Page last updated: 2024-08-05 15:15:53

histamine antagonist

Histamine antagonists are the drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists.

ChEBI ID: 37956

Members (21)

MemberDefinitionClass
buclizineAn N-alkylpiperazine carrying (4-chlorophenyl)(phenyl)methyl and 4-tert-butylbenzyl groups.buclizine
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
cinnarizinecinnarizine
clemizoleA member of the class of benzimidazoles that is 1H-benzimidazole substituted by a pyrrolidin-1-ylmethyl and a 4-chlorobenzyl groups at positions 2 and 1 respectively.clemizole
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
cubebinA lignan that consists of tetrahydrofuran-2-ol substituted by two 1,3-benzodioxol-5-ylmethyl groups at positions 3 and 4 respectively (the 2S,3R,4R stereoisomer). It is isolated from the leaves of Piper nigrum and exhibits analgesic, anti-inflammatory, antimicrobial and trypanocidal activities.(-)-cubebin
demethylmirtazapineA benzazepine metabolite resulting from demethylation of the antidpressant, mirtazapine.N-demethylmirtazapine
doxylaminedoxylamine
epinastineA benzazepine that is 6,11-dihydro-5H-dibenzo[b,e]azepine in which the azepine ring is fused to the e side of 4,5-dihydro-1H-imidazol-2-amine.epinastine
methdilazineA phenothiazine substituted on nitrogen by a (1-methylpyrrolidin-3-yl)methyl group; a first-generation antihistamine with anticholinergic properties.methdilazine
methixenemetixene
mirtazapinemirtazapine
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
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
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
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
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
quetiapinequetiapine
thiethylperazineA member of the class of phenothiazines that is perazine substituted by a ethylsulfanyl group at position 2.thiethylperazine
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 (19,689)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19902,492 (12.66)18.7374
1990's3,409 (17.31)18.2507
2000's6,396 (32.49)29.6817
2010's5,511 (27.99)24.3611
2020's1,881 (9.55)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials3,264 (14.16%)5.53%
Reviews2,492 (10.81%)6.00%
Case Studies4,199 (18.21%)4.05%
Observational122 (0.53%)0.25%
Other12,976 (56.29%)84.16%

Protein Targets (344)

