Page last updated: 2024-08-05 15:03:25

muscarinic antagonist

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

ChEBI ID: 48876

Members (53)

MemberDefinitionClass
(S)-carbinoxamine maleateThe maleic acid salt of (S)-carbinoxamine.(S)-carbinoxamine maleate
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
aclidinium bromideA quaternary ammonium salt that is the bromide salt of aclidinium. A muscarinic acetylcholine M3 receptor antagonist, for the long-term maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease (COPD).aclidinium bromide
benzquinamidebenzquinamide
biperidenA member of the class of piperidines that is N-propylpiperidine in which the methyl hydrogens have been replaced by hydroxy, phenyl, and 5-norbornen-2-yl groups. A muscarinic antagonist affecting both the central and peripheral nervous systems, it is used in the treatment of all forms of Parkinson's disease.biperiden
biperiden hydrochlorideThe hydrochloride salt of biperiden. A muscarinic antagonist affecting both the central and peripheral nervous systems, it is used in the treatment of all forms of Parkinson's disease.biperiden hydrochloride
bromodiphenhydramineA tertiary amino compound that is the 4-bromobenzhydryl ether of 2-(dimethylamino)ethanol. An antihistamine with antimicrobial properties, it is used in the control of cutaneous allergies.bromazine
carbinoxamineAn organochlorine compound that is 2-(4-chlorobenzyl)pyridine in which one of the benzylic hydrogens is substituted by 2-(dimethylamino)ethoxy group. It is an ethanolamine-type antihistamine, used as its maleate salt for treating hay fever, as well as mild cases of Parkinson's disease.carbinoxamine
carbinoxamine maleateThe maleic acid salt of carbinoxamine. An ethanolamine-type antihistamine, used for treating hay fever, as well as mild cases of Parkinson's disease.carbinoxamine maleate
cinnarizinecinnarizine
clemastine2-[(2R)-1-Methylpyrrolidin-2-yl]ethanol in which the hydrogen of the hydroxy group is substituted by a 1-(4-chlorophenyl)-1-phenylethyl group (R configuration). An antihistamine with antimuscarinic and moderate sedative properties, it is used as its fumarate salt for the symptomatic relief of allergic conditions such as rhinitis, urticaria, conjunctivitis and in pruritic (severe itching) skin conditions.clemastine
clemastine fumarateThe fumaric acid salt of clemastine. An antihistamine with antimuscarinic and moderate sedative properties, it is used for the symptomatic relief of allergic conditions such as rhinitis, urticaria, conjunctivitis and in pruritic (severe itching) skin conditions.clemastine fumarate
clozapineA benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia.clozapine
cyclopentolateA carboxylic ester resulting from the formal condensation of (1-hydroxycyclopentyl)(phenyl)acetic acid with N,N-dimethylethanolamine. A tertiary amine antimuscarinic with actions similar to atropine, it is used as its hydrochloride salt to produce mydriasis (excessive dilation of the pupil) and cycloplegia (paralysis of the ciliary muscle of the eye) for opthalmic diagnostic procedures. It acts more quickly than atropine and has a shorter duration of action.cyclopentolate
cycrimineA member of the class of piperidines that is 3-(piperidin-1-yl)propan-1-ol in which one of the hydrogen atoms at the 1-position is substituted by cyclopentyl, and the other is substituted by phenyl. A central anticholinergic, it is used as its hydrochloride salt in the management and treatment of Parkinson's disease.cycrimine
darifenacin2-[(3S)-1-Ethylpyrrolidin-3-yl]-2,2-diphenylacetamide in which one of the hydrogens at the 2-position of the ethyl group is substituted by a 2,3-dihydro-1-benzofuran-5-yl group. It is a selective antagonist for the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions, and is used as the hydrobromide salt in the management of urinary incontinence.darifenacin
darifenacin hydrobromideThe hydrobromide salt of darifenacin. A selective antagonist for the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions, it is used in the management of urinary incontinence.darifenacin hydrobromide
dicyclomineThe ester resulting from the formal condensation of 1-cyclohexylcyclohexanecarboxylic acid with 2-(diethylamino)ethanol. An anticholinergic, it is used as the hydrochloride to treat or prevent spasm in the muscles of the gastrointestinal tract, particularly that associated with irritable bowel syndrome.dicyclomine
dicyclomine hydrochlorideThe hydrochloride salt of dicyclomine. An anticholinergic, it is used to treat or prevent spasm in the muscles of the gastrointestinal tract, particularly that associated with irritable bowel syndrome.dicyclomine hydrochloride
diphemanil methylsulfateThe alkene resulting from the formal Wittig olefination of benzophenone and 1,1-dimethyl-4-bromopiperidinium methylsulfate. A quaternary ammonium anticholinergic, it binds muscarinic acetycholine receptors and thereby decreases secretory excretion of stomach acids, saliva and sweat, It is used topically in the treatment of hyperhidorsis (excessive sweating).diphemanil methylsulfate
diphenhydramineAn ether that is the benzhydryl ether of 2-(dimethylamino)ethanol. It is a H1-receptor antagonist used as a antipruritic and antitussive drug.diphenhydramine
diphenhydramine hydrochlorideThe hydrochloride salt of diphenhydramine.diphenhydramine hydrochloride
flavoxateA carboxylic ester resulting from the formal condensation of 3-methylflavone-8-carboxylic acid with 2-(1-piperidinyl)ethanol.flavoxate
flavoxate hydrochlorideThe hydrochloride salt of flavoxate.flavoxate hydrochloride
