Page last updated: 2024-08-05 14:54:38

NMDA receptor antagonist

Any substance that inhibits the action of N-methyl-D-aspartate (NMDA) receptors. They tend to induce a state known as dissociative anesthesia, marked by catalepsy, amnesia, and analgesia, while side effects can include hallucinations, nightmares, and confusion. Due to their psychotomimetic effects, many NMDA receptor antagonists are used as recreational drugs.

ChEBI ID: 60643

Members (31)

MemberDefinitionClass
(R)-ketamineThe R- (less active) enantiomer of ketamine.(R)-ketamine
1-(1-phenylcyclohexyl)pyrrolidinePyrrolidine in which the hydrogen attached to the nitrogen is substituted by a 1-phenylcyclohex-1-yl group.rolicyclidine
2-amino-5-phosphonovalerateThe 5-phosphono derivative of 2-aminopentanoic acid; acts as an N-methyl-D-aspartate receptor antagonist.2-amino-5-phosphonopentanoic acid
7-chlorokynurenic acidA quinolinemonocarboxylic acid that is quinaldic acid which is substituted by a hydroxy group at position 4 and by a chlorine at position 7. It is a potent NMDA glutamate receptor antagonist which antagonizes the strychnine-insensitive glycine site of the NMDA receptor. It also prevents neurodegeneration produced by quinolinic acid.7-chlorokynurenic acid
amantadineA member of the class of adamantanes that is used as an antiviral and antiparkinson drug.amantadine
amantadine hydrochlorideA hydrochloride obtained by combining amantadine and hydrochloric acid in equimolar amounts.amantadine hydrochloride
dextromethadoneA 6-(dimethylamino)-4,4-diphenylheptan-3-one that has (S)-configuration. It is the less active enantiomer of methadone and has very little activity on opioid receptors and mainly responsible for the inhibition of hERG K+ channels and thus for cardiac toxicity. The drug is currently under clinical development for the treatment of major depressive disorder.dextromethadone
dextromethorphanA 6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene in which the sterocenters at positions 4a, 10 and 10a have S-configuration. It is a prodrug of dextrorphan and used as an antitussive drug for suppressing cough.dextromethorphan
dizocilpineAn organic heterotetracyclic compound that is 1-methyl-8-azabicyclo[3.2.1]octane ortho-fused to two benzene rings at positions 2-3 and 6-7 (the 5S,10R-stereoisomer). It is a non-competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor and affects cognitive function, learning, and memory.dizocilpine
dizocilpine maleateA maleate salt obtained by reaction of dizocilpine with one equivalent of maleic acid.dizocilpine maleate
esketamineThe S- (more active) enantiomer of ketamine.esketamine
ginsenoside rb3A ginsenoside found in Panax species that is dammarane which is substituted by hydroxy groups at the 3beta, 12beta and 20 pro-S positions, in which the hydroxy groups at positions 3 and 20 have been converted to the corresponding beta-D-glucopyranosyl-(1->2)-beta-D-glucopyranoside and beta-D-xylopyranosyl-(1->6)-beta-D-glucopyranoside respectively, and in which a double bond has been introduced at the 24-25 position.ginsenoside Rb3
isoliquiritigeninA member of the class of chalcones that is trans-chalcone hydroxylated at C-2', -4 and -4'.isoliquiritigenin
ketamineA member of the class of cyclohexanones in which one of the hydrogens at position 2 is substituted by a 2-chlorophenyl group, while the other is substituted by a methylamino group.ketamine
kynurenic acidA quinolinemonocarboxylic acid that is quinoline-2-carboxylic acid substituted by a hydroxy group at C-4.kynurenic acid
levomethadoneA 6-(dimethylamino)-4,4-diphenylheptan-3-one that has (R)-configuration. It is the active enantiomer of methadone and its hydrochloride salt is used to treat adults who are addicted to drugs such as heroin and morphine.levomethadone
memantineA primary aliphatic amine that is the 3,5-dimethyl derivative of 1-aminoadamantane. A low to moderate affinity uncompetitive (open-channel); NMDA receptor antagonist which binds preferentially to the NMDA receptor-operated cation channels.memantine
memantine hydrochlorideA hydrochloride obtained by reaction of memantine with one equivalent of hydrochloric acid. A low to moderate affinity uncompetitive (open-channel); NMDA receptor antagonist which binds preferentially to the NMDA receptor-operated cation channels.memantine hydrochloride
