Page last updated: 2024-08-05 14:58:09

cholinergic antagonist

Any drug that binds to but does not activate cholinergic receptors, thereby blocking the actions of acetylcholine or cholinergic agonists.

ChEBI ID: 48873

Members (22)

MemberDefinitionClass
3alpha-hydroxy-4alpha-methylergosta-8,24(28)-dien-7,11-dione-26-oic acidA steroid acid that is ergosta-8,24(28)-dien-26-oic acid substituted by a hydroxy group at position 3, a methyl group at position 4 and oxo groups at positions 7 and 11 (the 3alpha,4alpha,5alpha stereoisomer). Isolated from Antrodia cinnamomea and Antrodia camphorata, it exhibits cytotoxic, anticholinergic and antiserotonergic activities.zhankuic acid B
4-diphenylacetoxy-1,1-dimethylpiperidiniumA quaternary ammonium salt obtained by formal methylation of the tertiary amino function of 4-diphenylacetoxy-N-methylpiperidine.4-DAMP(1+)
4-diphenylacetoxy-n-methylpiperidine methiodideA quaternary ammonium salt obtained by combining equimolar amounts of 4-diphenylacetoxy-N-methylpiperidine and iodomethane.4-DAMP methiodide
alverine citrateThe citrate salt of alverine, resulting from the reaction of equimolar amounts of alvarine and citric acid. An antispasmodic that acts directly on intestinal and uterine smooth muscle, it is used in the treatment of irritable bowel syndrome.alverine citrate
antazolineA member of the class of imidazolines that is 2-aminomethyl-2-imidazoline in which the exocyclic amino hydrogens are replaced by benzyl and phenyl groups. Antazoline is only found in individuals that have taken the drug.antazoline
buclizineAn N-alkylpiperazine carrying (4-chlorophenyl)(phenyl)methyl and 4-tert-butylbenzyl groups.buclizine
cyclizineAn N-alkylpiperazine in which one nitrogen of the piperazine ring is substituted by a methyl group, while the other is substituted by a diphenylmethyl group.cyclizine
cyclizine hydrochlorideA hydrochloride salt consisting of equimolar amounts of cyclizine and hydrogen chloride.cyclizine hydrochloride
desipramineA dibenzoazepine consisting of 10,11-dihydro-5H-dibenzo[b,f]azepine substituted on nitrogen with a 3-(methylamino)propyl group.desipramine
desloratadineLoratadine in which the ethoxycarbonyl group attached to the piperidine ring is replaced by hydrogen. The major metabolite of loratidine, desloratadine is an antihistamine which is used for the symptomatic relief of allergic conditions including rhinitis and chronic urticaria. It does not readily enter the central nervous system, so does not cause drowsiness.desloratadine
diphenylpyralineA member of the class of piperidines that is the benzhydryl ether derivative of 1-methyl-4-hydroxypiperidine. A sedating antihistamine, it is used as the hydrochloride for the symptomatic relief of allergic conditions including rhinitis and hay fever, and in pruritic skin disorders. It is also used as the teoclate salt (piprinhydrinate) as an ingredient in compound preparations for the symptomatic relief of coughs and the common cold.diphenylpyraline
diphenylpyraline hydrochlorideThe hydrochloride salt of diphenylpyraline. A sedating antihistamine, it is used as the hydrochloride for the symptomatic relief of allergic conditions including rhinitis and hay fever, and in pruritic skin disorders.diphenylpyraline hydrochloride
doxylaminedoxylamine
loratadineA benzocycloheptapyridine that is 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine substituted by a chloro group at position 8 and a 1-(ethoxycarbonyl)piperidin-4-ylidene group at position 11. It is a H1-receptor antagonist commonly employed in the treatment of allergic disorders.loratadine
methdilazineA phenothiazine substituted on nitrogen by a (1-methylpyrrolidin-3-yl)methyl group; a first-generation antihistamine with anticholinergic properties.methdilazine
methotrimeprazineA member of the class of phenothiazines that is 10H-phenothiazine substituted by a (2R)-3-(dimethylamino)-2-methylpropyl group and a methoxy group at positions 10 and 2 respectively.methotrimeprazine
pancuroniumA steroid ester in which a 5alpha-androstane skeleton is C-3alpha- and C-17beta-disubstituted with acetoxy groups and 2beta- and 16beta-disubstituted with 1-methylpiperidinium-1-yl groups. It is a non-depolarizing curare-mimetic muscle relaxant.pancuronium
pancuronium bromideA bromide salt consisting of two bromide ions and one pancuronium dication.pancuronium bromide
prochlorperazineA member of the class of phenothiazines that is 10H-phenothiazine having a chloro substituent at the 2-position and a 3-(4-methylpiperazin-1-yl)propyl group at the N-10 position.prochlorperazine
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
strychnineA monoterpenoid indole alkaloid that is strychnidine bearing a keto substituent at the 10-position.strychnine
tolueneThe simplest member of the class toluenes consisting of a benzene core which bears a single methyl substituent.toluene

