Page last updated: 2024-12-05

protriptyline

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Protriptyline is a tricyclic antidepressant (TCA) medication. It was first synthesized in the 1960s and has been used to treat major depressive disorder (MDD) since then. Its mechanism of action involves blocking the reuptake of serotonin and norepinephrine in the brain. Protriptyline is considered a potent inhibitor of serotonin reuptake, with lesser effects on norepinephrine. Its efficacy in treating MDD has been demonstrated in clinical trials. Protriptyline is also used off-label for other conditions, such as chronic pain and anxiety disorders. However, its use is generally considered second-line therapy due to its potential side effects, including dry mouth, constipation, blurred vision, and sedation. The study of protriptyline continues to this day, with researchers investigating its potential for treating other conditions and exploring its effects on the brain. The compound remains a subject of interest due to its unique pharmacological profile and its potential for therapeutic applications.'

Protriptyline: Tricyclic antidepressant similar in action and side effects to IMIPRAMINE. It may produce excitation. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4976
CHEMBL ID668
CHEBI ID8597
SCHEMBL ID34267
MeSH IDM0017928

Synonyms (100)

Synonym
AC-15971
BIDD:PXR0157
BRD-K42098891-003-03-1
5h-dibenzo[a,d]cycloheptene-5-propanamine, n-methyl-
protriptyline [inn:ban]
n-methyl-5h-dibenzo(a,d)cycloheptene-5-propylamine
protriptylinum [inn-latin]
5h-dibenzo(a,d)cycloheptene-5-propylamine, n-methyl-
protryptyline
hsdb 3391
brn 2217411
5-(3-methylaminopropyl)-5h-dibenzo(a,d)cycloheptene
einecs 207-119-9
n-3-(5h-dibenzo(a,d)cyclohepten-5-yl)propyl-n-methylamine
protriptilina [inn-spanish]
5h-dibenzo(a,d)cycloheptene-5-propanamine, n-methyl-
cas-1225-55-4
NCGC00015851-01
NCGC00015851-02
lopac-p-8813
BPBIO1_000924
PRESTWICK3_000930
PRESTWICK2_000930
PDSP1_001390
PDSP2_001374
5h-dibenzo[a, d]cycloheptene-5-propanamine, n-methyl-, hydrochloride
vivactil
3-(11h-dibenzo[[?],[?]][7]annulen-11-yl)-n-methyl-propan-1-amine
vivactyl
AB00489964
protriptyline
C07408
438-60-8
DB00344
triptil
n-methyl-5h-dibenzo[a,d]cycloheptene-5-propanamine
BSPBIO_000840
7-(3-methylaminopropyl)-1,2:5,6-dibenzocycloheptatriene
5-(3-methylaminopropyl)-5h-dibenzo[a,d]cycloheptene
3-(5h-dibenzo[a,d][7]annulen-5-yl)-n-methylpropan-1-amine
amimetilina
CHEBI:8597 ,
n-methyl-5h-dibenzo[a,d]cycloheptene-5-propylamine
3-(5h-dibenzo[a,d]cyclohepten-5-yl)-n-methyl-1-propanamine
PRESTWICK0_000930
PRESTWICK1_000930
SPBIO_003019
LOPAC0_000974
NCGC00024439-03
NCGC00015851-03
NCGC00015851-07
CHEMBL668 ,
L000913
D08447
protriptyline (inn)
bdbm50176062
CCG-205054
AKOS015962184
NCGC00015851-06
NCGC00015851-05
NCGC00015851-04
4ndu154t12 ,
protriptylinum
protriptilina
unii-4ndu154t12
protriptyline [inn]
protriptyline [vandf]
protriptyline [who-dd]
protriptyline [mi]
protriptyline [hsdb]
3-(11h-dibenzo[1,2-a:1',2'-e][7]annulen-11-yl)-n-methylpropan-1-amine
gtpl7285
SCHEMBL34267
protryptyline hydrochloride
5h-dibenzo[a,d]cycloheptene-5-propylamine, n-methyl-
mk 240
vivactil (salt/mix)
3-(5h-dibenzo[a,d]cyclohepten-5-yl)-n-methyl-1-propanamine #
concordin (salt/mix)
AB00489964_10
DTXSID0023535 ,
methyl(3-{tricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,9,12,14-heptaen-2-yl}propyl)amine
SBI-0050947.P002
Q408432
n-methyl-3-(2-tricyclo[9.4.0.03,8]pentadeca-1(15),3,5,7,9,11,13-heptaenyl)propan-1-amine
SDCCGSBI-0050947.P003
NCGC00015851-15
EN300-18552820
methyl(3-{tricyclo[9.4.0.0,3,8]pentadeca-1(15),3,5,7,9,11,13-heptaen-2-yl}propyl)amine
CS-0013761
HY-B0949A
n-methyl-5h-dibenzo
protriptilina (inn-spanish)
dtxcid203535
n06aa11
3-(5h-dibenzo(a,d)(7)annulen-5-yl)-n-methylpropan-1-amine
n-methyl-5h-dibenzo(a,d)cycloheptene-5-propanamine
protriptylinum (inn-latin)
3-(5h-dibenzo(a,d)cyclohepten-5-yl)-n-methyl-1-propanamine
protriptylin