nitrous oxideA nitrogen oxide consisting of linear unsymmetrical molecules with formula N2O. While it is the most used gaseous anaesthetic in the world, its major commercial use, due to its solubility under pressure in vegetable fats combined with its non-toxicity in low concentrations, is as an aerosol spray propellant and aerating agent for canisters of 'whipped' cream.dinitrogen oxide
noribogaineAn organic heteropentacyclic compound that is ibogamine in which the indole hydrogen para to the indole nitrogen has been replaced by a hydroxy group. It is the primary (and long-lived) metabolite of ibogaine, the psychoactive indole alkaloid found in the African rainforest shrub Tabernanthe iboga.noribogaine
nortilidineAn ethyl 2-(methylamino)-1-phenylcyclohex-3-ene-1-carboxylate that is ent-dextilidine in which one of the methyl groups attached to the nitrogen is replaced by hydrogen. ent-Dextilidine is metabolised to (1R,2S)-nortilidine by the liver.(1R,2S)-nortilidine
orphenadrineA tertiary amino compound which is the phenyl-o-tolylmethyl ether of 2-(dimethylamino)ethanol.orphenadrine
orphenadrine citrateA citrate salt which comprises equimolar amounts of orphenadrine and citric acid.orphenadrine citrate
orphenadrine hydrochlorideA hydrochloride comprising equimolar amounts of ophenadrine and hydrogen chloride.orphenadrine hydrochloride
pentamidineA diether consisting of pentane-1,5-diol in which both hydroxyl hydrogens have been replaced by 4-amidinophenyl groups. A trypanocidal drug that is used for treatment of cutaneous leishmaniasis and Chagas disease.pentamidine
phencyclidineA member of the class of piperidines that is piperidine in which the nitrogen is substituted with a 1-phenylcyclohexyl group. Formerly used as an anaesthetic agent, it exhibits both hallucinogenic and neurotoxic effects.phencyclidine
ro 25-6981A member of the class of piperidines that is 4-benzylpiperidine substituted by a 3-hydroxy-3-(4-hydroxyphenyl)-2-methylpropyl group at position 1 (the 1R,2S-stereoisomer). It is a potent antagonist of the GluN2B subunit of the N-methyl-D-aspartate (NMDA) receptor.Ro 25-6981
sdz eaa 494A member of the class of piperazines that is piperazine substituted by a carboxy group at position 2R and a (1E)-1-phosphonoprop-1-en-3-yl group at position 4. It is an antagonist of N-methyl-D-aspartate receptors (NMDARs) and was in clinical development by Novartis for the treatment of cognition disorders and brain injuries (now discontinued).midafotel
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
tramadolA 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol in which both stereocentres have R-configuration; the (R,R)-enantiomer of the racemic opioid analgesic tramadol, it exhibits ten-fold higher analgesic potency than the (S,S)-enantiomer.(R,R)-tramadol
tramadol hydrochlorideA hydrochloride resulting from the reaction of (R,R)-tramadol with 1 molar equivalent of hydrogen chloride; the (R,R)-enantiomer of the racemic opioid analgesic tramadol hydrochloride, it exhibits ten-fold higher analgesic potency than the (S,S)-enantiomer.(R,R)-tramadol hydrochloride

Research

Studies (80,882)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199021,501 (26.58)18.7374
1990's15,084 (18.65)18.2507
2000's16,359 (20.23)29.6817
2010's19,139 (23.66)24.3611
2020's8,799 (10.88)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials6,993 (7.70%)5.53%
Reviews5,945 (6.55%)6.00%
Case Studies4,067 (4.48%)4.05%
Observational240 (0.26%)0.25%
Other73,583 (81.01%)84.16%

Protein Targets (320)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency25.530115
15-lipoxygenase, partialHomo sapiens (human)Potency39.810711
2,3-bisphosphoglycerate-independent phosphoglycerate mutaseLeishmania major strain FriedlinPotency37.933011
67.9K proteinVaccinia virusPotency16.803722
acetylcholinesteraseHomo sapiens (human)Potency0.870911
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.810711
alpha-galactosidaseHomo sapiens (human)Potency8.912511
Alpha-synucleinHomo sapiens (human)Potency32.642711
Amyloid-beta precursor proteinHomo sapiens (human)Potency16.360111
AR proteinHomo sapiens (human)Potency33.520458
aryl hydrocarbon receptorHomo sapiens (human)Potency26.603222
arylsulfatase AHomo sapiens (human)Potency37.933011
ATAD5 protein, partialHomo sapiens (human)Potency10.984544
Ataxin-2Homo sapiens (human)Potency25.118911
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency4.140526
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency30.131311
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency26.121611
