Page last updated: 2024-08-05 14:53:23

central nervous system depressant

A loosely defined group of drugs that tend to reduce the activity of the central nervous system.

ChEBI ID: 35488

Members (23)

MemberDefinitionClass
alfentanilA member of the class of piperidines that is piperidine having a 2-(4-ethyl-5-oxo-4,5-dihydro-1H-tetrazol-1-yl)ethyl group at the 1-position as well as N-phenylpropanamido- and methoxymethyl groups at the 4-position.alfentanil
baclofenA monocarboxylic acid that is butanoic acid substituted by an amino group at position 4 and a 4-chlorophenyl group at position 3. It acts as a central nervous system depressant, GABA agonist and muscle relaxant.baclofen zwitterion; baclofen
buclizineAn N-alkylpiperazine carrying (4-chlorophenyl)(phenyl)methyl and 4-tert-butylbenzyl groups.buclizine
chloroprocaineProcaine in which one of the hydrogens ortho- to the carboxylic acid group is substituted by chlorine. It is used as its monohydrochloride salt as a local anaesthetic, particularly for oral surgery. It has the advantage over lidocaine of constricting blood vessels, so reducing bleeding.chloroprocaine
cyclizineAn N-alkylpiperazine in which one nitrogen of the piperazine ring is substituted by a methyl group, while the other is substituted by a diphenylmethyl group.cyclizine
cyclizine hydrochlorideA hydrochloride salt consisting of equimolar amounts of cyclizine and hydrogen chloride.cyclizine hydrochloride
ecgonine methyl esterThe O-debenzoyl analogue of cocaine.ecgonine methyl ester
eszopicloneThe (5S)- (active) enantiomer of zopiclone. Unlike almost all other hypnotic sedatives, which are approved only for the relief of short-term (6-8 weeks) insomnia, eszopiclone is approved by the U.S. Food and Drug Administration for long-term use.eszopiclone
melatoninA member of the class of acetamides that is acetamide in which one of the hydrogens attached to the nitrogen atom is replaced by a 2-(5-methoxy-1H-indol-3-yl)ethyl group. It is a hormone secreted by the pineal gland in humans.melatonin
midazolamAn imidazobenzodiazepine that is 4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted by a methyl, 2-fluorophenyl and chloro groups at positions 1, 6 and 8, respectively.midazolam
midazolam hydrochlorideThe hydrochloride salt of midazolam.midazolam hydrochloride
naloxoneA synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose.naloxone
naloxone hydrochlorideA hydrochloride resulting from the formal reaction of equimolar amounts of naloxone and hydrogen chloride. A specific opioid antagonist, it is used to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose.naloxone hydrochloride
naltrexoneAn organic heteropentacyclic compound that is naloxone substituted in which the allyl group attached to the nitrogen is replaced by a cyclopropylmethyl group. A mu-opioid receptor antagonist, it is used to treat alcohol dependence.naltrexone
naltrexone hydrochlorideA hydrochloride obtained by reaction of oxycodone with one molar equivalent of hydrochloric acid. it is a mu-opioid receptor antagonist that is used to treat alcohol dependence.naltrexone hydrochloride
phenoxyethanolAn aromatic ether that is phenol substituted on oxygen by a 2-hydroxyethyl group.2-phenoxyethanol
procaineA benzoate ester, formally the result of esterification of 4-aminobenzoic acid with 2-diethylaminoethanol but formed experimentally by reaction of ethyl 4-aminobenzoate with 2-diethylaminoethanol.procaine
sevofluraneAn ether compound having fluoromethyl and 1,1,1,3,3,3-hexafluoroisopropyl as the two alkyl groups.sevoflurane
solasodineAn oxaspiro compound and steroid alkaloid sapogenin with formula C27H43NO2 found in the Solanum (nightshade) family. It is used as a precursor in the synthesis of complex steroidal compounds such as contraceptive pills.solasodine
suvorexantAn aromatic amide obtained by formal condensation of the carboxy group of 5-methyl-2-(2H-1,2,3-triazol-2-yl)benzoic acid with the secondary amino group of 5-chloro-2-[(5R)-5-methyl-1,4-diazepan-1-yl]-1,3-benzoxazole. An orexin receptor antagonist used for the management of insomnia.suvorexant
zaleplonA pyrazolo[1,5-a]pyrimidine having a nitrile group at position 3 and a 3-(N-ethylacetamido)phenyl substituent at the 7-position.zaleplon
zolpidemAn imidazo[1,2-a]pyridine compound having a 4-tolyl group at the 2-position, an N,N-dimethylcarbamoylmethyl group at the 3-position and a methyl substituent at the 6-position.zolpidem
zopicloneA pyrrolo[3,4-b]pyrazine compound having a 4-methylpiperazine-1-carboxyl group at the 5-position, a 5-chloropyridin-2-yl group at the 6-position and an oxo-substituent at the 7-position.zopiclone