Research Excerpts

Effects

Protriptyline (PRT) has been shown to preferentially stimulate upper airway inspiratory motorneurons relative to phrenic activity in hyperoxic hypercapnia in the decerebrate cat via a carotid body-independent mechanism. It is also shown to improve nocturnal and diurnal hypoxemia in patients with chronic obstructive pulmonary disease in short trials.

ExcerptReferenceRelevance
"Protriptyline has been used as an antidepressant. "( Effect of Protriptyline on [Ca²⁺]i and Viability in MDCK Renal Tubular Cells.
Cheng, HH; Chou, CT; Jan, CR; Kuo, CC; Liang, WZ; Shieh, P; Wang, JL, 2017
)
2.3
"Protriptyline (PRT) has been shown to preferentially stimulate upper airway inspiratory motorneurons relative to phrenic activity in hyperoxic hypercapnia in the decerebrate cat via a carotid body-independent mechanism. "( The carotid body in the motorneuron response to protriptyline.
Bruce, EN; Hudgel, DW; Oku, Y; Richmonds, CR, 1993
)
1.98
"Protriptyline has been shown to improve nocturnal and diurnal hypoxemia in patients with chronic obstructive pulmonary disease in short trials. "( Long-term effects of protriptyline in patients with chronic obstructive pulmonary disease.
Cormier, Y; La Forge, J; Marc, I; Sériès, F, 1993
)
2.05

Treatment

ExcerptReferenceRelevance
"In protriptyline (25 mg/kg) pretreated rats stereotactic 5,7-dihydroxytryptamine (5,7-DHT) lesions of the medial plus laternal 5-hydroxytryptamine (5-HE) bundles in the mesencephalon increased the 5-HT fluorescence in these bundles, and reduced the in vitro uptake of [3H] 5-HT in the hypothalamus to 16% of control values after 2 mug 5,7-DHT/4mul and 12% after 4 mug 5,7-DHT/4mul, and in the cortex cerebri to 35 and 34% of control values, respectively. "( Behavioral effects of 5, 7-dihydroxytryptamine lesions of ascending 5-hydroxytryptamine pathways.
Fuxe, K; Hole, K; Jonsson, G, 1976
)
0.88

Toxicity

ExcerptReferenceRelevance
" Dx infused intravenously to conscious or anaesthetized guinea-pigs proved as cardiotoxic as amitriptyline but more toxic than protriptyline, thus confirming our previous results in rabbits."( Prostaglandins and the cardiotoxic effects of doxepin in rabbits and guinea-pigs.
Elonen, E; Eränkö, P; Mattila, MJ; Puisto, EL, 1980
)
0.47
"Studies show that tricyclic antidepressants prescribed for migraines, anxiety, and child enuresis have numerous adverse effects in living cells."( In vitro studies of DNA damage caused by tricyclic antidepressants: a role of peroxidase in the side effects of the drugs.
Azar, N; Korobkova, EA; Ng, W; Nizamova, M; Venkatratnam, A; Williams, AK, 2010
)
0.36

Bioavailability

ExcerptReferenceRelevance
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34
", ip) indicate that the liver is the primary site of biotransformation of the compound, suggesting that both 22a and its metabolite(s) are active, compensating probably low bioavailability of the parent molecule."( Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Bednarski, M; Gunia-Krzyżak, A; Marona, H; Nitek, W; Pękala, E; Powroźnik, B; Słoczyńska, K; Walczak, M; Waszkielewicz, AM; Żesławska, E, 2016
)
0.43

