Page last updated: 2024-08-05 15:09:51

adrenergic uptake inhibitor

Adrenergic uptake inhibitors are drugs that block the transport of adrenergic transmitters into axon terminals or into storage vesicles within terminals. The tricyclic antidepressants and amphetamines are among the therapeutically important drugs that may act via inhibition of adrenergic transport. Many of these drugs also block transport of serotonin.

ChEBI ID: 35640

Members (17)

MemberDefinitionClass
ameziniumA pyridazinium ion that is pyridazin-1-ium which is substituted by a phenyl, amino and methoxy groups at positions 1, 4 and 6, respectively.amezinium
amitriptylineAn organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(dimethylamino)propylidene group at position 5.amitriptyline
amoxapineA dibenzooxazepine compound having a chloro substituent at the 2-position and a piperazin-1-yl group at the 11-position.amoxapine
atomoxetineA secondary amino compound having methyl and 3-(2-methylphenoxy)-3-phenylpropan-1-yl substituents.atomoxetine
atomoxetine hydrochlorideThe hydrochloride salt of atomoxetine.atomoxetine hydrochloride
benzphetamineDextroamphetamine in which the the hydrogens attached to the amino group are substituted by a methyl and a benzyl group. A sympathomimetic agent with properties similar to dextroamphetamine, it is used as its hydrochloride salt in the treatment of obesity.benzphetamine
cocaineA tropane alkaloid obtained from leaves of the South American shrub Erythroxylon coca.cocaine
desipramineA dibenzoazepine consisting of 10,11-dihydro-5H-dibenzo[b,f]azepine substituted on nitrogen with a 3-(methylamino)propyl group.desipramine
dextroamphetamineA 1-phenylpropan-2-amine that has S configuration.(S)-amphetamine
imipramineA dibenzoazepine that is 5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)propyl group at the nitrogen atom.imipramine
mianserinA dibenzoazepine (specifically 1,2,3,4,10,14b-hexahydrodibenzo[c,f]pyrazino[1,2-a]azepine) methyl-substituted on N-2. Closely related to (and now mostly superseded by) the tetracyclic antidepressant mirtazapinean, it is an atypical antidepressant used in the treatment of depression throughout Europe and elsewhere.mianserin
nisoxetineA secondary amino compound that is N-methyl-3-phenylpropan-1-amine substituted at position 3 by a 2-methoxyphenoxy group.nisoxetine
nortriptylineAn organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(methylamino)propylidene group at position 5. It is an active metabolite of amitriptyline.nortriptyline
reserpineAn alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria.reserpine
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
venlafaxineA tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-methoxyphenyl group.venlafaxine

Research

Studies (76,362)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199032,333 (42.34)18.7374
1990's13,974 (18.30)18.2507
2000's12,851 (16.83)29.6817
2010's13,261 (17.37)24.3611
2020's3,943 (5.16)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials7,821 (8.76%)5.53%
Reviews5,081 (5.69%)6.00%
Case Studies5,326 (5.96%)4.05%
Observational138 (0.15%)0.25%
Other70,960 (79.44%)84.16%

Protein Targets (371)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-lipoxygenase, partialHomo sapiens (human)Potency19.952611
67.9K proteinVaccinia virusPotency7.384212
acetylcholinesteraseHomo sapiens (human)Potency41.275222
activating transcription factor 6Homo sapiens (human)Potency19.032326
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency28.569615
AR proteinHomo sapiens (human)Potency35.4591934
aryl hydrocarbon receptorHomo sapiens (human)Potency41.280026
arylsulfatase AHomo sapiens (human)Potency12.758316
ATAD5 protein, partialHomo sapiens (human)Potency18.439624
Ataxin-2Homo sapiens (human)Potency15.852917
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency23.344226
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency7.568611
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency14.582916
Bloom syndrome protein isoform 1Homo sapiens (human)Potency17.782822
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency28.183811
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency68.450111
caspase-1 isoform alpha precursorHomo sapiens (human)Potency7.943311
caspase-3Homo sapiens (human)Potency68.450111
Caspase-7Homo sapiens (human)Potency7.943311
Cellular tumor antigen p53Homo sapiens (human)Potency34.036429
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency17.498223
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency18.256312
Chain A, Beta-lactamaseEscherichia coli K-12Potency28.796812
Chain A, Ferritin light chainEquus caballus (horse)Potency25.515422