Research

Studies (82,045)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199021,608 (26.34)18.7374
1990's16,127 (19.66)18.2507
2000's17,498 (21.33)29.6817
2010's18,762 (22.87)24.3611
2020's8,050 (9.81)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials11,585 (12.72%)5.53%
Reviews7,121 (7.82%)6.00%
Case Studies4,421 (4.85%)4.05%
Observational405 (0.44%)0.25%
Other67,563 (74.17%)84.16%

Protein Targets (227)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency29.903312
67.9K proteinVaccinia virusPotency9.657824
activating transcription factor 6Homo sapiens (human)Potency0.000211
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.810712
AR proteinHomo sapiens (human)Potency260.2775810
aryl hydrocarbon receptorHomo sapiens (human)Potency41.134927
ATAD5 protein, partialHomo sapiens (human)Potency14.766435
Ataxin-2Homo sapiens (human)Potency19.968212
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency4.624512
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency22.179923
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.100624
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency69.637211
caspase-3Homo sapiens (human)Potency69.637211
Cellular tumor antigen p53Homo sapiens (human)Potency471.427123
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency27.397913
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency7.000912
Chain A, Ferritin light chainEquus caballus (horse)Potency50.118712
Chain A, HADH2 proteinHomo sapiens (human)Potency35.716812
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency50.118711
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency8.436811
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency56.234111
Chain B, HADH2 proteinHomo sapiens (human)Potency35.716812
chromobox protein homolog 1Homo sapiens (human)Potency55.809223
ClpPBacillus subtilisPotency28.183811
cytochrome P450 2C9, partialHomo sapiens (human)Potency26.042912
cytochrome P450 2D6Homo sapiens (human)Potency22.858115
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency16.938514
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency15.034426
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency17.559713
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency32.960714
D(1A) dopamine receptorHomo sapiens (human)Potency0.580411
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency79.432811
estrogen nuclear receptor alphaHomo sapiens (human)Potency20.0227810
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency16.7256610
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency36.895317
EWS/FLI fusion proteinHomo sapiens (human)Potency5.886245
farnesoid X nuclear receptorHomo sapiens (human)Potency11.882311
GVesicular stomatitis virusPotency26.042912
GABA theta subunitRattus norvegicus (Norway rat)Potency15.034413
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency15.034413
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency15.034413
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency15.034413
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency15.034413
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency15.034413
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency15.034413
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency15.034413
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency15.034413
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency15.034413
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency15.034413
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency15.034413
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency15.034413
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency15.034413
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency15.034413
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency15.034413
gemininHomo sapiens (human)Potency9.699922
GLI family zinc finger 3Homo sapiens (human)Potency11.966028
glp-1 receptor, partialHomo sapiens (human)Potency14.125411
GLS proteinHomo sapiens (human)Potency22.387211
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency11.848647
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency10.590911
Guanine nucleotide-binding protein GHomo sapiens (human)Potency8.912511
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency7.943312
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency37.081413
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency26.042912
IDH1Homo sapiens (human)Potency11.582111
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency26.042914
Interferon betaHomo sapiens (human)Potency26.042912
interleukin 8Homo sapiens (human)Potency74.978011
lamin isoform A-delta10Homo sapiens (human)Potency3.977913
LuciferasePhotinus pyralis (common eastern firefly)Potency27.540411
M-phase phosphoprotein 8Homo sapiens (human)Potency0.177811
Microtubule-associated protein tauHomo sapiens (human)Potency0.891311
mitogen-activated protein kinase 1Homo sapiens (human)Potency15.848911
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency10.657123
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency11.220211
NFKB1 protein, partialHomo sapiens (human)Potency5.623422
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency25.154722
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency25.929011
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency2.131411
Nuclear receptor ROR-gammaHomo sapiens (human)Potency58.570612
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency6.309611
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency30.007636
P53Homo sapiens (human)Potency14.125411
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency44.668411
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency25.357412
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency84.921411
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency21.313811
phosphopantetheinyl transferaseBacillus subtilisPotency42.239512
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency7.943311
pregnane X nuclear receptorHomo sapiens (human)Potency27.959725
pregnane X receptorRattus norvegicus (Norway rat)Potency56.234111
progesterone receptorHomo sapiens (human)Potency29.849311
RAR-related orphan receptor gammaMus musculus (house mouse)Potency17.400628
ras-related protein Rab-9AHomo sapiens (human)Potency14.125411
regulator of G-protein signaling 4Homo sapiens (human)Potency1.112712
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency24.4121310
retinoid X nuclear receptor alphaHomo sapiens (human)Potency15.848911
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.810711
survival motor neuron protein isoform dHomo sapiens (human)Potency1.412511
TDP1 proteinHomo sapiens (human)Potency25.405528
thioredoxin glutathione reductaseSchistosoma mansoniPotency32.922713
thioredoxin reductaseRattus norvegicus (Norway rat)Potency18.476327
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency24.350224
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency0.004011
thyroid stimulating hormone receptorHomo sapiens (human)Potency26.565533
thyrotropin-releasing hormone receptorHomo sapiens (human)Potency14.726311
USP1 protein, partialHomo sapiens (human)Potency80.686612
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency21.130011
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency10.590911

