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antipsychotic agent

Antipsychotic drugs are agents that control agitated psychotic behaviour, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect.

ChEBI ID: 35476

Members (16)

MemberDefinitionClass
azaperoneAn N-arylpiperazine that is 2-(piperazin-1-yl)pyridine in which the amino hydrogen is replaced by a 3-(4-fluobenzoyl)propyl group. Used mainly as a tranquiliser for pigs and elephants.azaperone
benzquinamidebenzquinamide
chlormezanoneA 1,3-thiazine that is 1,3-thiazinan-4-one S,S-dioxide in which a hydrogen at position 2 is substituted by a 4-chlorophenyl group and the hydrogen attached to the nitrogen is substituted by methyl. A non-benzodiazepine muscle relaxant, it was used in the management of anxiety and in the treatment of muscle spasms until being discontinued worldwide by its manufacturer in 1996, due to rare but serious cutaneous reactions.chlormezanone
dapiprazoledapiprazole
etazolateA pyrazolopyridine that is 1H-pyrazolo[3,4-b]pyridine which is substituted at positions 1, 4, and 5 by ethyl, 2-isopropylidenehydrazino, and ethoxycarbonyl groups, respectively. A phosphodiesterase IV inhibitor with antidepressant and anxiolytic properties.etazolate
levosulpirideAn optically active form of sulpiride having (S)-configuration. The active enantiomer of the racemic drug sulpiride. Selective D2-like dopamine antagonist (Ki values are ~ 0.015. ~ 0.013, 1, ~ 45 and ~ 77 muM at D2, D3, D4, D1 and D5 receptors respectively).(S)-(-)-sulpiride
loxapineloxapine
ly 379268An organic heterobicyclic compound that is (1R,5S)-2-oxabicyclo[3.1.0]hexane carrying amino, carboxy, and carboxy groups at positions 4R, 4R and 6R, respectively. It is a potent agonist of group II metabotropic glutamate receptors mGluR2 and mGluR3 (EC50 = 2.69 nM and 4.48 nM, respectively) that exhibits antipsychotic-like action in animal models of schizophrenia.LY 379268
ly 404039An organic heterobicyclic compound that is (1S,5R)-2-thiabicyclo[3.1.0]hexane carrying oxo, oxo, amino, carboxy, and carboxy groups at positions 2, 2, 4S, 4S, and 6S, respectively. It is a potent agonist of group II metabotropic glutamate receptors mGluR2 mGluR3 (Ki = 149 nM and 92 nM, respectively) and exhibits antipsychotic and anxiolytic efficacy in animal models.LY404039
methiothepinA dibenzothiepine that is 10,11-dihydrodibenzo[b,f]thiepine bearing additional methylthio and 4-methylpiperazin-1-yl substituents at positions 8 and 10 respectively. Potent 5-HT2 antagonist, also active as 5-HT1 antagonist. Differentiates 5-HT1D sub-types. Also displays affinity for rodent 5-HT5B, 5-HT5A, 5-HT7 and 5-HT6 receptors (pK1 values are 6.6, 7.0, 8.4 and 8.7 respectively).methiothepin
n,n-dipropyl-2-(4-methoxy-3-(2-phenylethoxy)phenyl)ethylamine monohydrochlorideAn aromatic ether that is (2-phenoxyethyl)benzene which carries a 2-(dipropylamino)ethyl group at position 3 and a methoxy group at position 6. It is a potent and selective sigma1 receptor antagonist.N-{2-[4-methoxy-3-(2-phenylethoxy)phenyl]ethyl}-N-propylpropan-1-amine hydrochloride
pimavanserinA member of the class of ureas in which three of the four hydrogens are replaced by 4-fluorobenzyl, 1-methylpiperidin-4-yl, and 4-(isopropyloxy)benzyl groups. An atypical antipsychotic that is used (in the form of its tartrate salt) for treatment of hallucinations and delusions associated with Parkinson's disease.pimavanserin
ritanserinA thiazolopyrimidine that is 5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one which is substituted at position 7 by a methyl group and at position 6 by a 2-{4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl}ethyl group. A potent and long-acting seratonin (5-hydroxytryptamine, 5-HT) antagonist of the subtype 5-HT2 (Ki = 0.39 nM), it is used in the treatment of a variety of disorders including anxiety, depression and schizophrenia. It has little sedative action.ritanserin
spiperoneAn azaspiro compound that is 1,3,8-triazaspiro[4.5]decane which is substituted at positions 1, 4, and 8 by phenyl, oxo, and 4-(p-fluorophenyl)-4-oxobutyl groups, respectively.spiperone
sulpirideA member of the class of benzamides obtained from formal condensation between the carboxy group of 2-methoxy-5-sulfamoylbenzoic acid and the primary amino group of (1-ethylpyrrolidin-2-yl)methylamine.sulpiride
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 (9,721)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19903,633 (37.37)18.7374