himbacineA piperidine alkaloid that is decahydronaphtho[2,3-c]furan-1(3H)-one substituted by a methyl group at position 3 and a 2-[(2R,6S)-1,6-dimethylpiperidin-2-yl]ethenyl group at position 4. It has been isolated from the bark of Australian magnolias.himbacine
methixenemetixene
methoctramineA tetramine that is N,N'-bis(6-aminohexyl)octane-1,8-diamine where the primary amino groups both carry 2-methoxybenzyl substituents.methoctramine
methoctramineA hydrochloride obtained by combining methoctramine with four molar equivalents of hydrochloric acid.methoctramine tetrahydrochloride
nsc 23766An aminopyrimidine that is 6-methylpyrimidine-2,4-diamine in which the amino groups at positions 2 and 4 are substituted by 5-(diethylamino)pentan-2-yl and 4-amino-2-methylquinolin-6-yl groups respectively. An inhibitor of the signalling G-protein known as RAC1 (Ras-related C3 botulinum toxin substrate 1).NSC 23766
nsc 23766A hydrochloride resulting from the formal reaction of NSC 23766 with 3 mol eq. of hydrogen chloride. An inhibitor of the signalling G-protein known as RAC1 (Ras-related C3 botulinum toxin substrate 1).NSC 23766 trihydrochloride
octotropine methylbromideA quaternary ammonium salt resulting from the reaction of the amino group of anisotropine with methyl bromide.anisotropine methylbromide
olanzapineA benzodiazepine that is 10H-thieno[2,3-b][1,5]benzodiazepine substituted by a methyl group at position 2 and a 4-methylpiperazin-1-yl group at position 4.olanzapine
orphenadrineA tertiary amino compound which is the phenyl-o-tolylmethyl ether of 2-(dimethylamino)ethanol.orphenadrine
orphenadrine citrateA citrate salt which comprises equimolar amounts of orphenadrine and citric acid.orphenadrine citrate
orphenadrine hydrochlorideA hydrochloride comprising equimolar amounts of ophenadrine and hydrogen chloride.orphenadrine hydrochloride
oxybutyninA racemate comprising equimolar amounts of (R)-oxybutynin and esoxybutynin. An antispasmodic used for the treatment of overactive bladder.4-(diethylamino)but-2-yn-1-ol; oxybutynin
pirenzepinepirenzepine
pizotylineA benzocycloheptathiophene that is 9,10-dihydro-4H-benzo[4,5]cyclohepta[1,2-b]thiophene 4-ylidene)-1-methylpiperidine which is joined from the 4 position to the 4 position of an N-methylpiperidine moiety by a double bond. It is a sedating antihistamine, with strong serotonin antagonist and weak antimuscarinic activity. It is generally used as the malate salt for the treatment of migraine and the prevention of headache attacks during cluster periods.pizotifen
procyclidineA tertiary alcohol that consists of propan-1-ol substituted by a cyclohexyl and a phenyl group at position 1 and a pyrrolidin-1-yl group at position 3.procyclidine
profenamineA member of the class of phenothiazines that is phenothiazine in which the hydrogen attached to the nitrogen is substituted by a 2-(diethylamino)propyl group. An antimuscarinic, it is used as the hydrochloride for the symptomatic treatment of Parkinson's disease.profenamine
profenamine hydrochlorideThe monohydrochloride salt of profenamine. An antimuscarinic, it is used for the symptomatic treatment of Parkinson's disease.profenamine hydrochloride
promazineA phenothiazine deriative in which the phenothiazine tricycle has a 3-(dimethylaminopropyl) group at the N-10 position.promazine
propiomazineA member of the class of phenothiazines that is 10H-phenothiazine substituted by a 2-(dimethylamino)propyl group at nitrogen atom and a propanoyl group at position 2.propiomazine
propyromazineAn organic bromide salt of propyromazine. It is a muscarinic antagonist which has antispasmodic potential.propyromazine bromide
quinidineA cinchona alkaloid consisting of cinchonine with the hydrogen at the 6-position of the quinoline ring substituted by methoxy.quinidine
thiethylperazineA member of the class of phenothiazines that is perazine substituted by a ethylsulfanyl group at position 2.thiethylperazine
tiquizium bromideA organic bromide salt of tiquizium. It is an antispasmodic drug used for the treatment of convulsion and hypermobility in gastritis, gastric ulcer, duodenal ulcer, enteritis, irritable bowel syndrome, gallbladder disease, biliary tract disease and urolithiasis.tiquizium bromide
tolterodinetolterodine
tramadolA 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol in which both stereocentres have R-configuration; the (R,R)-enantiomer of the racemic opioid analgesic tramadol, it exhibits ten-fold higher analgesic potency than the (S,S)-enantiomer.(R,R)-tramadol
tramadol hydrochlorideA hydrochloride resulting from the reaction of (R,R)-tramadol with 1 molar equivalent of hydrogen chloride; the (R,R)-enantiomer of the racemic opioid analgesic tramadol hydrochloride, it exhibits ten-fold higher analgesic potency than the (S,S)-enantiomer.(R,R)-tramadol hydrochloride
tridihexethyltridihexethyl
ziprasidoneA piperazine compound having 1,2-benzothiazol-3-yl- and 2-(6-chloro-1,3-dihydro-2-oxindol-5-yl)ethyl substituents attached to the nitrogen atoms.ziprasidone

Research

Studies (40,508)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199011,645 (28.75)18.7374
1990's6,640 (16.39)18.2507
2000's9,390 (23.18)29.6817
2010's9,740 (24.04)24.3611
2020's3,093 (7.64)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials6,615 (13.74%)5.53%
Reviews4,277 (8.88%)6.00%
Case Studies6,296 (13.07%)4.05%
Observational233 (0.48%)0.25%
Other30,739 (63.83%)84.16%

Protein Targets (390)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency17.782811
15-lipoxygenase, partialHomo sapiens (human)Potency25.118911
67.9K proteinVaccinia virusPotency19.091922
