Page last updated: 2024-08-05 15:14:45

central nervous system stimulant

Any drug that enhances the activity of the central nervous system.

ChEBI ID: 35337

Members (19)

MemberDefinitionClass
1,7-dimethylxanthineA dimethylxanthine having the two methyl groups located at positions 1 and 7. It is a metabolite of caffeine and theobromine in animals.1,7-dimethylxanthine
8-chlorotheophylline1,3-Dimethylxanthine in which the hydrogen at position 8 is substituted by chlorine.8-chlorotheophylline
almitrineA triamino-1,3,5-triazine compound having allylamino substituents at the 2- and 4-positions and a 4-(bis(p-fluorophenyl)methyl)-1-piperazinyl group at the 6-position.almitrine
almitrine dimesylateThe dimethanesulfonate salt of almitrine.almitrine dimesylate
armodafinilA 2-[(diphenylmethyl)sulfinyl]acetamide that has R configuration at the sulfur atom. Like its racemate, modafinil, it is used for the treatment of sleeping disorders such as narcolepsy, obstructive sleep apnoea, and shift-work sleep disorder. Peak concentration in the blood later occurs later following administration than with modafinil, so it is thought that armodafinil may be more effective than modafinil in treating people with excessive daytime sleepiness.armodafinil
benzydamineA member of the class of indazoles carrying benzyl and 3-(dimethylamino)propyl groups at positions 1 and 3 respectively. A locally-acting nonsteroidal anti-inflammatory drug that also exhibits local anaesthetic and analgesic properties.benzydamine
bicucullineA benzylisoquinoline alkaloid that is 6-methyl-5,6,7,8-tetrahydro[1,3]dioxolo[4,5-g]isoquinoline which is substituted at the 5-pro-S position by a (6R)-8-oxo-6,8-dihydrofuro[3,4-e][1,3]benzodioxol-6-yl group. A light-sensitive competitive antagonist of GABAA receptors. It was originally identified in 1932 in plant alkaloid extracts and has been isolated from Dicentra cucullaria, Adlumia fungosa, Fumariaceae, and several Corydalis species.bicuculline
caffeineA trimethylxanthine in which the three methyl groups are located at positions 1, 3, and 7. A purine alkaloid that occurs naturally in tea and coffee.caffeine
cathinoneThe S stereoisomer of 2-aminopropiophenone.cathinone
cgs 15943A member of the class of triazoloquinazolines that is [1,2,4]triazolo[1,5-c]quinazoline substited at positions 2, 5 and 9 by furan-2-yl, amino and chloro groups respectively. A potent antagonist at adenosine A1 and adenosine A2A receptors.9-chloro-2-(2-furanyl)-[1,2,4]triazolo[1,5-c]quinazolin-5-amine; CGS 15943
cocaineA tropane alkaloid obtained from leaves of the South American shrub Erythroxylon coca.cocaine
cocaine hydrochlorideThe hydrochloride salt of cocaine. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse.cocaine hydrochloride
doxapramA member of the class of pyrrolidin-2-ones that is N-ethylpyrrolidin-2-one in which both of the hydrogens at the 3 position (adjacent to the carbonyl group) are substituted by phenyl groups, and one of the hydrogens at the 4 position is substituted by a 2-(morpholin-4-yl)ethyl group. A central and respiratory stimulant with a brief duration of action, it is used (generally as the hydrochloride or the hydrochloride hydrate) as a temporary treatment of acute respiratory failure, particularly when superimposed on chronic obstructive pulmonary disease, and of postoperative respiratory depression. It has also been used for treatment of postoperative shivering.doxapram
doxapram hydrochlorideThe hydrochloride salt of doxapram. A central and respiratory stimulant with a brief duration of action, both doxapram hydrochloride and its hydrate are used as a temporary treatment of acute respiratory failure, particularly when superimposed on chronic obstructive pulmonary disease, and of postoperative respiratory depression. It has also been used for treatment of postoperative shivering.doxapram hydrochloride (anhydrous)
methamphetamineA member of the class of amphetamines in which the amino group of (S)-amphetamine carries a methyl substituent.methamphetamine
norpseudoephedrineAn amphetamine that is propylbenzene substituted by a hydroxy group at position 1 and by an amino group at position 2 (the 1S,2S-stereoisomer).cathine
pemolineA member of the class of 1,3-oxazoles that is 1,3-oxazol-4(5H)-one which is substituted by an amino group at position 2 and by a phenyl group at position 5. A central nervous system stimulant, it was used to treat hyperactivity disorders in children, but withdrawn from use following reports of serious hepatotoxicity.pemoline
phenterminephentermine
tenocyclidineA tertiary amino compound that consists of cyclohexane having piperidin-1-yl and thiophen-2-yl groups attached at position 1. A dissociative anaesthetic drug with halluccinogenic and stimulant effects. Its effects are similar to those of phencyclidine (PCP, an analogue with the thienyl group replaced by phenyl), but it is rather more potent.tenocyclidine

