Page last updated: 2024-08-05 15:21:16

dopamine uptake inhibitor

A dopaminergic agent that blocks the transport of dopamine into axon terminals or into storage vesicles within terminals. Most of the adrenergic uptake inhibitors also inhibit dopamine uptake.

ChEBI ID: 51039

Members (15)

MemberDefinitionClass
1-(1-(2-benzo(b)thienyl)cyclohexyl)piperidineA tertiary amino compound that consists of cyclohexane having piperidin-1-yl and benzothiophen-2-yl groups attached at position 1. A potent dopamine re-uptake inhibitor with a behavioral profile different from that of phencyclidine (PCP) and similar to that of cocaine.1-[1-(1-benzothiophen-2-yl)cyclohexyl]piperidine
1-[2-(benzhydryloxy)ethyl]-4-(3-phenylpropyl)piperazine dihydrochlorideA hydrochloride salt that is obtained by reaction of 1-[2-(benzhydryloxy)ethyl]-4-(3-phenylpropyl)piperazine with two equivalents of hydrogen chloride. Potent and selective inhibitor of dopamine uptake (KD = 5.5 nM in rat striatal membranes).1-[2-(benzhydryloxy)ethyl]-4-(3-phenylpropyl)piperazine dihydrochloride
amineptinA carbocyclic fatty acid that is 5-aminoheptanoic acid in which one of the hydrogens attached to the nitrogen is replaced by a 10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-yl group. A tricyclic antidepressant, it was never approved in the US and was withdrawn from the French market in 1999 due to concerns over abuse, dependence and severe acne.amineptine
amperozideA member of the class of ureas that is urea in which three of the four hydrogens are replaced by ethyl and 4-[4,4-bis(4-fluorophenyl)butyl]piperazin-1-yl groups. An atypical antipsychotic which was in clinical development for the treatment of schizophrenia and substance-related disorders. It is a potent 5-HT2A antagonist and used in veterinary medicine because of its sedative effect on pigs.amperozide
amperozide hydrochlorideThe hydrochloride salt of amperozide.amperozide 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
dextroamphetamineA 1-phenylpropan-2-amine that has S configuration.(S)-amphetamine
gbr 12935An N-alkylpiperazine that consists of piperazine bearing 2-(benzhydryloxy)ethyl and 3-phenylpropyl groups at positions 1 and 4 respectively. Potent and selective inhibitor of dopamine uptake (KD = 5.5 nM in rat striatal membranes).1-[2-(benzhydryloxy)ethyl]-4-(3-phenylpropyl)piperazine
histidyl-proline diketopiperazineA homodetic cyclic peptide resulting from the formal condensation of both the amino and acid groups of L-histidine with the acid and amino groups of L-proline. It is a metabolite of thyrotropin-releasing hormone (TRH).cyclo(L-His-L-Pro)
minaprineminaprine
nomifensineAn N-methylated tetrahydroisoquinoline carrying phenyl and amino substituents at positions C-4 and C-8, respectively.nomifensine
vanoxerineAn N-alkylpiperazine that consists of piperazine bearing 2-bis(4-fluorophenyl)methoxy]ethyl and 3-phenylpropyl groups at positions 1 and 4 respectively. Potent, competitive inhibitor of dopamine uptake (Ki = 1 nM for inhibition of striatal dopamine uptake). Has > 100-fold lower affinity for the noradrenalin and 5-HT uptake carriers. Also a potent sigma ligand (IC50 = 48 nM). Centrally active following systemic administration.vanoxerine
vanoxerineA hydrochloride salt that is obtained by reaction of vanoxerine with two equivalents of hydrogen chloride. Potent, competitive inhibitor of dopamine uptake (Ki = 1 nM for inhibition of striatal dopamine uptake). Has > 100-fold lower affinity for the noradrenalin and 5-HT uptake carriers. Also a potent sigma ligand (IC50 = 48 nM). Centrally active following systemic administration.vanoxerine dihydrochloride
venlafaxineA tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-methoxyphenyl group.venlafaxine

Research

Studies (38,733)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199010,792 (27.86)18.7374
1990's9,101 (23.50)18.2507
2000's7,796 (20.13)29.6817
2010's8,417 (21.73)24.3611
2020's2,627 (6.78)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials1,965 (4.64%)5.53%
Reviews2,542 (6.00%)6.00%
Case Studies2,381 (5.62%)4.05%
Observational51 (0.12%)0.25%
Other35,397 (83.61%)84.16%