Dosage Studied

ExcerptRelevanceReference
" After 3 1/2 weeks treatment at dosage levels of 40 mg/day, protriptyline plasma levels ranged from 430 to 1430 nmol/l."( Pharmacokinetic aspects of protriptyline plasma levels.
MacDonald, AJ; Moody, JP; Naylor, GJ; Whyte, SF, 1977
)
0.8
" During programmed ventricular stimulation after 59 trials of 20 to 30 mg/kg body weight of oral bethanidine (acute dosing in 40 patients, and divided dosing over 24 hours in 19 patients), no ventricular tachyarrhythmias were inducible in 6 patients (11%), sustained ventricular tachycardia was converted to nonsustained ventricular tachycardia in 3 patients (5%), ventricular tachyarrhythmias remained inducible in 39 patients (70%) and spontaneous ventricular tachyarrhythmias occurred more frequently in 4 patients (7%)."( Bethanidine sulfate: efficacy in prevention of ventricular tachyarrhythmias during programmed stimulation. Report of a multicenter study of 56 patients.
Fisher, JD; Kim, SG; Matos, JA; Teichman, SL; Waspe, LE, 1985
)
0.27
"3 A second cannabis extract (II) with a different ratio of cannabinoids (also administered in dosage equivalent to 10 mg Delta(9)-THC/kg) failed to affect pentobarbitone anaesthesia in mice."( Interaction of cannabis and general anaesthetic agents in mice.
Chesher, GB; Jackson, DM; Starmer, GA, 1974
)
0.25
"3 microM) produced an approximately parallel shift to the right in the dose-response curve to NA."( Inhibitory effect of noradrenaline uptake inhibitors on contractions of rat aortic smooth muscle.
Huang, Y, 1996
)
0.29
" However, the vast majority of in vitro pharmacogenomic studies performed to date are limited to dose-response screening upon a single viability assay endpoint."( High content phenotypic screening identifies serotonin receptor modulators with selective activity upon breast cancer cell cycle and cytokine signaling pathways.
Carragher, NO; Dawson, JC; Hughes, RE; Makda, A; Munro, AF; Shepherd, E; Warchal, SJ, 2020
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
antidepressantAntidepressants are mood-stimulating drugs used primarily in the treatment of affective disorders and related conditions.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
carbotricyclic compoundA carbopolyclic compound comprising of three carbocyclic rings.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (40)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, HADH2 proteinHomo sapiens (human)Potency22.10610.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency22.10610.025120.237639.8107AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency14.12540.177814.390939.8107AID2147
thioredoxin reductaseRattus norvegicus (Norway rat)Potency39.81070.100020.879379.4328AID588456
NFKB1 protein, partialHomo sapiens (human)Potency8.91250.02827.055915.8489AID895; AID928
ThrombopoietinHomo sapiens (human)Potency10.00000.02517.304831.6228AID917; AID918
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency9.91500.00207.533739.8107AID891
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency10.00000.316212.443531.6228AID902
D(1A) dopamine receptorHomo sapiens (human)Potency6.63980.02245.944922.3872AID488982; AID488983
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency14.68920.00669.809418.4927AID1347050
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency12.28980.005612.367736.1254AID624032
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency8.28520.031610.279239.8107AID884; AID885
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.27830.00106.000935.4813AID943; AID944
lamin isoform A-delta10Homo sapiens (human)Potency0.00710.891312.067628.1838AID1487
chaperonin GroELMethanococcus maripaludis S2Potency100.000031.622831.622831.6228AID488978
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency8.28521.000012.224831.6228AID885
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency16.27100.316212.765731.6228AID881
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency8.28521.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency8.28521.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency8.28521.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency8.28521.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency8.28521.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency8.28521.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency8.28521.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency8.28521.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency8.28521.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency8.28521.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency16.27100.00638.235039.8107AID881
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency8.28521.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency8.28521.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency8.28521.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency8.28521.000012.224831.6228AID885
Ataxin-2Homo sapiens (human)Potency14.12540.011912.222168.7989AID588378
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency8.28521.000012.224831.6228AID885
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency33.80780.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)128.60000.11007.190310.0000AID1449628
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC50 (µMol)0.00490.00081.541620.0000AID1285673; AID1336372; AID1433985; AID255303; AID340275; AID346470; AID566243; AID663263; AID751837; AID752201
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki0.00300.00031.465610.0000AID1433985; AID346470; AID611940; AID663263; AID751837
Sulfotransferase 1A1Homo sapiens (human)Ki65.50000.00510.01200.0190AID1802453
Voltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)IC50 (µMol)14.00000.04004.113710.0000AID1850268
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Sodium-dependent noradrenaline transporter Homo sapiens (human)Kd0.00140.00080.25331.0600AID537546
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (75)

