Page last updated: 2024-08-05 15:12:42

antipruritic drug

A drug, usually applied topically, that relieves pruritus (itching).

ChEBI ID: 59683

Members (21)

MemberDefinitionClass
benzocaineA benzoate ester having 4-aminobenzoic acid as the acid component and ethanol as the alcohol component. A surface anaesthetic, it is used to suppress the gag reflex, and as a lubricant and topical anaesthetic on the larynx, mouth, nasal cavity, respiratory tract, oesophagus, rectum, urinary tract, and vagina.benzocaine
chlorpheniramineA tertiary amino compound that is propylamine which is substituted at position 3 by a pyridin-2-yl group and a p-chlorophenyl group and in which the hydrogens attached to the nitrogen are replaced by methyl groups. A histamine H1 antagonist, it is used to relieve the symptoms of hay fever, rhinitis, urticaria, and asthma.chlorphenamine
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
clocortolone pivalateThe 21-O-pivalate ester of clocortolone. It is used for the relief of inflammatory and pruritic (itching) skin disorders.clocortolone pivalate
crotamitonAn enamide resulting from the formal condensation of crotonic acid with N-ethyl-2-methylaniline. A colourless or pale yellow oily liquid, it is used in the treatment of pruritus (itching) by producing a counter-irritation: as it evaporates from the skin, it produces a cooling effect that diverts attention away from the itching. It has also been used as an acaricide in the treatment of scabies, though more effective drugs are usually preferred.crotamiton
cyproheptadineThe product resulting from the formal oxidative coupling of position 5 of 5H-dibenzo[a,d]cycloheptene with position 4 of 1-methylpiperidine resulting in the formation of a double bond between the two fragments. It is a sedating antihistamine with antimuscarinic and calcium-channel blocking actions. It is used (particularly as the hydrochloride sesquihydrate) for the relief of allergic conditions including rhinitis, conjunctivitis due to inhalant allergens and foods, urticaria and angioedema, and in pruritic skin disorders. Unlike other antihistamines, it is also a seratonin receptor antagonist, making it useful in conditions such as vascular headache and anorexia.cyproheptadine
desoximetasoneDexamethasone in which the hydroxy group at the 17alpha position is substituted by hydrogen. A synthetic corticosteroid with glucocorticoid activity, it is used as an anti-inflammatory and anti-pruritic in the treatment of various skin disorders, including skin allergies and psoriasis.desoximetasone
diflorasone diacetateThe 17,21-diacetate derivative of diflorasone. It is used topically for its anti-inflammatory and antipruritic properties in the treatment of various skin disorders.diflorasone diacetate
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
emedastine1-Methyl-1,4-diazepane in which the hydrogen attached to the nitrogen at position 4 is substituted by a 1-(2-ethoxyethyl)-1H-benzimidazol-2-yl group. A relatively selective histamine H1 antagonist, it is used as the difumatate salt for allergic rhinitis, urticaria, and pruritic skin disorders, and in eyedrops for the symptomatic relief of allergic conjuntivitis.emedastine
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
flumethasone pivalateflumethasone pivalate
fluocinolone acetonideA fluorinated steroid that is flunisolide in which the hydrogen at position 9 is replaced by fluorine. A corticosteroid with glucocorticoid activity, it is used (both as the anhydrous form and as the dihydrate) in creams, gels and ointments for the treatment of various skin disorders.fluocinolone acetonide
hydroxyzineA N-alkylpiperazine that is piperzine in which the nitrogens atoms are substituted by 2-(2-hydroxyethoxy)ethyl and (4-chlorophenyl)(phenyl)methyl groups respectively.hydroxyzine
mentholA p-menthan-3-ol which has (1R,2S,5R)-stereochemistry. It is the most common naturally occurring enantiomer.(-)-menthol
methdilazineA phenothiazine substituted on nitrogen by a (1-methylpyrrolidin-3-yl)methyl group; a first-generation antihistamine with anticholinergic properties.methdilazine
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
quercetin 3-o-glucopyranosideA quercetin O-glucoside that is quercetin with a beta-D-glucosyl residue attached at position 3. Isolated from Lepisorus contortus, it exhibits antineoplastic activityand has been found to decrease the rate of polymerization and sickling of red blood cellsquercetin 3-O-beta-D-glucopyranoside