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC500.225011
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.064011
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC500.373011
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.238011
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC501.021011
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.535011
5-hydroxytryptamine receptor 3AHomo sapiens (human)Ki0.060011
5-hydroxytryptamine receptor 3BHomo sapiens (human)Ki0.060011
5-hydroxytryptamine receptor 3CHomo sapiens (human)Ki0.060011
5-hydroxytryptamine receptor 3DHomo sapiens (human)Ki0.060011
5-hydroxytryptamine receptor 3EHomo sapiens (human)Ki0.060011
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC501.021011
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.535011
AcetylcholinesteraseHomo sapiens (human)IC500.100012
Acetylcholinesterase Bos taurus (cattle)IC500.100023
Adenosine receptor A1Homo sapiens (human)Ki50.000011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC500.000511
Alpha-1D adrenergic receptorHomo sapiens (human)IC501.215011
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.597011
Alpha-2A adrenergic receptorHomo sapiens (human)IC501.551011
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.582011
AromataseHomo sapiens (human)IC5011.300011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000016
ATP-dependent translocase ABCB1Homo sapiens (human)IC5065.500044
ATP-dependent translocase ABCB1Mus musculus (house mouse)IC5041.500044
Beta-2 adrenergic receptorCavia porcellus (domestic guinea pig)IC500.005511
Bile salt export pumpHomo sapiens (human)IC50316.1427415
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000016
Carboxylic ester hydrolase Equus caballus (horse)IC500.100011
CholinesteraseHomo sapiens (human)IC500.100012
Cytochrome P450 1A1Homo sapiens (human)Ki59.000011
Cytochrome P450 1A2Homo sapiens (human)Ki12.000011
Cytochrome P450 1A2 Rattus norvegicus (Norway rat)Ki0.000311
Cytochrome P450 1B1Homo sapiens (human)Ki14.000011
Cytochrome P450 2C11 Rattus norvegicus (Norway rat)Ki0.000311
Cytochrome P450 2C9 Homo sapiens (human)IC5050.000011
Cytochrome P450 2D6Homo sapiens (human)IC503.072513
Cytochrome P450 2D6Homo sapiens (human)Ki0.000311
Cytochrome P450 2J2Homo sapiens (human)IC5050.000011
Cytochrome P450 3A4Homo sapiens (human)IC502.742733
D(3) dopamine receptorHomo sapiens (human)IC502.992011
D(3) dopamine receptorHomo sapiens (human)Ki1.016011
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki20.000011
Delta-type opioid receptorHomo sapiens (human)IC500.09532333
Delta-type opioid receptorMus musculus (house mouse)IC5050.0160410
Delta-type opioid receptorRattus norvegicus (Norway rat)IC500.0148411
Delta-type opioid receptorHomo sapiens (human)Ki0.06475669
Delta-type opioid receptorMus musculus (house mouse)Ki0.0456910
Delta-type opioid receptorRattus norvegicus (Norway rat)Ki0.0402912
GABA theta subunitRattus norvegicus (Norway rat)IC500.038522
GABA theta subunitRattus norvegicus (Norway rat)Ki0.025033
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC500.038522
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)Ki1.36141139
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki0.80191313
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC500.038522
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)Ki1.4693937
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki0.383099
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC500.038522
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)Ki1.50891139
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki0.298688
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC500.038522
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)Ki2.2599230
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki0.025033
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC500.038522
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)Ki3.9175836
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Ki3.351766
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC500.038522
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)Ki3.4150533
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Ki4.056988
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC500.038522
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)Ki0.053011
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Ki0.025033
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC500.038522
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)Ki2.4630535
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Ki1.88642525
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC500.038522
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)Ki3.08193030
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Ki2.022055
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC500.038522
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Ki0.025033
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC500.038522
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Ki0.025033
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC500.038522
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Ki0.025033
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC500.038522
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)Ki2.70783666
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Ki2.11832727
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC500.038522
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Ki0.025033
