500.035011
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.008022
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Ki0.004011
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC500.046011
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.006822
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)Ki0.004011
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC500.016011
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.003122
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)Ki0.004011
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC500.003811
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki0.003422
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)Ki0.004011
MyeloperoxidaseHomo sapiens (human)IC502.675022
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex assembly factor 2Homo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex assembly factor 3Homo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex assembly factor 4Homo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 1Homo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 10, mitochondrialHomo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 11Homo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 12Homo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 13Homo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 2 Homo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 3Homo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 4-like 2Homo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 5Homo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 6Homo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 7Homo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 8Homo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 9, mitochondrialHomo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 beta subcomplex subunit 1Homo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 beta subcomplex subunit 10Homo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 beta subcomplex subunit 11, mitochondrialHomo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 beta subcomplex subunit 2, mitochondrialHomo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 beta subcomplex subunit 3Homo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 beta subcomplex subunit 4 Homo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 beta subcomplex subunit 5, mitochondrialHomo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 beta subcomplex subunit 6Homo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 beta subcomplex subunit 7Homo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 beta subcomplex subunit 8, mitochondrialHomo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 beta subcomplex subunit 9Homo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 subunit C1, mitochondrialHomo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] 1 subunit C2Homo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] flavoprotein 1, mitochondrialHomo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] flavoprotein 2, mitochondrialHomo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] flavoprotein 3, mitochondrialHomo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] iron-sulfur protein 2, mitochondrialHomo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] iron-sulfur protein 3, mitochondrialHomo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] iron-sulfur protein 4, mitochondrialHomo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] iron-sulfur protein 5Homo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] iron-sulfur protein 6, mitochondrialHomo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] iron-sulfur protein 7, mitochondrialHomo sapiens (human)IC5014.500022
NADH dehydrogenase [ubiquinone] iron-sulfur protein 8, mitochondrialHomo sapiens (human)IC5014.500022
NADH-ubiquinone oxidoreductase 75 kDa subunit, mitochondrialHomo sapiens (human)IC5014.500022
NADH-ubiquinone oxidoreductase chain 1Homo sapiens (human)IC5014.500022
NADH-ubiquinone oxidoreductase chain 2Homo sapiens (human)IC5014.500022
NADH-ubiquinone oxidoreductase chain 3Homo sapiens (human)IC5014.500022
NADH-ubiquinone oxidoreductase chain 4Homo sapiens (human)IC5014.500022
NADH-ubiquinone oxidoreductase chain 4LHomo sapiens (human)IC5014.500022
NADH-ubiquinone oxidoreductase chain 5Homo sapiens (human)IC5014.500022
NADH-ubiquinone oxidoreductase chain 6Homo sapiens (human)IC5014.500022
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)IC5017.049111
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)Ki13.967911
Polyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)IC5023.900011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC505.065367
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki13.967911
Prostaglandin G/H synthase 1Ovis aries (sheep)Ki0.001611
Sodium-dependent noradrenaline transporterMus musculus (house mouse)Ki0.290011
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC500.564011
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki0.424522
Sodium-dependent serotonin transporterHomo sapiens (human)Ki4.100011
Sodium-dependent serotonin transporterMus musculus (house mouse)Ki4.100011
Solute carrier family 22 member 1 Homo sapiens (human)IC5094.800011
Trans-sialidaseTrypanosoma cruziIC50570.000011
TransporterRattus norvegicus (Norway rat)Ki0.290011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 3AHomo sapiens (human)Kd0.050111
5-hydroxytryptamine receptor 3BHomo sapiens (human)Kd0.050111
5-hydroxytryptamine receptor 3CHomo sapiens (human)Kd0.050111
5-hydroxytryptamine receptor 3DHomo sapiens (human)Kd0.050111
5-hydroxytryptamine receptor 3EHomo sapiens (human)Kd0.050111
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)EC500.009422
5-hydroxytryptamine receptor 4Homo sapiens (human)EC500.004855
AlbuminRattus norvegicus (Norway rat)Kd1,370.000011
Delta-type opioid receptorHomo sapiens (human)EC5010.000011
Histamine H1 receptorHomo sapiens (human)Kd5.400011
Mu-type opioid receptorHomo sapiens (human)EC500.001011
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC509.120055

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)ED5024.100011
UDP-glucuronosyltransferase 1A3Homo sapiens (human)Km240.000011
UDP-glucuronosyltransferase 1A4Homo sapiens (human)Km106.000022