Page last updated: 2024-08-05 15:14:30

local anaesthetic

Any member of a group of drugs that reversibly inhibit the propagation of signals along nerves. Wide variations in potency, stability, toxicity, water-solubility and duration of action determine the route used for administration, e.g. topical, intravenous, epidural or spinal block.

ChEBI ID: 36333

Members (38)

MemberDefinitionClass
1-octanesulfonic acidoctane-1-sulfonic acid
benoxinateA benzoate ester in which 4-amino-3-butoxybenzoic acid and 2-(diethylamino)ethanol have combined to form the ester bond; an ester-based local anaesthetic (ester "caine") used especially in ophthalmology and otolaryngology.oxybuprocaine
benoxinate hydrochlorideThe monohydrochloride salt of oxybuprocaine.oxybuprocaine hydrochloride
benzydamineA member of the class of indazoles carrying benzyl and 3-(dimethylamino)propyl groups at positions 1 and 3 respectively. A locally-acting nonsteroidal anti-inflammatory drug that also exhibits local anaesthetic and analgesic properties.benzydamine
bromoethaneA bromoalkane that is ethane carrying a bromo substituent. It is an alkylating agent used as a chemical intermediate in various organic syntheses.bromoethane
buclizineAn N-alkylpiperazine carrying (4-chlorophenyl)(phenyl)methyl and 4-tert-butylbenzyl groups.buclizine
bupivacaine hydrochlorideA racemate composed of equimolar amounts of dextrobupivacaine hydrochloride and levobupivacaine hydrochloride. The monohydrate form is commonly used as a local anaesthetic.1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide hydrochloride; bupivacaine hydrochloride (anhydrous)
butambenAn amino acid ester resulting from the formal condensation of the carboxy group of 4-aminobenzoic acid with the hydroxy group of butan-1-ol. Its local anaesthetic properties have been used for surface anaesthesia of the skin and mucous membranes, and for relief of pain and itching associated with some anorectal disorders.butamben
cassaineA tricyclic diterpenoid isolated from several plant species of the genus Erythrophleum.cassaine
chloroprocaineProcaine in which one of the hydrogens ortho- to the carboxylic acid group is substituted by chlorine. It is used as its monohydrochloride salt as a local anaesthetic, particularly for oral surgery. It has the advantage over lidocaine of constricting blood vessels, so reducing bleeding.chloroprocaine
cocaineA tropane alkaloid obtained from leaves of the South American shrub Erythroxylon coca.cocaine
cocaine hydrochlorideThe hydrochloride salt of cocaine. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse.cocaine hydrochloride
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
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
ethyl chlorideThe simplest and least toxic member of the class of chloroethanes, that is ethane in which a single hydrogen is substituted by a chlorine. A colourless gas at room temperature and pressure (boiling point 12degreeC), it is used as a mild topical anaesthetic to numb the skin prior to ear piercing, skin biopsies, etc., and is also used in the treatment of sports injuries. It was formerly used in the production of tetraethyllead.chloroethane
etidocaineAn amino acid amide in which 2-[ethyl(propyl)amino]butanoic acid and 2,6-dimethylaniline have combined to form the amide bond. Used as a local anaesthetic (amide caine), it has rapid onset and long action properties, similar to bupivacaine, and is given by injection during surgical procedures and during labour and delivery.etidocaine
levobupivacaineThe (S)-(-)-enantiomer of bupivacaine.levobupivacaine
levobupivacaine hydrochlorideThe monohydrochloride salt of levobupivacaine.levobupivacaine hydrochloride (anhydrous)
lidocaineThe monocarboxylic acid amide resulting from the formal condensation of N,N-diethylglycine with 2,6-dimethylaniline.lidocaine
lidocaine hydrochlorideThe anhydrous form of the hydrochloride salt of lidocaine.lidocaine hydrochloride
lidocaine hydrochlorideThe monohydrate form of lidocaine hydrochloride.lidocaine hydrochloride monohydrate
mepivacaineA piperidinecarboxamide in which N-methylpipecolic acid and 2,6-dimethylaniline have combined to form the amide bond. It is used as a local amide-type anaesthetic.mepivacaine
mepivacaine hydrochlorideThe hydrochloride salt of mepivacaine. It is used as a local anaesthetic.mepivacaine 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
phenazopyridineA diaminopyridine that is 2,6-diaminopyridine substituted at position 3 by a phenylazo group. A local anesthetic that has topical analgesic effect on mucosa lining of the urinary tract. Its use is limited by problems with toxicity (primarily blood disorders) and potential carcinogenicity.phenazopyridine