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 virusPotency10.000011
acetylcholinesteraseHomo sapiens (human)Potency26.115725
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency25.118912
AR proteinHomo sapiens (human)Potency19.5853928
aryl hydrocarbon receptorHomo sapiens (human)Potency26.645224
arylsulfatase AHomo sapiens (human)Potency16.015415
ATAD5 protein, partialHomo sapiens (human)Potency5.161223
Ataxin-2Homo sapiens (human)Potency22.089925
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency8.832725
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency21.265823
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency8.492111
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency16.720613
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.003522
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency69.661413
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency33.491511
caspase-3Homo sapiens (human)Potency33.491511
Cellular tumor antigen p53Homo sapiens (human)Potency11.601815
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency25.118911
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency24.035312
Chain A, Beta-lactamaseEscherichia coli K-12Potency194.568723
Chain A, CruzipainTrypanosoma cruziPotency39.810711
Chain A, Ferritin light chainEquus caballus (horse)Potency10.000011
Chain A, HADH2 proteinHomo sapiens (human)Potency33.191323
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency79.432811
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency1.601012
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency14.532913
Chain B, HADH2 proteinHomo sapiens (human)Potency33.191323
chaperonin-containing TCP-1 beta subunit homologHomo sapiens (human)Potency15.848911
chromobox protein homolog 1Homo sapiens (human)Potency42.147114
cytochrome P450 2C19 precursorHomo sapiens (human)Potency6.392014
cytochrome P450 2C9 precursorHomo sapiens (human)Potency21.659913
cytochrome P450 2C9, partialHomo sapiens (human)Potency19.373813
cytochrome P450 2D6Homo sapiens (human)Potency9.271115
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency5.269315
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency14.4231214
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency17.6071210
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency22.687412
D(1A) dopamine receptorHomo sapiens (human)Potency6.142235
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency19.952611
DNA polymerase betaHomo sapiens (human)Potency40.605612
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency79.432811
DNA polymerase kappa isoform 1Homo sapiens (human)Potency28.183811
dopamine D1 receptorHomo sapiens (human)Potency0.092011
endonuclease IVEscherichia coliPotency1.778311
estrogen nuclear receptor alphaHomo sapiens (human)Potency20.7370722
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency33.491513
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency19.9119915
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency11.808017
EWS/FLI fusion proteinHomo sapiens (human)Potency26.2267412
farnesoid X nuclear receptorHomo sapiens (human)Potency22.500124
flap endonuclease 1Homo sapiens (human)Potency6.145414
Fumarate hydrataseHomo sapiens (human)Potency24.905312
GVesicular stomatitis virusPotency19.373813
GABA theta subunitRattus norvegicus (Norway rat)Potency14.423117
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency14.423117
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency14.423117
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency14.423117
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency14.423117
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency14.423117
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency14.423117
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency14.423117
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency14.423117
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency14.423117
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency14.423117
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency14.423117
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency14.423117
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency14.423117
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency14.423117
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency14.423117
gemininHomo sapiens (human)Potency14.631338
GLI family zinc finger 3Homo sapiens (human)Potency11.1731211
glp-1 receptor, partialHomo sapiens (human)Potency10.000011
GLS proteinHomo sapiens (human)Potency16.747026
glucocerebrosidaseHomo sapiens (human)Potency13.548113
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency15.142437
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)Potency14.1898219
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency39.810711
Histone H2A.xCricetulus griseus (Chinese hamster)Potency61.931512
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency19.373813
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency15.986613
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency12.127226
IDH1Homo sapiens (human)Potency10.322511
importin subunit beta-1 isoform 1Homo sapiens (human)Potency3.662611
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency19.373816
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency8.573816
Interferon betaHomo sapiens (human)Potency12.979026
lamin isoform A-delta10Homo sapiens (human)Potency12.131917
lethal factor (plasmid)Bacillus anthracis str. A2012Potency31.622811
LuciferasePhotinus pyralis (common eastern firefly)Potency40.533411
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency7.903034
M-phase phosphoprotein 8Homo sapiens (human)Potency18.240612
Microtubule-associated protein tauHomo sapiens (human)Potency19.291825
mitogen-activated protein kinase 1Homo sapiens (human)Potency18.735327
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency2.646325
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency10.000011
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)Potency25.278333
NFKB1 protein, partialHomo sapiens (human)Potency1.000022
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency19.234424
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency20.140312
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency17.021724
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency10.995437
Ornithine decarboxylaseRattus norvegicus (Norway rat)Potency0.007911
ParkinHomo sapiens (human)Potency39.810711
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency11.372313
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency47.754811
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency16.930111
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency18.689137
PINK1Homo sapiens (human)Potency39.810711
polyproteinZika virusPotency24.905312
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency12.589311
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency7.466815
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency8.978118
PPM1D proteinHomo sapiens (human)Potency6.584212
pregnane X nuclear receptorHomo sapiens (human)Potency18.007025
progesterone receptorHomo sapiens (human)Potency23.617437
pyruvate kinase PKM isoform bHomo sapiens (human)Potency0.007922
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency125.892011
RAR-related orphan receptor gammaMus musculus (house mouse)Potency12.844825
regulator of G-protein signaling 4Homo sapiens (human)Potency32.164712
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency21.481239
retinoid X nuclear receptor alphaHomo sapiens (human)Potency6.913124
snurportin-1Homo sapiens (human)Potency3.662611
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency14.572429
survival motor neuron protein isoform dHomo sapiens (human)Potency12.589312
TAR DNA-binding protein 43Homo sapiens (human)Potency0.354811
TDP1 proteinHomo sapiens (human)Potency20.7155229
thioredoxin glutathione reductaseSchistosoma mansoniPotency21.421512
thioredoxin reductaseRattus norvegicus (Norway rat)Potency22.971547
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency20.6742218
thyroid stimulating hormone receptorHomo sapiens (human)Potency25.589836
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency3.981111
transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Potency12.589311
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency19.952611
USP1 protein, partialHomo sapiens (human)Potency32.375614
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency10.970228
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency7.842222
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency66.896812
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)IC501.264636
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki0.70331937
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.2944911
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC500.725735
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki0.434624
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)IC500.0838511
5-hydroxytryptamine receptor 2AMus musculus (house mouse)IC500.028011
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC500.08511112
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.02554980
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.01052430
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC500.189427
5-hydroxytryptamine receptor 2BMus musculus (house mouse)IC500.028011
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC500.035578
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.1030611
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki0.013678
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC500.521537
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC500.032889
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.19202648
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki0.01271112
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)Ki0.750346
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)IC500.711825
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.439824
5-hydroxytryptamine receptor 4Homo sapiens (human)Ki0.223911
5-hydroxytryptamine receptor 5AHomo sapiens (human)Ki1.000011
5-hydroxytryptamine receptor 6Homo sapiens (human)IC500.016345
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.05002844
