Page last updated: 2024-11-11

zimeldine

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

Description

Zimeldine: One of the SEROTONIN UPTAKE INHIBITORS formerly used for depression but was withdrawn worldwide in September 1983 because of the risk of GUILLAIN-BARRE SYNDROME associated with its use. (From Martindale, The Extra Pharmacopoeia, 29th ed, p385) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5365247
CHEMBL ID37744
CHEBI ID135357
CHEBI ID92824
SCHEMBL ID35029
MeSH IDM0023127
PubMed CID5458656
CHEMBL ID354646
SCHEMBL ID11289888
MeSH IDM0023127

Synonyms (92)

Synonym
2-propen-1-amine, 3-(4-bromophenyl)-n,n-dimethyl-3-(3-pyridinyl)-, (z)-
allylamine, 3-(p-bromophenyl)-n,n-dimethyl-3-(3-pyridyl)-
normud
zelmid
zimeldine [inn:ban]
brn 0479680
a 23140
cis-h 102/09
zimeldina [spanish]
zimelidine (z)
zimeldinum [latin]
LOPAC0_001280
(z)-zimelidine
zimelidine
zimeldine
cis-zimelidine
(z)-3-(4'-bromophenyl)-3-(3''-pyridyl)dimethylallylamine
DB04832
NCI305352
PRESTWICK2_000092
NCGC00025286-02
56775-88-3
CHEBI:135357
NCGC00025286-03
CHEMBL37744 ,
L001151
trans-[3-(4-bromo-phenyl)-3-pyridin-3-yl-allyl]-dimethyl-amine;c2h4o4
[3-(4-bromo-phenyl)-3-pyridin-3-yl-allyl]-dimethyl-amine(zimeldine)
bdbm50020706
[3-(4-bromo-phenyl)-3-pyridin-3-yl-allyl]-dimethyl-amine (zimelidine)
[3-(4-bromo-phenyl)-3-pyridin-3-yl-allyl]-dimethyl-amine
cis -[3-(4-bromo-phenyl)-3-pyridin-3-yl-allyl]-dimethyl-amine;hcl
NCGC00188940-01
CCG-37384
zimeldina
5-22-10-00534 (beilstein handbook reference)
unii-3j928617dw
3j928617dw ,
zimeldinum
hsdb 7697
2-propen-1-amine, 3-(4-bromophenyl)-n,n-dimethyl-3-(3-pyridinyl)-
BRD-K94173644-300-01-3
SCHEMBL35029
zimeldine [inn]
zimeldine [hsdb]
zimeldine [mi]
zimeldine [who-dd]
(z)-3-(1-(p-bromophenyl)-3-(dimethylamino)propenyl)pyridine
n,n-dimethyl-3-(3-pyridyl)-3-(4-bromophenyl)prop-2-enamine (zimelidine)
n,n-dimethyl-3-(3-pyridyl)-3-(4-bromophenyl)prop-2-enamine
OYPPVKRFBIWMSX-SXGWCWSVSA-N
zimelidinedihydrochloride
AKOS025118603
a-23140
(z)-3-(4-bromophenyl)-n,n-dimethyl-3-(3-pyridinyl)-2-propen-1-amine
CHEBI:92824
SBI-0051246.P002
DTXSID6048462
Q203483
SDCCGSBI-0051246.P003
NCGC00025286-07
EN300-21042894
[(2z)-3-(4-bromophenyl)-3-(pyridin-3-yl)prop-2-en-1-yl]dimethylamine
CS-0068635
HY-118835
BRD-K47207162-312-02-2
tocris-1767
NCGC00025286-01
NCGC00014683-02
lopac-z-101
PRESTWICK3_000092
NCGC00014683
BSPBIO_000044
BPBIO1_000050
AB00514675
NCGC00097786-01
CHEMBL354646
zimelidine (z-isomer)
zimelidine (e-isomer)
SCHEMBL11289888
NCGC00014683-03
AKOS015891576
(e)-3-(4-bromophenyl)-n,n-dimethyl-3-pyridin-3-ylprop-2-en-1-amine;hydrate;hydrochloride
(e)-3-(4-bromophenyl)-n,n-dimethyl-3-(3-pyridinyl)-2-propen-1-amine;hydrate;hydrochloride
bdbm66978
cid_24871308
[(e)-3-(4-bromophenyl)-3-(3-pyridyl)allyl]-dimethyl-amine;hydrate;hydrochloride
(e)-3-(4-bromophenyl)-n,n-dimethyl-3-pyridin-3-yl-prop-2-en-1-amine;hydrate;hydrochloride
56775-89-4
(e)-3-(4-bromophenyl)-n,n-dimethyl-3-(3-pyridyl) allylamine
(2e)-3-(4-bromophenyl)-n,n-dimethyl-3-(3-pyridinyl)-2-propen-1-amine
DTXSID001160540