Processvia Protein(s)Taxonomy
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
phospholipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell population proliferationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell migrationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
prostate gland developmentPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
regulation of epithelial cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of chemokine productionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of keratinocyte differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell cyclePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of growthPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
endocannabinoid signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cannabinoid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
monoamine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent noradrenaline transporter Homo sapiens (human)
chemical synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent noradrenaline transporter Homo sapiens (human)
response to painSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent noradrenaline transporter Homo sapiens (human)
neuron cellular homeostasisSodium-dependent noradrenaline transporter Homo sapiens (human)
amino acid transportSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent noradrenaline transporter Homo sapiens (human)
sulfationSulfotransferase 1A1Homo sapiens (human)
ethanol catabolic processSulfotransferase 1A1Homo sapiens (human)
catecholamine metabolic processSulfotransferase 1A1Homo sapiens (human)
xenobiotic metabolic processSulfotransferase 1A1Homo sapiens (human)
estrogen metabolic processSulfotransferase 1A1Homo sapiens (human)
amine metabolic processSulfotransferase 1A1Homo sapiens (human)
flavonoid metabolic processSulfotransferase 1A1Homo sapiens (human)
3'-phosphoadenosine 5'-phosphosulfate metabolic processSulfotransferase 1A1Homo sapiens (human)
sulfationSulfotransferase 1A1Homo sapiens (human)
modulation of chemical synaptic transmissionVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
response to amyloid-betaVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
chemical synaptic transmissionVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
sulfationSulfotransferase 2A1Homo sapiens (human)
ethanol catabolic processSulfotransferase 2A1Homo sapiens (human)
xenobiotic metabolic processSulfotransferase 2A1Homo sapiens (human)
steroid metabolic processSulfotransferase 2A1Homo sapiens (human)
cholesterol metabolic processSulfotransferase 2A1Homo sapiens (human)
lipid catabolic processSulfotransferase 2A1Homo sapiens (human)
bile acid catabolic processSulfotransferase 2A1Homo sapiens (human)
thyroid hormone metabolic processSulfotransferase 2A1Homo sapiens (human)
3'-phosphoadenosine 5'-phosphosulfate metabolic processSulfotransferase 2A1Homo sapiens (human)
sulfationSulfotransferase 2A1Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (37)

Processvia Protein(s)Taxonomy
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 9S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
actin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
protein bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
alpha-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
metal ion bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
beta-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
aryl sulfotransferase activitySulfotransferase 1A1Homo sapiens (human)
protein bindingSulfotransferase 1A1Homo sapiens (human)
sulfotransferase activitySulfotransferase 1A1Homo sapiens (human)
flavonol 3-sulfotransferase activitySulfotransferase 1A1Homo sapiens (human)
steroid sulfotransferase activitySulfotransferase 1A1Homo sapiens (human)
3'-phosphoadenosine 5'-phosphosulfate bindingSulfotransferase 1A1Homo sapiens (human)
amyloid-beta bindingVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
calcium ion bindingVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
protein bindingVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
ATP bindingVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
alcohol sulfotransferase activitySulfotransferase 2A1Homo sapiens (human)
protein bindingSulfotransferase 2A1Homo sapiens (human)
sulfotransferase activitySulfotransferase 2A1Homo sapiens (human)
bile-salt sulfotransferase activitySulfotransferase 2A1Homo sapiens (human)
steroid sulfotransferase activitySulfotransferase 2A1Homo sapiens (human)
3'-phosphoadenosine 5'-phosphosulfate bindingSulfotransferase 2A1Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (29)

Processvia Protein(s)Taxonomy
nucleusPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytoskeletonPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
adherens junctionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
focal adhesionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
cell surfaceSodium-dependent noradrenaline transporter Homo sapiens (human)
membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
presynaptic membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
axonSodium-dependent noradrenaline transporter Homo sapiens (human)
cytosolSulfotransferase 1A1Homo sapiens (human)
cytoplasmSulfotransferase 1A1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
plasma membraneVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
synapseVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
neuronal cell bodyVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
cytosolSulfotransferase 2A1Homo sapiens (human)
cytoplasmSulfotransferase 2A1Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (83)