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki0.28423043
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki0.009422
AcetylcholinesteraseHomo sapiens (human)IC50437.297167
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 B1Homo sapiens (human)IC504.500011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC502.900723
Aldo-keto reductase family 1 member B1Sus scrofa (pig)IC5016.000011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki2.133012
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 receptorHomo sapiens (human)IC501.586622
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC500.075389
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.02381020
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.50991121
Alpha-1B adrenergic receptorHomo sapiens (human)IC500.011011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC500.075389
Alpha-1B adrenergic receptorHomo sapiens (human)Ki0.0225917
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.51281121
Alpha-1D adrenergic receptorHomo sapiens (human)IC500.280325
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC500.075389
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.05071021
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.5924918
Alpha-2A adrenergic receptorHomo sapiens (human)IC500.730325
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC502.435323
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.2692516
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki0.104369
Alpha-2B adrenergic receptorHomo sapiens (human)IC500.602025
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC502.435323
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.3183312
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki0.117147
Alpha-2C adrenergic receptorHomo sapiens (human)IC500.362225
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC502.435323
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.1923415
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki0.117147
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC5037.523723
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki8.660611
Angiotensin-converting enzymeRattus norvegicus (Norway rat)Ki0.018013
Arginase Leishmania amazonensisIC502.000011
Aspartate aminotransferase, cytoplasmicHomo sapiens (human)IC505.390011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000015
Aurora kinase BHomo sapiens (human)IC5010.700011
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 receptorRattus norvegicus (Norway rat)Ki10.000011
Beta-3 adrenergic receptorRattus norvegicus (Norway rat)Ki10.000011
Bifunctional epoxide hydrolase 2Homo sapiens (human)IC5028.430011
Bile salt export pumpHomo sapiens (human)IC50171.4162413
Bile salt export pumpRattus norvegicus (Norway rat)IC50196.500011
Calmodulin-1Homo sapiens (human)IC5080.000022
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000015
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
Carboxylic ester hydrolase Equus caballus (horse)Ki0.020011
Chloroquine resistance transporterPlasmodium falciparum (malaria parasite P. falciparum)IC5054.000011
Cholecystokinin receptor type ACavia porcellus (domestic guinea pig)Ki0.060011
CholinesteraseEquus caballus (horse)IC501.160012
CholinesteraseHomo sapiens (human)IC500.703333
CholinesteraseHomo sapiens (human)Ki4,033.346733
CruzipainTrypanosoma cruziIC50212.000022
Cytochrome P450 2C9 Homo sapiens (human)IC5014.100011
Cytochrome P450 2J2Homo sapiens (human)IC5014.100011
Cytochrome P450 3A4Homo sapiens (human)Ki0.028016
DBos taurus (cattle)IC504.090022
DRattus norvegicus (Norway rat)IC500.9957813
DBos taurus (cattle)Ki0.4200813
DRattus norvegicus (Norway rat)Ki0.35231324
D(1A) dopamine receptorHomo sapiens (human)IC500.202813
D(1A) dopamine receptorHomo sapiens (human)Ki0.34681325
D(1B) dopamine receptorRattus norvegicus (Norway rat)IC500.931257
D(1B) dopamine receptorHomo sapiens (human)Ki0.489022
D(1B) dopamine receptorRattus norvegicus (Norway rat)Ki0.174222
D(2) dopamine receptorBos taurus (cattle)IC501.804055
D(2) dopamine receptorHomo sapiens (human)IC500.3129813
D(2) dopamine receptorMus musculus (house mouse)IC500.290012
D(2) dopamine receptorRattus norvegicus (Norway rat)IC500.61641929
D(2) dopamine receptorBos taurus (cattle)Ki0.690011
D(2) dopamine receptorChlorocebus aethiops (grivet)Ki0.254022
D(2) dopamine receptorHomo sapiens (human)Ki0.146286119
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.17742756
D(3) dopamine receptorHomo sapiens (human)IC500.440225
D(3) dopamine receptorRattus norvegicus (Norway rat)IC500.931257
D(3) dopamine receptorChlorocebus aethiops (grivet)Ki0.466011
D(3) dopamine receptorHomo sapiens (human)Ki0.43243757
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki0.281356
D(4) dopamine receptorHomo sapiens (human)IC500.08681213
D(4) dopamine receptorRattus norvegicus (Norway rat)IC500.931257
D(4) dopamine receptorHomo sapiens (human)Ki0.25935266
D(4) dopamine receptorRattus norvegicus (Norway rat)Ki0.088055
Dihydrofolate reductase Bacillus anthracisIC50102.000011
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
Heat sensitive channel TRPV3Rattus norvegicus (Norway rat)IC5020.000011
Histamine H1 receptorHomo sapiens (human)IC500.039525
Histamine H1 receptorRattus norvegicus (Norway rat)IC500.023012
Histamine H1 receptorCavia porcellus (domestic guinea pig)Ki0.050413
Histamine H1 receptorHomo sapiens (human)Ki0.02591329
Histamine H1 receptorRattus norvegicus (Norway rat)Ki0.005012
Histamine H2 receptorHomo sapiens (human)IC503.610011
Histamine H2 receptorHomo sapiens (human)Ki3.550011
Histamine H3 receptorHomo sapiens (human)Ki0.815522
Histamine H4 receptorHomo sapiens (human)Ki0.192533
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
Mu-type opioid receptorHomo sapiens (human)IC502.272011
Mu-type opioid receptorHomo sapiens (human)Ki0.922011
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC501.100011
Multidrug and toxin extrusion protein 2Homo sapiens (human)IC5029.800011
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000015
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC501.031435
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC500.353759
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki1.1501820
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki0.013622
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC501.910412
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC500.441057
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki1.239726
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Ki0.035622
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC500.410713
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)IC500.441057
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.906027
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)Ki0.025111
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC501.359714
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC500.441057
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.6354311
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)Ki0.025111
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC500.953214
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC500.441057
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki1.102428
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)Ki0.025111
NeuraminidaseInfluenza A virus (A/USSR/90/1977(H1N1))IC50423.650022
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)IC5055.285512
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)Ki8.660611
Pancreatic triacylglycerol lipaseSus scrofa (pig)IC5070.000011
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CIC502.300011
Polyunsaturated fatty acid lipoxygenase ALOX15Oryctolagus cuniculus (rabbit)IC502.768011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC5012.93181540
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki17.400157
Receptor-type tyrosine-protein kinase FLT3Homo sapiens (human)IC5010.000011
Short transient receptor potential channel 3Homo sapiens (human)IC509.100011
Short transient receptor potential channel 4 Mus musculus (house mouse)IC506.400011
Short transient receptor potential channel 5Mus musculus (house mouse)IC501.100011
Short transient receptor potential channel 6Homo sapiens (human)IC5011.300011
Short transient receptor potential channel 7Mus musculus (house mouse)IC5026.500011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC501.166812
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)Ki3.160323
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC5016.900011
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC502.115927
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)Ki0.239245
Sodium-dependent dopamine transporter Homo sapiens (human)IC506.820522
Sodium-dependent dopamine transporter Homo sapiens (human)Ki0.448723
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC5068.100723
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki1.423323
Sodium-dependent serotonin transporterHomo sapiens (human)IC5050.667224
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)IC500.700023
Sodium-dependent serotonin transporterHomo sapiens (human)Ki4.806338
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Ki0.021011
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)IC5014.000011
Solute carrier family 22 member 1 Homo sapiens (human)IC5020.460011
Solute carrier family 22 member 2Homo sapiens (human)IC504.300011
Solute carrier family 22 member 2Rattus norvegicus (Norway rat)IC5026.000011
Transient receptor potential cation channel subfamily V member 1Rattus norvegicus (Norway rat)IC5020.000011
Transient receptor potential cation channel subfamily V member 2Rattus norvegicus (Norway rat)IC5020.000011
Transient receptor potential cation channel subfamily V member 4 Mus musculus (house mouse)IC5020.000011
TransporterRattus norvegicus (Norway rat)IC500.506723
TransporterRattus norvegicus (Norway rat)Ki0.916127
Type-2 angiotensin II receptorRattus norvegicus (Norway rat)Ki0.018011
TyrosinaseHomo sapiens (human)IC5050.000011
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC503.600011
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC503.600011
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC503.600011
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC503.600011
Xanthine dehydrogenase/oxidaseHomo sapiens (human)IC5025.970023