Chain A, HADH2 proteinHomo sapiens (human)Potency16.531122
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency56.234111
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency165.667413
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency27.728114
Chain B, HADH2 proteinHomo sapiens (human)Potency16.531122
chromobox protein homolog 1Homo sapiens (human)Potency40.995525
cytochrome P450 2C19 precursorHomo sapiens (human)Potency0.316211
cytochrome P450 2C9, partialHomo sapiens (human)Potency13.141612
cytochrome P450 2D6Homo sapiens (human)Potency6.4329110
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency13.0403112
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency12.9249216
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency16.209429
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency29.322514
D(1A) dopamine receptorHomo sapiens (human)Potency5.7816316
D(1A) dopamine receptorSus scrofa (pig)Potency16.230415
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency19.952611
DNA dC->dU-editing enzyme APOBEC-3F isoform aHomo sapiens (human)Potency31.622811
DNA polymerase betaHomo sapiens (human)Potency31.622811
DNA polymerase eta isoform 1Homo sapiens (human)Potency7.943311
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency10.000011
dopamine D1 receptorHomo sapiens (human)Potency3.883212
endonuclease IVEscherichia coliPotency15.714212
estrogen nuclear receptor alphaHomo sapiens (human)Potency36.16771146
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency19.931825
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency24.8454932
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency24.1477211
EWS/FLI fusion proteinHomo sapiens (human)Potency21.0388411
farnesoid X nuclear receptorHomo sapiens (human)Potency20.299244
flap endonuclease 1Homo sapiens (human)Potency11.846414
Fumarate hydrataseHomo sapiens (human)Potency34.422012
GVesicular stomatitis virusPotency13.141612
GABA theta subunitRattus norvegicus (Norway rat)Potency12.924918
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency12.924918
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency12.924918
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency12.924918
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency12.924918
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency12.924918
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency12.924918
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency12.924918
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency12.924918
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency12.924918
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency12.924918
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency12.924918
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency12.924918
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency12.924918
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency12.924918
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency12.924918
gemininHomo sapiens (human)Potency15.4056411
GLI family zinc finger 3Homo sapiens (human)Potency15.8666215
glp-1 receptor, partialHomo sapiens (human)Potency13.168423
GLS proteinHomo sapiens (human)Potency7.828025
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency18.4970411
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency44.037213
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency11.582111
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency38.440612
heat shock protein beta-1Homo sapiens (human)Potency37.912523
hemoglobin subunit betaHomo sapiens (human)Potency31.622811
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency15.5215118
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency4.246012
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency28.183811
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency13.141612
huntingtin isoform 2Homo sapiens (human)Potency32.027223
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency29.154824
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency7.943322
IDH1Homo sapiens (human)Potency25.499612
importin subunit beta-1 isoform 1Homo sapiens (human)Potency28.125222
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency13.141614
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency7.943414
Integrin alpha-IIbHomo sapiens (human)Potency19.952611
Integrin beta-3Homo sapiens (human)Potency19.952611
Interferon betaHomo sapiens (human)Potency13.141612
interleukin 8Homo sapiens (human)Potency66.824211
isocitrate dehydrogenase 1, partialHomo sapiens (human)Potency50.118711
lamin isoform A-delta10Homo sapiens (human)Potency7.626219
