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muscle relaxant

A drug used to produce muscle relaxation (excepting neuromuscular blocking agents). Its primary clinical and therapeutic use is the treatment of muscle spasm and immobility associated with strains, sprains, and injuries of the back and, to a lesser degree, injuries to the neck. Also used for the treatment of a variety of clinical conditions that have in common only the presence of skeletal muscle hyperactivity, for example, the muscle spasms that can occur in multiple sclerosis.

ChEBI ID: 51371

Members (43)

MemberDefinitionClass
6-methoxybenzoxazolinoneA 2-benzoxazolinone that is substituted by a methoxy group at position 6.6-methoxy-2-benzoxazolinone; Coixol
8-bromocyclic gmpA 3',5'-cyclic purine nucleotide that is 3',5'-cyclic GMP bearing an additional bromo substituent at position 8 on the guanine ring. A membrane permeable cGMP analogue that activates protein kinase G (PKG). It is 4.3-fold more potent than cGMP in activating PKG1alpha and promotes relaxation of tracheal and vascular smooth muscle tissue in vitro.8-bromo-3',5'-cyclic GMP
8-bromocyclic gmp, sodium saltAn organic sodium salt having 8-bromoguanosine 3',5'-cyclic phosphate as the counterion. A membrane permeable cGMP analogue that activates protein kinase G (PKG). It is 4.3-fold more potent than cGMP in activating PKG1alpha and promotes relaxation of tracheal and vascular smooth muscle tissue in vitro.sodium 8-bromo-3',5'-cyclic GMP
alprazolamA member of the class of triazolobenzodiazepines that is 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine carrying methyl, phenyl and chloro substituents at positions 1, 6 and 8 respectively. Alprazolam is only found in individuals that have taken this drug.alprazolam
atracuriumA diester compound consisting of pentane-1,5-diol with both hydroxyls bearing 3-[1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-2-methyl-3,4-dihydroisoquinolinium-2(1H)-yl]propanoyl groups.atracurium
atracurium besylateThe bisbenzenesulfonate salt of atracurium.atracurium besylate
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
beta-erythroidineAn organic heterotetracyclic indole alkaloid isolated from the seeds and other parts of Erythrina species. It differs from the alpha isomer in having the double bond of the dihydropyranone ring located beta,gamma- to the lactone carbonyl group instead of alpha,beta-.beta-erythroidine
carisoprodolA carbamate ester that is the mono-N-isopropyl derivative of meprobamate (which is a significant metabolite). Carisoprodol interrupts neuronal communication within the reticular formation and spinal cord, resulting in sedation and alteration in pain perception. It is used as a muscle relaxant in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm.carisoprodol
chlormezanoneA 1,3-thiazine that is 1,3-thiazinan-4-one S,S-dioxide in which a hydrogen at position 2 is substituted by a 4-chlorophenyl group and the hydrogen attached to the nitrogen is substituted by methyl. A non-benzodiazepine muscle relaxant, it was used in the management of anxiety and in the treatment of muscle spasms until being discontinued worldwide by its manufacturer in 1996, due to rare but serious cutaneous reactions.chlormezanone
chlorphenesinGlycerol in which the hydrogen of one of the primary hydroxy groups is substituted by a 4-chlorophenyl group. It has antifungal and antibacterial properties, and is used for treatment of cutaneous and vaginal infections. Its 1-carbamate is used as a skeletal muscle relaxant for the treatment of painful muscle spasm.chlorphenesin
chlorphenesin carbamateThe carbamate ester of the primary hydroxy group of chlorphenesin. A centrally acting skeletal muscle relaxant, it is used in the symptomatic treatment of painful muscle spasm.chlorphenesin carbamate
chlorzoxazoneA member of the class of 1,3-benzoxazoles that is 1,3-benzoxazol-2-ol in which the hydrogen atom at position 5 is substituted by chlorine. A centrally acting muscle relaxant with sedative properties, it is used for the symptomatic treatment of painful muscle spasm.chlorzoxazone
cisatracuriumA diester that is the (1R,1'R,2R,2'R)-diastereoisomer of atracurium, a quaternary ammonium ion consisting of pentane-1,5-diol with both hydroxy functions bearing 3-[1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-2-methyl-3,4-dihydroisoquinolinium-2(1H)-yl]propanoyl groups. The active species in the skeletal muscle relaxant cisatracurium besylate.cisatracurium
cyclobenzaprine5-Methylidene-5H-dibenzo[a,d]cycloheptene in which one of the hydrogens of the methylidene group is substituted by a 2-(dimethylamino)ethyl group. A centrally acting skeletal muscle relaxant, it is used as its hydrochloride salt in the symptomatic treatment of painful muscle spasm.cyclobenzaprine
cyclobenzaprine hydrochlorideThe hydrochloride salt of cyclobenzaprine. A centrally acting skeletal muscle relaxant, it is used in the symptomatic treatment of painful muscle spasm.cyclobenzaprine hydrochloride