Research

Studies (25,121)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199011,461 (45.62)18.7374
1990's4,476 (17.82)18.2507
2000's4,570 (18.19)29.6817
2010's3,673 (14.62)24.3611
2020's941 (3.75)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials2,001 (7.22%)5.53%
Reviews942 (3.40%)6.00%
Case Studies1,290 (4.66%)4.05%
Observational17 (0.06%)0.25%
Other23,456 (84.66%)84.16%

Protein Targets (280)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-lipoxygenase, partialHomo sapiens (human)Potency25.118911
67.9K proteinVaccinia virusPotency16.874723
acetylcholinesteraseHomo sapiens (human)Potency40.479623
activating transcription factor 6Homo sapiens (human)Potency0.436411
alpha-galactosidaseHomo sapiens (human)Potency50.118711
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency15.848911
AR proteinHomo sapiens (human)Potency30.8717816
arylsulfatase AHomo sapiens (human)Potency12.935814
ATAD5 protein, partialHomo sapiens (human)Potency16.940824
Ataxin-2Homo sapiens (human)Potency22.887125
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency0.756911
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency28.153813
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency17.487212
Bloom syndrome protein isoform 1Homo sapiens (human)Potency14.104424
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency51.434614
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency33.491511
caspase-3Homo sapiens (human)Potency33.491511
Cellular tumor antigen p53Homo sapiens (human)Potency36.568126
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency20.205825
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency16.626813
Chain A, Beta-lactamaseEscherichia coli K-12Potency36.718828
Chain A, CruzipainTrypanosoma cruziPotency32.799214
Chain A, HADH2 proteinHomo sapiens (human)Potency7.943311
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency30.724813
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency26.790412
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency15.811411
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency63.095711
Chain B, HADH2 proteinHomo sapiens (human)Potency7.943311
chaperonin-containing TCP-1 beta subunit homologHomo sapiens (human)Potency89.125111
chromobox protein homolog 1Homo sapiens (human)Potency48.313524
cytochrome P450 2C19 precursorHomo sapiens (human)Potency7.707914
cytochrome P450 2C9 precursorHomo sapiens (human)Potency18.566513
cytochrome P450 2C9, partialHomo sapiens (human)Potency5.536812
cytochrome P450 2D6Homo sapiens (human)Potency5.976015
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency12.6767111
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency11.9425210
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency14.208725
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency51.040612
D(1A) dopamine receptorHomo sapiens (human)Potency2.944725
D(1A) dopamine receptorSus scrofa (pig)Potency13.890512
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency12.589311
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency6.239612
endonuclease IVEscherichia coliPotency14.125411
estrogen nuclear receptor alphaHomo sapiens (human)Potency33.7132820
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency26.927824
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency23.2148818
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency29.0324115
EWS/FLI fusion proteinHomo sapiens (human)Potency25.634244
farnesoid X nuclear receptorHomo sapiens (human)Potency23.122624
flap endonuclease 1Homo sapiens (human)Potency25.153812
Fumarate hydrataseHomo sapiens (human)Potency37.221211
GVesicular stomatitis virusPotency5.536812
GABA theta subunitRattus norvegicus (Norway rat)Potency11.942515
GALC proteinHomo sapiens (human)Potency0.707911
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency11.942515
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency11.942515
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency11.942515
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency11.942515
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency11.942515
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency11.942515
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency11.942515
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency11.942515
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency11.942515
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency11.942515
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency11.942515
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency11.942515
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency11.942515
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency11.942515
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency11.942515
gemininHomo sapiens (human)Potency15.7176414
GLI family zinc finger 3Homo sapiens (human)Potency18.801139
glp-1 receptor, partialHomo sapiens (human)Potency9.949314