Research

Studies (17,658)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19909,775 (55.36)18.7374
1990's2,422 (13.72)18.2507
2000's2,448 (13.86)29.6817
2010's2,363 (13.38)24.3611
2020's650 (3.68)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials2,635 (12.88%)5.53%
Reviews995 (4.86%)6.00%
Case Studies2,038 (9.96%)4.05%
Observational34 (0.17%)0.25%
Other14,759 (72.13%)84.16%

Protein Targets (285)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
acetylcholinesteraseHomo sapiens (human)Potency36.066636
activating transcription factor 6Homo sapiens (human)Potency54.941011
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency38.730612
Alpha-synucleinHomo sapiens (human)Potency3.548111
AR proteinHomo sapiens (human)Potency19.70051067
aryl hydrocarbon receptorHomo sapiens (human)Potency35.678727
arylsulfatase AHomo sapiens (human)Potency0.012011
ATAD5 protein, partialHomo sapiens (human)Potency13.138634
Ataxin-2Homo sapiens (human)Potency29.671927
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency23.051523
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency42.301824
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency8.492111
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency17.474512
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.006322
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency44.668411
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency57.192813
caspase-3Homo sapiens (human)Potency57.192813
Cellular tumor antigen p53Homo sapiens (human)Potency31.9646212
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency13.404224
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency19.137313
Chain A, Beta-lactamaseEscherichia coli K-12Potency25.118911
Chain A, CruzipainTrypanosoma cruziPotency19.952611
Chain A, HADH2 proteinHomo sapiens (human)Potency19.952611
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency79.432811
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency10.758914
Chain B, HADH2 proteinHomo sapiens (human)Potency19.952611
chaperonin GroELMethanococcus maripaludis S2Potency100.000011
chromobox protein homolog 1Homo sapiens (human)Potency56.751924
cytochrome P450 2C19 precursorHomo sapiens (human)Potency11.467415
cytochrome P450 2C9 precursorHomo sapiens (human)Potency31.622811
cytochrome P450 2C9, partialHomo sapiens (human)Potency19.637015
cytochrome P450 2D6Homo sapiens (human)Potency1.986615
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency7.363918
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency13.7606211
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency11.269028
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency18.626219
D(1A) dopamine receptorHomo sapiens (human)Potency3.917624
D(1A) dopamine receptorSus scrofa (pig)Potency14.689211
DNA polymerase betaHomo sapiens (human)Potency1.778311
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency65.811412
endonuclease IVEscherichia coliPotency50.118711
estrogen nuclear receptor alphaHomo sapiens (human)Potency27.83921057
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency39.730827
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency38.8102745
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency19.0024210
EWS/FLI fusion proteinHomo sapiens (human)Potency24.4222410
eyes absent homolog 2 isoform aHomo sapiens (human)Potency22.387211
farnesoid X nuclear receptorHomo sapiens (human)Potency34.422612
flap endonuclease 1Homo sapiens (human)Potency8.436812
Fumarate hydrataseHomo sapiens (human)Potency20.799913
GVesicular stomatitis virusPotency19.637015
GABA theta subunitRattus norvegicus (Norway rat)Potency13.447216
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency13.447216
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency13.447216
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency13.447216
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency13.447216
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency13.447216
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency13.447216
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency13.447216
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency13.447216
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency13.447216
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency13.447216
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency13.447216
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency13.447216
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency13.447216
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency13.447216
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency13.447216
gemininHomo sapiens (human)Potency9.495438
GLI family zinc finger 3Homo sapiens (human)Potency23.7184223
glp-1 receptor, partialHomo sapiens (human)Potency7.313322
GLS proteinHomo sapiens (human)Potency21.177023
glucocerebrosidaseHomo sapiens (human)Potency17.782811
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency13.0212326
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency26.028116
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency1.158211
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency19.3568217
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency39.810711
Histone H2A.xCricetulus griseus (Chinese hamster)Potency71.249025
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency70.794611
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency19.637015
huntingtin isoform 2Homo sapiens (human)Potency33.048813
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency12.907012
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency2.5213210
IDH1Homo sapiens (human)Potency1.227912
importin subunit beta-1 isoform 1Homo sapiens (human)Potency1.158211
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency19.6370110
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency1.065013
Integrin alpha-IIbHomo sapiens (human)Potency12.589311
Integrin beta-3Homo sapiens (human)Potency12.589311
Interferon betaHomo sapiens (human)Potency15.824339
lamin isoform A-delta10Homo sapiens (human)Potency12.796518
lethal factor (plasmid)Bacillus anthracis str. A2012Potency9.275814
LuciferasePhotinus pyralis (common eastern firefly)Potency27.485223
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency3.548111
M-phase phosphoprotein 8Homo sapiens (human)Potency33.245112
Microtubule-associated protein tauHomo sapiens (human)Potency11.464212
mitogen-activated protein kinase 1Homo sapiens (human)Potency11.454325
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.517226
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency10.000011
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency1.995311
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency34.526739
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency0.020125
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-gamma isoform 1Mus musculus (house mouse)Potency14.733412
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency4.928214
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency45.2603314
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency20.026014
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency84.921412
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency23.129947
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency38.3898512
phosphopantetheinyl transferaseBacillus subtilisPotency66.848424
plasminogen precursorMus musculus (house mouse)Potency2.238711
polyproteinZika virusPotency20.799913
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency16.728417
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency12.333216
PPM1D proteinHomo sapiens (human)Potency14.740312
pregnane X nuclear receptorHomo sapiens (human)Potency24.1339312
progesterone receptorHomo sapiens (human)Potency10.8834311
RAR-related orphan receptor gammaMus musculus (house mouse)Potency23.8944213
regulator of G-protein signaling 4Homo sapiens (human)Potency7.838614
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency37.3393325
retinoid X nuclear receptor alphaHomo sapiens (human)Potency29.8824311
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency18.500023
SMAD family member 2Homo sapiens (human)Potency29.968024
SMAD family member 3Homo sapiens (human)Potency29.968024
Smad3Homo sapiens (human)Potency0.100011
snurportin-1Homo sapiens (human)Potency1.158211
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency26.463927
survival motor neuron protein isoform dHomo sapiens (human)Potency1.704714
TAR DNA-binding protein 43Homo sapiens (human)Potency17.320413
TDP1 proteinHomo sapiens (human)Potency25.0994222
thioredoxin glutathione reductaseSchistosoma mansoniPotency11.220211
thioredoxin reductaseRattus norvegicus (Norway rat)Potency38.967136
ThrombopoietinHomo sapiens (human)Potency5.031624
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency33.7293323
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency3.548111
thyroid stimulating hormone receptorHomo sapiens (human)Potency23.7837613
thyrotropin-releasing hormone receptorHomo sapiens (human)Potency17.376811
transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Potency15.848911
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency2.238711
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency2.238711
USP1 protein, partialHomo sapiens (human)Potency39.810712
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency16.8506217
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency42.767438
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency94.562612
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency26.028116