Research Excerpts

Overview

Zimeldine is a selective serotonin reuptake blocker, which according to studies in humans and animals, has no serious cardiovascular side effects in therapeutic doses.

ExcerptReferenceRelevance
"Zimeldine is a selective 5-HT reuptake inhibitor based on the "chemical lead" of brompheniramine--an antihistamine with some 5-HT reuptake inhibitory properties."( The research and development of a 5-HT selective reuptake blocker. Preclinical aspects.
Agurell, S, 1983
)
0.99
"that zimeldine is an effective antidepressant)."( The new antidepressant zimeldine in general practice. A surveillance study of 15,000 patients.
Fünfgeld, EW, 1983
)
1.03
"Zimeldine is a selective serotonin reuptake blocker, which according to studies in humans and animals, has no serious cardiovascular side effects in therapeutic doses."( Torsade de pointes tachycardias induced by overdosage of zimeldine.
Edvardsson, N; Liljeqvist, JA, 1989
)
1.24

Actions

ExcerptReferenceRelevance
"Zimeldine did not enhance the effects of ethanol; it even showed some antagonism of ethanol-induced body sway in the standing steadiness test."( Effects of zimeldine, mianserin and amitriptyline on psychomotor skills and their interaction with ethanol a placebo controlled cross-over study.
Bergman, I; Seppälä, T; Strömberg, C, 1984
)
1.38

Treatment

Zimeldine treatment in lesioned rats gave a significant additional 50% increase in waking the first 2 h and a corresponding decrease in total slow wave sleep. Treatment during 3 consecutive days induced in both helpless and control rats, a decrease in the inhibitory response of serotonergic neurons to the citalopram challenge.

ExcerptReferenceRelevance
"The zimeldine treatment group had significantly lower mean HAM-D scale total scores than the placebo and imipramine groups at week 4 and last available assessment."( A double-blind, controlled evaluation of zimeldine, imipramine and placebo in patients with primary affective disorders.
Feighner, JP; Merideth, CH, 1983
)
1.01
"Zimeldine treatment in lesioned rats gave a significant additional 50% increase in waking the first 2 h and a corresponding decrease in total slow wave sleep, suggesting a potentiation of these effects."( Lesion of descending 5-HT pathways increases zimeldine-induced waking in rats.
Bjorvatn, B; Bjørkum, AA; Neckelmann, D; Ursin, R, 1995
)
1.27
"Treatment with zimeldine during 3 consecutive days induced in both helpless and control rats, a decrease in the inhibitory response of serotonergic neurons to the citalopram challenge, which resulted in a normalization of the neuronal reactivity in the helpless group (ED50 = 0.31 +/- 0.03 mg/kg IV)."( Antidepressant treatment in helpless rats: effect on the electrophysiological activity of raphe dorsalis serotonergic neurons.
Adrien, J; Dangoumau, L; Hamon, M; Martin, P; Maudhuit, C; Prévot, E, 1997
)
0.64