dantroleneThe hydrazone resulting from the formal condensation of 5-(4-nitrophenyl)furfural with 1-aminohydantoin. A ryanodine receptor antagonist used for the relief of chronic severe spasticity and malignant hyperthermia.dantrolene
decamethoniumA quaternary ammonium ion that is a depolarising muscle relaxant whose structure comprises a decane-1,10-diamine core in which each amino group carries three methyl substituents.decamethonium
dyphyllineAn oxopurine that is theophylline bearing a 2,3-dihydroxypropyl group at the 7 position. It has broncho- and vasodilator properties, and is used in the treatment of asthma, cardiac dyspnea, and bronchitis. It is also an ingredient in preparations that have been promoted for coughs.dyphylline
glaucineAn aporphine alkaloid that is (S)-1,2,9,10-tetrahydroxy-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline in which the four phenolic hydrogens have been replaced by methyl groups.(S)-glaucine
lanperisoneA 2-methyl-3-(pyrrolidin-1-yl)-1-[4-(trifluoromethyl)phenyl]propan-1-one in which the methyl group at position 2 adopts R-configuration. It is a muscle relaxant and induces ferroptosis in cancer cells.lanperisone
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
nitroglycerinA nitroglycerol that is glycerol in which the hydrogen atoms of all three hydroxy groups are replaced by nitro groups. It acts as a prodrug, releasing nitric oxide to open blood vessels and so alleviate heart pain.nitroglycerin
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
oxybutyninA racemate comprising equimolar amounts of (R)-oxybutynin and esoxybutynin. An antispasmodic used for the treatment of overactive bladder.4-(diethylamino)but-2-yn-1-ol; oxybutynin
pancuroniumA steroid ester in which a 5alpha-androstane skeleton is C-3alpha- and C-17beta-disubstituted with acetoxy groups and 2beta- and 16beta-disubstituted with 1-methylpiperidinium-1-yl groups. It is a non-depolarizing curare-mimetic muscle relaxant.pancuronium
pancuronium bromideA bromide salt consisting of two bromide ions and one pancuronium dication.pancuronium bromide
pridinolA piperidine substituted at position 1 by a 3-hydroxy-3,3-diphenylpropyl group.pridinol
quinineA cinchona alkaloid that is cinchonidine in which the hydrogen at the 6-position of the quinoline ring is substituted by methoxy.quinine
rocuroniumA 5alpha-androstane compound having 3alpha-hydroxy-, 17beta-acetoxy-, 2beta-morpholino- and 16beta-N-allyllyrrolidinium substituents.rocuronium
rocuronium bromideThe organic bromide salt of a 5alpha androstane compound having 3alpha-hydroxy-, 17beta-acetoxy-, 2beta-morpholino- and 16beta-N-allyllyrrolidinium substituents.rocuronium bromide
succinylcholineA quaternary ammonium ion that is the bis-choline ester of succinic acid.succinylcholine
suxamethonium chlorideA chloride salt in which the negative charge of the chloride ions is balanced by succinylcholine dications.succinylcholine chloride (anhydrous)
theophyllineA dimethylxanthine having the two methyl groups located at positions 1 and 3. It is structurally similar to caffeine and is found in green and black tea.theophylline
tizanidine2,1,3-Benzothiadiazole substituted at C-4 by a Delta(1)-imidazolin-2-ylamino group and at C-4 by a chloro group. It is an agonist at alpha2-adrenergic receptor sites.tizanidine
tolterodinetolterodine
tubocurarineA benzylisoquinoline alkaloid muscle relaxant which constitutes the active component of curare.tubocurarine
vecuroniumA 5alpha-androstane compound having 3alpha-acetoxy-, 17beta-acetoxy-, 2beta-piperidino- and 16beta-N-methylpiperidinium substituents.vecuronium
vecuronium bromideThe organic bromide salt of a 5alpha-androstane compound having 3alpha-acetoxy-, 17beta-acetoxy-, 2beta-piperidinino- and 16beta-N-methylpiperidinium substituents.vecuronium bromide
xylazineA methyl benzene that is 1,3-dimethylbenzene which is substituted by a 5,6-dihydro-4H-1,3-thiazin-2-ylnitrilo group at position 2. It is an alpha2 adrenergic receptor agonist and frequently used in veterinary medicine as an emetic and sedative with analgesic and muscle relaxant properties.xylazine

Research

Studies (78,019)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199032,934 (42.21)18.7374
1990's16,941 (21.71)18.2507
2000's13,343 (17.10)29.6817
2010's11,414 (14.63)24.3611
2020's3,387 (4.34)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials12,862 (14.49%)5.53%
Reviews5,158 (5.81%)6.00%
Case Studies7,450 (8.40%)4.05%
Observational338 (0.38%)0.25%
Other62,935 (70.92%)84.16%

Protein Targets (311)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency15.848911
15-lipoxygenase, partialHomo sapiens (human)Potency39.810711
67.9K proteinVaccinia virusPotency3.162311
acetylcholinesteraseHomo sapiens (human)Potency24.994838
activating transcription factor 6Homo sapiens (human)Potency4.511113