Assay IDTitleYearJournalArticle
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1656410Antiproliferative activity against human HCC1954 cells assessed as cell viability incubated for 72 hrs Alamar blue assay2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
High content phenotypic screening identifies serotonin receptor modulators with selective activity upon breast cancer cell cycle and cytokine signaling pathways.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID346470Displacement of radiolabeled protriptyline from human NET2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.
AID1433985Displacement of [3H]nisoxetine from human recombinant norepinephrine transporter expressed in CHO cells after 120 mins by scintillation counting2017Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID205268Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID680714TP_TRANSPORTER: increase in Rhodamine 123 intracellular accumulation (R123: 150 uM, Protriptyline: 0.25 ug/mL) in MDR1-expressing Caco-2 cells2000The Journal of pharmacology and experimental therapeutics, Dec, Volume: 295, Issue:3
Influence of antipsychotic, antiemetic, and Ca(2+) channel blocker drugs on the cellular accumulation of the anticancer drug daunorubicin: P-glycoprotein modulation.
AID611940Displacement of [3H]nisoxetine from human NE transporter2011Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15
Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators.
AID663263Displacement of [3H]nisoxetine from human NET expressed in CHO cells after 120 mins by scintillation counting2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
First-in-class, dual-action, 3,5-disubstituted indole derivatives having human nitric oxide synthase (nNOS) and norepinephrine reuptake inhibitory (NERI) activity for the treatment of neuropathic pain.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1656409Induction of morphological changes in human HCC1954 cells assessed as number of nuclei incubated for 48 hrs by Hoechst 33342, SYTO14, Phalloidin-594, Wheat germ agglutinin-594, Concavalin-488, MitoTracker DeepRed staining based wide field fluorescent micr2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
High content phenotypic screening identifies serotonin receptor modulators with selective activity upon breast cancer cell cycle and cytokine signaling pathways.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID255303Percent inhibition against Norepinephrine transporter at 1 uM nonselective2005Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID1656406Antiproliferative activity against human HCC1954 cells assessed as reduction in cell number at 10 uM incubated for 72 hrs Alamar blue assay2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
High content phenotypic screening identifies serotonin receptor modulators with selective activity upon breast cancer cell cycle and cytokine signaling pathways.
AID116717Acute cytotoxicity was evaluated as LD50 in mice (ip)1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
2,4-Dihydro-3H-1,2,4-triazole-3-thiones as potential antidepressant agents.
AID1656407Induction of morphological changes in human T47D cells assessed as number of nuclei incubated for 48 hrs by Hoechst 33342, SYTO14, Phalloidin-594, Wheat germ agglutinin-594, Concavalin-488, MitoTracker DeepRed staining based wide field fluorescent microsc2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
High content phenotypic screening identifies serotonin receptor modulators with selective activity upon breast cancer cell cycle and cytokine signaling pathways.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1285673Displacement of [3H]nisoxentine from human recombinant norepinephrine transporter expressed in CHO cells2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
AID43581Inhibition of beta-lactamase at 100 uM2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID227718Binding energy by using the equation deltaG obsd = -RT ln KD1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Functional group contributions to drug-receptor interactions.
AID751837Binding affinity to human norepinephrine transporter by radioligand displacement assay2013European journal of medicinal chemistry, May, Volume: 63Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1656404Antiproliferative activity against human T47D cells assessed reduction in cell number at 10 uM incubated for 72 hrs by Alamar blue assay2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
High content phenotypic screening identifies serotonin receptor modulators with selective activity upon breast cancer cell cycle and cytokine signaling pathways.
AID114157Antidepressant activity was evaluated by measuring its ability to antagonize reserpine-induced ptosis in mice1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
2,4-Dihydro-3H-1,2,4-triazole-3-thiones as potential antidepressant agents.
AID205267Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID22293Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1656424Antiproliferative activity against human T47D cells assessed reduction in cell number at 1 uM incubated for 72 hrs by Alamar blue assay2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
High content phenotypic screening identifies serotonin receptor modulators with selective activity upon breast cancer cell cycle and cytokine signaling pathways.
AID566243Inhibition of human aorepinephrine transporter2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: de