Protein Targets (265)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-lipoxygenase, partialHomo sapiens (human)Potency18.854112
67.9K proteinVaccinia virusPotency16.803722
activating transcription factor 6Homo sapiens (human)Potency16.940923
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency17.935116
Alpha-synucleinHomo sapiens (human)Potency22.387211
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency15.848911
AR proteinHomo sapiens (human)Potency15.4295815
aryl hydrocarbon receptorHomo sapiens (human)Potency14.439322
arylsulfatase AHomo sapiens (human)Potency8.991513
ATAD5 protein, partialHomo sapiens (human)Potency17.581036
Ataxin-2Homo sapiens (human)Potency19.343825
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency6.876313
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency8.412711
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency19.311712
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency17.487212
Bloom syndrome protein isoform 1Homo sapiens (human)Potency25.479326
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency63.095711
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency33.491511
caspase-3Cricetulus griseus (Chinese hamster)Potency23.710111
caspase-3Homo sapiens (human)Potency33.491511
Caspase-7Cricetulus griseus (Chinese hamster)Potency23.710111
Cellular tumor antigen p53Homo sapiens (human)Potency22.530823
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency21.745926
Chain A, Beta-lactamaseEscherichia coli K-12Potency12.602822
Chain A, Ferritin light chainEquus caballus (horse)Potency11.519012
Chain A, HADH2 proteinHomo sapiens (human)Potency39.810711
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency1.122011
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency26.865315
Chain B, HADH2 proteinHomo sapiens (human)Potency39.810711
chromobox protein homolog 1Homo sapiens (human)Potency24.014614
cytochrome P450 2C19 precursorHomo sapiens (human)Potency12.632815
cytochrome P450 2C9 precursorHomo sapiens (human)Potency25.453314
cytochrome P450 2C9, partialHomo sapiens (human)Potency9.771711
cytochrome P450 2D6Homo sapiens (human)Potency11.287214
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency4.989019
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency14.0150212
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency16.224812
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency18.069513
D(1A) dopamine receptorHomo sapiens (human)Potency5.341537
D(1A) dopamine receptorSus scrofa (pig)Potency16.591012
DNA polymerase kappa isoform 1Homo sapiens (human)Potency37.685811
dopamine D1 receptorHomo sapiens (human)Potency2.716412
endonuclease IVEscherichia coliPotency22.245713
estrogen nuclear receptor alphaHomo sapiens (human)Potency18.2920817
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency20.435223
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency11.18131021
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency21.7830110
EWS/FLI fusion proteinHomo sapiens (human)Potency25.4218411
farnesoid X nuclear receptorHomo sapiens (human)Potency33.488922
Fumarate hydrataseHomo sapiens (human)Potency35.386614
GVesicular stomatitis virusPotency9.771711
GABA theta subunitRattus norvegicus (Norway rat)Potency14.015016
GALC proteinHomo sapiens (human)Potency35.481311
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency14.015016
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency14.015016
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency14.015016
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency14.015016
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency14.015016
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency14.015016
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency14.015016
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency14.015016
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency14.015016
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency14.015016
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency14.015016
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency14.015016
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency14.015016
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency14.015016
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency14.015016
gemininHomo sapiens (human)Potency18.450348
GLI family zinc finger 3Homo sapiens (human)Potency12.166426
glp-1 receptor, partialHomo sapiens (human)Potency8.912511