Research

Studies (73,059)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199017,766 (24.32)18.7374
1990's15,606 (21.36)18.2507
2000's15,777 (21.59)29.6817
2010's17,666 (24.18)24.3611
2020's6,244 (8.55)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials4,442 (5.59%)5.53%
Reviews5,309 (6.68%)6.00%
Case Studies3,470 (4.36%)4.05%
Observational148 (0.19%)0.25%
Other66,165 (83.19%)84.16%

Protein Targets (248)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
2,3-bisphosphoglycerate-independent phosphoglycerate mutaseLeishmania major strain FriedlinPotency21.331311
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.810711
AR proteinHomo sapiens (human)Potency32.136279
arylsulfatase AHomo sapiens (human)Potency2.393411
ATAD5 protein, partialHomo sapiens (human)Potency17.795722
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency42.561511
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency4.775511
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.631022
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency15.848912
Chain A, Ferritin light chainEquus caballus (horse)Potency14.217522
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency6.309611
chromobox protein homolog 1Homo sapiens (human)Potency78.767723
CREB-binding proteinHomo sapiens (human)Potency10.578533
cytochrome P450 2C9 precursorHomo sapiens (human)Potency31.622811
cytochrome P450 2D6Homo sapiens (human)Potency13.636812
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency10.266312
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency23.877024
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency6.575812
D(1A) dopamine receptorHomo sapiens (human)Potency3.804622
D(1A) dopamine receptorSus scrofa (pig)Potency18.492711
DNA dC->dU-editing enzyme APOBEC-3G isoform 1Homo sapiens (human)Potency0.595711
DNA polymerase betaHomo sapiens (human)Potency79.432811
DNA polymerase kappa isoform 1Homo sapiens (human)Potency11.917311
endonuclease IVEscherichia coliPotency10.000011
estrogen nuclear receptor alphaHomo sapiens (human)Potency42.460369
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency17.7280711
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency7.502117
farnesoid X nuclear receptorHomo sapiens (human)Potency22.143011
GABA theta subunitRattus norvegicus (Norway rat)Potency23.877012
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency23.877012
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency23.877012
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency23.877012
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency23.877012
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency23.877012
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency23.877012
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency23.877012
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency23.877012
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency23.877012
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency23.877012
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency23.877012
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency23.877012
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency23.877012
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency23.877012
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency23.877012
gemininHomo sapiens (human)Potency4.180733
GLI family zinc finger 3Homo sapiens (human)Potency22.059324
GLS proteinHomo sapiens (human)Potency42.800022
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency0.017811
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency33.515712
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency24.009425
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency19.968312
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency65.811412
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency5.660724
importin subunit beta-1 isoform 1Homo sapiens (human)Potency40.397312
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency31.622811
lamin isoform A-delta10Homo sapiens (human)Potency5.620113
lethal factor (plasmid)Bacillus anthracis str. A2012Potency4.949413
M-phase phosphoprotein 8Homo sapiens (human)Potency50.118711
Microtubule-associated protein tauHomo sapiens (human)Potency24.059324
mitogen-activated protein kinase 1Homo sapiens (human)Potency3.981111
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.035511
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency35.481311
Nrf2Homo sapiens (human)Potency1.458111
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency11.690624
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency8.141113
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency35.365724
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency5.489711
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency61.427212
phosphopantetheinyl transferaseBacillus subtilisPotency89.125111
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency12.589311
pregnane X nuclear receptorHomo sapiens (human)Potency15.720224
progesterone receptorHomo sapiens (human)Potency2.984911
RAR-related orphan receptor gammaMus musculus (house mouse)Potency11.754524
ras-related protein Rab-9AHomo sapiens (human)Potency1.258911
regulator of G-protein signaling 4Homo sapiens (human)Potency0.418912
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency69.427523
retinoid X nuclear receptor alphaHomo sapiens (human)Potency19.734911
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency13.009933
snurportin-1Homo sapiens (human)Potency40.397312
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency11.220211
TDP1 proteinHomo sapiens (human)Potency4.206927
thioredoxin reductaseRattus norvegicus (Norway rat)Potency31.278425
ThrombopoietinHomo sapiens (human)Potency12.589322
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency18.723222
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency0.001022
thyroid stimulating hormone receptorHomo sapiens (human)Potency25.082055
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency21.721323
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency1.899611
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency50.118711
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency33.515712