AR proteinHomo sapiens (human)Potency14.3286924
aryl hydrocarbon receptorHomo sapiens (human)Potency19.249226
arylsulfatase AHomo sapiens (human)Potency16.563118
ATAD5 protein, partialHomo sapiens (human)Potency12.574148
Ataxin-2Homo sapiens (human)Potency18.020623
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency5.356715
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency21.718924
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency37.933012
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency16.481611
Bloom syndrome protein isoform 1Homo sapiens (human)Potency71.149128
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency34.381013
Cellular tumor antigen p53Homo sapiens (human)Potency17.196518
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency12.589311
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency25.118911
Chain A, Beta-lactamaseEscherichia coli K-12Potency50.315512
Chain A, Ferritin light chainEquus caballus (horse)Potency100.000011
Chain A, HADH2 proteinHomo sapiens (human)Potency31.622811
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency39.151212
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency27.513029
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency0.794311
Chain B, HADH2 proteinHomo sapiens (human)Potency31.622811
chromobox protein homolog 1Homo sapiens (human)Potency35.146525
cytochrome P450 2C9, partialHomo sapiens (human)Potency13.292213
cytochrome P450 2D6Homo sapiens (human)Potency11.8621114
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency15.497216
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency4.210326
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency14.3587212
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency5.051114
D(1A) dopamine receptorHomo sapiens (human)Potency1.061125
D(1A) dopamine receptorSus scrofa (pig)Potency26.121611
DNA polymerase betaHomo sapiens (human)Potency100.000011
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency63.135613
DNA polymerase kappa isoform 1Homo sapiens (human)Potency35.481311
endonuclease IVEscherichia coliPotency25.118911
estrogen nuclear receptor alphaHomo sapiens (human)Potency13.0995936
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency33.491511
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency23.590245
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency23.3167118
EWS/FLI fusion proteinHomo sapiens (human)Potency15.5778413
farnesoid X nuclear receptorHomo sapiens (human)Potency11.908013
flap endonuclease 1Homo sapiens (human)Potency8.436813
Fumarate hydrataseHomo sapiens (human)Potency33.173412
GVesicular stomatitis virusPotency13.292213
GABA theta subunitRattus norvegicus (Norway rat)Potency4.210313
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency4.210313
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency4.210313
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency4.210313
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency4.210313
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency4.210313
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency4.210313
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency4.210313
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency4.210313
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency4.210313
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency4.210313
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency4.210313
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency4.210313
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency4.210313
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency4.210313
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency4.210313
gemininHomo sapiens (human)Potency9.6795213
GLI family zinc finger 3Homo sapiens (human)Potency12.1700217
glp-1 receptor, partialHomo sapiens (human)Potency10.000011
GLS proteinHomo sapiens (human)Potency18.353026
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency15.1794313
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency15.861312
Guanine nucleotide-binding protein GHomo sapiens (human)Potency11.220211
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency19.220316
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency18.627813
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency13.292213
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency3.162322
IDH1Homo sapiens (human)Potency16.179513
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency13.292216
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency5.546116
Interferon betaHomo sapiens (human)Potency12.500426
lamin isoform A-delta10Homo sapiens (human)Potency13.3863115
lethal factor (plasmid)Bacillus anthracis str. A2012Potency0.794311
M-phase phosphoprotein 8Homo sapiens (human)Potency15.467412
Microtubule-associated protein tauHomo sapiens (human)Potency20.246612
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency7.385827