GLS proteinHomo sapiens (human)Potency14.821113
glucocerebrosidaseHomo sapiens (human)Potency27.005012
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency15.082436
glucokinase regulatory proteinHomo sapiens (human)Potency12.589311
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency21.271812
heat shock protein beta-1Homo sapiens (human)Potency29.108322
hexokinase-4 isoform 1Homo sapiens (human)Potency12.589311
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency21.4179224
Histone H2A.xCricetulus griseus (Chinese hamster)Potency21.974111
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency9.771711
huntingtin isoform 2Homo sapiens (human)Potency25.118911
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency24.073122
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency21.017126
IDH1Homo sapiens (human)Potency16.360111
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency9.771712
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency7.493426
Integrin alpha-IIbHomo sapiens (human)Potency15.714212
Integrin beta-3Homo sapiens (human)Potency15.714212
Interferon betaHomo sapiens (human)Potency25.955335
lamin isoform A-delta10Homo sapiens (human)Potency10.319127
lethal factor (plasmid)Bacillus anthracis str. A2012Potency22.613015
LuciferasePhotinus pyralis (common eastern firefly)Potency24.545411
M-phase phosphoprotein 8Homo sapiens (human)Potency27.802515
Microtubule-associated protein tauHomo sapiens (human)Potency33.470313
mitogen-activated protein kinase 1Homo sapiens (human)Potency26.635725
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency8.977327
neuropeptide S receptor isoform AHomo sapiens (human)Potency14.219112
NFKB1 protein, partialHomo sapiens (human)Potency11.294724
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency12.672812
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency58.047911
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency14.433424
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency29.092911
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency24.073122
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency32.478425
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency31.622811
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency31.640236
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency79.432812
ParkinHomo sapiens (human)Potency9.200011
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency11.493224
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency40.777513
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency7.585634
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency22.411034
phosphopantetheinyl transferaseBacillus subtilisPotency76.110412
polyproteinZika virusPotency35.386614
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency6.309611
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency17.382616
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency0.223414
PPM1D proteinHomo sapiens (human)Potency32.999312
pregnane X nuclear receptorHomo sapiens (human)Potency26.778914
progesterone receptorHomo sapiens (human)Potency22.427824
RAR-related orphan receptor gammaMus musculus (house mouse)Potency9.079625
ras-related protein Rab-9AHomo sapiens (human)Potency68.740414
regulator of G-protein signaling 4Homo sapiens (human)Potency22.190512
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency35.442737
retinoid X nuclear receptor alphaHomo sapiens (human)Potency13.744124
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency18.892647
SMAD family member 2Homo sapiens (human)Potency23.914511
SMAD family member 3Homo sapiens (human)Potency23.914511
survival motor neuron protein isoform dHomo sapiens (human)Potency16.436716
TDP1 proteinHomo sapiens (human)Potency12.2564216
thioredoxin reductaseRattus norvegicus (Norway rat)Potency13.194336
ThrombopoietinHomo sapiens (human)Potency15.902726
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency25.642638
thyroid stimulating hormone receptorHomo sapiens (human)Potency20.9596313
transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Potency31.622811
tumor susceptibility gene 101 proteinHomo sapiens (human)Potency35.481312
USP1 protein, partialHomo sapiens (human)Potency37.895814
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency18.210224
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency25.714023
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency21.271812