GLS proteinHomo sapiens (human)Potency20.724426
glucocerebrosidaseHomo sapiens (human)Potency31.622811
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency40.979635
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency43.866912
Guanine nucleotide-binding protein GHomo sapiens (human)Potency39.810711
heat shock protein beta-1Homo sapiens (human)Potency39.277424
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency14.6606227
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency29.903312
Histone H2A.xCricetulus griseus (Chinese hamster)Potency78.955713
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency39.810711
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency5.536812
huntingtin isoform 2Homo sapiens (human)Potency35.481311
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency35.077524
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency20.483924
IDH1Homo sapiens (human)Potency24.255613
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency5.536814
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency1.339725
Integrin alpha-IIbHomo sapiens (human)Potency23.735812
Integrin beta-3Homo sapiens (human)Potency23.735812
Interferon betaHomo sapiens (human)Potency14.789223
isocitrate dehydrogenase 1, partialHomo sapiens (human)Potency50.118711
lamin isoform A-delta10Homo sapiens (human)Potency14.8431212
lethal factor (plasmid)Bacillus anthracis str. A2012Potency16.584115
M-phase phosphoprotein 8Homo sapiens (human)Potency28.655213
Microtubule-associated protein tauHomo sapiens (human)Potency21.887616
mitogen-activated protein kinase 1Homo sapiens (human)Potency21.916425
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency4.452528
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency79.432811
neuropeptide S receptor isoform AHomo sapiens (human)Potency12.408214
NFKB1 protein, partialHomo sapiens (human)Potency17.559424
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency14.120914
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency58.047911
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency27.023825
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency26.995113
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency18.126723
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency25.533038
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency44.668411
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency94.562612
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency17.578214
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency27.278512
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency26.420824
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency51.439234
phosphopantetheinyl transferaseBacillus subtilisPotency42.239512
plasminogen precursorMus musculus (house mouse)Potency12.589311
polyproteinZika virusPotency37.221211
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency39.810711
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency12.707719
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency14.413216
pregnane X nuclear receptorHomo sapiens (human)Potency26.570937
progesterone receptorHomo sapiens (human)Potency24.480225
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency12.589311
RAR-related orphan receptor gammaMus musculus (house mouse)Potency10.136625
ras-related protein Rab-9AHomo sapiens (human)Potency100.000012
regulator of G-protein signaling 4Homo sapiens (human)Potency13.423812
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency37.149037
retinoid X nuclear receptor alphaHomo sapiens (human)Potency11.885523
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency16.150049
SMAD family member 2Homo sapiens (human)Potency23.733813
SMAD family member 3Homo sapiens (human)Potency23.733813
Smad3Homo sapiens (human)Potency31.622811
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency34.846214
survival motor neuron protein isoform dHomo sapiens (human)Potency14.946113
TDP1 proteinHomo sapiens (human)Potency16.4363222
thioredoxin glutathione reductaseSchistosoma mansoniPotency24.324712
thioredoxin reductaseRattus norvegicus (Norway rat)Potency2.962923
ThrombopoietinHomo sapiens (human)Potency19.220326
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency11.5033210
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency98.654723
thyroid stimulating hormone receptorHomo sapiens (human)Potency24.6185515
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency12.589311
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency12.589311
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency12.589311
USP1 protein, partialHomo sapiens (human)Potency47.300816
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency18.704724
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency42.523812
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency46.485213
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency43.866912