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)IC500.038522
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Ki0.025033
Gamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)IC500.050011
Gamma-aminobutyric acid type B receptor subunit 1Rattus norvegicus (Norway rat)IC500.276246
Gamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)Ki6.000011
Gamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)IC500.050011
Gamma-aminobutyric acid type B receptor subunit 2Rattus norvegicus (Norway rat)IC500.276246
Gamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)Ki6.000011
Gamma-aminobutyric acid type B receptor subunit 2Rattus norvegicus (Norway rat)Ki0.220011
Histamine H1 receptorHomo sapiens (human)IC500.038011
Histamine H1 receptorHomo sapiens (human)Ki0.004411
Histamine H3 receptorHomo sapiens (human)Ki0.000511
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)IC502.5104712
Kappa-type opioid receptorHomo sapiens (human)IC500.04651522
Kappa-type opioid receptorMus musculus (house mouse)IC50250.003022
Kappa-type opioid receptorRattus norvegicus (Norway rat)IC500.001337
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)Ki0.01012333
Kappa-type opioid receptorHomo sapiens (human)Ki0.01273946
Kappa-type opioid receptorMus musculus (house mouse)Ki0.002734
Kappa-type opioid receptorRattus norvegicus (Norway rat)Ki0.004045
kappa-type opioid receptor isoform 1Homo sapiens (human)IC500.368024
Melatonin receptor type 1AHomo sapiens (human)IC500.00251818
Melatonin receptor type 1AGallus gallus (chicken)Ki0.000778
Melatonin receptor type 1AHomo sapiens (human)Ki0.00036769
Melatonin receptor type 1BHomo sapiens (human)IC500.00351212
Melatonin receptor type 1BGallus gallus (chicken)Ki0.000789
Melatonin receptor type 1BHomo sapiens (human)Ki0.00046264
Melatonin receptor type 1CGallus gallus (chicken)Ki0.000778
Metabotropic glutamate receptor 1Rattus norvegicus (Norway rat)IC500.000422
Mu-type opioid receptorCavia porcellus (domestic guinea pig)IC500.006746
Mu-type opioid receptorHomo sapiens (human)IC500.01972636
Mu-type opioid receptorMus musculus (house mouse)IC50100.007755
Mu-type opioid receptorRattus norvegicus (Norway rat)IC500.006048
Mu-type opioid receptorCavia porcellus (domestic guinea pig)Ki0.00121823
Mu-type opioid receptorHomo sapiens (human)Ki0.00995365
Mu-type opioid receptorMus musculus (house mouse)Ki0.00131213
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki0.00261623
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000016
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC500.675011
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki0.163011
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki0.001115
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC501.158011
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.412011
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Ki0.001115
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC500.748011
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.159011
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)Ki0.001115
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC500.852011
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.119011
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)Ki0.001115
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC500.633011
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki0.455011
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)Ki0.001115
MyeloperoxidaseHomo sapiens (human)IC503.000011
Neuronal acetylcholine receptor subunit alpha-7Rattus norvegicus (Norway rat)Ki10.000011
Nociceptin receptorHomo sapiens (human)Ki10.000011
Nociceptin receptorMus musculus (house mouse)Ki0.000311
Orexin receptor type 1Homo sapiens (human)IC500.087344
Orexin receptor type 1Homo sapiens (human)Ki0.001066
Orexin receptor type 1Mus musculus (house mouse)Ki0.001711
Orexin receptor type 2Homo sapiens (human)IC500.061355
Orexin receptor type 2Homo sapiens (human)Ki0.002755
Orexin receptor type 2Mus musculus (house mouse)Ki0.008711
Palmitoleoyl-protein carboxylesterase NOTUMHomo sapiens (human)IC5075.400011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50416.869011
Ribosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)IC507.316188
Ribosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)Ki0.042222
Sigma non-opioid intracellular receptor 1Cavia porcellus (domestic guinea pig)IC5010.000011
Sigma non-opioid intracellular receptor 1Cavia porcellus (domestic guinea pig)Ki0.103011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki100.000011
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)Ki0.001722
Sodium-dependent dopamine transporter Homo sapiens (human)IC500.763011
Sodium-dependent dopamine transporter Homo sapiens (human)Ki0.606011
Solute carrier family 22 member 1 Homo sapiens (human)IC50157.510011
Solute carrier family 22 member 1 Homo sapiens (human)Ki3.700011
Sphingosine-1-phosphate lyase 1Mus musculus (house mouse)Ki0.765011
Substance-K receptorCavia porcellus (domestic guinea pig)Ki0.000411
Translocator proteinRattus norvegicus (Norway rat)IC504.700011
Translocator proteinRattus norvegicus (Norway rat)Ki0.002011
UDP-glucuronosyltransferase 1-6Homo sapiens (human)IC5075.500014
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)IC5075.500014
UDP-glucuronosyltransferase 1A4Homo sapiens (human)IC5075.500014
UDP-glucuronosyltransferase 2B10 Homo sapiens (human)IC5075.500014
UDP-glucuronosyltransferase 2B7Homo sapiens (human)IC5075.500014