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC500.085522
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC500.085522
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC500.085522
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 5ARattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 5BRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 6Rattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki0.301011
AcetylcholinesteraseHomo sapiens (human)IC507.250011
Acidic mammalian chitinaseHomo sapiens (human)IC502,500.000011
Adenosine receptor A1Rattus norvegicus (Norway rat)IC5075.668723
Adenosine receptor A1Cavia porcellus (domestic guinea pig)Ki83.335056
Adenosine receptor A1Homo sapiens (human)Ki31.26521717
Adenosine receptor A1Rattus norvegicus (Norway rat)Ki31.01543540
Adenosine receptor A2aHomo sapiens (human)IC5010.242022
Adenosine receptor A2aRattus norvegicus (Norway rat)IC5028.6379211
Adenosine receptor A2aCavia porcellus (domestic guinea pig)Ki50.000033
Adenosine receptor A2aHomo sapiens (human)Ki11.04253639
Adenosine receptor A2aRattus norvegicus (Norway rat)Ki130.55173137
Adenosine receptor A2bHomo sapiens (human)IC500.630422
Adenosine receptor A2bRattus norvegicus (Norway rat)IC5031.5014110
Adenosine receptor A2bHomo sapiens (human)Ki20.31432325
Adenosine receptor A2bMus musculus (house mouse)Ki23.000011
Adenosine receptor A2bRattus norvegicus (Norway rat)Ki35.30501520
Adenosine receptor A3Homo sapiens (human)IC500.406011
Adenosine receptor A3Rattus norvegicus (Norway rat)IC500.060711
Adenosine receptor A3Homo sapiens (human)Ki16.96783030
Adenosine receptor A3Rattus norvegicus (Norway rat)Ki56.666766
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC505.754411
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC505.754411
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC505.754411
Amine oxidase [flavin-containing] AHomo sapiens (human)IC5050.000011
Amine oxidase [flavin-containing] BHomo sapiens (human)IC5050.000011
Amine oxidase [flavin-containing] BBos taurus (cattle)Ki550.000011
Amine oxidase [flavin-containing] BHomo sapiens (human)Ki3,700.000022
Amine oxidase [flavin-containing] BRattus norvegicus (Norway rat)Ki270.000011
Amyloid-beta precursor proteinHomo sapiens (human)IC500.338011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000012
Bile salt export pumpHomo sapiens (human)IC50350.250034
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC5014,000.000011
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BRattus norvegicus (Norway rat)IC5070.000011
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CRattus norvegicus (Norway rat)IC5070.000011
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)IC50747.000011
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)Ki1.115011
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)Ki1.115011
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)Ki1.115011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000012
Carbonic anhydrase 1Homo sapiens (human)IC5028,500.000012
Carbonic anhydrase 2Homo sapiens (human)IC5028,500.000012
Casein kinase I isoform alphaHomo sapiens (human)IC500.820011
Casein kinase I isoform deltaHomo sapiens (human)IC500.240011
Casein kinase I isoform epsilonHomo sapiens (human)IC500.490011
Chain A, ChitinaseClonostachys roseaKi19,700.000011
Chain A, EndochitinaseSaccharomyces cerevisiae (brewer's yeast)Ki600.000013
Chain A, Glycogen PhosphorylaseOryctolagus cuniculus (rabbit)Ki100.000011
Chitotriosidase-1Homo sapiens (human)IC50363.000012
CholinesteraseHomo sapiens (human)IC5050.000011
Cytochrome P450 11B1, mitochondrialRattus norvegicus (Norway rat)Ki0.004411
Cytochrome P450 2C9 Homo sapiens (human)IC5050.000011
Cytochrome P450 2D6Homo sapiens (human)IC500.100011
Cytochrome P450 2J2Homo sapiens (human)IC5050.000011
DRattus norvegicus (Norway rat)IC505.754411
D(2) dopamine receptorHomo sapiens (human)IC500.002111
D(2) dopamine receptorHomo sapiens (human)Ki100.000011
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.330011
D(3) dopamine receptorHomo sapiens (human)Ki39.000011
D(4) dopamine receptorHomo sapiens (human)Ki100.000011