lethal factor (plasmid)Bacillus anthracis str. A2012Potency14.219112
lethal(3)malignant brain tumor-like protein 1 isoform IHomo sapiens (human)Potency28.183811
M-phase phosphoprotein 8Homo sapiens (human)Potency27.585813
Microtubule-associated protein tauHomo sapiens (human)Potency7.343812
mitogen-activated protein kinase 1Homo sapiens (human)Potency3.975612
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency2.7697212
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency39.810711
neuropeptide S receptor isoform AHomo sapiens (human)Potency20.811412
NFKB1 protein, partialHomo sapiens (human)Potency10.286926
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency4.466811
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency58.047911
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency37.929649
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency25.929011
nuclear factor NF-kappa-B p105 subunit isoform 1Homo sapiens (human)Potency42.239512
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency26.159614
Nuclear receptor ROR-gammaHomo sapiens (human)Potency37.578011
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency34.4818312
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency28.247923
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency13.627416
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency37.304612
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency18.7781510
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency25.0019410
phosphopantetheinyl transferaseBacillus subtilisPotency70.524633
polyproteinZika virusPotency34.422012
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency15.521519
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency8.898518
pregnane X nuclear receptorHomo sapiens (human)Potency22.383838
progesterone receptorHomo sapiens (human)Potency9.179725
RAR-related orphan receptor gammaMus musculus (house mouse)Potency25.760729
ras-related protein Rab-9AHomo sapiens (human)Potency58.047912
regulator of G-protein signaling 4Homo sapiens (human)Potency7.089814
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency33.532037
retinoid X nuclear receptor alphaHomo sapiens (human)Potency18.418349
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency19.9029413
SMAD family member 2Homo sapiens (human)Potency21.052126
SMAD family member 3Homo sapiens (human)Potency21.052126
snurportin-1Homo sapiens (human)Potency28.125222
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency25.109114
survival motor neuron protein isoform dHomo sapiens (human)Potency5.865412
TAR DNA-binding protein 43Homo sapiens (human)Potency7.943311
TDP1 proteinHomo sapiens (human)Potency20.9609219
thioredoxin glutathione reductaseSchistosoma mansoniPotency89.125111
thioredoxin reductaseRattus norvegicus (Norway rat)Potency30.408826
ThrombopoietinHomo sapiens (human)Potency16.700428
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency26.9177319
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency35.620123
thyroid stimulating hormone receptorHomo sapiens (human)Potency18.3774513
transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Potency22.387211
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency19.952611
USP1 protein, partialHomo sapiens (human)Potency28.342415
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency15.5257212
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency18.776559
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency52.930915
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency44.037213

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1AHomo sapiens (human)IC500.398122
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC501.293028
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki2.382235
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.781346
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC501.293028
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki1.341157
5-hydroxytryptamine receptor 1DHomo sapiens (human)IC500.380222
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)IC501.121615
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Ki0.660333
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)IC501.121615
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)Ki0.660333
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC500.045847
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC500.825637
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.06671623
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.050977
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC500.055814
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC500.825637