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
AlbuminHomo sapiens (human)Kd63.000011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)EC5031.500012
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)EC5031.500012
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)EC5031.500012
Beta-galactosidaseEscherichia coliEC5031.500012
calcineurin A1, putativeCandida dubliniensis CD36EC50180.000011
Delta-type opioid receptorHomo sapiens (human)EC500.009144
Delta-type opioid receptorMus musculus (house mouse)EC500.004411
Delta-type opioid receptorRattus norvegicus (Norway rat)EC500.001012
Delta-type opioid receptorHomo sapiens (human)Kd0.001322
Delta-type opioid receptorMus musculus (house mouse)Kd0.000211
Delta-type opioid receptorRattus norvegicus (Norway rat)Kd0.120024
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)EC500.229844
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)EC50100.000011
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)EC500.849033
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)EC502.000022
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)EC502.000022
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)EC500.236733
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)EC50100.000011
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)EC501.210033
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)EC500.668055
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)EC50100.000011
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)EC501.000011
Gamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)EC501.700011
Gamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)EC501.700011
heat shock protein 90Candida albicansEC50120.033034
Histidine decarboxylaseRattus norvegicus (Norway rat)EC500.001012
Kappa-type opioid receptorHomo sapiens (human)EC500.004555
Kappa-type opioid receptorMus musculus (house mouse)EC500.000811
Kappa-type opioid receptorRattus norvegicus (Norway rat)EC500.001012
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)Kd0.018011
Kappa-type opioid receptorHomo sapiens (human)Kd0.001011
Kappa-type opioid receptorRattus norvegicus (Norway rat)Kd0.093535
kappa-type opioid receptor isoform 1Homo sapiens (human)EC505.000011
Melatonin receptor type 1AGallus gallus (chicken)EC500.022611
Melatonin receptor type 1AHomo sapiens (human)EC500.00081111
Melatonin receptor type 1BGallus gallus (chicken)EC500.022611
Melatonin receptor type 1BHomo sapiens (human)EC500.00251212
Melatonin receptor type 1CGallus gallus (chicken)EC500.022611
Melatonin receptor type 1CXenopus laevis (African clawed frog)EC500.000133
Mu-type opioid receptorCavia porcellus (domestic guinea pig)EC500.001911
Mu-type opioid receptorHomo sapiens (human)EC500.005733
Mu-type opioid receptorMus musculus (house mouse)EC500.000222
Mu-type opioid receptorRattus norvegicus (Norway rat)EC500.001012
Mu-type opioid receptorCavia porcellus (domestic guinea pig)Kd0.000211
Mu-type opioid receptorHomo sapiens (human)Kd0.000444
Mu-type opioid receptorRattus norvegicus (Norway rat)Kd0.078446
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)EC500.191011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Cytochrome P450 2D6Homo sapiens (human)Kb0.000611
Delta-type opioid receptorHomo sapiens (human)Kb0.011111
Delta-type opioid receptorHomo sapiens (human)Ke0.028399
Delta-type opioid receptorMus musculus (house mouse)Ke0.03821014
Kappa-type opioid receptorHomo sapiens (human)Kb0.003011
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)Ke0.009057
Kappa-type opioid receptorHomo sapiens (human)Ke0.00401111
Kappa-type opioid receptorMus musculus (house mouse)Ke0.015912
Kappa-type opioid receptorHomo sapiens (human)pA20.009711
Mu-type opioid receptorHomo sapiens (human)Kb0.000611
Mu-type opioid receptorCavia porcellus (domestic guinea pig)Ke0.001056
Mu-type opioid receptorHomo sapiens (human)Ke0.00201920
Mu-type opioid receptorMus musculus (house mouse)Ke0.000822
Nuclear factor erythroid 2-related factor 2Homo sapiens (human)CD60.000011
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)Km1,310.000011
UDP-glucuronosyltransferase 1A8Homo sapiens (human)Km1,000.000012