Bloom syndrome protein isoform 1Homo sapiens (human)Potency42.6207210
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency89.125111
Cellular tumor antigen p53Homo sapiens (human)Potency22.104226
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency28.236815
Chain A, Beta-lactamaseEscherichia coli K-12Potency31.689414
Chain A, HADH2 proteinHomo sapiens (human)Potency20.359624
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency58.654412
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency24.9426110
Chain B, HADH2 proteinHomo sapiens (human)Potency20.359624
chromobox protein homolog 1Homo sapiens (human)Potency49.067026
cytochrome P450 2C19 precursorHomo sapiens (human)Potency11.966912
cytochrome P450 2C9 precursorHomo sapiens (human)Potency19.783012
cytochrome P450 2C9, partialHomo sapiens (human)Potency1.737711
cytochrome P450 2D6Homo sapiens (human)Potency9.771711
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency2.511911
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency13.737228
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency12.462113
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency13.421612
D(1A) dopamine receptorHomo sapiens (human)Potency6.976435
DNA polymerase betaHomo sapiens (human)Potency50.118711
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency56.199213
DNA polymerase kappa isoform 1Homo sapiens (human)Potency44.567012
endonuclease IVEscherichia coliPotency0.631011
estrogen nuclear receptor alphaHomo sapiens (human)Potency19.139149
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency11.734012
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency23.9094117
EWS/FLI fusion proteinHomo sapiens (human)Potency18.407948
Fatty-acid amide hydrolase 1Rattus norvegicus (Norway rat)Potency19.952611
flap endonuclease 1Homo sapiens (human)Potency8.436811
GVesicular stomatitis virusPotency1.737711
GABA theta subunitRattus norvegicus (Norway rat)Potency13.737214
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency13.737214
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency13.737214
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency13.737214
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency13.737214
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency13.737214
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency13.737214
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency13.737214
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency13.737214
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency13.737214
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency13.737214
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency13.737214
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency13.737214
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency13.737214
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency13.737214
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency13.737214
gemininHomo sapiens (human)Potency15.2854412
GLI family zinc finger 3Homo sapiens (human)Potency14.9924210
glp-1 receptor, partialHomo sapiens (human)Potency17.246722
GLS proteinHomo sapiens (human)Potency5.214313
glucocerebrosidaseHomo sapiens (human)Potency11.263769
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency37.031424
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency6.513111
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency23.799612
heat shock protein beta-1Homo sapiens (human)Potency13.332211
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency19.0301210
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency39.810711
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency40.870812
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency1.737711
huntingtin isoform 2Homo sapiens (human)Potency35.481311
IDH1Homo sapiens (human)Potency16.221012
importin subunit beta-1 isoform 1Homo sapiens (human)Potency66.202622
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency1.737712
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency11.220211
Interferon betaHomo sapiens (human)Potency29.148527
lamin isoform A-delta10Homo sapiens (human)Potency8.2471111
lethal factor (plasmid)Bacillus anthracis str. A2012Potency12.589313
LuciferasePhotinus pyralis (common eastern firefly)Potency10.691011
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency0.251211
M-phase phosphoprotein 8Homo sapiens (human)Potency35.481311