phenazopyridine hydrochlorideA hydrochloride obtained by combining phenazopyridine with one equivalent of hydrochloric acid. A local anesthetic that has topical analgesic effect on mucosa lining of the urinary tract. Its use is limited by problems with toxicity (primarily blood disorders) and potential carcinogenicity.phenazopyridine hydrochloride
pramoxineA member of the class of morpholines that is morpholine substituted at the nitrogen atom by a 3-(4-butoxyphenoxy)propyl group.pramocaine
prilocaineAn amino acid amide in which N-propyl-DL-alanine and 2-methylaniline have combined to form the amide bond; used as a local anaesthetic.prilocaine
prilocaine hydrochlorideThe monohydrochloride salt of prilocaine.prilocaine hydrochloride
procaineA benzoate ester, formally the result of esterification of 4-aminobenzoic acid with 2-diethylaminoethanol but formed experimentally by reaction of ethyl 4-aminobenzoate with 2-diethylaminoethanol.procaine
promethazineA tertiary amine that is a substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropan-2-amine moiety.promethazine
promethazine hydrochlorideThe hydrochloride salt of promethazine.promethazine hydrochloride
qx-314QX-314
ropivacaineThe anhydrous form of (S)-ropivacaine hydrochloride.(S)-ropivacaine hydrochloride (anhydrous)
ropivacaineA piperidinecarboxamide-based amide-type local anaesthetic (amide caine) in which (S)-N-propylpipecolic acid and 2,6-dimethylaniline are combined to form the amide bond.(S)-ropivacaine
tetracaineA benzoate ester in which 4-N-butylbenzoic acid and 2-(dimethylamino)ethanol have combined to form the ester bond; a local ester anaesthetic (ester caine) used for surface and spinal anaesthesia.tetracaine
tocainideA monocarboxylic acid amide in which 2,6-dimethylphenylaniline and isobutyric acid have combined to form the amide bond; used as a local anaesthetic.tocainide

Research

Studies (81,600)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199027,655 (33.89)18.7374
1990's15,500 (19.00)18.2507
2000's15,550 (19.06)29.6817
2010's17,286 (21.18)24.3611
2020's5,609 (6.87)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials13,559 (13.99%)5.53%
Reviews5,208 (5.37%)6.00%
Case Studies7,232 (7.46%)4.05%
Observational288 (0.30%)0.25%
Other70,611 (72.87%)84.16%

Protein Targets (320)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency19.952611
15-lipoxygenase, partialHomo sapiens (human)Potency32.464812
67.9K proteinVaccinia virusPotency28.183811
acetylcholinesteraseHomo sapiens (human)Potency48.236748
activating transcription factor 6Homo sapiens (human)Potency24.630612
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency22.356314
Alpha-synucleinHomo sapiens (human)Potency3.548111
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency28.183811
AR proteinHomo sapiens (human)Potency28.08341054
aryl hydrocarbon receptorHomo sapiens (human)Potency22.0467314
arylsulfatase AHomo sapiens (human)Potency3.714413
ATAD5 protein, partialHomo sapiens (human)Potency19.605524
Ataxin-2Homo sapiens (human)Potency22.682028
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency16.906912
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency22.2330212
beta-2 adrenergic receptorHomo sapiens (human)Potency3.162311
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.004824
BRCA1Homo sapiens (human)Potency12.589311
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency30.014913
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency68.589611
caspase-3Homo sapiens (human)Potency68.589611
Cellular tumor antigen p53Homo sapiens (human)Potency43.5291215
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency8.624213
Chain A, Beta-lactamaseEscherichia coli K-12Potency21.090614
Chain A, CruzipainTrypanosoma cruziPotency25.787712
Chain A, Ferritin light chainEquus caballus (horse)Potency28.819313
Chain A, HADH2 proteinHomo sapiens (human)Potency31.622811
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency79.432811
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency543.190313
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency18.986814
Chain B, HADH2 proteinHomo sapiens (human)Potency31.622811
chromobox protein homolog 1Homo sapiens (human)Potency74.203527
cytochrome P450 2C19 precursorHomo sapiens (human)Potency8.971612
cytochrome P450 2C9 precursorHomo sapiens (human)Potency22.749613
cytochrome P450 2C9, partialHomo sapiens (human)Potency16.302313
cytochrome P450 2D6Homo sapiens (human)Potency13.9980111
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency11.134818
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency15.2452216
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency13.9312210
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency17.612316
D(1A) dopamine receptorHomo sapiens (human)Potency4.614823
D(1A) dopamine receptorSus scrofa (pig)Potency14.689211
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency3.981112