1990's2,448 (25.18)18.2507
2000's1,858 (19.11)29.6817
2010's1,498 (15.41)24.3611
2020's284 (2.92)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials967 (8.88%)5.53%
Reviews538 (4.94%)6.00%
Case Studies648 (5.95%)4.05%
Observational11 (0.10%)0.25%
Other8,725 (80.13%)84.16%

Protein Targets (318)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency28.183811
15-lipoxygenase, partialHomo sapiens (human)Potency31.622811
67.9K proteinVaccinia virusPotency33.997212
acetylcholinesteraseHomo sapiens (human)Potency29.3671310
activating transcription factor 6Homo sapiens (human)Potency14.318523
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency17.900812
alpha-galactosidaseHomo sapiens (human)Potency39.810711
AR proteinHomo sapiens (human)Potency21.79861031
aryl hydrocarbon receptorHomo sapiens (human)Potency47.302624
arylsulfatase AHomo sapiens (human)Potency16.274316
ATAD5 protein, partialHomo sapiens (human)Potency17.036336
Ataxin-2Homo sapiens (human)Potency22.998625
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency11.998613
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency28.899323
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency23.934111
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency21.301612
Bloom syndrome protein isoform 1Homo sapiens (human)Potency5.928326
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency42.800012
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency33.491511
caspase-3Homo sapiens (human)Potency33.491511
Cellular tumor antigen p53Homo sapiens (human)Potency22.934215
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency13.911524
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency35.481311
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency6.309611
Chain A, Beta-lactamaseEscherichia coli K-12Potency14.329523
Chain A, CruzipainTrypanosoma cruziPotency39.810711
Chain A, Ferritin light chainEquus caballus (horse)Potency40.074822
Chain A, HADH2 proteinHomo sapiens (human)Potency32.644825
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency39.810711
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency28.173023
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency15.848911
Chain B, HADH2 proteinHomo sapiens (human)Potency32.644825
chromobox protein homolog 1Homo sapiens (human)Potency33.403614
CREB-binding proteinHomo sapiens (human)Potency5.441533
cytochrome P450 2C19 precursorHomo sapiens (human)Potency12.001914
cytochrome P450 2C9 precursorHomo sapiens (human)Potency23.110313
cytochrome P450 2C9, partialHomo sapiens (human)Potency25.191815
cytochrome P450 2D6Homo sapiens (human)Potency5.760416
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency8.026516
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency13.9667212
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency19.0761210
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency25.509815
D(1A) dopamine receptorHomo sapiens (human)Potency3.7150311
D(1A) dopamine receptorSus scrofa (pig)Potency18.492711
D(3) dopamine receptor isoform eHomo sapiens (human)Potency0.089111
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency15.848911
DNA polymerase III, partialBacillus subtilisPotency21.192311
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency28.258012
DNA polymerase kappa isoform 1Homo sapiens (human)Potency29.934911
dopamine D1 receptorHomo sapiens (human)Potency0.058011
estrogen nuclear receptor alphaHomo sapiens (human)Potency18.8641828
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency16.652925
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency21.5650924
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency27.3723111
EWS/FLI fusion proteinHomo sapiens (human)Potency20.9587413
farnesoid X nuclear receptorHomo sapiens (human)Potency23.875124
flap endonuclease 1Homo sapiens (human)Potency26.679511
Fumarate hydrataseHomo sapiens (human)Potency31.403015
GVesicular stomatitis virusPotency25.191815
GABA theta subunitRattus norvegicus (Norway rat)Potency13.966716
GALC proteinHomo sapiens (human)Potency0.707911
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency13.966716
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency13.966716
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency13.966716
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency13.966716