Toxicity

ExcerptReferenceRelevance
" In Sweden, the combined use of spontaneous adverse drug reaction (ADR) reporting data and different registers has yielded much valuable information on safety problems with different drugs."( Regulatory decisions. Emphasis on safety issues.
Strandberg, K; Wiholm, BE, 1986
)
0.27
"The side effect profile and safety of fluoxetine are reviewed."( The side effect profile and safety of fluoxetine.
Wernicke, JF, 1985
)
0.27
" The reasons for termination were mainly ineffectiveness of the drug and adverse reactions."( The safety of zimeldine in long-term use in depressive illness.
Arberg-Wistedt, A; Jozwiak, H; Nyström, C; von Knorring, L; Wålinder, J, 1983
)
0.63
" Zimeldine was launched in the international market but had to be withdrawn when it caused severe unexpected adverse reactions."( Problems with toxicity studies in the assessment of new drugs.
Werkö, L, 1993
)
1.2
"Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites."( Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
Jones, LH; Nadanaciva, S; Rana, P; Will, Y, 2016
)
0.43

Pharmacokinetics

ExcerptReferenceRelevance
" The plasma half-life of zimeldine was also significantly longer in the chronically liver damaged patients."( Pharmacokinetics of zimeldine in male alcoholics.
Alling, C; Gottfries, CG; Grind, M; Lundström, J, 1986
)
0.9
" Blood samples were collected on day 5 for pharmacokinetic analysis of temazepam."( A study of the effects of zimelidine on the pharmacokinetics and pharmacodynamics of temazepam in healthy volunteers.
Fagan, D; Scott, DB; Tiplady, B, 1984
)
0.27
"To evaluate the clinical efficacy, tolerance and pharmacokinetic properties of zimelidine in elderly people, twelve hospitalized depressed patients with a mean age of 80 years were included in a clinical trial."( Zimelidine to geriatric patients: a pharmacokinetic and clinical study.
Björnsson, G; Dehlin, O; Lundström, J, 1981
)
0.26

Compound-Compound Interactions

ExcerptReferenceRelevance
"Sleep and waking stages in cats were studied 8 h following administration of zimeldine and alaproclate, in combination with saline or 5-hydroxy-1-tryptophan (5-HTP)."( The effects of zimeldine and alaproclate combined with a small dose of 5-HTP on waking and sleep stages in cats.
Sommerfelt, L; Ursin, R, 1987
)
0.85

Bioavailability

ExcerptReferenceRelevance
"The possible influence of concomitant food intake on the bioavailability of the novel antidepressant zimeldine and its active metabolite norzimeldine was assessed in ten healthy female volunteers, who ingested a single dose of 200 mg zimeldine on an empty stomach and together with a standardized breakfast of 1 840 kJ."( Influence of food intake on the bioavailability of zimeldine and its active metabolite, norzimeldine.
Melander, A; Wahlén, A; Wåhlin-Boll, E; Westerlund, D, 1983
)
0.73
" The results obtained may indicate a reduction in the rate of metabolism for zimelidine in the elderly, possibly combined with increased total bioavailability of the drug."( Zimelidine to geriatric patients: a pharmacokinetic and clinical study.
Björnsson, G; Dehlin, O; Lundström, J, 1981
)
0.26
" It appears that zimelidine is completely absorbed from the gastrointestinal tract and "first-pass metabolism" in the liver reduces the bioavailability to 50%."( Pharmacokinetics of zimelidine in humans--plasma levels and urinary excretion of zimelidine and norzimelidine after intravenous and oral administration of zimelidine.
Chaturvedi, S; Love, BL; Moore, RG; Thomas, J, 1981
)
0.26

Dosage Studied

Zimeldine can be administered in a once daily dosage regimen to elderly patients, but they should be given a lower dose than younger patients. The dosage of both zimeldin and alaproclate was 200 mg daily.