Delta-type opioid receptorMus musculus (house mouse)Ki0.000411
DNA-dependent protein kinase catalytic subunitHomo sapiens (human)IC505,000.070022
EndochitinaseSaccharomyces cerevisiae S288CKi340.000011
Endochitinase A1Aspergillus fumigatusIC50410.000011
Endochitinase B1Aspergillus fumigatusIC50363.000012
Fatty acid-binding protein, heartHomo sapiens (human)IC500.367011
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)IC5071.000022
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)IC5071.000022
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)IC5071.000022
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)IC5071.000022
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)IC5071.000022
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)IC5071.000022
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)IC5071.000022
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)IC5071.000022
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)IC5071.000022
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)IC5071.000022
Gamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)IC5071.000022
Gamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)IC5071.000022
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)IC5071.000022
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)IC5071.000022
Gamma-aminobutyric acid receptor subunit piHomo sapiens (human)IC5071.000022
Gamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)IC5071.000022
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Ki10.000011
Glycogen phosphorylase, liver formRattus norvegicus (Norway rat)IC50648.000011
Glycogen phosphorylase, muscle formOryctolagus cuniculus (rabbit)IC50159.19331315
Glycogen phosphorylase, muscle formRattus norvegicus (Norway rat)IC50182.000011
Guanine deaminaseHomo sapiens (human)Ki10.200011
Leukotriene B4 receptor 1Homo sapiens (human)Ki0.524011
Leukotriene B4 receptor 2Homo sapiens (human)Ki0.524011
Lysosomal Pro-X carboxypeptidaseHomo sapiens (human)IC500.020011
Lysosomal Pro-X carboxypeptidaseHomo sapiens (human)Ki10.000011
Mu-type opioid receptorCavia porcellus (domestic guinea pig)Ki0.000411
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki1.930011
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000012
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki61.398522
Muscarinic acetylcholine receptor M2Sus scrofa (pig)Ki0.234411
Palmitoleoyl-protein carboxylesterase NOTUMHomo sapiens (human)IC5018.600011
Phenylethanolamine N-methyltransferaseBos taurus (cattle)Ki3,700.000011
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)IC501.280011
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)IC508.480011
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)IC500.970011
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)IC501,815.055022
Phosphodiesterase Rattus norvegicus (Norway rat)IC5070.000011
Potassium channel subfamily K member 3Rattus norvegicus (Norway rat)IC500.410011
Potassium channel subfamily K member 9Rattus norvegicus (Norway rat)IC5026.500022
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC505.541066
ReninHomo sapiens (human)Ki15.000011
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC50100.000011
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusIC50100.000011
Serine-protein kinase ATMHomo sapiens (human)IC50200.000011
Serine/threonine-protein kinase ATRHomo sapiens (human)IC501,100.000011
Serine/threonine-protein kinase mTORHomo sapiens (human)IC50400.000011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC501.050012
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)IC500.240011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki8.575022
Sodium-dependent dopamine transporterMus musculus (house mouse)IC500.200011
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC501.34964767
Sodium-dependent dopamine transporterMus musculus (house mouse)Ki0.850011
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)Ki25.24952641
Sodium-dependent dopamine transporter Homo sapiens (human)IC500.53353939
Sodium-dependent dopamine transporter Homo sapiens (human)Ki0.42323236
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC508.28852424