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency13.966716
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency13.966716
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency13.966716
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency13.966716
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency13.966716
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency13.966716
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency13.966716
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency13.966716
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency13.966716
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency13.966716
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency13.966716
gemininHomo sapiens (human)Potency10.8425311
GLI family zinc finger 3Homo sapiens (human)Potency14.201328
glp-1 receptor, partialHomo sapiens (human)Potency19.091912
GLS proteinHomo sapiens (human)Potency12.698624
glucocerebrosidaseHomo sapiens (human)Potency17.782811
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency25.4348312
glucokinase regulatory proteinHomo sapiens (human)Potency35.481311
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency17.508012
Guanine nucleotide-binding protein GHomo sapiens (human)Potency28.183811
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency16.034123
heat shock protein beta-1Homo sapiens (human)Potency33.488922
hexokinase-4 isoform 1Homo sapiens (human)Potency35.481311
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency18.0750217
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency37.646012
histone deacetylase 9 isoform 3Homo sapiens (human)Potency29.014422
Histone H2A.xCricetulus griseus (Chinese hamster)Potency52.195222
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency25.191815
huntingtin isoform 2Homo sapiens (human)Potency35.481311
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency17.296612
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency12.665828
IDH1Homo sapiens (human)Potency23.109311
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency25.1918110
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency3.548111
Integrin alpha-IIbHomo sapiens (human)Potency18.317412
Integrin beta-3Homo sapiens (human)Potency18.317412
Interferon betaHomo sapiens (human)Potency27.219326
lamin isoform A-delta10Homo sapiens (human)Potency16.824028
lethal factor (plasmid)Bacillus anthracis str. A2012Potency14.026013
M-phase phosphoprotein 8Homo sapiens (human)Potency30.568713
Microtubule-associated protein tauHomo sapiens (human)Potency18.748427
mitogen-activated protein kinase 1Homo sapiens (human)Potency13.623523
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency8.100525
neuropeptide S receptor isoform AHomo sapiens (human)Potency10.226912
NFKB1 protein, partialHomo sapiens (human)Potency5.011922
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency19.321812
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency80.078314
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency12.063426
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency25.859813
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency25.133425
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency14.989326
Ornithine decarboxylaseRattus norvegicus (Norway rat)Potency0.006312
ParkinHomo sapiens (human)Potency25.929011
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency32.897012
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency64.634012
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency18.148834
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency26.278825
phosphopantetheinyl transferaseBacillus subtilisPotency45.285213
polyproteinZika virusPotency31.403015
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency12.410314
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency7.447917
pregnane X nuclear receptorHomo sapiens (human)Potency9.726225
progesterone receptorHomo sapiens (human)Potency26.592036
pyruvate kinase PKM isoform bHomo sapiens (human)Potency0.006323
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency39.810711
RAR-related orphan receptor gammaMus musculus (house mouse)Potency22.382628
ras-related protein Rab-9AHomo sapiens (human)Potency63.628614
regulator of G-protein signaling 4Homo sapiens (human)Potency25.212713
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency22.986137
retinoid X nuclear receptor alphaHomo sapiens (human)Potency17.189929