ExcerptRelevanceReference
" The primary adverse events associated with serotonin reuptake inhibitors involve the gastrointestinal system, although side effects may be less frequent at lower dosage levels."( Clinical overview of serotonin reuptake inhibitors.
Rickels, K; Schweizer, E, 1990
)
0.28
" The dosage of both zimeldine and alaproclate was 200 mg daily."( Alaproclate a novel antidepressant? A biochemical and clinical comparison with zimeldine.
Aberg-Wistedt, A; Alvariza, M; Bertilsson, L; Malmgren, R; Wachtmeister, H, 1985
)
0.82
"The sensitivity of neurones in the cingulate cortex of the rat to iontophoretically applied substance P (SP) was tested one hour after a single dose of various antidepressant drugs and also 1 day following the termination of a chronic dosing schedule (14 once daily injections) of the same agents."( An increase in sensitivity of rat cingulate cortical neurones to substance P occurs following withdrawal of chronic administration of antidepressant drugs.
Jones, RS; Olpe, HR, 1984
)
0.27
" The dosage was flexible, maintenance doses varying between 50-150 mg in the amitriptyline group and 50-300 mg in the zimelidine group."( A double-blind comparison of zimelidine and amitriptyline in depressive out-patients.
Lehtinen, V; Salminen, J; Syvälahti, E, 1982
)
0.26
" An initial dosage of 150 mg/day was used for up to 6 weeks."( Zimelidine: a placebo-controlled trial in depression.
Burrows, GD; Davies, BM; Marriott, PF; McIntyre, IM; Moore, RG; Norman, TR, 1983
)
0.27
" Dosage range was 75-300 mg/day for active medications."( A double-blind evaluation of zimelidine in comparison to placebo and amitriptyline in patients with major depressive disorder.
Behrnetz, S; Bush, DF; Claghorn, J; Gershon, S; Goldstein, BJ; Huitfeldt, B, 1983
)
0.27
" The results suggest that zimeldine can be administered in a once daily dosage regimen to elderly patients, but they should be given a lower dose than younger patients."( Zimeldine to geriatric patients in once daily dosage. A pharmacokinetic and clinical study.
Björnson, G; Dehlin, O; Lundström, J; Nörgård, J, 1984
)
2.01
" Dosage range was 75-300 mg/day for active medications, and the scheduled treatment period was 4 weeks."( Zimeldine tolerability in comparison to amitriptyline and placebo: findings from a multicentre trial.
Claghorn, J; Gershon, S; Goldstein, BJ, 1983
)
1.71
"The acute interaction of zimelidine (Z) with ethanol (E) was examined in six healthy men aged 20 to 37 yr who randomly received each of four treatments 1 wk apart: Z, 200 mg by mouth, preceded by 1 hr and followed for 7 hr of oral E in juice dosed to maintain blood alcohol concentrations between 800 and 1000 mg/l; placebo Z and E; Z and juice; and placebo Z and juice."( Acute kinetic and dynamic interactions of zimelidine with ethanol.
Hamilton, C; Kaplan, HL; Khouw, V; Naranjo, CA; Sellers, EM, 1984
)
0.27
" With the applied, probably suboptimal, dosage the therapeutic response was only satisfactory in five cases."( Plasma levels of zimelidine and norzimelidine in endogenous depression.
Hansen, LB; Hvidberg, EF; Larsen, NE; Thomsen, IS; Vestergård, P, 1980
)
0.26
" These three dosage schedules were studied."( Zimelidine: comparison of different dosage regimes in general practice.
Tiplady, B; Watson, JM, 1981
)
0.26
" Blood and urine samples were collected for a period of 28 hours after dosing and the concentrations of zimelidine and norzimelidine determined."( Pharmacokinetics of zimelidine in humans--plasma levels and urinary excretion of zimelidine and norzimelidine after intravenous and oral administration of zimelidine.
Chaturvedi, S; Love, BL; Moore, RG; Thomas, J, 1981
)
0.26
" Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process."( Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential.
Gehlhaar, D; Greene, N; Johnson, TO; Pelletier, DJ; Tilloy-Ellul, A,
)
0.13
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
0.37