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency0.794311
neuropeptide S receptor isoform AHomo sapiens (human)Potency12.569412
NFKB1 protein, partialHomo sapiens (human)Potency6.793326
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency33.6486210
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency13.195012
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency23.914511
Nuclear receptor ROR-gammaHomo sapiens (human)Potency42.163211
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency11.122425
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency18.474627
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency112.946012
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency7.947026
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency72.908213
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency15.556814
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency50.024913
phosphopantetheinyl transferaseBacillus subtilisPotency66.967513
polyproteinZika virusPotency33.173412
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency19.220313
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency10.863716
PPM1D proteinHomo sapiens (human)Potency11.708612
pregnane X nuclear receptorHomo sapiens (human)Potency24.6540312
progesterone receptorHomo sapiens (human)Potency14.925022
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency35.481311
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency5.623411
RAR-related orphan receptor gammaMus musculus (house mouse)Potency17.5558212
ras-related protein Rab-9AHomo sapiens (human)Potency4.928812
regulator of G-protein signaling 4Homo sapiens (human)Potency33.935115
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency34.2108315
retinoid X nuclear receptor alphaHomo sapiens (human)Potency21.0815211
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency14.270233
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency26.679511
shiga toxin 1 B subunitEscherichia coli O157:H7Potency0.317711
shiga toxin 1 variant A subunitEscherichia coli O157:H7Potency0.317711
SMAD family member 2Homo sapiens (human)Potency10.682211
SMAD family member 3Homo sapiens (human)Potency10.682211
Smad3Homo sapiens (human)Potency0.106112
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency13.468416
survival motor neuron protein isoform dHomo sapiens (human)Potency1.122011
TAR DNA-binding protein 43Homo sapiens (human)Potency11.220211
TDP1 proteinHomo sapiens (human)Potency24.1161227
thioredoxin glutathione reductaseSchistosoma mansoniPotency25.118911
thioredoxin reductaseRattus norvegicus (Norway rat)Potency7.500519
ThrombopoietinHomo sapiens (human)Potency7.987424
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency27.2711325
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency54.635233
thyroid stimulating hormone receptorHomo sapiens (human)Potency20.2751614
thyrotropin-releasing hormone receptorHomo sapiens (human)Potency14.088422
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency7.079511
transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Potency22.387211
USP1 protein, partialHomo sapiens (human)Potency0.452123
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency17.9044210
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency15.696412
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency100.000011
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency15.861312

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki43.085522
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC500.436011
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.685733
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC502.091512
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.927023
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC500.534011
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.304022
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC500.534011
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.280011
5-hydroxytryptamine receptor 6Homo sapiens (human)IC501.121011
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.521011
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)IC5032.100014
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki0.043011
AcetylcholinesteraseHomo sapiens (human)IC505.900011
AcetylcholinesteraseTorpedo marmorata (marbled electric ray)IC501.063011
AcetylcholinesteraseHomo sapiens (human)Ki3,000.230022
AcetylcholinesteraseMus musculus (house mouse)Ki8.320023
Adenosine receptor A1Bos taurus (cattle)IC501,006,650,005.043333
Adenosine receptor A1Homo sapiens (human)IC5017.104011
Adenosine receptor A1Rattus norvegicus (Norway rat)IC5019.000022
Adenosine receptor A1Bos taurus (cattle)Ki4.114377
Adenosine receptor A1Cavia porcellus (domestic guinea pig)Ki21.333366
Adenosine receptor A1Gallus gallus (chicken)Ki6.000011
Adenosine receptor A1Homo sapiens (human)Ki6.63991818