Microtubule-associated protein tauHomo sapiens (human)Potency9.712115
mitogen-activated protein kinase 1Homo sapiens (human)Potency10.554913
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency7.566025
neuropeptide S receptor isoform AHomo sapiens (human)Potency12.218213
NFKB1 protein, partialHomo sapiens (human)Potency6.409224
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency11.896112
Nrf2Homo sapiens (human)Potency16.592822
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency34.376211
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency12.594126
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency25.118911
P53Homo sapiens (human)Potency50.118711
ParkinHomo sapiens (human)Potency1.835611
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency21.331311
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency22.977824
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency49.668115
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency20.960812
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency50.024923
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency8.912511
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency17.900812
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency11.719216
PPM1D proteinHomo sapiens (human)Potency33.717014
pregnane X nuclear receptorHomo sapiens (human)Potency17.868635
putative alpha-glucosidaseOryza sativa Japonica Group (Japanese rice)Potency28.183812
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency125.892011
RAR-related orphan receptor gammaMus musculus (house mouse)Potency19.570624
regulator of G-protein signaling 4Homo sapiens (human)Potency44.984012
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency39.572426
retinoid X nuclear receptor alphaHomo sapiens (human)Potency29.194512
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency19.601513
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency26.679511
signal transducer and activator of transcription 6, interleukin-4 inducedHomo sapiens (human)Potency100.000011
Smad3Homo sapiens (human)Potency10.032412
snurportin-1Homo sapiens (human)Potency66.202622
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency4.287112
survival motor neuron protein isoform dHomo sapiens (human)Potency1.584911
TDP1 proteinHomo sapiens (human)Potency17.1155215
thioredoxin glutathione reductaseSchistosoma mansoniPotency89.125111
thioredoxin reductaseRattus norvegicus (Norway rat)Potency12.8082310
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency25.5503217
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency0.796922
thyroid stimulating hormone receptorHomo sapiens (human)Potency21.384048
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency15.848911
transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Potency19.952611
USP1 protein, partialHomo sapiens (human)Potency47.888914
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency25.170526
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency75.086514

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
10 kDa chaperonin Escherichia coliIC50175.000022
10 kDa heat shock protein, mitochondrialHomo sapiens (human)IC50175.000022
17-beta-hydroxysteroid dehydrogenase type 1Homo sapiens (human)IC502.830011
17-beta-hydroxysteroid dehydrogenase type 2Homo sapiens (human)IC500.360011
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC501.037512
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.296512
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC503.391011
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki2.158011
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC501.906012
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.998512
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC501.906012
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.998512
5-hydroxytryptamine receptor 6Homo sapiens (human)IC501.121011
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.521011
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)IC5019.900014
60 kDa chaperonin Escherichia coliIC50175.000022
60 kDa heat shock protein, mitochondrialHomo sapiens (human)IC50175.000022
72 kDa type IV collagenaseHomo sapiens (human)IC500.010011
AcetylcholinesteraseElectrophorus electricus (electric eel)IC5010.000012
AcetylcholinesteraseHomo sapiens (human)IC500.004911
AcrosinSus scrofa (pig)Ki2.300011
Aldo-keto reductase family 1 member B1Homo sapiens (human)IC500.320011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC502.440012