" However, the intermingling of science and commerce also strained the relationship between scientific and commercial priorities further along the trajectory of the drug; for example, concerning issues such as dosage strategy and drug use in primary care, where corporate management allegedly took decisions contrary to the recommendations of both academic and company scientists."( Divergence and convergence of commercial and scientific priorities in drug development: The case of Zelmid, the first SSRI antidepressant.
Mulinari, S, 2015
)
0.42
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
styrenes
[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 (42)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency1.77830.100020.879379.4328AID588453
regulator of G-protein signaling 4Homo sapiens (human)Potency21.19230.531815.435837.6858AID504845
arylsulfatase AHomo sapiens (human)Potency0.00541.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency11.22020.035520.977089.1251AID504332
D(1A) dopamine receptorHomo sapiens (human)Potency7.59110.02245.944922.3872AID488982; AID488983
chromobox protein homolog 1Homo sapiens (human)Potency0.00600.006026.168889.1251AID488953
Ataxin-2Homo sapiens (human)Potency5.01190.011912.222168.7989AID588378
15-lipoxygenase, partialHomo sapiens (human)Potency10.60580.012610.691788.5700AID887
NFKB1 protein, partialHomo sapiens (human)Potency3.54810.02827.055915.8489AID895; AID928
TDP1 proteinHomo sapiens (human)Potency29.85540.000811.382244.6684AID686978
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency1.25890.00137.762544.6684AID914; AID915
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency4.41070.00207.533739.8107AID891
cytochrome P450 2C19 precursorHomo sapiens (human)Potency14.55000.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency5.01190.00636.904339.8107AID883
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency7.17440.031610.279239.8107AID884; AID885
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency17.03900.00106.000935.4813AID943; AID944
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency7.17441.000012.224831.6228AID885
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency11.07920.316212.765731.6228AID881
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency7.17441.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency7.17441.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency7.17441.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency7.17441.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency7.17441.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency7.17441.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency7.17441.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency7.17441.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency7.17441.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency7.17441.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency8.47900.00638.235039.8107AID881; AID883
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency7.17441.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency7.17441.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency7.17441.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency7.17441.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency7.17441.000012.224831.6228AID885
[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)229.70000.11007.190310.0000AID1449628
DRattus norvegicus (Norway rat)IC50 (µMol)4.50000.00030.50267.7625AID179927
D(3) dopamine receptorRattus norvegicus (Norway rat)IC50 (µMol)4.50000.00030.39075.4000AID179927
D(1B) dopamine receptorRattus norvegicus (Norway rat)IC50 (µMol)4.50000.00030.35635.4000AID179927
D(4) dopamine receptorRattus norvegicus (Norway rat)IC50 (µMol)4.50000.00030.38715.4000AID179927
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)IC50 (µMol)4.50000.00030.81978.4900AID179927
D(2) dopamine receptorRattus norvegicus (Norway rat)IC50 (µMol)4.50000.00010.54948.4000AID179927
TransporterRattus norvegicus (Norway rat)IC50 (µMol)4.50000.00081.95628.8000AID179927
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (49)