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
1-acylglycerol-3-phosphate O-acyltransferase ABHD5 isoform aHomo sapiens (human)IC502.635022
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC500.650022
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.543011
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC500.650022
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki0.543011
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)IC500.350011
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)IC500.350011
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC500.088413
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC500.350011
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.047235
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC500.190814
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC500.350011
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.121814
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC500.376313
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC500.350011
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.197313
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)IC500.350011
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)IC500.350011
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC500.376313
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.197313
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)IC500.350011
5-hydroxytryptamine receptor 5ARattus norvegicus (Norway rat)IC500.350011
5-hydroxytryptamine receptor 5BRattus norvegicus (Norway rat)IC500.350011
5-hydroxytryptamine receptor 6Homo sapiens (human)IC501.219012
5-hydroxytryptamine receptor 6Rattus norvegicus (Norway rat)IC500.350011
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.566012
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)IC5053.200014
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)IC500.350011
AcetylcholinesteraseHomo sapiens (human)IC502.452622
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC500.758012
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki0.751512
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC500.000211
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC500.003411
Alpha-1D adrenergic receptorHomo sapiens (human)IC500.624512
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.306512
Alpha-2A adrenergic receptorHomo sapiens (human)IC500.573423
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.322512
Alpha-2B adrenergic receptorHomo sapiens (human)IC500.718823
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.492412
Alpha-2C adrenergic receptorHomo sapiens (human)IC500.041122
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.012011
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC5022.928113
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki18.784513
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000015
ATP-dependent translocase ABCB1Homo sapiens (human)IC5027.200012
Bile acid receptorHomo sapiens (human)IC503.070011
Bile salt export pumpHomo sapiens (human)IC50277.7077313
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000015
Cholecystokinin receptor type ACavia porcellus (domestic guinea pig)IC50800.000011
Cholecystokinin receptor type ARattus norvegicus (Norway rat)IC50250.000011
Cytochrome P450 1A2Homo sapiens (human)IC502.000011
Cytochrome P450 2C19Homo sapiens (human)IC500.016011
Cytochrome P450 2C9 Homo sapiens (human)IC5050.000011
Cytochrome P450 2D6Homo sapiens (human)IC503.258812
Cytochrome P450 2J2Homo sapiens (human)IC5050.000011
D(1A) dopamine receptorHomo sapiens (human)IC500.155011
D(1A) dopamine receptorHomo sapiens (human)Ki0.078011
D(2) dopamine receptorHomo sapiens (human)IC500.011011
D(2) dopamine receptorHomo sapiens (human)Ki0.003611
D(3) dopamine receptorHomo sapiens (human)IC501.637013
D(3) dopamine receptorHomo sapiens (human)Ki0.555813
D(4) dopamine receptorHomo sapiens (human)IC502.311011
D(4) dopamine receptorHomo sapiens (human)Ki0.810011
fMet-Leu-Phe receptorHomo sapiens (human)IC5066.700011
Glycine receptor subunit alpha-1Homo sapiens (human)IC500.18431420
Glycine receptor subunit alpha-1Homo sapiens (human)Ki0.050333
Glycine receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki0.012011
Glycine receptor subunit betaHomo sapiens (human)IC500.287169
hepatocyte nuclear factor 4-alpha isoform 2Homo sapiens (human)IC5039.841011
Histamine H1 receptorHomo sapiens (human)IC500.089036
Histamine H1 receptorRattus norvegicus (Norway rat)IC500.000812
Histamine H1 receptorHomo sapiens (human)Ki0.088159
Histamine H2 receptorCavia porcellus (domestic guinea pig)IC503.800011
Histamine H2 receptorHomo sapiens (human)IC501.099011
Histamine H2 receptorRattus norvegicus (Norway rat)IC502,500.000011
Histamine H2 receptorHomo sapiens (human)Ki1.080011
Histamine H3 receptorHomo sapiens (human)Ki5.000011
Histamine H3 receptorRattus norvegicus (Norway rat)Ki5.000011
Histamine H4 receptorHomo sapiens (human)Ki10.000011
Mcl-1Homo sapiens (human)IC503.773311
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000015
Muscarinic acetylcholine receptor DM1Drosophila melanogaster (fruit fly)Ki0.016522
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC500.489924
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki0.118024
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC501.108024
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.395024
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC500.22671012
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.0580810
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC500.284479
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.059746
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC500.143568