acetylcholinesteraseHomo sapiens (human)Potency20.3645212
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency21.986514
Alpha-synucleinHomo sapiens (human)Potency3.441913
AR proteinHomo sapiens (human)Potency20.9819940
aryl hydrocarbon receptorHomo sapiens (human)Potency28.872726
arylsulfatase AHomo sapiens (human)Potency19.090216
ATAD5 protein, partialHomo sapiens (human)Potency9.017425
Ataxin-2Homo sapiens (human)Potency25.064728
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency11.984537
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency21.265823
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency8.390313
Bloom syndrome protein isoform 1Homo sapiens (human)Potency44.075128
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency72.104314
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency33.491513
caspase-3Cricetulus griseus (Chinese hamster)Potency29.849311
caspase-3Homo sapiens (human)Potency33.491513
Caspase-7Cricetulus griseus (Chinese hamster)Potency29.849311
Cellular tumor antigen p53Homo sapiens (human)Potency19.4382216
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency14.789326
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency20.365214
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency27.829822
Chain A, Beta-lactamaseEscherichia coli K-12Potency144.741014
Chain A, CruzipainTrypanosoma cruziPotency39.810711
Chain A, Ferritin light chainEquus caballus (horse)Potency10.000011
Chain A, HADH2 proteinHomo sapiens (human)Potency26.527225
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency44.245213
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency45.553615
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency10.577215
Chain B, HADH2 proteinHomo sapiens (human)Potency26.527225
chaperonin-containing TCP-1 beta subunit homologHomo sapiens (human)Potency15.848911
chromobox protein homolog 1Homo sapiens (human)Potency42.998929
cytochrome P450 2C19 precursorHomo sapiens (human)Potency13.044115
cytochrome P450 2C9 precursorHomo sapiens (human)Potency29.796914
cytochrome P450 2C9, partialHomo sapiens (human)Potency15.369917
cytochrome P450 2D6Homo sapiens (human)Potency6.5155120
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency12.5252115
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency10.8633228
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency13.4983222
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency16.982215
D(1A) dopamine receptorHomo sapiens (human)Potency5.4660311
D(1A) dopamine receptorSus scrofa (pig)Potency14.689211
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency16.271012
DNA polymerase betaHomo sapiens (human)Potency59.621812
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency70.351913
DNA polymerase kappa isoform 1Homo sapiens (human)Potency12.955113
dopamine D1 receptorHomo sapiens (human)Potency1.860312
endonuclease IVEscherichia coliPotency25.948512
estrogen nuclear receptor alphaHomo sapiens (human)Potency21.34521040
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency26.058626
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency32.1075937
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency23.8341223
EWS/FLI fusion proteinHomo sapiens (human)Potency28.1640416
eyes absent homolog 2 isoform aHomo sapiens (human)Potency22.387211
farnesoid X nuclear receptorHomo sapiens (human)Potency20.666525
flap endonuclease 1Homo sapiens (human)Potency14.514915
Fumarate hydrataseHomo sapiens (human)Potency26.469816
GVesicular stomatitis virusPotency15.369917
GABA theta subunitRattus norvegicus (Norway rat)Potency11.0007115
GALC proteinHomo sapiens (human)Potency0.389312
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency11.0007115
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency11.0007115
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency11.0007115
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency11.0007115
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency11.0007115
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency11.0007115
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency11.0007115
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency11.0007115
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency11.0007115
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency11.0007115
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency11.0007115
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency11.0007115
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency11.0007115
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency11.0007115
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency11.0007115
gemininHomo sapiens (human)Potency9.1959310
GLI family zinc finger 3Homo sapiens (human)Potency16.2860238
glp-1 receptor, partialHomo sapiens (human)Potency12.046222
GLS proteinHomo sapiens (human)Potency17.958229
glucocerebrosidaseHomo sapiens (human)Potency13.548113
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency24.6538313
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency30.047412
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency3.662611
heat shock protein beta-1Homo sapiens (human)Potency33.488923
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency20.5004232
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency34.857014
Histone H2A.xCricetulus griseus (Chinese hamster)Potency53.380126
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency31.622811
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency15.369917
huntingtin isoform 2Homo sapiens (human)Potency35.481311
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency17.968614