Adenosine receptor A1Rattus norvegicus (Norway rat)Ki9.27813137
Adenosine receptor A2aHomo sapiens (human)IC5012.007011
Adenosine receptor A2aCavia porcellus (domestic guinea pig)Ki14.000022
Adenosine receptor A2aHomo sapiens (human)Ki8.54862727
Adenosine receptor A2aRattus norvegicus (Norway rat)Ki15.96522431
Adenosine receptor A2bHomo sapiens (human)Ki10.14261919
Adenosine receptor A2bRattus norvegicus (Norway rat)Ki15.38961824
Adenosine receptor A3Homo sapiens (human)Ki54.86572020
Adenosine receptor A3Rattus norvegicus (Norway rat)Ki45.405689
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC502.630612
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki2.608312
Alkaline phosphatase, tissue-nonspecific isozymeHomo sapiens (human)IC5052.500022
Alkaline phosphatase, tissue-nonspecific isozymeHomo sapiens (human)Ki82.000011
Alpha-2A adrenergic receptorHomo sapiens (human)IC502.156011
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.809011
Alpha-2B adrenergic receptorHomo sapiens (human)IC501.895011
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.865011
Amyloid-beta precursor proteinHomo sapiens (human)Ki0.005911
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.0000111
ATP-dependent translocase ABCB1Homo sapiens (human)IC50115.89171212
ATP-dependent translocase ABCB1Mus musculus (house mouse)IC5041.500044
ATP-dependent translocase ABCB1Homo sapiens (human)Ki12.000011
Bile salt export pumpHomo sapiens (human)IC50211.3428425
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)IC50320.000011
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)IC50340.400055
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)IC50300.500044
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)IC50320.000011
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)IC50320.000011
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)IC50574.250044
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)Ki530.000011
cAMP-specific 3',5'-cyclic phosphodiesterase 4ARattus norvegicus (Norway rat)Ki530.000011
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50527.750044
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)Ki530.000011
cAMP-specific 3',5'-cyclic phosphodiesterase 4BRattus norvegicus (Norway rat)Ki530.000011
cAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)IC50637.000033
cAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)Ki530.000011
cAMP-specific 3',5'-cyclic phosphodiesterase 4CRattus norvegicus (Norway rat)Ki530.000011
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC50637.000033
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)Ki530.000011
cAMP-specific 3',5'-cyclic phosphodiesterase 4D Rattus norvegicus (Norway rat)Ki530.000011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.0000111
cGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC50210.000011
cGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)IC50300.000022
cGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)IC50300.000022
Chain A, Pyridoxal kinaseHomo sapiens (human)Ki50.000012
Chitotriosidase-1Homo sapiens (human)IC501,000.000012
Cholecystokinin receptor type ACavia porcellus (domestic guinea pig)IC5064.000011
Cholecystokinin receptor type ARattus norvegicus (Norway rat)IC5064.000011
Cytochrome P450 2C19Homo sapiens (human)IC500.600011
Cytochrome P450 2C9 Homo sapiens (human)IC5050.000011
Cytochrome P450 2D1Rattus norvegicus (Norway rat)IC5046.500011
Cytochrome P450 2D26Rattus norvegicus (Norway rat)IC500.094011
Cytochrome P450 2D3Rattus norvegicus (Norway rat)IC5012.000011
Cytochrome P450 2D4Rattus norvegicus (Norway rat)IC501.700011
Cytochrome P450 2D6Homo sapiens (human)IC500.582855
Cytochrome P450 2D6Homo sapiens (human)Ki15.000011
Cytochrome P450 2J2Homo sapiens (human)IC5050.000011
Cytochrome P450 3A4Homo sapiens (human)IC502.742733
DRattus norvegicus (Norway rat)Ki2.900011
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki2.800011
D(3) dopamine receptorHomo sapiens (human)IC500.428811
D(3) dopamine receptorHomo sapiens (human)Ki0.145611
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki0.000611
Endochitinase B1Aspergillus fumigatusIC501,000.000012
GABA theta subunitRattus norvegicus (Norway rat)Ki0.002622
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)Ki0.000811
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki0.002622
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)Ki0.000611
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki0.002622
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)Ki0.001411
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki0.002622
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki0.002622
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)Ki0.001511
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Ki0.002622
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Ki0.002622
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Ki0.002622
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)Ki0.001144