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency17.892945
SMAD family member 2Homo sapiens (human)Potency27.010522
SMAD family member 3Homo sapiens (human)Potency27.010522
Smad3Homo sapiens (human)Potency14.333512
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.810711
survival motor neuron protein isoform dHomo sapiens (human)Potency28.466114
TDP1 proteinHomo sapiens (human)Potency17.8144215
thioredoxin glutathione reductaseSchistosoma mansoniPotency31.622811
thioredoxin reductaseRattus norvegicus (Norway rat)Potency5.037427
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency18.3058210
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency81.160322
thyroid stimulating hormone receptorHomo sapiens (human)Potency21.9596511
thyrotropin-releasing hormone receptorHomo sapiens (human)Potency9.987822
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency15.848911
USP1 protein, partialHomo sapiens (human)Potency45.911526
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency14.269926
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency23.946034
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency56.084614
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency17.508012

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
3-hydroxy-3-methylglutaryl-coenzyme A reductase Rattus norvegicus (Norway rat)Ki0.013011
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC504.260022
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki0.04951315
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.357677
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC502.060011
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki2.045733
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Ki0.160011
5-hydroxytryptamine receptor 1EHomo sapiens (human)IC5050.000011
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)Ki0.160011
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC500.0741711
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC500.125878
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.01701924
5-hydroxytryptamine receptor 2AMus musculus (house mouse)Ki0.000811
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki1.93201314
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC500.192726
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC500.167766
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.336822
5-hydroxytryptamine receptor 2BMus musculus (house mouse)Ki0.000811
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki3.375878
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC500.120926
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC500.286677
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.33161722
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki2.9606910
5-hydroxytryptamine receptor 2C Mus musculus (house mouse)Ki0.000811
5-hydroxytryptamine receptor 3AHomo sapiens (human)Ki0.398111
5-hydroxytryptamine receptor 3BHomo sapiens (human)Ki0.398111
5-hydroxytryptamine receptor 3CHomo sapiens (human)Ki0.398111
5-hydroxytryptamine receptor 3DHomo sapiens (human)Ki0.398111
5-hydroxytryptamine receptor 3EHomo sapiens (human)Ki0.398111
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC500.625011
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.327011
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)IC5035.000011
5-hydroxytryptamine receptor 5AHomo sapiens (human)Ki12.626745
5-hydroxytryptamine receptor 6Homo sapiens (human)IC500.030055
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.18681719
5-hydroxytryptamine receptor 6Rattus norvegicus (Norway rat)Ki0.067933
5-hydroxytryptamine receptor 7Homo sapiens (human)IC500.007555
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki0.16721824
5-hydroxytryptamine receptor 7 Mus musculus (house mouse)Ki0.063011
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki0.018237
Alpha-1A adrenergic receptorHomo sapiens (human)IC500.011011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC501.842766
Alpha-1A adrenergic receptorBos taurus (cattle)Ki0.013511
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.009044
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki1.5138810
Alpha-1B adrenergic receptorHomo sapiens (human)IC500.011011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC502.740544
Alpha-1B adrenergic receptorHomo sapiens (human)Ki0.008655