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency14.240026
IDH1Homo sapiens (human)Potency19.253212
importin subunit beta-1 isoform 1Homo sapiens (human)Potency3.662611
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency15.3699114
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency7.4570112
Integrin alpha-IIbHomo sapiens (human)Potency12.589312
Integrin beta-3Homo sapiens (human)Potency12.589312
Interferon betaHomo sapiens (human)Potency13.1053314
lamin isoform A-delta10Homo sapiens (human)Potency13.5502216
lethal factor (plasmid)Bacillus anthracis str. A2012Potency17.418316
LuciferasePhotinus pyralis (common eastern firefly)Potency21.698913
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency9.354633
M-phase phosphoprotein 8Homo sapiens (human)Potency32.238216
Microtubule-associated protein tauHomo sapiens (human)Potency18.549628
mitogen-activated protein kinase 1Homo sapiens (human)Potency17.9831211
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency1.0096218
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency11.220211
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Potency11.220211
neuropeptide S receptor isoform AHomo sapiens (human)Potency18.927236
NFKB1 protein, partialHomo sapiens (human)Potency1.000022
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency7.079511
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency22.4564312
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency22.027414
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency15.280314
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency17.6096316
P53Homo sapiens (human)Potency70.794611
ParkinHomo sapiens (human)Potency39.810711
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency16.250316
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency61.255116
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency22.812725
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency27.3280415
phosphopantetheinyl transferaseBacillus subtilisPotency76.110412
PINK1Homo sapiens (human)Potency39.810711
plasminogen precursorMus musculus (house mouse)Potency1.258911
polyproteinZika virusPotency26.469816
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency12.589311
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency14.9225110
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency8.3160122
PPM1D proteinHomo sapiens (human)Potency9.146414
pregnane X nuclear receptorHomo sapiens (human)Potency21.1193318
progesterone receptorHomo sapiens (human)Potency23.629038
RAR-related orphan receptor gammaMus musculus (house mouse)Potency20.8845211
regulator of G-protein signaling 4Homo sapiens (human)Potency22.850217
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency27.1708325
retinoid X nuclear receptor alphaHomo sapiens (human)Potency16.8029313
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency11.081923
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency26.679511
shiga toxin 1 B subunitEscherichia coli O157:H7Potency0.317711
shiga toxin 1 variant A subunitEscherichia coli O157:H7Potency0.317711
SMAD family member 2Homo sapiens (human)Potency39.599423
SMAD family member 3Homo sapiens (human)Potency39.599423
Smad3Homo sapiens (human)Potency0.112211
snurportin-1Homo sapiens (human)Potency3.662611
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency16.2384222
survival motor neuron protein isoform dHomo sapiens (human)Potency14.480914
TAR DNA-binding protein 43Homo sapiens (human)Potency0.631011
TDP1 proteinHomo sapiens (human)Potency21.2162261
thioredoxin glutathione reductaseSchistosoma mansoniPotency60.374012
thioredoxin reductaseRattus norvegicus (Norway rat)Potency28.8877411
ThrombopoietinHomo sapiens (human)Potency11.5543210
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency27.8198246
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency95.657033
thyroid stimulating hormone receptorHomo sapiens (human)Potency25.4026621
thyrotropin-releasing hormone receptorHomo sapiens (human)Potency13.450411
transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Potency12.589311
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency16.271012
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency1.258911
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency1.258911
USP1 protein, partialHomo sapiens (human)Potency42.248515
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency19.7479230
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency0.595511
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency80.729714
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency30.047412

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
3-hydroxy-3-methylglutaryl-coenzyme A reductase Rattus norvegicus (Norway rat)Ki0.014013
5-hydroxytryptamine receptor 1AHomo sapiens (human)IC500.150011
5-hydroxytryptamine receptor 1AMus musculus (house mouse)IC502.000011
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC501.888836
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki0.81811730
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.45221012
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC501.474835
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki0.969624
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)IC500.587011
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Ki0.023211
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)IC500.587011
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)Ki0.023211
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC500.1886515
5-hydroxytryptamine receptor 2AMus musculus (house mouse)IC500.028011