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC501.359012
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.777012
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC501.359012
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki0.777012
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC500.283625
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC500.003111
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.056758
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.001611
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC500.307914
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC500.003111
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.195814
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC500.273414
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC500.003111
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.116825
5-hydroxytryptamine receptor 2C Mus musculus (house mouse)Ki0.011011
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC500.273414
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.143214
5-hydroxytryptamine receptor 6Homo sapiens (human)IC500.929013
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.431313
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)IC5020.000014
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki0.088022
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki0.050111
Aldo-keto reductase family 1 member B1Homo sapiens (human)IC504.500011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC503.166025
Aldo-keto reductase family 1 member B1Sus scrofa (pig)IC5016.000011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki2.833814
alkaline phosphatase, germ cell type preproproteinHomo sapiens (human)IC50100.000011
alkaline phosphatase, intestinalHomo sapiens (human)IC507.105022
alkaline phosphatase, tissue-nonspecific isozyme isoform 1 preproproteinHomo sapiens (human)IC5014.000011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.175022
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.175022
Alpha-1D adrenergic receptorHomo sapiens (human)IC500.107313
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.052713
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.175022
Alpha-2A adrenergic receptorHomo sapiens (human)IC500.382313
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.150224
Alpha-2B adrenergic receptorHomo sapiens (human)IC500.134013
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.165424
Alpha-2C adrenergic receptorHomo sapiens (human)IC501.267013
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.194024
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC5016.434413
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki13.464313
Angiotensin-converting enzyme 2 Homo sapiens (human)IC5013.645012
Arginase Leishmania amazonensisIC502.000011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000013
Aurora kinase BHomo sapiens (human)IC5010.700011
Bifunctional epoxide hydrolase 2Homo sapiens (human)IC5028.430011
Bile salt export pumpHomo sapiens (human)IC50210.370039
Calcium release-activated calcium channel protein 1Homo sapiens (human)IC50500.000022
Calmodulin-1Homo sapiens (human)IC5060.000011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000013
Carbonic anhydrase 1Homo sapiens (human)Ki10.000022
Carbonic anhydrase 12Homo sapiens (human)Ki0.111022
Carbonic anhydrase 2Homo sapiens (human)Ki3.310622
Carbonic anhydrase 4Homo sapiens (human)Ki0.075711
Carbonic anhydrase 7Homo sapiens (human)Ki0.003811
Chloroquine resistance transporterPlasmodium falciparum (malaria parasite P. falciparum)IC5069.500012
Cytochrome P450 2C19Homo sapiens (human)IC500.600011
Cytochrome P450 2C9 Homo sapiens (human)IC5050.000011
Cytochrome P450 2D6Homo sapiens (human)IC503.000011
Cytochrome P450 2J2Homo sapiens (human)IC5050.000011
DRattus norvegicus (Norway rat)Ki0.063011
D(1A) dopamine receptorHomo sapiens (human)IC501.479013
D(1A) dopamine receptorHomo sapiens (human)Ki0.739313
D(1B) dopamine receptorRattus norvegicus (Norway rat)Ki0.063011
D(2) dopamine receptorHomo sapiens (human)IC500.294824
D(2) dopamine receptorRattus norvegicus (Norway rat)IC500.140011
D(2) dopamine receptorHomo sapiens (human)Ki0.170035
D(2) dopamine receptorMus musculus (house mouse)Ki0.112011
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.063011
D(3) dopamine receptorHomo sapiens (human)IC500.204813
D(3) dopamine receptorHomo sapiens (human)Ki0.069513
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki0.063011
D(4) dopamine receptorRattus norvegicus (Norway rat)Ki0.063011
Endothelin receptor type BHomo sapiens (human)Ki0.050122
Endothelin receptor type BRattus norvegicus (Norway rat)Ki0.050111
Glucocorticoid receptorHomo sapiens (human)IC500.004013
Glucocorticoid receptorHomo sapiens (human)Ki0.001813
Glycine receptor subunit alpha-1Rattus norvegicus (Norway rat)IC500.004013
Glycine receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki0.001813