AID106806Inhibition of malate dehydrogenase (MDH) at 400 uM2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1850268Inhibition of endogenous human CaV2.2 in human SH-SY5Y cells in presence of nifedipine by Calcium 4 dye based calcium influx fluorescence-imaging assay2022RSC medicinal chemistry, Feb-23, Volume: 13, Issue:2
Inhibition of N-type calcium ion channels by tricyclic antidepressants - experimental and theoretical justification for their use for neuropathic pain.
AID26304Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1656408Antiproliferative activity against human T47D cells assessed as cell viability incubated for 72 hrs Alamar blue assay2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
High content phenotypic screening identifies serotonin receptor modulators with selective activity upon breast cancer cell cycle and cytokine signaling pathways.
AID752201Binding affinity to human nonepinephrine transporter by radioligand displacement assay2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID52790Inhibition of chymotrypsin at 250 uM2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID1656425Antiproliferative activity against human HCC1954 cells assessed as reduction in cell number at 1 uM incubated for 72 hrs Alamar blue assay2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
High content phenotypic screening identifies serotonin receptor modulators with selective activity upon breast cancer cell cycle and cytokine signaling pathways.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID311932Inhibition of ASM in human H4 cells assessed as residual activity at 10 uM2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID1336372Displacement of [3H]nisoxetine from human recombinant norepinephrine transporter expressed in CHO cells measured after 120 mins by scintillation counting method2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID340275Inhibition of human NET2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID114156Antidepressant activity was evaluated by measuring its ability to antagonize RO 4-1284-induced hypothermia in mice1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
2,4-Dihydro-3H-1,2,4-triazole-3-thiones as potential antidepressant agents.
AID19006Calculated membrane partition coefficient (Kmemb)2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Surface activity profiling of drugs applied to the prediction of blood-brain barrier permeability.
AID1656405Induction of morphological changes in human HCC1954 cells at 10 uM incubated for 48 hrs by Hoechst 33342, SYTO14, Phalloidin-594, Wheat germ agglutinin-594, Concavalin-488, MitoTracker DeepRed staining based wide field fluorescent microscopic method2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
High content phenotypic screening identifies serotonin receptor modulators with selective activity upon breast cancer cell cycle and cytokine signaling pathways.
AID1656403Induction of morphological changes in human T47D cells at 10 uM incubated for 48 hrs by Hoechst 33342, SYTO14, Phalloidin-594, Wheat germ agglutinin-594, Concavalin-488, MitoTracker DeepRed staining based wide field fluorescent microscopic method2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
High content phenotypic screening identifies serotonin receptor modulators with selective activity upon breast cancer cell cycle and cytokine signaling pathways.
AID537546Inhibition of human NET2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Diaryldiamines with dual inhibition of the histamine H(3) receptor and the norepinephrine transporter and the efficacy of 4-(3-(methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in pain.
AID1346943Human SERT (Monoamine transporter subfamily)1997European journal of pharmacology, Dec-11, Volume: 340, Issue:2-3
Pharmacological profile of antidepressants and related compounds at human monoamine transporters.
AID1346971Human NET (Monoamine transporter subfamily)1997European journal of pharmacology, Dec-11, Volume: 340, Issue:2-3
Pharmacological profile of antidepressants and related compounds at human monoamine transporters.
AID1346971Human NET (Monoamine transporter subfamily)2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
First-in-class, dual-action, 3,5-disubstituted indole derivatives having human nitric oxide synthase (nNOS) and norepinephrine reuptake inhibitory (NERI) activity for the treatment of neuropathic pain.
AID1346971Human NET (Monoamine transporter subfamily)2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1802453Amoxapine and Protriptyline Inhibition Assay from Article 10.1074/jbc.M113.510974: \\High accuracy in silico sulfotransferase models.\\2013The Journal of biological chemistry, Nov-29, Volume: 288, Issue:48
High accuracy in silico sulfotransferase models.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (218)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990139 (63.76)18.7374
1990's31 (14.22)18.2507
2000's15 (6.88)29.6817
2010's23 (10.55)24.3611
2020's10 (4.59)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 51.80

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index51.80 (24.57)
Research Supply Index5.53 (2.92)
Research Growth Index4.46 (4.65)
Search Engine Demand Index83.98 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (51.80)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials22 (9.57%)5.53%
Reviews17 (7.39%)6.00%
Case Studies19 (8.26%)4.05%
Observational0 (0.00%)0.25%
Other172 (74.78%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Single Dose, 2-Period, 2-way Crossover Bioequivalency Study of Protriptyline Tablets 10 mg Under Fasted Conditions [NCT00754962]38 participants (Actual)Interventional2006-12-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]