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC500.08511112
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.01854774
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.01082329
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC500.6748212
5-hydroxytryptamine receptor 2BMus musculus (house mouse)IC500.028011
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC500.035578
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.3551414
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki0.013678
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC500.2300311
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC500.032889
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.03512547
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki0.01341011
5-hydroxytryptamine receptor 2C Mus musculus (house mouse)IC500.028011
5-hydroxytryptamine receptor 3ACavia porcellus (domestic guinea pig)IC50110.000011
5-hydroxytryptamine receptor 3AHomo sapiens (human)Ki0.320435
5-hydroxytryptamine receptor 3AMus musculus (house mouse)Ki0.032011
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Ki0.053011
5-hydroxytryptamine receptor 3BHomo sapiens (human)Ki0.353924
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)Ki0.053011
5-hydroxytryptamine receptor 3CHomo sapiens (human)Ki0.353924
5-hydroxytryptamine receptor 3DHomo sapiens (human)Ki0.353924
5-hydroxytryptamine receptor 3EHomo sapiens (human)Ki0.353924
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC500.270929
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.146528
5-hydroxytryptamine receptor 4Homo sapiens (human)Ki0.223911
5-hydroxytryptamine receptor 5AHomo sapiens (human)Ki1.000011
5-hydroxytryptamine receptor 6Homo sapiens (human)IC500.513149
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.06192847
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)IC5037.125018
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki0.29013041
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki0.009422
AcetylcholinesteraseElectrophorus electricus (electric eel)IC5022.720011
AcetylcholinesteraseHomo sapiens (human)IC50280.23281011
AcetylcholinesteraseHomo sapiens (human)Ki3,492.517167
Acetylcholinesterase Bos taurus (cattle)Ki173.200022
Adenosine receptor A1Rattus norvegicus (Norway rat)Ki0.219012
Adenylate cyclase type 1 Rattus norvegicus (Norway rat)IC500.140011
Adenylate cyclase type 2Rattus norvegicus (Norway rat)IC500.140011
Adenylate cyclase type 3Rattus norvegicus (Norway rat)IC500.140011
Adenylate cyclase type 4Rattus norvegicus (Norway rat)IC500.140011
Adenylate cyclase type 5Rattus norvegicus (Norway rat)IC500.140011
Adenylate cyclase type 6Rattus norvegicus (Norway rat)IC500.140011
Adenylate cyclase type 8Rattus norvegicus (Norway rat)IC500.140011
Adenylyl cyclase 7 Rattus norvegicus (Norway rat)IC500.140011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC502.314917
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki2.295517
Alpha-1A adrenergic receptorHomo sapiens (human)IC500.011011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC500.056778
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.02391017
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.45661018
Alpha-1B adrenergic receptorHomo sapiens (human)IC500.011011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC500.056778
Alpha-1B adrenergic receptorHomo sapiens (human)Ki0.0223914
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.46011018
Alpha-1D adrenergic receptorHomo sapiens (human)IC500.225026
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC500.056778
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.05101019
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.5450815
Alpha-2A adrenergic receptorHomo sapiens (human)IC500.625216
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC502.435323
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.2087616
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki0.067668
Alpha-2B adrenergic receptorHomo sapiens (human)IC500.818316
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC502.435323
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.3139413
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki0.070246
Alpha-2C adrenergic receptorHomo sapiens (human)IC500.307815
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC502.435323
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.1353514
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki0.070246
Amyloid-beta precursor proteinHomo sapiens (human)Ki0.005911
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC5027.074727
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki14.341115
Aspartate aminotransferase, cytoplasmicHomo sapiens (human)IC505.390011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000016
ATP-dependent translocase ABCB1Homo sapiens (human)IC5049.233399
ATP-dependent translocase ABCB1Mus musculus (house mouse)IC5011.500044
ATP-dependent translocase ABCB1Homo sapiens (human)Ki3.624055
Beta-1 adrenergic receptorHomo sapiens (human)IC500.316211
Beta-1 adrenergic receptorHomo sapiens (human)Ki0.180011
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)Ki18.000022
Beta-1 adrenergic receptor Cavia porcellus (domestic guinea pig)Ki0.150011
Beta-2 adrenergic receptorRattus norvegicus (Norway rat)IC500.140011
Beta-2 adrenergic receptorCavia porcellus (domestic guinea pig)Ki0.015911
Beta-2 adrenergic receptorHomo sapiens (human)Ki0.038422
Beta-2 adrenergic receptorRattus norvegicus (Norway rat)Ki10.000011
Beta-3 adrenergic receptorRattus norvegicus (Norway rat)Ki10.000011