DNA polymerase eta isoform 1Homo sapiens (human)Potency89.125111
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency69.957713
DNA polymerase kappa isoform 1Homo sapiens (human)Potency100.000011
endonuclease IVEscherichia coliPotency50.118711
estrogen nuclear receptor alphaHomo sapiens (human)Potency24.41741269
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency35.6213211
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency31.5260741
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency19.8833216
EWS/FLI fusion proteinHomo sapiens (human)Potency29.018933
eyes absent homolog 2 isoform aHomo sapiens (human)Potency22.387212
farnesoid X nuclear receptorHomo sapiens (human)Potency42.571526
flap endonuclease 1Homo sapiens (human)Potency54.218412
Fumarate hydrataseHomo sapiens (human)Potency34.327312
GVesicular stomatitis virusPotency16.302313
GABA theta subunitRattus norvegicus (Norway rat)Potency15.245218
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency15.245218
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency15.245218
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency15.245218
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency15.245218
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency15.245218
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency15.245218
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency15.245218
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency15.245218
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency15.245218
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency15.245218
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency15.245218
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency15.245218
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency15.245218
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency15.245218
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency15.245218
gemininHomo sapiens (human)Potency15.7893313
GLI family zinc finger 3Homo sapiens (human)Potency14.1858217
glp-1 receptor, partialHomo sapiens (human)Potency3.548111
GLS proteinHomo sapiens (human)Potency20.144127
glucocerebrosidaseHomo sapiens (human)Potency17.782811
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency25.7692417
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency18.504516
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency12.995311
heat shock protein beta-1Homo sapiens (human)Potency49.247911
hemoglobin subunit betaHomo sapiens (human)Potency16.059934
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency20.6038215
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency11.607114
histone deacetylase 9 isoform 3Homo sapiens (human)Potency12.281526
Histone H2A.xCricetulus griseus (Chinese hamster)Potency70.223315
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency70.794611
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency16.302313
huntingtin isoform 2Homo sapiens (human)Potency31.832612
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency48.972211
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency7.740126
IDH1Homo sapiens (human)Potency2.061812
importin subunit beta-1 isoform 1Homo sapiens (human)Potency12.995311
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency16.302316
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency0.801324
Interferon betaHomo sapiens (human)Potency12.227124
interleukin 8Homo sapiens (human)Potency118.832011
lamin isoform A-delta10Homo sapiens (human)Potency11.9708112
lethal factor (plasmid)Bacillus anthracis str. A2012Potency0.158511
LuciferasePhotinus pyralis (common eastern firefly)Potency17.5809410
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency30.107624
M-phase phosphoprotein 8Homo sapiens (human)Potency33.245112
Microtubule-associated protein tauHomo sapiens (human)Potency11.033329
mitogen-activated protein kinase 1Homo sapiens (human)Potency16.4707210
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency14.7707210
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency5.623411
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency30.107612
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Potency30.107612
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency26.1150419
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency18.646212
nuclear factor NF-kappa-B p105 subunit isoform 1Homo sapiens (human)Potency25.118911
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency11.038812
Nuclear receptor ROR-gammaHomo sapiens (human)Potency45.399613
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency9.093326
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency32.4696325
P53Homo sapiens (human)Potency50.118711
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency15.763625
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency84.921412