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.035614
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki0.067355
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC500.006925
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC500.825637
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.0176712
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki0.056366
5-hydroxytryptamine receptor 2C Mus musculus (house mouse)Ki0.160011
5-hydroxytryptamine receptor 3AHomo sapiens (human)IC501.412522
5-hydroxytryptamine receptor 3AMus musculus (house mouse)IC501.412511
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)IC501.121615
5-hydroxytryptamine receptor 3AMus musculus (house mouse)Ki0.252011
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Ki0.185522
5-hydroxytryptamine receptor 3BHomo sapiens (human)IC501.412522
5-hydroxytryptamine receptor 3BMus musculus (house mouse)IC501.412511
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)IC501.121615
5-hydroxytryptamine receptor 3BMus musculus (house mouse)Ki0.252011
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)Ki0.185522
5-hydroxytryptamine receptor 3CHomo sapiens (human)IC501.412522
5-hydroxytryptamine receptor 3DHomo sapiens (human)IC501.412522
5-hydroxytryptamine receptor 3EHomo sapiens (human)IC501.412522
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC500.006714
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.003514
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)IC501.121615
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 5ARattus norvegicus (Norway rat)IC501.121615
5-hydroxytryptamine receptor 5ARattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 5BRattus norvegicus (Norway rat)IC501.121615
5-hydroxytryptamine receptor 5BRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 6Homo sapiens (human)IC500.213814
5-hydroxytryptamine receptor 6Rattus norvegicus (Norway rat)IC501.121615
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki1.317349
5-hydroxytryptamine receptor 6Rattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)IC5030.266716
5-hydroxytryptamine receptor 7Homo sapiens (human)IC500.114811
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki2.831357
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)IC501.121615
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki0.154733
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC500.582015
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki0.576815
Alpha-1A adrenergic receptorHomo sapiens (human)IC500.407422
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC500.090136
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.104045
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC500.181133
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.104045
Alpha-1D adrenergic receptorHomo sapiens (human)IC500.191814
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC500.270022
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.094214
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.104045
Alpha-2A adrenergic receptorHomo sapiens (human)IC500.273539
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC503.117623
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.184225
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki3.287323
Alpha-2B adrenergic receptorHomo sapiens (human)IC500.089128
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC503.117623
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.081414
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki3.287323
Alpha-2C adrenergic receptorHomo sapiens (human)IC500.3701410
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC503.117623
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.105925
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki3.287323
Amine oxidase [flavin-containing] AHomo sapiens (human)Ki14.400011
Amine oxidase [flavin-containing] BBos taurus (cattle)Ki300.000011
Amine oxidase [flavin-containing] BHomo sapiens (human)Ki280.000011
Amine oxidase [flavin-containing] BRattus norvegicus (Norway rat)Ki370.000022
Amyloid-beta precursor proteinHomo sapiens (human)IC500.338011
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC5022.719512
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki18.613612
Angiotensin-converting enzymeRattus norvegicus (Norway rat)Ki0.500013
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000018
ATP-dependent translocase ABCB1Homo sapiens (human)IC503.20921010
ATP-dependent translocase ABCB1Homo sapiens (human)Ki5.416055
ATP-dependent translocase ABCB1Mus musculus (house mouse)Ki10.965022
Beta-2 adrenergic receptorCavia porcellus (domestic guinea pig)IC500.027011