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Ki0.002622
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Ki0.002622
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Ki0.002622
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Ki0.002622
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Ki0.002622
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)Ki0.001144
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Ki0.002622
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Ki0.002622
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Ki0.002622
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
Glutamate receptor ionotropic, NMDA 1Homo sapiens (human)Ki6.000011
Glutamate receptor ionotropic, NMDA 2AHomo sapiens (human)Ki6.000011
Glutamate receptor ionotropic, NMDA 2BHomo sapiens (human)Ki6.000011
Glutamate receptor ionotropic, NMDA 2CHomo sapiens (human)Ki6.000011
Glutamate receptor ionotropic, NMDA 2DHomo sapiens (human)Ki6.000011
Glutamate receptor ionotropic, NMDA 3AHomo sapiens (human)Ki6.000011
Glutamate receptor ionotropic, NMDA 3BHomo sapiens (human)Ki6.000011
High affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7AHomo sapiens (human)IC50200.000011
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
Histamine H3 receptorHomo sapiens (human)IC500.820011
Histidine-rich protein PFHRP-IIPlasmodium falciparum (malaria parasite P. falciparum)IC507,400,000.000011
Intestinal-type alkaline phosphataseHomo sapiens (human)IC505.000011
Lethal(3)malignant brain tumor-like protein 1Homo sapiens (human)IC50100.000011
Lethal(3)malignant brain tumor-like protein 3Homo sapiens (human)IC5054.000011
Lethal(3)malignant brain tumor-like protein 4Homo sapiens (human)IC50100.000011
MBT domain-containing protein 1Homo sapiens (human)IC50100.000011
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki0.000811
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC5025.433323
Multidrug and toxin extrusion protein 2Homo sapiens (human)IC5060.233323
Multidrug resistance-associated protein 4Homo sapiens (human)IC50121.7818111
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC500.075812
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki0.008345
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki0.005911
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC500.201512
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.026657
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Ki0.009323
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC500.088912
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.006179
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)Ki0.004423
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC500.063512
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.006034
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC500.015612
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki0.009734
Neuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)IC501.700011
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki1.100011
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Ki1.100011
Neuronal acetylcholine receptor subunit beta-4Homo sapiens (human)IC501.700011
NischarinHomo sapiens (human)Ki0.028312
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)IC502,904.000011
Phosphodiesterase Bos taurus (cattle)IC50250.333366
Phosphodiesterase Bos taurus (cattle)Ki77.000011
Phospholipase A-2-activating proteinHomo sapiens (human)IC505.000011
Potassium channel subfamily K member 2Homo sapiens (human)IC503.850011
Potassium voltage-gated channel subfamily D member 3Homo sapiens (human)IC5012.589211
Potassium voltage-gated channel subfamily E member 1Homo sapiens (human)IC5079.432811
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC500.233055
Potassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)IC5079.432811
ReninHomo sapiens (human)Ki2.325012
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC50100.000011
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusIC50100.000011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC500.024211
Sigma non-opioid intracellular receptor 1Cavia porcellus (domestic guinea pig)Ki7.900011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.010211
Small conductance calcium-activated potassium channel protein 1Rattus norvegicus (Norway rat)IC506.800011
Small conductance calcium-activated potassium channel protein 2Rattus norvegicus (Norway rat)IC506.800011
Small conductance calcium-activated potassium channel protein 3Rattus norvegicus (Norway rat)IC506.800011
Small conductance calcium-activated potassium channel protein 3Rattus norvegicus (Norway rat)Ki5.900011
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC5018.966222
Sodium-dependent dopamine transporter Homo sapiens (human)IC500.085511
Sodium-dependent dopamine transporter Homo sapiens (human)Ki0.067911
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC502.630612