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki2.419512
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.180011
Alpha-1B adrenergic receptorHomo sapiens (human)Ki0.180011
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.180011
Alpha-2A adrenergic receptorHomo sapiens (human)IC501.765512
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.662512
Alpha-2B adrenergic receptorHomo sapiens (human)IC501.895011
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.865011
Amiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)Ki0.290011
Amine oxidase [flavin-containing] AHomo sapiens (human)IC500.793011
Amine oxidase [flavin-containing] A Rattus norvegicus (Norway rat)IC5015.600022
Amine oxidase [flavin-containing] BRattus norvegicus (Norway rat)IC5047.200011
Amyloid-beta precursor proteinHomo sapiens (human)IC5019.700011
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC5015.721511
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki12.880211
AromataseHomo sapiens (human)IC503.800011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000012
Aurora kinase BHomo sapiens (human)IC50100.000011
Beta-secretase 1Homo sapiens (human)IC5042.250022
Bile salt export pumpHomo sapiens (human)IC50505.142937
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000012
CholinesteraseEquus caballus (horse)IC5010.000012
CholinesteraseHomo sapiens (human)IC5016.000011
CholinesteraseMus musculus (house mouse)Ki0.522422
Coagulation factor XHomo sapiens (human)IC5010.400011
Collagenase 3Homo sapiens (human)IC500.014011
Cytochrome P450 1A2Homo sapiens (human)IC5056.317244
Cytochrome P450 2B6Homo sapiens (human)Ki10.000011
Cytochrome P450 2C19Homo sapiens (human)IC5075.000033
Cytochrome P450 2C9 Homo sapiens (human)IC5055.275255
Cytochrome P450 2D1Rattus norvegicus (Norway rat)IC50264.000011
Cytochrome P450 2D26Rattus norvegicus (Norway rat)IC505.600011
Cytochrome P450 2D3Rattus norvegicus (Norway rat)IC5018.600011
Cytochrome P450 2D4Rattus norvegicus (Norway rat)IC50136.000011
Cytochrome P450 2D6Homo sapiens (human)IC507.11531010
Cytochrome P450 2J2Homo sapiens (human)IC5050.000011
Cytochrome P450 3A4Homo sapiens (human)IC5056.317244
D(3) dopamine receptorHomo sapiens (human)IC503.998011
D(3) dopamine receptorHomo sapiens (human)Ki1.358011
Delta-type opioid receptorMus musculus (house mouse)IC500.006011
Delta-type opioid receptorHomo sapiens (human)Ki10.000011
Diamine acetyltransferase 1Homo sapiens (human)Ki2.000011
DNA topoisomerase 1Homo sapiens (human)IC50250.000011
DNA topoisomerase 2-alphaHomo sapiens (human)IC50250.000011
Estrogen receptorHomo sapiens (human)IC501.870011
Estrogen receptor betaHomo sapiens (human)IC500.269011
G-protein coupled receptor 35Homo sapiens (human)IC5039.000011
G-protein coupled receptor 35Homo sapiens (human)Ki137.000011
GABA theta subunitRattus norvegicus (Norway rat)Ki100.000011
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)IC502,900.000011
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki100.000011
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)IC502,900.000011
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki70.433522
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)IC502,900.000011
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki100.000011
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)IC502,900.000011
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki100.000011
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)IC502,900.000011
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Ki100.000011
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)IC502,900.000011
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Ki100.000011
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)IC502,900.000011
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Ki100.000011
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)IC502,900.000011
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Ki100.000011
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)IC502,900.000011
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Ki100.000011
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Ki100.000011
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Ki100.000011
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Ki100.000011
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Ki100.000011
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Ki100.000011