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki2.160467
Alpha-1D adrenergic receptorHomo sapiens (human)IC500.009722
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC502.740544
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.008055
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki1.893178
Alpha-2A adrenergic receptorHomo sapiens (human)IC502.019011
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC500.151411
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.512333
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki0.007211
Alpha-2B adrenergic receptorHomo sapiens (human)IC501.153011
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC500.151411
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.435333
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki0.007211
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC500.151411
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.390022
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki0.007211
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki0.002212
Aspartate aminotransferase, cytoplasmicHomo sapiens (human)IC505.390011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000011
Beta-carbonic anhydrase 1Mycobacterium tuberculosis H37RvKi2.300011
Beta-caseinRattus norvegicus (Norway rat)Ki0.001511
Bile salt export pumpHomo sapiens (human)IC50354.800034
Bile salt export pumpRattus norvegicus (Norway rat)IC501,000.000011
Calcitonin gene-related peptide type 1 receptorHomo sapiens (human)Ki0.052011
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)Ki60.000011
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)Ki60.000011
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)Ki60.000011
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC500.390011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000011
Carbonic anhydraseCandida albicans SC5314Ki0.760022
Carbonic anhydraseHelicobacter pylori 26695Ki0.191522
Carbonic anhydraseSaccharomyces cerevisiae S288CKi0.124011
Carbonic anhydraseStylophora pistillataKi0.415011
Carbonic anhydrase Anopheles gambiae (African malaria mosquito)Ki0.029511
Carbonic anhydrase Astrosclera willeyanaKi0.378011
Carbonic anhydrase Cryptococcus neoformans var. grubiiKi0.812011
Carbonic anhydrase Nakaseomyces glabratus CBS 138Ki0.113011
Carbonic anhydrase Stylophora pistillataKi0.430022
Carbonic anhydrase Sulfurihydrogenibium sp. YO3AOP1Ki0.067411
Carbonic anhydrase 1Homo sapiens (human)IC501.200011
Carbonic anhydrase 1Homo sapiens (human)Ki4.21833335
Carbonic anhydrase 12Homo sapiens (human)Ki0.003933
Carbonic anhydrase 15Mus musculus (house mouse)Ki0.073011
Carbonic anhydrase 2Homo sapiens (human)IC500.040011
Carbonic anhydrase 2Homo sapiens (human)Ki0.31704043
Carbonic anhydrase 2Mycobacterium tuberculosis H37RvKi0.266011
Carbonic anhydrase 3Homo sapiens (human)Ki10.600011
Carbonic anhydrase 4Bos taurus (cattle)IC500.620011
Carbonic anhydrase 5A, mitochondrialHomo sapiens (human)Ki0.174011
Carbonic anhydrase 5B, mitochondrialHomo sapiens (human)Ki0.018011
Carbonic anhydrase 6Homo sapiens (human)Ki2.007246
Carbonic anhydrase 7Homo sapiens (human)Ki2.421233
Carbonic anhydrase 9Homo sapiens (human)Ki0.040967
Carbonic anhydrase, alpha family Hydrogenovibrio crunogenus XCL-2Ki0.873011
cGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)Ki12.000011
cGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)Ki12.000011
Cytochrome P450 1A2Homo sapiens (human)IC5052.000011
Cytochrome P450 2C19Homo sapiens (human)IC5049.800011
Cytochrome P450 2C9 Homo sapiens (human)IC5075.000022
Cytochrome P450 2D6Homo sapiens (human)IC50100.000011
Cytochrome P450 2J2Homo sapiens (human)IC5050.000011
Cytochrome P450 3A4Homo sapiens (human)IC50100.000011
Cytochrome P450 3A4Homo sapiens (human)Ki0.061012
DMus musculus (house mouse)IC5035.000011
DRattus norvegicus (Norway rat)IC500.575722
DBos taurus (cattle)Ki50.000022
DRattus norvegicus (Norway rat)Ki1.151044
D(1A) dopamine receptorHomo sapiens (human)IC5010.000011
D(1A) dopamine receptorHomo sapiens (human)Ki0.094245
D(1B) dopamine receptorMus musculus (house mouse)IC5035.000011
D(1B) dopamine receptorRattus norvegicus (Norway rat)Ki0.801022
D(2) dopamine receptorCanis lupus familiaris (dog)IC500.200011
D(2) dopamine receptorHomo sapiens (human)IC501.0446910
D(2) dopamine receptorMus musculus (house mouse)IC5035.000011
D(2) dopamine receptorRattus norvegicus (Norway rat)IC500.21081416