Bile salt export pumpHomo sapiens (human)IC50224.2825520
Bile salt export pumpRattus norvegicus (Norway rat)IC50196.500011
Calcium release-activated calcium channel protein 1Homo sapiens (human)IC50500.000022
Calmodulin-1Homo sapiens (human)IC5080.000022
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000016
Carboxylic ester hydrolase Rattus norvegicus (Norway rat)IC500.977211
Carboxylic ester hydrolase Equus caballus (horse)Ki0.020011
Cholecystokinin receptor type ACavia porcellus (domestic guinea pig)Ki0.060011
CholinesteraseEquus caballus (horse)IC503.230023
CholinesteraseHomo sapiens (human)IC500.896077
CholinesteraseHomo sapiens (human)Ki4,033.346733
CruzipainTrypanosoma cruziIC50212.000022
Cytochrome P450 2C19Homo sapiens (human)IC500.600012
Cytochrome P450 2C9 Homo sapiens (human)IC5032.050012
Cytochrome P450 2C9 Homo sapiens (human)Ki32.000011
Cytochrome P450 2D1Rattus norvegicus (Norway rat)IC5019.900011
Cytochrome P450 2D26Rattus norvegicus (Norway rat)IC502.800011
Cytochrome P450 2D3Rattus norvegicus (Norway rat)IC5026.900011
Cytochrome P450 2D4Rattus norvegicus (Norway rat)IC5047.200011
Cytochrome P450 2D6Homo sapiens (human)IC502.13094648
Cytochrome P450 2D6Homo sapiens (human)Ki0.035744
Cytochrome P450 2J2Homo sapiens (human)IC5032.050012
Cytochrome P450 3A4Homo sapiens (human)IC5039.000022
Cytochrome P450 3A4Homo sapiens (human)Ki0.028016
DBos taurus (cattle)IC502.770033
DRattus norvegicus (Norway rat)IC501.0016915
DBos taurus (cattle)Ki0.4200813
DRattus norvegicus (Norway rat)Ki0.18651323
D(1A) dopamine receptorHomo sapiens (human)IC501.044514
D(1A) dopamine receptorHomo sapiens (human)Ki0.19681323
D(1B) dopamine receptorRattus norvegicus (Norway rat)IC500.955469
D(1B) dopamine receptorHomo sapiens (human)Ki0.489022
D(1B) dopamine receptorRattus norvegicus (Norway rat)Ki0.174222
D(2) dopamine receptorBos taurus (cattle)IC501.525066
D(2) dopamine receptorHomo sapiens (human)IC501.8999915
D(2) dopamine receptorMus musculus (house mouse)IC500.290012
D(2) dopamine receptorRattus norvegicus (Norway rat)IC500.66532029
D(2) dopamine receptorBos taurus (cattle)Ki0.690011
D(2) dopamine receptorChlorocebus aethiops (grivet)Ki0.254022
D(2) dopamine receptorHomo sapiens (human)Ki0.094286113
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.12992654
D(3) dopamine receptorHomo sapiens (human)IC500.361128
D(3) dopamine receptorRattus norvegicus (Norway rat)IC500.955469
D(3) dopamine receptorChlorocebus aethiops (grivet)Ki0.466011
D(3) dopamine receptorHomo sapiens (human)Ki0.32553654
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki0.281356
D(4) dopamine receptorHomo sapiens (human)IC500.08681213
D(4) dopamine receptorRattus norvegicus (Norway rat)IC500.955469
D(4) dopamine receptorHomo sapiens (human)Ki0.17525161
D(4) dopamine receptorRattus norvegicus (Norway rat)Ki0.088055
Delta-type opioid receptorHomo sapiens (human)Ki10.000011
Endothelin receptor type BHomo sapiens (human)Ki0.012622
Endothelin receptor type BRattus norvegicus (Norway rat)Ki0.012611
Estrogen receptor 1Homo sapiens (human)IC5050.000011
estrogen receptor beta isoform 1Homo sapiens (human)IC5050.000011
GABA theta subunitRattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC501.000013
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)IC501.000012
Gastrin/cholecystokinin type B receptorMus musculus (house mouse)Ki0.003812
Glucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)Ki497.200011
Glutamate receptor ionotropic, NMDA 1Homo sapiens (human)IC500.138011
Glutamate receptor ionotropic, NMDA 1Homo sapiens (human)Ki3.850012
Glutamate receptor ionotropic, NMDA 2AHomo sapiens (human)IC500.138011
Glutamate receptor ionotropic, NMDA 2AHomo sapiens (human)Ki3.850012
Glutamate receptor ionotropic, NMDA 2BHomo sapiens (human)Ki3.850012
Glutamate receptor ionotropic, NMDA 2CHomo sapiens (human)Ki3.850012
Glutamate receptor ionotropic, NMDA 2DHomo sapiens (human)Ki3.850012
Glutamate receptor ionotropic, NMDA 3AHomo sapiens (human)Ki3.850012
Glutamate receptor ionotropic, NMDA 3BHomo sapiens (human)Ki3.850012
Histamine H1 receptorHomo sapiens (human)IC5011.9469210
Histamine H1 receptorRattus norvegicus (Norway rat)IC500.023012
Histamine H1 receptorCavia porcellus (domestic guinea pig)Ki0.012612
Histamine H1 receptorHomo sapiens (human)Ki0.03411225
Histamine H1 receptorRattus norvegicus (Norway rat)Ki0.005012
Histamine H2 receptorHomo sapiens (human)IC503.084815
Histamine H2 receptorHomo sapiens (human)Ki3.033415
Histamine H3 receptorHomo sapiens (human)Ki0.815522
Histamine H4 receptorHomo sapiens (human)Ki10.808844
Histidine-rich protein PFHRP-IIPlasmodium falciparum (malaria parasite P. falciparum)IC50325.000011
Kappa-type opioid receptorHomo sapiens (human)Ki10.000011
Lethal(3)malignant brain tumor-like protein 1Homo sapiens (human)IC50100.000011
Lethal(3)malignant brain tumor-like protein 3Homo sapiens (human)IC5054.000011
Lethal(3)malignant brain tumor-like protein 4Homo sapiens (human)IC50100.000011
MBT domain-containing protein 1Homo sapiens (human)IC50100.000011
Mu-type opioid receptorHomo sapiens (human)IC502.272011
Mu-type opioid receptorHomo sapiens (human)Ki1.661022
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki0.000811
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC5038.100022
Multidrug and toxin extrusion protein 2Homo sapiens (human)IC50100.000011
Multidrug resistance-associated protein 4Homo sapiens (human)IC50118.466716
Muscarinic acetylcholine receptorCavia porcellus (domestic guinea pig)Ki0.065722
Muscarinic acetylcholine receptor DM1Drosophila melanogaster (fruit fly)Ki1.260526
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC500.16632127