Bile salt export pumpHomo sapiens (human)IC50146.6033521
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC5016.900933
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)Ki1.115011
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)Ki1.115011
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)Ki1.115011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50124.925018
Canalicular multispecific organic anion transporter 1Homo sapiens (human)Ki295.000011
Chromaffin granule amine transporterHomo sapiens (human)IC500.050022
Cytochrome P450 1A1Homo sapiens (human)IC500.007911
Cytochrome P450 1A2Homo sapiens (human)IC500.007911
Cytochrome P450 2C19Homo sapiens (human)IC503.000011
Cytochrome P450 2C8Homo sapiens (human)Ki49.900011
Cytochrome P450 2C9 Homo sapiens (human)IC5050.000012
Cytochrome P450 2D1Rattus norvegicus (Norway rat)IC50204.000011
Cytochrome P450 2D26Rattus norvegicus (Norway rat)IC501.900011
Cytochrome P450 2D3Rattus norvegicus (Norway rat)IC5014.200011
Cytochrome P450 2D4Rattus norvegicus (Norway rat)IC5019.300011
Cytochrome P450 2D6Homo sapiens (human)IC502.725678
Cytochrome P450 2J2Homo sapiens (human)IC5050.000012
DRattus norvegicus (Norway rat)IC503.317623
DRattus norvegicus (Norway rat)Ki1.420011
D(1A) dopamine receptorHomo sapiens (human)IC500.457214
D(1A) dopamine receptorHomo sapiens (human)Ki0.200625
D(1B) dopamine receptorRattus norvegicus (Norway rat)IC500.810011
D(1B) dopamine receptorHomo sapiens (human)Ki0.170011
D(2) dopamine receptorHomo sapiens (human)IC503.155645
D(2) dopamine receptorRattus norvegicus (Norway rat)IC502.635433
D(2) dopamine receptorHomo sapiens (human)Ki0.704445
D(2) dopamine receptorMus musculus (house mouse)Ki0.726011
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.789534
D(3) dopamine receptorHomo sapiens (human)IC501.655235
D(3) dopamine receptorRattus norvegicus (Norway rat)IC500.810011
D(3) dopamine receptorHomo sapiens (human)Ki0.643235
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki1.524011
D(4) dopamine receptorHomo sapiens (human)IC503.311322
D(4) dopamine receptorRattus norvegicus (Norway rat)IC500.810011
D(4) dopamine receptorHomo sapiens (human)Ki0.034011
Delta-type opioid receptorHomo sapiens (human)Ki10.000011
DNA topoisomerase 1Homo sapiens (human)IC50160.000011
Endothelin receptor type BHomo sapiens (human)Ki0.063122
Endothelin receptor type BRattus norvegicus (Norway rat)Ki0.063111
Endothelin-1 receptorHomo sapiens (human)IC500.114811
Fatty acid-binding protein, heartHomo sapiens (human)IC500.367011
G-protein coupled receptor Apis mellifera (honey bee)IC5073.000011
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit piHomo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)IC50127.000011
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)IC5014.000011
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)IC5014.000011
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)IC5014.000011
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)IC5014.000011
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)IC5014.000011
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)IC5014.000011
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)IC5014.000011
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Ki10.000011
High affinity nerve growth factor receptorHomo sapiens (human)IC5060.000011
Histamine H1 receptorHomo sapiens (human)IC500.030936
Histamine H1 receptorRattus norvegicus (Norway rat)IC500.0002110
Histamine H1 receptorHomo sapiens (human)Ki0.004347
Histamine H2 receptorCavia porcellus (domestic guinea pig)IC502.848015
Histamine H2 receptorHomo sapiens (human)IC501.357313
Histamine H2 receptorHomo sapiens (human)Ki1.335013
Histamine H3 receptorHomo sapiens (human)Ki3.000022
Histamine H3 receptorRattus norvegicus (Norway rat)Ki5.000011
Histamine H4 receptorHomo sapiens (human)Ki5.012011
Kappa-type opioid receptorHomo sapiens (human)Ki10.000011
Krueppel-like factor 10Homo sapiens (human)IC50100.000022
Leukotriene B4 receptor 1Homo sapiens (human)Ki0.524011
Leukotriene B4 receptor 2Homo sapiens (human)Ki0.524011
Lysosomal Pro-X carboxypeptidaseHomo sapiens (human)Ki10.000011
Mu-type opioid receptorHomo sapiens (human)IC504.152011
Mu-type opioid receptorHomo sapiens (human)Ki2.043022
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC5010.000011
Multidrug and toxin extrusion protein 2Homo sapiens (human)IC50100.000011
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000018
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC500.677014
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC500.300014
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki0.163214