D(2) dopamine receptorHomo sapiens (human)Ki0.04133440
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.07971728
D(3) dopamine receptorHomo sapiens (human)IC500.141378
D(3) dopamine receptorMus musculus (house mouse)IC5035.000011
D(3) dopamine receptorHomo sapiens (human)Ki0.03192126
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki0.801022
D(4) dopamine receptorHomo sapiens (human)IC500.007222
D(4) dopamine receptorMus musculus (house mouse)IC5035.000011
D(4) dopamine receptorHomo sapiens (human)Ki0.34251619
D(4) dopamine receptorRattus norvegicus (Norway rat)Ki0.801022
Delta carbonic anhydraseConticribra weissflogiiKi0.259011
Delta-type opioid receptorMus musculus (house mouse)Ki0.620022
Delta-type opioid receptorRattus norvegicus (Norway rat)Ki0.040011
Diacylglycerol kinase alphaHomo sapiens (human)IC5012.850022
Endothelin receptor type BHomo sapiens (human)Ki0.017924
Endothelin receptor type BRattus norvegicus (Norway rat)Ki0.017912
GABA theta subunitRattus norvegicus (Norway rat)Ki1.000011
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki1.000011
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki1.000011
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki1.000011
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki1.000011
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Ki1.000011
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Ki1.000011
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Ki1.000011
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Ki1.000011
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Ki1.000011
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Ki1.000011
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Ki1.000011
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Ki1.000011
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Ki1.000011
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Ki1.000011
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Ki1.000011
Glutamate receptor 1Rattus norvegicus (Norway rat)IC50100.000011
Glutamate receptor 2Rattus norvegicus (Norway rat)IC50100.000011
Glutamate receptor 3Rattus norvegicus (Norway rat)IC50100.000011
Glutamate receptor 4Rattus norvegicus (Norway rat)IC50100.000011
Glutamate receptor ionotropic, kainate 1Rattus norvegicus (Norway rat)IC50100.000011
Glutamate receptor ionotropic, kainate 2Rattus norvegicus (Norway rat)IC50100.000011
Glutamate receptor ionotropic, kainate 3Rattus norvegicus (Norway rat)IC50100.000011
Glutamate receptor ionotropic, kainate 4Rattus norvegicus (Norway rat)IC50100.000011
Glutamate receptor ionotropic, kainate 5Rattus norvegicus (Norway rat)IC50100.000011
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)IC501.000011
Glycogen phosphorylase, brain formHomo sapiens (human)Ki49.600011
Glycogen phosphorylase, muscle formHomo sapiens (human)Ki49.600011
Histamine H1 receptorCavia porcellus (domestic guinea pig)IC500.097011
Histamine H1 receptorRattus norvegicus (Norway rat)IC501.000012
Histamine H1 receptorCavia porcellus (domestic guinea pig)Ki0.006011
Histamine H1 receptorHomo sapiens (human)Ki0.153144
Histamine H4 receptorHomo sapiens (human)Ki4.275922
Metabotropic glutamate receptor 1Homo sapiens (human)Ki100.000011
Metabotropic glutamate receptor 2Homo sapiens (human)Ki0.369436
Metabotropic glutamate receptor 3Homo sapiens (human)Ki0.193736
Metabotropic glutamate receptor 4Homo sapiens (human)Ki21.000011
Metabotropic glutamate receptor 5Homo sapiens (human)Ki100.000011
Metabotropic glutamate receptor 6Homo sapiens (human)Ki0.400011
Metabotropic glutamate receptor 7Homo sapiens (human)Ki100.000011
Metabotropic glutamate receptor 8Homo sapiens (human)Ki1.700011
Mu-type opioid receptorCavia porcellus (domestic guinea pig)Ki0.040011
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki1.200011
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000011
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC505.500011
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki17.425044
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki49.600011
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki27.300022
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Ki49.600011
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki27.300022
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)Ki49.600011
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki27.300022