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Ki100.000011
Glutamate receptor 1Rattus norvegicus (Norway rat)IC50127.000012
Glutamate receptor 1Rattus norvegicus (Norway rat)Ki100.000011
Glutamate receptor 2Rattus norvegicus (Norway rat)IC50127.000012
Glutamate receptor 3Rattus norvegicus (Norway rat)IC50127.000012
Glutamate receptor 4Rattus norvegicus (Norway rat)IC50127.000012
Glutamate receptor ionotropic, kainate 1Rattus norvegicus (Norway rat)IC501,000.000014
Glutamate receptor ionotropic, kainate 2Rattus norvegicus (Norway rat)IC501,000.000014
Glutamate receptor ionotropic, kainate 3Rattus norvegicus (Norway rat)IC501,000.000014
Glutamate receptor ionotropic, kainate 3Rattus norvegicus (Norway rat)Ki100.000011
Glutamate receptor ionotropic, kainate 4Rattus norvegicus (Norway rat)IC501,000.000014
Glutamate receptor ionotropic, kainate 5Rattus norvegicus (Norway rat)IC501,000.000014
Glutamate receptor ionotropic, NMDA 1Homo sapiens (human)IC503.03442027
Glutamate receptor ionotropic, NMDA 1Homo sapiens (human)Ki1.22351119
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)IC5045.24893859
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Ki0.48872937
Glutamate receptor ionotropic, NMDA 2AHomo sapiens (human)IC505.42751419
Glutamate receptor ionotropic, NMDA 2AHomo sapiens (human)Ki1.3081917
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)IC5049.57243353
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Ki0.35712735
Glutamate receptor ionotropic, NMDA 2BHomo sapiens (human)IC503.05761315
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)IC5046.07773655
Glutamate receptor ionotropic, NMDA 2BHomo sapiens (human)Ki1.22321119
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Ki0.35712735
Glutamate receptor ionotropic, NMDA 2CHomo sapiens (human)IC505.004033
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)IC5052.74923048
Glutamate receptor ionotropic, NMDA 2CHomo sapiens (human)Ki1.3786816
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Ki0.36872837
Glutamate receptor ionotropic, NMDA 2DHomo sapiens (human)IC505.004033
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)IC5052.74923048
Glutamate receptor ionotropic, NMDA 2DHomo sapiens (human)Ki1.3786816
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Ki0.36242634
Glutamate receptor ionotropic, NMDA 3AHomo sapiens (human)IC505.004033
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)IC5052.74923048
Glutamate receptor ionotropic, NMDA 3AHomo sapiens (human)Ki1.3786816
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Ki0.36242634
Glutamate receptor ionotropic, NMDA 3BHomo sapiens (human)IC505.004033
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)IC5052.74923048
Glutamate receptor ionotropic, NMDA 3BHomo sapiens (human)Ki1.3786816
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Ki0.36242634
Glyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)IC5050.000011
Histamine H1 receptorHomo sapiens (human)IC5049.482322
Histamine H1 receptorHomo sapiens (human)Ki0.144011
Histamine H2 receptorHomo sapiens (human)IC506.961011
Histamine H2 receptorHomo sapiens (human)Ki6.845011
Integrase Human immunodeficiency virus 1IC50100.000022
Interstitial collagenaseHomo sapiens (human)IC500.016011
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)IC50250.000011
Kappa-type opioid receptorHomo sapiens (human)Ki10.000011
Lysosomal Pro-X carboxypeptidaseHomo sapiens (human)IC500.038813
MatrilysinHomo sapiens (human)IC500.008011
Matrix metalloproteinase-9Homo sapiens (human)IC500.010011
Matrix protein 2Influenza A virus (A/Puerto Rico/8/1934(H1N1))IC50153.925044
Matrix protein 2Influenza A virus (A/udorn/1972(H3N2))IC50109.860055
Mitogen-activated protein kinase 11Homo sapiens (human)Ki1,300.000011
Mitogen-activated protein kinase 12Homo sapiens (human)Ki1,300.000011
Mitogen-activated protein kinase 13Homo sapiens (human)Ki1,300.000011
Mitogen-activated protein kinase 14Homo sapiens (human)Ki1,300.000011
Mu-type opioid receptorHomo sapiens (human)Ki2.400011
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki100.000011
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC5021.582045
Multidrug and toxin extrusion protein 2Homo sapiens (human)IC5037.700033
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000012
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC500.148011
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki0.036011
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki100.000011