Glycine receptor subunit alpha-2Rattus norvegicus (Norway rat)IC500.004013
Glycine receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki0.001813
Glycine receptor subunit alpha-3Rattus norvegicus (Norway rat)IC500.004013
Glycine receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki0.001813
Glycine receptor subunit betaRattus norvegicus (Norway rat)IC500.004013
Glycine receptor subunit betaRattus norvegicus (Norway rat)Ki0.001813
Glycogen phosphorylase, brain formHomo sapiens (human)Ki0.004011
Glycogen phosphorylase, muscle formHomo sapiens (human)Ki0.004011
Histamine H1 receptorHomo sapiens (human)IC500.041636
Histamine H1 receptorHomo sapiens (human)Ki0.005659
Histamine H2 receptorHomo sapiens (human)IC500.577713
Histamine H2 receptorHomo sapiens (human)Ki0.568313
Histamine H4 receptorHomo sapiens (human)Ki26.329022
Histone-lysine N-methyltransferase SETD7Homo sapiens (human)IC508.133333
Histone-lysine N-methyltransferase SETD7Homo sapiens (human)Ki15.000011
intestinal alkaline phosphatase precursorMus musculus (house mouse)IC501.660011
Lethal(3)malignant brain tumor-like protein 1Homo sapiens (human)IC5041.000011
Lethal(3)malignant brain tumor-like protein 3Homo sapiens (human)IC5042.000011
Lethal(3)malignant brain tumor-like protein 4Homo sapiens (human)IC50100.000011
Lysine-specific histone demethylase 1AHomo sapiens (human)IC500.950011
Lysine-specific histone demethylase 1AHomo sapiens (human)Ki1.000011
MBT domain-containing protein 1Homo sapiens (human)IC5034.000011
Mitogen-activated protein kinase 10Homo sapiens (human)IC5041.433313
Mitogen-activated protein kinase 14Homo sapiens (human)IC5041.433313
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000013
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC500.125313
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki0.022835
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki0.004011
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC500.373313
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.103735
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Ki0.004011
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC500.188014
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.036536
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)Ki0.004011
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC500.103914
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.019336
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)Ki0.004011
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC500.044714
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki0.026636
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)Ki0.004011
NeuraminidaseInfluenza A virus (A/USSR/90/1977(H1N1))IC50423.650022
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)IC5016.434413
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)Ki13.464313
Pancreatic triacylglycerol lipaseSus scrofa (pig)IC5070.000011
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CIC5017.700011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC5017.1148713
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki10.137824
Procathepsin LHomo sapiens (human)IC5013.645012
Prostaglandin G/H synthase 1Ovis aries (sheep)Ki0.001611
Protein orai-2Homo sapiens (human)IC50500.000022
Protein orai-3Homo sapiens (human)IC50500.000022
Receptor-type tyrosine-protein kinase FLT3Homo sapiens (human)IC5010.000011
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 2IC5013.645012
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusIC5013.645012
Sigma intracellular receptor 2Homo sapiens (human)Ki0.025111
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC500.160512
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.048023
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC5041.000011
Sodium-dependent dopamine transporter Homo sapiens (human)IC500.678011
Sodium-dependent dopamine transporter Homo sapiens (human)Ki0.538011
Sodium-dependent noradrenaline transporterMus musculus (house mouse)Ki0.290011
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC502.857514
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki2.325025
Sodium-dependent serotonin transporterHomo sapiens (human)IC505.800022
Sodium-dependent serotonin transporterHomo sapiens (human)Ki3.115022
Sodium-dependent serotonin transporterMus musculus (house mouse)Ki4.100011
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)IC5019.000012
Solute carrier family 22 member 1 Homo sapiens (human)IC5020.000012
Solute carrier family 22 member 2Rattus norvegicus (Norway rat)IC5029.000012
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)Ki0.290011
Trypanothione reductaseTrypanosoma cruziIC50271.000011
Trypanothione reductaseTrypanosoma cruziKi216.000011
TyrosinaseHomo sapiens (human)IC5050.000011
Voltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)IC5018.000011
Xanthine dehydrogenase/oxidaseHomo sapiens (human)IC5025.970023