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki0.137446
neutrophil cytosol factor 1Homo sapiens (human)IC5050.000011
Nitric oxide synthase, inducibleMus musculus (house mouse)IC509.600011
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)IC5022.928113
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)Ki18.784513
perilipin-1Homo sapiens (human)IC502.261011
perilipin-5Homo sapiens (human)IC502.635022
Platelet-activating factor receptorHomo sapiens (human)IC50135.000011
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CIC505.650012
Potassium channel subfamily K member 9Homo sapiens (human)IC5063.400011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC504.9774916
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki18.784513
Prostaglandin G/H synthase 1Ovis aries (sheep)Ki0.160011
Protein farnesyltransferase subunit betaHomo sapiens (human)IC5065.000011
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)IC5065.000011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC500.054011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.023011
Small conductance calcium-activated potassium channel protein 1Rattus norvegicus (Norway rat)IC506.800011
Small conductance calcium-activated potassium channel protein 2Rattus norvegicus (Norway rat)IC506.800011
Small conductance calcium-activated potassium channel protein 3Rattus norvegicus (Norway rat)IC506.800011
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC501.520011
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC507.800011
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)Ki7.000022
Sodium-dependent dopamine transporter Homo sapiens (human)IC5026.797168
Sodium-dependent dopamine transporter Homo sapiens (human)Ki1.152637
Sodium-dependent neutral amino acid transporter B(0)AT2Homo sapiens (human)IC5088.000012
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC500.08701718
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki0.12421517
Sodium-dependent serotonin transporterHomo sapiens (human)IC500.363956
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)IC5020.000011
Sodium-dependent serotonin transporterHomo sapiens (human)Ki0.254323
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Ki0.163011
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)IC5017.500011
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)Ki2.800011
Solute carrier family 22 member 1 Homo sapiens (human)IC5038.526723
Solute carrier family 22 member 1 Homo sapiens (human)Ki5.360011
Solute carrier family 22 member 2Rattus norvegicus (Norway rat)IC5010.000011
Solute carrier family 22 member 2Homo sapiens (human)Ki16.000011
Solute carrier family 22 member 3Rattus norvegicus (Norway rat)IC5068.000011
Solute carrier family 22 member 3Homo sapiens (human)Ki14.000011
Solute carrier family 22 member 4Rattus norvegicus (Norway rat)IC5080.000011
TransporterRattus norvegicus (Norway rat)IC5010.650022
TransporterRattus norvegicus (Norway rat)Ki0.007423
Tryptophan 5-hydroxylase 1Rattus norvegicus (Norway rat)Ki0.000511
Tyrosine-protein kinase FynHomo sapiens (human)IC505.684011
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC5011.400011
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC5011.400011
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC5011.400011
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC5011.400011
Voltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)IC5011.000011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
AlbuminHomo sapiens (human)Kd851.138011
Angiotensin-converting enzyme 2 Homo sapiens (human)EC502.500011
EndolysinTequatrovirus T4Kd248.666766
Histamine H1 receptorCavia porcellus (domestic guinea pig)Kd0.072422
Histamine H1 receptorHomo sapiens (human)Kd0.107012
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC508.900044
Procathepsin LHomo sapiens (human)EC502.500011
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusEC502.500011
Replicase polyprotein 1abBetacoronavirus England 1EC502.500011
Replicase polyprotein 1abHuman coronavirus 229EEC502.500011
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2EC502.500011
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusEC502.500011
short transient receptor potential channel 6 isoform 1Mus musculus (house mouse)EC508.065012
Sodium-dependent noradrenaline transporter Homo sapiens (human)Kd0.000811
Spike glycoproteinBetacoronavirus England 1EC502.500011
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusEC502.500011
Taste receptor type 2 member 10Homo sapiens (human)EC5022.500022
Taste receptor type 2 member 46Homo sapiens (human)EC500.690011
Transmembrane protease serine 2Homo sapiens (human)EC502.500011
voltage-dependent T-type calcium channel subunit alpha-1H isoform aHomo sapiens (human)EC500.000011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Gamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)Kb69.000011
Gamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)Kb69.000011
Gamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)Kb69.000011
Histamine H2 receptorCavia porcellus (domestic guinea pig)K0.50.045417
Muscarinic acetylcholine receptor M1Homo sapiens (human)KA0.021011
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Kb0.008512
Muscarinic acetylcholine receptor M2Homo sapiens (human)Kb0.008511
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Kb0.008512
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)Kb0.008512
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)Kb0.008512
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)Kb0.008512
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CINH67.600012
Snq2pSaccharomyces cerevisiae EC1118INH53.300012
Taste receptor type 2 member 10Homo sapiens (human)Activity1.550022