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC500.900512
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.320512
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Ki55.000022
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC500.175011
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.037011
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)Ki100.000011
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC500.852512
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.118512
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)Ki100.000011
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC500.971723
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki1.046512
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)Ki100.000011
NACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)IC505.820022
Neuronal acetylcholine receptor subunit alpha-3Rattus norvegicus (Norway rat)IC508.525022
Neuronal acetylcholine receptor subunit alpha-6Rattus norvegicus (Norway rat)IC506.000011
Neuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)IC507.000011
Neuronal acetylcholine receptor subunit beta-4Rattus norvegicus (Norway rat)IC508.525022
Nuclear factor NF-kappa-B p100 subunit Homo sapiens (human)IC5032.000011
Nuclear factor NF-kappa-B p105 subunitHomo sapiens (human)IC5032.000011
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)IC5015.721511
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)Ki12.880211
PlasminogenHomo sapiens (human)IC5028.400035
Polyunsaturated fatty acid 5-lipoxygenaseRattus norvegicus (Norway rat)IC5035.000011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC5012.814555
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki12.880211
Prolyl endopeptidaseSus scrofa (pig)IC500.006011
Proteasome subunit beta type-5Homo sapiens (human)IC504.880011
Protein arginine N-methyltransferase 1Homo sapiens (human)IC5081.000022
Protein arginine N-methyltransferase 5Homo sapiens (human)IC50582.000011
Protein disulfide-isomeraseHomo sapiens (human)Ki36.100011
Protein S100-BHomo sapiens (human)IC50100.000011
Protein tyrosine phosphatase type IVA 1Homo sapiens (human)IC500.300011
Protein tyrosine phosphatase type IVA 2Homo sapiens (human)IC500.300011
Protein tyrosine phosphatase type IVA 3Homo sapiens (human)IC5035.833333
Sigma non-opioid intracellular receptor 1Cavia porcellus (domestic guinea pig)IC500.123622
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)IC500.823313
Sigma non-opioid intracellular receptor 1Cavia porcellus (domestic guinea pig)Ki0.036522
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki29.943034
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)Ki21.775733
Sodium channel protein type 1 subunit alphaRattus norvegicus (Norway rat)IC505.650022
Sodium channel protein type 2 subunit alphaRattus norvegicus (Norway rat)IC505.650022
Sodium channel protein type 3 subunit alphaRattus norvegicus (Norway rat)IC505.650022
Sodium channel protein type 4 subunit alphaHomo sapiens (human)IC501,550.000022
Sodium-dependent dopamine transporter Homo sapiens (human)IC503.159011
Sodium-dependent dopamine transporter Homo sapiens (human)Ki2.510011
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC502.440012
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki2.419512
Sodium-dependent serotonin transporterHomo sapiens (human)IC500.230412
Sodium-dependent serotonin transporterHomo sapiens (human)Ki0.122212
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Ki1.090014
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)IC50285.433333
Solute carrier family 22 member 1 Homo sapiens (human)IC5039.444357
Solute carrier family 22 member 2Homo sapiens (human)IC508.900033
Solute carrier family 22 member 2Rattus norvegicus (Norway rat)IC50256.966733
Solute carrier family 22 member 3Homo sapiens (human)IC509.500011
Stromelysin-1Homo sapiens (human)IC500.081011
Suppressor of tumorigenicity 14 proteinHomo sapiens (human)Ki1.160011
Transcription factor p65Homo sapiens (human)IC5032.000011
Trypsin-1Homo sapiens (human)IC5043.333313
Tyrosine-protein phosphatase non-receptor type 1Homo sapiens (human)IC5055.000022
Tyrosyl-DNA phosphodiesterase 1Homo sapiens (human)IC5055.000011
Urokinase-type plasminogen activatorHomo sapiens (human)IC5043.333313
Vesicular glutamate transporter 3Rattus norvegicus (Norway rat)Ki945.000022
Xanthine dehydrogenase/oxidaseBos taurus (cattle)IC5047.300011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Aryl hydrocarbon receptorHomo sapiens (human)EC500.300011