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency30.2284410
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency42.766458
phosphopantetheinyl transferaseBacillus subtilisPotency59.684813
polyproteinZika virusPotency34.327312
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency17.385113
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency16.600717
pregnane X nuclear receptorHomo sapiens (human)Potency25.5822315
pregnane X receptorRattus norvegicus (Norway rat)Potency23.445112
progesterone receptorHomo sapiens (human)Potency41.261128
RAR-related orphan receptor gammaMus musculus (house mouse)Potency16.9064219
regulator of G-protein signaling 4Homo sapiens (human)Potency9.101013
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency23.0452326
retinoid X nuclear receptor alphaHomo sapiens (human)Potency37.608849
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency14.689222
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency29.934911
SMAD family member 2Homo sapiens (human)Potency49.475911
SMAD family member 3Homo sapiens (human)Potency49.475911
Smad3Homo sapiens (human)Potency35.481311
snurportin-1Homo sapiens (human)Potency12.995311
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency32.559713
survival motor neuron protein isoform dHomo sapiens (human)Potency16.445014
TAR DNA-binding protein 43Homo sapiens (human)Potency12.816214
TDP1 proteinHomo sapiens (human)Potency16.6519218
thioredoxin reductaseRattus norvegicus (Norway rat)Potency15.101039
ThrombopoietinHomo sapiens (human)Potency0.063122
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency36.4231328
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency2.274012
thyroid stimulating hormone receptorHomo sapiens (human)Potency28.8670514
thyrotropin-releasing hormone receptorHomo sapiens (human)Potency17.376811
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency30.669412
transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Potency15.848911
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency3.981112
USP1 protein, partialHomo sapiens (human)Potency39.263516
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency18.4301213
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency42.997746
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency96.375013
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency18.504516

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC502.596011
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.892522
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC502.596011
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki0.892522
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC501.005025
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC500.085522
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.357214
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC500.587814
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC500.085522
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.374014
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC501.320314
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC500.085522
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.691614
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC501.320214
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.691614
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 5ARattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 5BRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 6Homo sapiens (human)IC502.429011
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki1.128011
5-hydroxytryptamine receptor 6Rattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)IC5035.100012
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki0.301011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC503.458413
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki3.429913
Alpha-1D adrenergic receptorHomo sapiens (human)IC500.699012
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.343512
Alpha-2A adrenergic receptorHomo sapiens (human)IC501.116012
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC505.754411
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.419012
Alpha-2B adrenergic receptorHomo sapiens (human)IC500.053011
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC505.754411
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.024011
Alpha-2C adrenergic receptorHomo sapiens (human)IC502.431011
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC505.754411
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.353011
Amine oxidase [flavin-containing] AHomo sapiens (human)IC500.317011
Amyloid-beta precursor proteinHomo sapiens (human)IC500.338011
Amyloid-beta precursor proteinHomo sapiens (human)Ki0.005911
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC5031.859011