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki61.398522
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC501.032314
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC500.300013
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.367014
Muscarinic acetylcholine receptor M2Sus scrofa (pig)Ki0.234411
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC500.845814
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)IC500.300013
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.179414
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC500.975814
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC500.300013
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.135914
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC500.302814
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC500.620025
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki0.217714
Nociceptin receptorHomo sapiens (human)IC505.000011
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)IC5022.719512
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)Ki18.613612
Phenylethanolamine N-methyltransferaseBos taurus (cattle)Ki435.333323
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CIC5022.000011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC505.72762037
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki18.613612
Prostaglandin G/H synthase 1Homo sapiens (human)IC502.700012
Prostaglandin G/H synthase 1Ovis aries (sheep)Ki0.160012
Quinolone resistance protein NorAStaphylococcus aureusIC508.542977
Sigma intracellular receptor 2Rattus norvegicus (Norway rat)Ki2.107011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC501.043723
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki4.631522
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)Ki0.343011
Sodium channel protein type 1 subunit alphaHomo sapiens (human)IC5011.800022
Sodium channel protein type 10 subunit alphaHomo sapiens (human)IC5011.800022
Sodium channel protein type 11 subunit alphaHomo sapiens (human)IC5011.800022
Sodium channel protein type 2 subunit alphaHomo sapiens (human)IC508.900033
Sodium channel protein type 3 subunit alphaHomo sapiens (human)IC5011.800022
Sodium channel protein type 4 subunit alphaHomo sapiens (human)IC5011.800022
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC506.680044
Sodium channel protein type 7 subunit alphaHomo sapiens (human)IC5011.800022
Sodium channel protein type 8 subunit alphaHomo sapiens (human)IC5011.800022
Sodium channel protein type 9 subunit alphaHomo sapiens (human)IC507.900044
Sodium- and chloride-dependent betaine transporterMus musculus (house mouse)IC50170.412012
Sodium- and chloride-dependent GABA transporter 1Mus musculus (house mouse)IC50389.022512
Sodium- and chloride-dependent GABA transporter 2Mus musculus (house mouse)IC50269.576512
Sodium- and chloride-dependent GABA transporter 3Mus musculus (house mouse)IC50250.094512
Sodium-dependent dopamine transporterMus musculus (house mouse)IC500.200011
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC501.42965178
Sodium-dependent dopamine transporterMus musculus (house mouse)Ki5.425022
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)Ki24.41352743
Sodium-dependent dopamine transporter Homo sapiens (human)IC505.60165361
Sodium-dependent dopamine transporter Homo sapiens (human)Ki0.75903647
Sodium-dependent noradrenaline transporterMus musculus (house mouse)Ki0.014022
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC500.66435776
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki0.92785063
Sodium-dependent serotonin transporterHomo sapiens (human)IC500.54535973
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)IC501.65982125
Sodium-dependent serotonin transporterHomo sapiens (human)Ki0.32405667
Sodium-dependent serotonin transporterMus musculus (house mouse)Ki0.023522
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Ki0.44952334
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)IC5016.750022
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)Ki11.400012
Solute carrier family 22 member 1 Homo sapiens (human)IC5033.384347
Solute carrier family 22 member 1 Homo sapiens (human)Ki5.360011
Solute carrier family 22 member 2Homo sapiens (human)IC500.600011
Solute carrier family 22 member 2Rattus norvegicus (Norway rat)IC509.950022
Solute carrier family 22 member 2Homo sapiens (human)Ki16.000011
Solute carrier family 22 member 3Rattus norvegicus (Norway rat)IC5068.000011
Solute carrier family 22 member 3Homo sapiens (human)Ki28.000012
Solute carrier family 22 member 4Rattus norvegicus (Norway rat)IC5080.000011
Sphingomyelin phosphodiesteraseHomo sapiens (human)IC505.000011