bcl-2-like protein 11 isoform 1Homo sapiens (human)EC50350.000011
Chain A, BCL-2-RELATED PROTEIN A1Homo sapiens (human)EC50350.000011
Chain A, ImmunoglobulinMus musculus (house mouse)Kd0.002011
Chain B, ImmunoglobulinMus musculus (house mouse)Kd0.002011
G protein-coupled receptor GPR35Rattus norvegicus (Norway rat)EC5066.000011
G-protein coupled receptor 35Homo sapiens (human)EC50199.800099
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Kd0.037211
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Kd0.037211
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Kd0.037211
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Kd0.037211
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Kd0.037211
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Kd0.037211
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Kd0.037211
Histamine H3 receptorRattus norvegicus (Norway rat)EC50500.000011
Matrix protein 2Influenza A virus (A/udorn/1972(H3N2))EC500.660022
Matrix protein 2Influenza A virus (A/Puerto Rico/8/1934(H1N1))Kd0.320011
Matrix protein 2Influenza A virus (A/udorn/1972(H3N2))Kd58.292544
Mu-type opioid receptorHomo sapiens (human)EC501.000011
Muscarinic acetylcholine receptor M1Mus musculus (house mouse)Kd9.100011
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Kd9.100011
Muscarinic acetylcholine receptor M2Mus musculus (house mouse)Kd9.100011
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Kd9.100011
Muscarinic acetylcholine receptor M3Mus musculus (house mouse)Kd9.100011
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)Kd9.100011
Muscarinic acetylcholine receptor M4Mus musculus (house mouse)Kd9.100011
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)Kd9.100011
Muscarinic acetylcholine receptor M5Mus musculus (house mouse)Kd9.100011
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)Kd9.100011
Neuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)EC5011.600011
Protein S100-BHomo sapiens (human)Kd1.000011
Protein S100-BRattus norvegicus (Norway rat)Kd47.000022
SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2, isoform CRA_aHomo sapiens (human)EC5091.140011
Taste receptor type 2 member 46Homo sapiens (human)EC5031.000011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Cytochrome P450 2D6Homo sapiens (human)Km1.400011
Delta-type opioid receptorMus musculus (house mouse)K0.526.000012
Glutamate receptor 1Rattus norvegicus (Norway rat)Kb86.000024
Glutamate receptor 2Rattus norvegicus (Norway rat)Kb86.000024
Glutamate receptor 3Rattus norvegicus (Norway rat)Kb86.000024
Glutamate receptor 4Rattus norvegicus (Norway rat)Kb86.000024
Glutamate receptor ionotropic, kainate 1Rattus norvegicus (Norway rat)Kb69.500012
Glutamate receptor ionotropic, kainate 2Rattus norvegicus (Norway rat)Kb69.500012
Glutamate receptor ionotropic, kainate 3Rattus norvegicus (Norway rat)Kb69.500012
Glutamate receptor ionotropic, kainate 4Rattus norvegicus (Norway rat)Kb69.500012
Glutamate receptor ionotropic, kainate 5Rattus norvegicus (Norway rat)Kb69.500012
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Kb53.731149
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Kb53.731149
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Kb53.731149
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)K0.50.250011
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Kb53.731149
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Kb53.731149
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Kb53.731149
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Kb53.731149
Kappa-type opioid receptorMus musculus (house mouse)K0.526.000012
Mu-type opioid receptorMus musculus (house mouse)K0.526.000012
Muscarinic acetylcholine receptor M1Mus musculus (house mouse)K0.530.000012
Muscarinic acetylcholine receptor M2Mus musculus (house mouse)K0.530.000012
Muscarinic acetylcholine receptor M3Mus musculus (house mouse)K0.530.000012
Muscarinic acetylcholine receptor M4Mus musculus (house mouse)K0.530.000012
Muscarinic acetylcholine receptor M5Mus musculus (house mouse)K0.530.000012
Quinone oxidoreductaseMus musculus (house mouse)Activity4.643333
Quinone oxidoreductaseMus musculus (house mouse)CD6.233333
Solute carrier family 22 member 1 Homo sapiens (human)Activity18.400011
Solute carrier family 22 member 2Homo sapiens (human)Km30.500012
Substance-P receptorCavia porcellus (domestic guinea pig)CD11.000011