Processvia Protein(s)Taxonomy
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)
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)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (18)

Processvia Protein(s)Taxonomy
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)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
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)
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)
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)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (97)

Assay IDTitleYearJournalArticle
AID132672In vitro inhibition of the accumulation of (-)-[3H]Norepinephrine in slices from the middle part of the mouse brain.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Homoallylic amines related to zimeldine. A comparative study on neuronal serotonin and norepinephrine reuptake based on conformational analysis.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID681116TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing MDCKII cells2002The Journal of pharmacology and experimental therapeutics, Dec, Volume: 303, Issue:3
Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs.
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID1636400Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 80.2 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of N2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID232042Selectivity expressed as ratio between NE and 5-HT uptake inhibition in rat synaptosomes1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Homoallylic amines related to zimeldine. A comparative study on neuronal serotonin and norepinephrine reuptake based on conformational analysis.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID132670In vitro inhibition of the accumulation of (-)-[3H]-5-HT in slices from the middle part of the mouse brain1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Homoallylic amines related to zimeldine. A comparative study on neuronal serotonin and norepinephrine reuptake based on conformational analysis.
AID179927Inhibition of 5-HT uptake in synaptosomal preparation from rat corpus striatum, using [3H]5-HT1984Journal of medicinal chemistry, Nov, Volume: 27, Issue:11
Nontricyclic antidepressant agents derived from cis- and trans-1-amino-4-aryltetralins.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
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.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID232041Selectivity expressed as ratio between NE and 5-HT uptake inhibition in mouse brain slices1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Homoallylic amines related to zimeldine. A comparative study on neuronal serotonin and norepinephrine reuptake based on conformational analysis.
AID679751TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: ? uM, Zimeldine: 100 uM) in MDR1-expressing MDCKII cells2002The Journal of pharmacology and experimental therapeutics, Dec, Volume: 303, Issue:3
Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID540237Phospholipidosis-positive literature compound observed in rat
AID179960Inhibition of dopamine uptake in synaptosomal preparation in rat corpus striatum, using [3H]dopamine1984Journal of medicinal chemistry, Nov, Volume: 27, Issue:11
Nontricyclic antidepressant agents derived from cis- and trans-1-amino-4-aryltetralins.
AID179973Inhibition of norepinephrine uptake in synaptosomal preparation fro rat hypothalamus, using [3H]norepinephrine1984Journal of medicinal chemistry, Nov, Volume: 27, Issue:11
Nontricyclic antidepressant agents derived from cis- and trans-1-amino-4-aryltetralins.
AID1636510Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 210.8 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of 2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID179753In vitro inhibition of the accumulation of (-)-[3H]Norepinephrine in synaptosomes from the rat brain cortex1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Homoallylic amines related to zimeldine. A comparative study on neuronal serotonin and norepinephrine reuptake based on conformational analysis.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
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.
AID179752In vitro inhibition of the accumulation of (-)-[3H]-5-HT in synaptosomes from the rat brain cortex1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Homoallylic amines related to zimeldine. A comparative study on neuronal serotonin and norepinephrine reuptake based on conformational analysis.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID132433Ex vivo inhibition of the accumulation of (-)-[3H]Norepinephrine in slices from the middle part of the mouse brain. (i.p.)1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Homoallylic amines related to zimeldine. A comparative study on neuronal serotonin and norepinephrine reuptake based on conformational analysis.
AID540239Phospholipidosis-positive literature compound observed in dog
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.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID132666In vitro inhibition of accumulation of [14C]5-HT (5-HT) in mouse brain slices1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis of pyridylallylamines related to zimelidine and their inhibition of neuronal monoamine uptake.
AID132432Ex vivo inhibition of the accumulation of (-)-[3H]-5-HT in slices from the middle part of the mouse brain. (i.p.)1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Homoallylic amines related to zimeldine. A comparative study on neuronal serotonin and norepinephrine reuptake based on conformational analysis.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID130700In vivo inhibition of accumulation of [14C]5-HT (5-HT) in mouse brain slices after intraperitoneal administration1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis of pyridylallylamines related to zimelidine and their inhibition of neuronal monoamine uptake.
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.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID625276FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
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.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID130699In vivo inhibition of accumulation of (-)-[3H]Norepinephrine (NA) in mouse brain slices after intraperitoneal administration1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis of pyridylallylamines related to zimelidine and their inhibition of neuronal monoamine uptake.
AID1636459Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 129.2 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of 2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID132665In vitro inhibition of accumulation of (-)-[3H]Norepinephrine (NA) in mouse brain slices1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis of pyridylallylamines related to zimelidine and their inhibition of neuronal monoamine uptake.