Sulfotransferase 1A1Homo sapiens (human)Ki80.000012
Sulfotransferase 2A1Homo sapiens (human)Ki80.000012
Synaptic vesicular amine transporterHomo sapiens (human)IC500.014733
Synaptic vesicular amine transporterRattus norvegicus (Norway rat)IC500.0177110
Synaptic vesicular amine transporterBos taurus (cattle)Ki0.001011
Synaptic vesicular amine transporterHomo sapiens (human)Ki0.348433
TransporterRattus norvegicus (Norway rat)IC503.39091821
TransporterRattus norvegicus (Norway rat)Ki1.44822130
Tryptophan 5-hydroxylase 1Rattus norvegicus (Norway rat)Ki0.173523
Type-1 angiotensin II receptorBos taurus (cattle)IC500.180011
Type-2 angiotensin II receptorRattus norvegicus (Norway rat)IC500.210011
Type-2 angiotensin II receptorRattus norvegicus (Norway rat)Ki0.500011
Voltage-dependent L-type calcium channel subunit alpha-1CCavia porcellus (domestic guinea pig)IC508.300012
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC509.950022
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC509.950022
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC509.950022
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC509.950022
Voltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)IC5016.400015

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1AHomo sapiens (human)Kd0.398111
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 5ARattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 5BRattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 6Rattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Kd4.466812
AlbuminHomo sapiens (human)Kd851.138011
AlbuminRattus norvegicus (Norway rat)Kd322.500012
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Kd1.974022
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Kd1.974022
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Kd1.974022
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Kd1.095822
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Kd1.095822
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Kd1.095822
Chain A, CHIMERA OF IG KAPPA CHAIN: HUMAN CONSTANT REGION AND MOUSE VARIABLE REGIONsynthetic constructKd0.400011
Chain B, CHIMERA OF IG GAMMA-1 CHAIN: HUMAN CONSTANT REGION AND MOUSE VARIABLE REGIONsynthetic constructKd0.400011
Chain H, Fab M82G2, Heavy chainMus musculus (house mouse)Kd0.140012
Chain L, Fab M82g2, Light ChainMus musculus (house mouse)Kd0.140012
Envelope glycoproteinEbola virus - Mayinga, Zaire, 1976Kd584.000011
High affinity nerve growth factor receptorHomo sapiens (human)EC5086.000011
High affinity nerve growth factor receptorHomo sapiens (human)Kd2,050.000044
Major prion proteinHomo sapiens (human)EC5010.000011
Mu-type opioid receptorHomo sapiens (human)EC501.000011
Sigma non-opioid intracellular receptor 1Cavia porcellus (domestic guinea pig)EC5086.000011
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)EC500.990011
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)EC500.025011
Sodium-dependent dopamine transporter Homo sapiens (human)EC500.990011
Sodium-dependent dopamine transporter Homo sapiens (human)Kd5.190012
Sodium-dependent noradrenaline transporter Homo sapiens (human)EC500.210011
Sodium-dependent noradrenaline transporter Homo sapiens (human)Kd0.354323
Sodium-dependent serotonin transporterHomo sapiens (human)EC500.140011
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)EC501.765011
Sodium-dependent serotonin transporterHomo sapiens (human)Kd0.008912
Synaptic vesicular amine transporterHomo sapiens (human)Kd0.008011
Trace amine-associated receptor 1Homo sapiens (human)EC500.666344
Trace amine-associated receptor 1Macaca mulatta (Rhesus monkey)EC501.010011
Trace amine-associated receptor 1Mus musculus (house mouse)EC500.103955
Trace amine-associated receptor 1Rattus norvegicus (Norway rat)EC500.532866

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 6Homo sapiens (human)Kb0.030011
Cytochrome P450 1A2Homo sapiens (human)Km5.000011
Cytochrome P450 2C19Homo sapiens (human)Km5.000011
Cytochrome P450 3A4Homo sapiens (human)Km5.000011
Histamine H2 receptorCavia porcellus (domestic guinea pig)K0.50.0269213
Liver carboxylesterase 1Homo sapiens (human)Km120.000011
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CINH166.000011
Quinolone resistance protein NorAStaphylococcus aureusMMC6.570011
Snq2pSaccharomyces cerevisiae EC1118INH198.000011
Sodium-dependent dopamine transporter Homo sapiens (human)IC50.048011
Sodium-dependent serotonin transporterHomo sapiens (human)IC50.048011
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Km0.200011
UDP-glucuronosyltransferase 1A3Homo sapiens (human)Km369.500012
UDP-glucuronosyltransferase 1A4Homo sapiens (human)Km190.000025