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1AHomo sapiens (human)Kd3.135412
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
Calmodulin Bos taurus (cattle)Kd61.000011
glycogen synthase kinase-3 beta isoform 1Homo sapiens (human)EC5015.800011
Histamine H1 receptorHomo sapiens (human)EC500.000411
Histamine H1 receptorHomo sapiens (human)Kd0.001612
Histamine H4 receptorHomo sapiens (human)Kd0.029444
Muscarinic acetylcholine receptor M1Homo sapiens (human)EC5040.000013
Muscarinic acetylcholine receptor M2Homo sapiens (human)EC5010.000011
Muscarinic acetylcholine receptor M3Homo sapiens (human)EC5010.000011
Muscarinic acetylcholine receptor M4Homo sapiens (human)EC5010.000011
Procathepsin LHomo sapiens (human)EC507.860011
Proteasome subunit alpha type-6Homo sapiens (human)EC5011.900011
Pyruvate kinase PKMHomo sapiens (human)EC500.001311
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)EC5015.850011
Spike glycoproteinBetacoronavirus England 1EC507.860011
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusEC507.860011
Transmembrane protease serine 2Homo sapiens (human)EC507.860011

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
Arginase Leishmania amazonensisKis6.900011
ATP-dependent translocase ABCB1Homo sapiens (human)Km26.200013
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
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CINH5.600011
Snq2pSaccharomyces cerevisiae EC1118INH3.200011
UDP-glucuronosyltransferase 1A4Homo sapiens (human)Km144.500022