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki26.101311
Angiotensin-converting enzyme 2 Homo sapiens (human)IC5013.645012
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000014
Bile salt export pumpHomo sapiens (human)IC50302.3800415
Calcium release-activated calcium channel protein 1Homo sapiens (human)IC50500.000022
Calmodulin-1Homo sapiens (human)IC5060.000011
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)Ki1.115011
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)Ki1.115011
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)Ki1.115011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000014
Chloroquine resistance transporterPlasmodium falciparum (malaria parasite P. falciparum)IC5085.000011
Cytochrome P450 2C19Homo sapiens (human)IC500.600011
Cytochrome P450 2C9 Homo sapiens (human)IC5050.000012
Cytochrome P450 2D6Homo sapiens (human)IC502.271313
Cytochrome P450 2J2Homo sapiens (human)IC5050.000012
DRattus norvegicus (Norway rat)IC505.754411
D(1A) dopamine receptorHomo sapiens (human)IC502.744011
D(1A) dopamine receptorHomo sapiens (human)Ki1.372011
D(2) dopamine receptorHomo sapiens (human)IC500.439522
D(2) dopamine receptorHomo sapiens (human)Ki0.260011
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.330011
D(3) dopamine receptorHomo sapiens (human)IC501.326613
D(3) dopamine receptorHomo sapiens (human)Ki0.450513
Fatty acid-binding protein, heartHomo sapiens (human)IC500.367011
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit piHomo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)IC50127.000011
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Ki10.000011
Histamine H1 receptorHomo sapiens (human)IC500.054324
Histamine H1 receptorHomo sapiens (human)Ki0.009924
Histamine H2 receptorHomo sapiens (human)IC501.165011
Histamine H2 receptorHomo sapiens (human)Ki1.146011
Histamine H4 receptorHomo sapiens (human)Ki42.657911
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
Leukotriene B4 receptor 1Homo sapiens (human)Ki0.524011
Leukotriene B4 receptor 2Homo sapiens (human)Ki0.524011
Lysosomal Pro-X carboxypeptidaseHomo sapiens (human)Ki10.000011
MBT domain-containing protein 1Homo sapiens (human)IC50100.000011
Metabotropic glutamate receptor 5Rattus norvegicus (Norway rat)IC5054.300011
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki0.965422
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC50500.000011
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000014
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC500.259614
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki0.042336
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki40.934333
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC500.567514
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.120447
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Ki0.010522
Muscarinic acetylcholine receptor M2Sus scrofa (pig)Ki0.234411
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC500.354414
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.043547
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)Ki0.003122
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC500.308414
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.035225
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC500.200714
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki0.118225
NAD(+) hydrolase SARM1Homo sapiens (human)IC50145.000011
NAD(+) hydrolase SARM1Homo sapiens (human)Ki70.000011
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)IC5031.859011
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)Ki26.101311
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CIC5017.700011
Potassium channel subfamily K member 18Homo sapiens (human)IC50100.000011
Potassium channel subfamily K member 2Homo sapiens (human)IC50193.500022
Potassium channel subfamily K member 3Homo sapiens (human)IC50338.200015
Potassium voltage-gated channel subfamily A member 5Homo sapiens (human)IC502,188.000011
Potassium voltage-gated channel subfamily D member 2Rattus norvegicus (Norway rat)IC501,210.000011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50135.97891526
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki26.101311
Procathepsin LHomo sapiens (human)IC5013.645012
Protein orai-2Homo sapiens (human)IC50500.000022
Protein orai-3Homo sapiens (human)IC50500.000022
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusIC5013.645012
Replicase polyprotein 1abBetacoronavirus England 1IC5013.645012
Replicase polyprotein 1abHuman coronavirus 229EIC5013.645012
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC5018.430023
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusIC5013.645012
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC500.700926
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki1.942825