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Angiotensin-converting enzyme 2 Homo sapiens (human)EC5011.246713
Calmodulin Bos taurus (cattle)Kd50.000011
glycogen synthase kinase-3 beta isoform 1Homo sapiens (human)EC5015.800011
Histamine H1 receptorHomo sapiens (human)Kd5.400011
Major prion proteinHomo sapiens (human)EC508.000011
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC5031.600011
Nuclear receptor subfamily 1 group I member 2Rattus norvegicus (Norway rat)EC5010.000011
Procathepsin LHomo sapiens (human)EC5011.246713
Pyruvate kinase PKMHomo sapiens (human)EC500.001311
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusEC5011.246713
Replicase polyprotein 1abBetacoronavirus England 1EC5011.246713
Replicase polyprotein 1abHuman coronavirus 229EEC5011.246713
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2EC5011.246713
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusEC5011.246713
Spike glycoproteinBetacoronavirus England 1EC5011.246713
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusEC5011.246713
Transient receptor potential cation channel subfamily A member 1Homo sapiens (human)EC5096.000011
Transient receptor potential cation channel subfamily M member 8Homo sapiens (human)EC5010.100011
Transmembrane protease serine 2Homo sapiens (human)EC5011.246713

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Arginase Leishmania amazonensisKis6.900011
bioAMycobacterium tuberculosis UT205AC509.060011
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
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CINH285.000011
Snq2pSaccharomyces cerevisiae EC1118INH117.000011
UDP-glucuronosyltransferase 1A3Homo sapiens (human)Km240.000011
UDP-glucuronosyltransferase 1A4Homo sapiens (human)Km106.000022