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)Ki49.600011
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki27.300022
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)Ki49.600011
MyeloperoxidaseHomo sapiens (human)IC507.680011
Potassium channel subfamily K member 2Homo sapiens (human)IC5020.000011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC500.2481910
Sigma intracellular receptor 2Homo sapiens (human)Ki0.051112
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC500.955011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.405212
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC500.151412
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)Ki0.294146
Sodium-dependent dopamine transporter Homo sapiens (human)Ki0.003122
Sodium-dependent serotonin transporterHomo sapiens (human)Ki0.066222
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Ki0.021011
sphingosine 1-phosphate receptor 3Homo sapiens (human)IC5050.000011
TransporterRattus norvegicus (Norway rat)Ki0.048011
ubiquitin-conjugating enzyme E2 NHomo sapiens (human)IC5020.000011
Vesicular acetylcholine transporterRattus norvegicus (Norway rat)Ki1.033011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1AHomo sapiens (human)Kd0.097023
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Kd0.000822
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Kd0.001611
5-hydroxytryptamine receptor 2CHomo sapiens (human)EC500.000411
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Kd0.001611
5-hydroxytryptamine receptor 7Homo sapiens (human)EC500.000611
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Kd0.000111
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Kd0.031612
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Kd0.031612
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Kd0.031612
alternatively spliced Trp4Mus musculus (house mouse)EC506.682711
D(2) dopamine receptorHomo sapiens (human)Kd0.001033
D(3) dopamine receptorHomo sapiens (human)Kd0.039811
G protein-coupled receptorHuman betaherpesvirus 5EC500.330612
G-protein coupled receptor homolog US28Human herpesvirus 5 strain AD169EC500.352412
Histamine H4 receptorHomo sapiens (human)EC500.218811
HLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)Kd2.500011
Metabotropic glutamate receptor 1Homo sapiens (human)EC50100.000011
Metabotropic glutamate receptor 2Homo sapiens (human)EC500.007934
Metabotropic glutamate receptor 3Homo sapiens (human)EC500.015434
Metabotropic glutamate receptor 4Homo sapiens (human)EC5021.100011
Metabotropic glutamate receptor 6Homo sapiens (human)EC5050.200522
Metabotropic glutamate receptor 7Homo sapiens (human)EC50100.000011
Metabotropic glutamate receptor 8Homo sapiens (human)EC5017.051023
Potassium channel subfamily K member 2Homo sapiens (human)EC5019.700011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Kb0.014011
5-hydroxytryptamine receptor 2AHomo sapiens (human)Activity0.000311
5-hydroxytryptamine receptor 2AHomo sapiens (human)Kb0.000611
5-hydroxytryptamine receptor 6Homo sapiens (human)Kb0.003711
5-hydroxytryptamine receptor 7Homo sapiens (human)Kb0.000122
Carbonic anhydrase Brucella suis 1330Kinact0.019011
Carbonic anhydrase 1Homo sapiens (human)Kinact1.200022
Carbonic anhydrase 2Homo sapiens (human)Kinact0.040022
Carbonic anhydrase 9Homo sapiens (human)Kinact0.031011
D(2) dopamine receptorHomo sapiens (human)Activity0.009711
D(2) dopamine receptorRattus norvegicus (Norway rat)K 0.50.000222
D(2) dopamine receptorHomo sapiens (human)Kb0.003011
D(3) dopamine receptorHomo sapiens (human)K0.008111
D(3) dopamine receptorRattus norvegicus (Norway rat)K 0.50.000411
D(3) dopamine receptorHomo sapiens (human)Kb0.040011
Histamine H1 receptorHomo sapiens (human)Activity0.043011
Histamine H2 receptorCavia porcellus (domestic guinea pig)K0.50.272012
Metabotropic glutamate receptor 1Homo sapiens (human)Activity100.000011
Metabotropic glutamate receptor 2Homo sapiens (human)Activity0.003011
Metabotropic glutamate receptor 3Homo sapiens (human)Activity0.005011
Metabotropic glutamate receptor 4Homo sapiens (human)Activity21.000011
Metabotropic glutamate receptor 5Homo sapiens (human)Activity100.000011
Metabotropic glutamate receptor 6Homo sapiens (human)Activity0.400011
Metabotropic glutamate receptor 7Homo sapiens (human)Activity100.000011
Metabotropic glutamate receptor 8Homo sapiens (human)Activity2.000011
UDP-glucuronosyltransferase 1A4Homo sapiens (human)Km27.000011