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki1.63833234
Sodium-dependent serotonin transporterHomo sapiens (human)IC5010.18822424
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)IC500.88851518
Sodium-dependent serotonin transporterHomo sapiens (human)Ki0.36343336
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Ki0.54331928
Solute carrier family 22 member 3Rattus norvegicus (Norway rat)IC50248.000011
Synaptic vesicular amine transporterRattus norvegicus (Norway rat)Ki41.280022
TransporterRattus norvegicus (Norway rat)IC503.22771315
TransporterRattus norvegicus (Norway rat)Ki2.34151619
Tryptophan 5-hydroxylase 1Rattus norvegicus (Norway rat)Ki0.490011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Kd3.020012
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Kd3.020012
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Kd3.020012
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)Kd3.020012
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Kd3.020012
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Kd3.020012
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Kd3.020012
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Kd3.020012
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)Kd3.020012
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)Kd3.020012
5-hydroxytryptamine receptor 5ARattus norvegicus (Norway rat)Kd3.020012
5-hydroxytryptamine receptor 5BRattus norvegicus (Norway rat)Kd3.020012
5-hydroxytryptamine receptor 6Rattus norvegicus (Norway rat)Kd3.020012
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Kd3.020012
Adenosine receptor A1Homo sapiens (human)Kd22.537722
Adenosine receptor A2aHomo sapiens (human)Kd10.210733
Adenosine receptor A2bHomo sapiens (human)Kd0.010011
Chain A, CHIMERA OF IG KAPPA CHAIN: HUMAN CONSTANT REGION AND MOUSE VARIABLE REGIONsynthetic constructKd0.400011
Chain A, Glycogen phosphorylase, liver formHomo sapiens (human)Kd100.000018
Chain B, CHIMERA OF IG GAMMA-1 CHAIN: HUMAN CONSTANT REGION AND MOUSE VARIABLE REGIONsynthetic constructKd0.400011
Chain H, Fab M82G2, Heavy chainMus musculus (house mouse)Kd0.140012
Chain L, Fab M82g2, Light ChainMus musculus (house mouse)Kd0.140012
Guanylate cyclase soluble subunit alpha-1Homo sapiens (human)EC501.020011
Guanylate cyclase soluble subunit alpha-2Homo sapiens (human)EC501.020011
Guanylate cyclase soluble subunit beta-1Homo sapiens (human)EC501.020011
Guanylate cyclase soluble subunit beta-2Homo sapiens (human)EC501.020011
Palmitoleoyl-protein carboxylesterase NOTUMHomo sapiens (human)EC5045.800011
Palmitoleoyl-protein carboxylesterase NOTUMHomo sapiens (human)Kd85.000011
Potassium channel subfamily K member 2Homo sapiens (human)EC50377.000011
Sodium-dependent noradrenaline transporter Homo sapiens (human)EC500.920011
Sodium-dependent serotonin transporterHomo sapiens (human)EC501.300011
Trace amine-associated receptor 1Homo sapiens (human)EC502.756733
Trace amine-associated receptor 1Macaca mulatta (Rhesus monkey)EC505.300011
Trace amine-associated receptor 1Mus musculus (house mouse)EC500.621755
Trace amine-associated receptor 1Rattus norvegicus (Norway rat)EC500.817344

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Adenosine receptor A1Homo sapiens (human)Affinity constant30.000011
Adenosine receptor A1Rattus norvegicus (Norway rat)Kb60.000014
Adenosine receptor A1Homo sapiens (human)KD hydro150,000.000011
Adenosine receptor A2aHomo sapiens (human)Affinity constant30.000011
Adenosine receptor A2aHomo sapiens (human)ED500.300011
Adenosine receptor A2aRattus norvegicus (Norway rat)Kb36.000011
Adenosine receptor A2aRattus norvegicus (Norway rat)Ratio24.001714
Adenosine receptor A2bHomo sapiens (human)Affinity constant30.000011
Adenosine receptor A2bMus musculus (house mouse)Kb25.000011
Adenosine receptor A2bRattus norvegicus (Norway rat)Ratio24.001714
Adenylate cyclase type 1Homo sapiens (human)Kb30.000011
Liver carboxylesterase 1Homo sapiens (human)Km120.000011
Muscarinic acetylcholine receptorCavia porcellus (domestic guinea pig)Kb25.000011
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Km0.200011
Vasopressin V2 receptorSus scrofa (pig)Kb30.000011