Muscarinic acetylcholine receptor M1Mus musculus (house mouse)IC500.750013
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC500.56933853
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki0.45653649
Muscarinic acetylcholine receptor M1Mus musculus (house mouse)Ki0.107211
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki0.04031015
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC500.26111318
Muscarinic acetylcholine receptor M2Mus musculus (house mouse)IC500.510036
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC500.60294052
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.21582838
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Ki1.15741217
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC500.15911624
Muscarinic acetylcholine receptor M3Mus musculus (house mouse)IC500.750013
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)IC500.59733951
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.41692942
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)Ki0.2152912
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC500.34021321
Muscarinic acetylcholine receptor M4Mus musculus (house mouse)IC500.750013
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC500.59723850
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.22221830
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)Ki0.0799710
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC500.1435917
Muscarinic acetylcholine receptor M5Mus musculus (house mouse)IC500.750013
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC500.59723850
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki0.31711525
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)Ki0.062646
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)IC5031.253816
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)Ki14.341115
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CIC506.800012
Polyunsaturated fatty acid lipoxygenase ALOX15Oryctolagus cuniculus (rabbit)IC502.768011
Potassium voltage-gated channel subfamily A member 5Homo sapiens (human)IC507.300011
Potassium voltage-gated channel subfamily D member 2Rattus norvegicus (Norway rat)IC502.200011
Potassium voltage-gated channel subfamily D member 3Homo sapiens (human)IC5012.589222
Potassium voltage-gated channel subfamily E member 1Homo sapiens (human)IC5049.692722
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC505.92322151
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki15.4170612
Potassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)IC5049.692722
Protein orai-2Homo sapiens (human)IC50500.000022
Protein orai-3Homo sapiens (human)IC50500.000022
Ras-related C3 botulinum toxin substrate 1Homo sapiens (human)IC5095.000011
Ras-related C3 botulinum toxin substrate 1Mus musculus (house mouse)IC506.300022
Sigma intracellular receptor 2Homo sapiens (human)Ki0.025111
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC500.074815
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)IC501.000011
Sigma non-opioid intracellular receptor 1Cavia porcellus (domestic guinea pig)Ki0.009011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki1.238237
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC5017.336266
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC502.952914
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)Ki0.239245
Sodium-dependent dopamine transporter Homo sapiens (human)IC500.801513
Sodium-dependent dopamine transporter Homo sapiens (human)Ki0.390425
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC502.314917
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki2.009128
Sodium-dependent serotonin transporterHomo sapiens (human)IC500.642615
Sodium-dependent serotonin transporterHomo sapiens (human)Ki2.304439
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Ki0.021011
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)IC5018.350022
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)Ki10.300022
Solute carrier family 22 member 1 Homo sapiens (human)IC5047.640058
Solute carrier family 22 member 1 Homo sapiens (human)Ki17.500011
Solute carrier family 22 member 2Homo sapiens (human)IC502.500011
Solute carrier family 22 member 2Rattus norvegicus (Norway rat)IC5023.300022
Solute carrier family 22 member 2Rattus norvegicus (Norway rat)Ki19.100011
Solute carrier organic anion transporter family member 1A1Rattus norvegicus (Norway rat)Ki9.270011
Solute carrier organic anion transporter family member 1A4Rattus norvegicus (Norway rat)Ki120.000011
Testosterone 17-beta-dehydrogenase 3Rattus norvegicus (Norway rat)IC500.000111
TransporterRattus norvegicus (Norway rat)Ki0.818625
Trypanothione reductaseTrypanosoma cruziIC50108.000011
Trypanothione reductaseTrypanosoma cruziKi59.100011
UDP-glucuronosyltransferase 1-6Homo sapiens (human)IC50273.200015
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)IC50273.200015
UDP-glucuronosyltransferase 1A4Homo sapiens (human)IC50273.200015
UDP-glucuronosyltransferase 2B10 Homo sapiens (human)IC50273.200015
UDP-glucuronosyltransferase 2B7Homo sapiens (human)IC50273.200015
Voltage-dependent L-type calcium channel subunit alpha-1CCavia porcellus (domestic guinea pig)IC5016.600011
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC50327.965855
Voltage-dependent L-type calcium channel subunit alpha-1CRattus norvegicus (Norway rat)Ki1.080011
Voltage-dependent L-type calcium channel subunit alpha-1DRattus norvegicus (Norway rat)Ki1.080011
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC505.000022
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC505.000022