AID625293Drug Induced Liver Injury Prediction System (DILIps) validation dataset; compound DILI positive/negative as observed in LTKB-BD2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1508628Confirmatory 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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
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.
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.
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.
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.
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.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508628Confirmatory 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.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID132666In vitro inhibition of accumulation of [14C]5-HT (5-HT) in mouse brain slices1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis of pyridylallylamines related to zimelidine and their inhibition of neuronal monoamine uptake.
AID132432Ex vivo inhibition of the accumulation of (-)-[3H]-5-HT in slices from the middle part of the mouse brain. (i.p.)1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Homoallylic amines related to zimeldine. A comparative study on neuronal serotonin and norepinephrine reuptake based on conformational analysis.
AID130700In vivo inhibition of accumulation of [14C]5-HT (5-HT) in mouse brain slices after intraperitoneal administration1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis of pyridylallylamines related to zimelidine and their inhibition of neuronal monoamine uptake.
AID232041Selectivity expressed as ratio between NE and 5-HT uptake inhibition in mouse brain slices1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Homoallylic amines related to zimeldine. A comparative study on neuronal serotonin and norepinephrine reuptake based on conformational analysis.
AID130699In vivo inhibition of accumulation of (-)-[3H]Norepinephrine (NA) in mouse brain slices after intraperitoneal administration1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis of pyridylallylamines related to zimelidine and their inhibition of neuronal monoamine uptake.
AID318872Inhibition of cruzain in presence of 0.01% Triton X-1002008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Comprehensive mechanistic analysis of hits from high-throughput and docking screens against beta-lactamase.
AID132665In vitro inhibition of accumulation of (-)-[3H]Norepinephrine (NA) in mouse brain slices1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis of pyridylallylamines related to zimelidine and their inhibition of neuronal monoamine uptake.
AID132433Ex vivo inhibition of the accumulation of (-)-[3H]Norepinephrine in slices from the middle part of the mouse brain. (i.p.)1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Homoallylic amines related to zimeldine. A comparative study on neuronal serotonin and norepinephrine reuptake based on conformational analysis.
AID318868Inhibition of chymotrypsin in presence of 0.1% Triton X-1002008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Comprehensive mechanistic analysis of hits from high-throughput and docking screens against beta-lactamase.
AID232042Selectivity expressed as ratio between NE and 5-HT uptake inhibition in rat synaptosomes1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Homoallylic amines related to zimeldine. A comparative study on neuronal serotonin and norepinephrine reuptake based on conformational analysis.
AID318869Inhibition of malate dehydrogenase2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Comprehensive mechanistic analysis of hits from high-throughput and docking screens against beta-lactamase.
AID179753In vitro inhibition of the accumulation of (-)-[3H]Norepinephrine in synaptosomes from the rat brain cortex1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Homoallylic amines related to zimeldine. A comparative study on neuronal serotonin and norepinephrine reuptake based on conformational analysis.
AID318870Inhibition of malate dehydrogenase in presence of 0.1% Triton X-1002008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Comprehensive mechanistic analysis of hits from high-throughput and docking screens against beta-lactamase.
AID318866Inhibition of beta-lactamase AmpC in presence of 0.1% Triton X-1002008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Comprehensive mechanistic analysis of hits from high-throughput and docking screens against beta-lactamase.
AID318865Inhibition of beta-lactamase AmpC2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Comprehensive mechanistic analysis of hits from high-throughput and docking screens against beta-lactamase.
AID132671In vitro inhibition of the accumulation of (-)-[3H]-5-HT in slices from the middle part of the mouse brain.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Homoallylic amines related to zimeldine. A comparative study on neuronal serotonin and norepinephrine reuptake based on conformational analysis.
AID132672In vitro inhibition of the accumulation of (-)-[3H]Norepinephrine in slices from the middle part of the mouse brain.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Homoallylic amines related to zimeldine. A comparative study on neuronal serotonin and norepinephrine reuptake based on conformational analysis.
AID318871Inhibition of cruzain2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Comprehensive mechanistic analysis of hits from high-throughput and docking screens against beta-lactamase.
AID179752In vitro inhibition of the accumulation of (-)-[3H]-5-HT in synaptosomes from the rat brain cortex1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Homoallylic amines related to zimeldine. A comparative study on neuronal serotonin and norepinephrine reuptake based on conformational analysis.
AID318867Inhibition of chymotrypsin2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Comprehensive mechanistic analysis of hits from high-throughput and docking screens against beta-lactamase.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (470)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990344 (73.19)18.7374
1990's82 (17.45)18.2507
2000's24 (5.11)29.6817
2010's15 (3.19)24.3611
2020's5 (1.06)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 22.45

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index22.45 (24.57)
Research Supply Index6.38 (2.92)
Research Growth Index4.16 (4.65)
Search Engine Demand Index29.35 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (22.45)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials99 (20.20%)5.53%
Trials0 (0.00%)5.53%
Reviews29 (5.92%)6.00%
Reviews0 (0.00%)6.00%
Case Studies23 (4.69%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other339 (69.18%)84.16%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]