Snake venom metalloproteinase BaP1Bothrops asper (terciopelo)IC5054.300011
Sodium channel protein type 1 subunit alphaRattus norvegicus (Norway rat)IC5056.000012
Sodium channel protein type 2 subunit alphaHomo sapiens (human)IC500.795022
Sodium channel protein type 2 subunit alphaRattus norvegicus (Norway rat)IC5056.000012
Sodium channel protein type 3 subunit alphaHomo sapiens (human)IC505.620022
Sodium channel protein type 3 subunit alphaRattus norvegicus (Norway rat)IC5056.000012
Sodium channel protein type 4 subunit alphaHomo sapiens (human)IC502.000011
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC5025.171766
Sodium channel protein type 7 subunit alphaHomo sapiens (human)IC500.056011
Sodium channel protein type 8 subunit alphaHomo sapiens (human)IC500.520011
Sodium channel protein type 9 subunit alphaHomo sapiens (human)IC505.402377
Sodium channel protein type 9 subunit alphaHomo sapiens (human)Ki6.250022
Sodium-dependent dopamine transporterMus musculus (house mouse)IC500.200011
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC501.34964767
Sodium-dependent dopamine transporterMus musculus (house mouse)Ki0.850011
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)Ki25.24952641
Sodium-dependent dopamine transporter Homo sapiens (human)IC500.37263839
Sodium-dependent dopamine transporter Homo sapiens (human)Ki0.41243236
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC501.51152426
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki1.78353337
Sodium-dependent serotonin transporterHomo sapiens (human)IC500.96462525
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)IC500.88851518
Sodium-dependent serotonin transporterHomo sapiens (human)Ki0.41123437
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Ki0.54331928
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)IC5024.000011
Solute carrier family 22 member 1 Homo sapiens (human)IC5035.100011
Solute carrier family 22 member 2Rattus norvegicus (Norway rat)IC5032.000011
Spike glycoproteinBetacoronavirus England 1IC5013.645012
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusIC5013.645012
Transmembrane protease serine 2Homo sapiens (human)IC5013.645012
TransporterRattus norvegicus (Norway rat)IC503.22771315
TransporterRattus norvegicus (Norway rat)Ki2.34151619
Trypanothione reductaseTrypanosoma cruziIC50271.000011
Trypanothione reductaseTrypanosoma cruziKi216.000011
Tryptophan 5-hydroxylase 1Rattus norvegicus (Norway rat)Ki0.490011
Voltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)IC5018.000011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Angiotensin-converting enzyme 2 Homo sapiens (human)EC509.670012
Calmodulin Bos taurus (cattle)Kd50.000011
cGMP-gated cation channel alpha-1Bos taurus (cattle)Kd9.400022
Chain A, CHIMERA OF IG KAPPA CHAIN: HUMAN CONSTANT REGION AND MOUSE VARIABLE REGIONsynthetic constructKd0.400011
Chain B, CHIMERA OF IG GAMMA-1 CHAIN: HUMAN CONSTANT REGION AND MOUSE VARIABLE REGIONsynthetic constructKd0.400011
Chain H, Fab M82G2, Heavy chainMus musculus (house mouse)Kd0.140012
Chain L, Fab M82G2, Light chainMus musculus (house mouse)Kd0.140012
Guanylate cyclase soluble subunit alpha-1Homo sapiens (human)EC501.020011
Guanylate cyclase soluble subunit alpha-2Homo sapiens (human)EC501.020011
Guanylate cyclase soluble subunit beta-1Homo sapiens (human)EC501.020011
Guanylate cyclase soluble subunit beta-2Homo sapiens (human)EC501.020011
Major prion proteinHomo sapiens (human)EC508.000011
Muscarinic acetylcholine receptorCavia porcellus (domestic guinea pig)Kd0.079411
Muscarinic acetylcholine receptor M2Homo sapiens (human)Kd0.039811
Procathepsin LHomo sapiens (human)EC509.670012
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusEC509.670012
Replicase polyprotein 1abBetacoronavirus England 1EC509.670012
Replicase polyprotein 1abHuman coronavirus 229EEC509.670012
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2EC509.670012
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusEC509.670012
Spike glycoproteinBetacoronavirus England 1EC509.670012
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusEC509.670012
Transmembrane protease serine 2Homo sapiens (human)EC509.670012

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Cytochrome P450 1A2 Rattus norvegicus (Norway rat)KmH2,881.000022
DNA repair protein RAD52 homolog isoform aHomo sapiens (human)AC5033.920011
FAD-linked sulfhydryl oxidase ALRHomo sapiens (human)AC500.367011
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
Liver carboxylesterase 1Homo sapiens (human)Km120.000011
Muscarinic acetylcholine receptor M1Homo sapiens (human)Kb0.010011
Muscarinic acetylcholine receptor M2Homo sapiens (human)Kb0.098014
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CINH285.000011
Snq2pSaccharomyces cerevisiae EC1118INH117.000011
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Km0.200011