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC505.000022
Voltage-dependent L-type calcium channel subunit alpha-1SRattus norvegicus (Norway rat)Ki1.080011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1AHomo sapiens (human)Kd1.258911
5-hydroxytryptamine receptor 2BHomo sapiens (human)EC500.020011
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Kd0.125912
5-hydroxytryptamine receptor 2CHomo sapiens (human)EC500.250011
AlbuminRattus norvegicus (Norway rat)Kd78.800011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Kd0.512911
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Kd0.512911
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Kd0.512911
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Kd20.417411
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Kd20.417411
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Kd20.417411
Angiotensin-converting enzyme 2 Homo sapiens (human)EC507.860011
Beta-1 adrenergic receptorHomo sapiens (human)EC500.039811
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)EC502.310011
Beta-2 adrenergic receptorHomo sapiens (human)EC500.004944
Calmodulin Bos taurus (cattle)Kd61.000011
D(2) dopamine receptorHomo sapiens (human)EC5010.000011
Histamine H1 receptorHomo sapiens (human)EC500.000411
Histamine H1 receptorHomo sapiens (human)Kd0.001612
Histamine H4 receptorHomo sapiens (human)Kd0.029444
Major prion proteinHomo sapiens (human)EC505.000011
Mu-type opioid receptorHomo sapiens (human)EC501.000011
Muscarinic acetylcholine receptorCavia porcellus (domestic guinea pig)Kd0.255124
Muscarinic acetylcholine receptor M1Homo sapiens (human)EC5055.000012
Muscarinic acetylcholine receptor M1Homo sapiens (human)Kd0.056233
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Kd1.995311
Muscarinic acetylcholine receptor M2Homo sapiens (human)EC5010.000011
Muscarinic acetylcholine receptor M2Sus scrofa (pig)EC502.999211
Muscarinic acetylcholine receptor M2Homo sapiens (human)Kd0.018446
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Kd1.995311
Muscarinic acetylcholine receptor M3Homo sapiens (human)EC502.522044
Muscarinic acetylcholine receptor M3Homo sapiens (human)Kd0.007411
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)Kd1.995311
Muscarinic acetylcholine receptor M4Homo sapiens (human)EC5010.000011
Muscarinic acetylcholine receptor M4Homo sapiens (human)Kd0.007411
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)Kd1.995311
Muscarinic acetylcholine receptor M5Homo sapiens (human)Kd0.007411
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)Kd1.995311
ORF73Human gammaherpesvirus 8EC5075.000011
Procathepsin LHomo sapiens (human)EC507.860011
Proteasome subunit alpha type-6Homo sapiens (human)EC5011.900011
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusEC507.860011
Replicase polyprotein 1abBetacoronavirus England 1EC507.860011
Replicase polyprotein 1abHuman coronavirus 229EEC507.860011
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2EC507.860011
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusEC507.860011
short transient receptor potential channel 6 isoform 1Mus musculus (house mouse)EC508.065012
Spike glycoproteinBetacoronavirus England 1EC507.860011
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusEC507.860011
Transmembrane protease serine 2Homo sapiens (human)EC507.860011
voltage-dependent T-type calcium channel subunit alpha-1H isoform aHomo sapiens (human)EC500.000011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 2AHomo sapiens (human)Activity0.002812
5-hydroxytryptamine receptor 2AHomo sapiens (human)INH0.005411
5-hydroxytryptamine receptor 6Homo sapiens (human)INH0.006411
ATP-dependent translocase ABCB1Homo sapiens (human)Km22.480034
Cytochrome P450 2C19Homo sapiens (human)Km25.300011
Cytochrome P450 2C9 Homo sapiens (human)Km25.300011
Cytochrome P450 2D6Homo sapiens (human)Km43.766733
Cytochrome P450 2J2Homo sapiens (human)Km25.300011
Cytochrome P450 3A4Homo sapiens (human)Km45.240045
D(1A) dopamine receptorHomo sapiens (human)Kb10.000011
D(1B) dopamine receptorHomo sapiens (human)Kb10.000011
D(2) dopamine receptorHomo sapiens (human)Activity0.132812
D(2) dopamine receptorHomo sapiens (human)Kb10.000011
D(2) dopamine receptorHomo sapiens (human)pKi0.006911
D(3) dopamine receptorHomo sapiens (human)Kb10.000011
D(3) dopamine receptorHomo sapiens (human)pKi0.006611
D(4) dopamine receptorHomo sapiens (human)Kb10.000011
D(4) dopamine receptorHomo sapiens (human)pKi0.007311
FAD-linked sulfhydryl oxidase ALRHomo sapiens (human)AC500.369011
Histamine H1 receptorHomo sapiens (human)Activity0.022112
Histamine H1 receptorHomo sapiens (human)INH0.001211
Histamine H1 receptorCavia porcellus (domestic guinea pig)K0.50.006111
Histamine H2 receptorCavia porcellus (domestic guinea pig)K0.50.004117
Histamine H3 receptorCavia porcellus (domestic guinea pig)K0.50.006111
Histamine N-methyltransferaseHomo sapiens (human)Activity0.010011
Multidrug resistance protein 1aRattus norvegicus (Norway rat)Km5.000011
Muscarinic acetylcholine receptor M1Homo sapiens (human)KA0.016012
Muscarinic acetylcholine receptor M1Homo sapiens (human)Kb0.010011
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Kb0.008512
Muscarinic acetylcholine receptor M2Homo sapiens (human)Kb0.080125
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 S288CINH50.800012
RAC-alpha serine/threonine-protein kinaseHomo sapiens (human)Activity50.000011
Snq2pSaccharomyces cerevisiae EC1118INH67.100012
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)Km2.200011
Solute carrier family 22 member 1 Homo sapiens (human)Activity5.400011
UDP-glucuronosyltransferase 1A4Homo sapiens (human)Km144.500022