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki2.608312
Sodium-dependent serotonin transporterHomo sapiens (human)IC500.458011
Sodium-dependent serotonin transporterHomo sapiens (human)Ki0.243011
Solute carrier family 22 member 1Mus musculus (house mouse)IC500.280011
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)IC502.033333
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)Ki2.615022
Solute carrier family 22 member 1 Homo sapiens (human)IC5054.733323
Solute carrier family 22 member 1 Homo sapiens (human)Ki94.650024
Solute carrier family 22 member 2Homo sapiens (human)IC5028.266723
Solute carrier family 22 member 2Mus musculus (house mouse)IC502.800011
Solute carrier family 22 member 2Rattus norvegicus (Norway rat)IC5025.500022
Solute carrier family 22 member 2Homo sapiens (human)Ki3.400011
Solute carrier family 22 member 2Rattus norvegicus (Norway rat)Ki55.000011
Solute carrier organic anion transporter family member 1A1Rattus norvegicus (Norway rat)Ki76.700011
Solute carrier organic anion transporter family member 1A4Rattus norvegicus (Norway rat)Ki3.810011
Thyroid hormone receptor betaRattus norvegicus (Norway rat)Ki14.000011
Translocator proteinRattus norvegicus (Norway rat)Ki0.002011
UDP-glucuronosyltransferase 1-6Homo sapiens (human)IC50200.222219
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)IC50200.222219
UDP-glucuronosyltransferase 1A4Homo sapiens (human)IC50200.222219
UDP-glucuronosyltransferase 2B10 Homo sapiens (human)IC50200.222219
UDP-glucuronosyltransferase 2B7Homo sapiens (human)IC50200.222219
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC5025.118911
Voltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)IC5010.000011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Adenosine receptor A1Homo sapiens (human)Kd12.000011
Adenosine receptor A2aHomo sapiens (human)EC5028.200011
Adenosine receptor A2aHomo sapiens (human)Kd2.811533
AlbuminHomo sapiens (human)Kd309.030011
Alpha-1A adrenergic receptorBos taurus (cattle)EC500.264011
Alpha-1B adrenergic receptor Cricetulus griseus (Chinese hamster)EC500.322011
Alpha-2A adrenergic receptorHomo sapiens (human)EC500.086011
Alpha-2C adrenergic receptorHomo sapiens (human)EC501.231011
Amine oxidase [flavin-containing] A Rattus norvegicus (Norway rat)Kd6.400011
Bromodomain-containing protein 4Homo sapiens (human)Kd2.460011
cAMP-dependent protein kinase catalytic subunit beta isoform 1Mus musculus (house mouse)EC507.827022
cAMP-dependent protein kinase catalytic subunit beta isoform 3Homo sapiens (human)EC502.155022
cAMP-dependent protein kinase type I-alpha regulatory subunitBos taurus (cattle)EC507.827022
cAMP-dependent protein kinase type II-beta regulatory subunitHomo sapiens (human)EC502.155022
Chain A, AcetylcholinesteraseMus musculus (house mouse)Kd35.0000114
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)EC500.037011
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)EC50100.000011
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)EC500.012011
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)EC500.069011
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)EC500.010011
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)EC50100.000011
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)EC50100.000011
Gamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)EC501.700011
Gamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)EC501.700011
Muscarinic acetylcholine receptorCavia porcellus (domestic guinea pig)Kd0.049712
Muscarinic acetylcholine receptor M2Homo sapiens (human)Kd0.027812
NPYLR7BAedes aegypti (yellow fever mosquito)EC5020.000011
Palmitoleoyl-protein carboxylesterase NOTUMHomo sapiens (human)Kd6,800.000011
Potassium channel subfamily K member 2Homo sapiens (human)EC50486.000011
Small conductance calcium-activated potassium channel protein 3Rattus norvegicus (Norway rat)Kd6.400011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Adenosine receptor A1Homo sapiens (human)Affinity constant10.000011
Adenosine receptor A1Rattus norvegicus (Norway rat)Kb8.700011
Adenosine receptor A1Homo sapiens (human)KD hydro2,500.000011
Adenosine receptor A2aHomo sapiens (human)Affinity constant10.000011
Adenosine receptor A2aRattus norvegicus (Norway rat)Kb13.700011
Adenosine receptor A2aRattus norvegicus (Norway rat)Ratio25.000012
Adenosine receptor A2bHomo sapiens (human)Affinity constant10.000011
Adenosine receptor A2bMus musculus (house mouse)Kb16.000011
Adenosine receptor A2bRattus norvegicus (Norway rat)Ratio25.000012
Adenylate cyclase type 1Homo sapiens (human)Kb14.000011
ATP-dependent translocase ABCB1Homo sapiens (human)Km10.000011
Muscarinic acetylcholine receptor M1Homo sapiens (human)Kb0.010011
Muscarinic acetylcholine receptor M2Homo sapiens (human)Kb0.098014
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)Km0.270011
Solute carrier family 22 member 2Homo sapiens (human)Km2.600011
Vasopressin V2 receptorSus scrofa (pig)Kb14.000011