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki0.163522
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC500.085522
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC500.085522
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC500.085522
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 5ARattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 5BRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 6Rattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki0.301011
AcetylcholinesteraseElectrophorus electricus (electric eel)IC50600.000011
AcetylcholinesteraseHomo sapiens (human)IC5085.000011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC502.708011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki2.685011
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC505.754411
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC505.754411
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC505.754411
Amine oxidase [flavin-containing] AHomo sapiens (human)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
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000011
Beta-2 adrenergic receptorCavia porcellus (domestic guinea pig)IC500.027011
Bile salt export pumpHomo sapiens (human)IC50653.600045
Bile salt export pumpRattus norvegicus (Norway rat)IC501,000.000011
Calcium/calmodulin-dependent protein kinase type II subunit alphaHomo sapiens (human)IC50100.000011
Calcium/calmodulin-dependent protein kinase type II subunit betaHomo sapiens (human)IC50100.000011
Calcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)IC50100.000011
Calcium/calmodulin-dependent protein kinase type II subunit gammaHomo sapiens (human)IC50100.000011
cAMP-dependent protein kinase catalytic subunit alphaHomo sapiens (human)IC50100.000011
cAMP-dependent protein kinase catalytic subunit betaHomo sapiens (human)IC50100.000011
cAMP-dependent protein kinase catalytic subunit gammaHomo sapiens (human)IC50100.000011
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)Ki1.115011
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)Ki1.115011
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)Ki1.115011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000011
Cytochrome P450 2C19Homo sapiens (human)IC500.031611
Cytochrome P450 2D6Homo sapiens (human)IC5020.000011
DRattus norvegicus (Norway rat)IC503.734133
D(1B) dopamine receptorRattus norvegicus (Norway rat)IC502.724022
D(2) dopamine receptorRattus norvegicus (Norway rat)IC502.724022
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.069025
D(3) dopamine receptorRattus norvegicus (Norway rat)IC502.724022
D(4) dopamine receptorRattus norvegicus (Norway rat)IC502.724022
Delta-type opioid receptorHomo sapiens (human)IC5010.000011
Fatty acid-binding protein, heartHomo sapiens (human)IC500.367011
Fatty-acid amide hydrolase 1Homo sapiens (human)IC500.897522
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)Ki10.000012
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Ki10.000012
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Ki10.000012
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Ki10.000012
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Ki10.000012
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Ki10.000012
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Ki10.000012
Kappa-type opioid receptorHomo sapiens (human)IC502.140011
Leukotriene B4 receptor 1Homo sapiens (human)Ki0.524011
Leukotriene B4 receptor 2Homo sapiens (human)Ki0.524011
Lysosomal Pro-X carboxypeptidaseHomo sapiens (human)Ki10.000012
Mu-type opioid receptorHomo sapiens (human)IC503.530011
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000011
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki17.000011
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki61.398522
Muscarinic acetylcholine receptor M2Sus scrofa (pig)Ki0.234411
Phenylethanolamine N-methyltransferaseBos taurus (cattle)Ki435.333323
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CIC50400.000011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC508.606677
Protein kinase C alpha typeHomo sapiens (human)IC50100.000011
Protein kinase C beta typeHomo sapiens (human)IC50100.000011
Protein kinase C delta typeHomo sapiens (human)IC50100.000011
Protein kinase C epsilon typeHomo sapiens (human)IC50100.000011
Protein kinase C eta typeHomo sapiens (human)IC50100.000011
Protein kinase C gamma typeHomo sapiens (human)IC50100.000011
Protein kinase C iota typeHomo sapiens (human)IC50100.000011
Protein kinase C theta typeHomo sapiens (human)IC50100.000011
Protein kinase C zeta typeHomo sapiens (human)IC50100.000011
Serine/threonine-protein kinase D1Homo sapiens (human)IC50100.000011
Serine/threonine-protein kinase D3Homo sapiens (human)IC50100.000011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC500.363046
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki4.574012
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)Ki0.116011
Small conductance calcium-activated potassium channel protein 1Rattus norvegicus (Norway rat)IC500.185512
Small conductance calcium-activated potassium channel protein 2Rattus norvegicus (Norway rat)IC500.185512
Small conductance calcium-activated potassium channel protein 3Rattus norvegicus (Norway rat)IC500.185512
Sodium-dependent dopamine transporterMus musculus (house mouse)IC500.200011
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC500.854069111
Sodium-dependent dopamine transporterMus musculus (house mouse)Ki0.850011
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)Ki14.38973672
Sodium-dependent dopamine transporter Homo sapiens (human)IC500.98096167
Sodium-dependent dopamine transporter Homo sapiens (human)Ki0.43754856
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC501.32033742
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki1.34943743
Sodium-dependent serotonin transporterHomo sapiens (human)IC501.33353641
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)IC500.80022431
Sodium-dependent serotonin transporterHomo sapiens (human)Ki0.59613947
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Ki0.40072948
TransporterRattus norvegicus (Norway rat)IC502.87241719
TransporterRattus norvegicus (Norway rat)Ki2.53932126
Tryptophan 5-hydroxylase 1Rattus norvegicus (Norway rat)Ki0.490011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
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
AlbuminRattus norvegicus (Norway rat)Kd511.000011
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
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)Kd9.300011
Sodium-dependent noradrenaline transporter Homo sapiens (human)EC500.210011
Sodium-dependent noradrenaline transporter Homo sapiens (human)Kd1.060011
Sodium-dependent serotonin transporterHomo sapiens (human)EC500.140011
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)EC501.765011
Sodium-dependent serotonin transporterHomo sapiens (human)Kd0.008911
Trace amine-associated receptor 1Homo sapiens (human)EC500.666244
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
Histamine H2 receptorCavia porcellus (domestic guinea pig)K0.50.009312
Liver carboxylesterase 1Homo sapiens (human)Km120.000011
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CINH433.000011
Snq2pSaccharomyces cerevisiae EC1118INH433.000011
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Km0.200011