Page last updated: 2024-12-05

n-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-n-(2-pyridinyl)cyclohexanecarboxamide

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

Cross-References

ID SourceID
PubMed CID5684
CHEMBL ID31354
CHEBI ID125619
SCHEMBL ID84178
MeSH IDM0238906

Synonyms (50)

Synonym
HY-10349
gtpl80
gtpl3251
n-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-n-pyridin-2-ylcyclohexanecarboxamide-tritiated
[3h]way100635
way-100635 ,
lopac-w-108
NCGC00016092-01
LOPAC0_001229
PDSP1_001716
PDSP2_001699
NCGC00162372-01
cyclohexanecarboxamide, n-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-n-2-pyridinyl-
162760-96-5
way100635
way-100,635
CHEBI:125619
NCGC00016092-03
CHEMBL31354 ,
L000012
cyclohexanecarboxamide, n-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-n-2-pyridinyl-
n-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-n-pyridin-2-ylcyclohexanecarboxamide
CCG-205303
cas_146714-97-8
bdbm86708
nsc_104911
71ih826feg ,
rec 0/0277
unii-71ih826feg
NCGC00016092-02
n-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-n-(pyridin-2-yl)cyclohexanecarboxamide
634908-75-1
CS-0418
SCHEMBL84178
DTXSID20167467
EX-A1053
AKOS027313833
AS-74088
NCGC00016092-13
n-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-n-2-pyridinyl-cyclohexanecarboxamide trihydrochloride
n-(2-(4-(2-methoxyphenyl)piperazin-1-yl)ethyl)-n-(pyridin-2-yl)cyclohexanecarboxamide
FT-0728251
Q7946879
SB19513
SDCCGSBI-0051196.P002
NCGC00016092-14
E77981
A925015
WFA71497
n-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-n-2-pyridinylcyclohexanecarboxamide

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" Of these, 35, which showed the highest oral bioavailability in vivo in rats, was resolved into its two isomers 36 and 37."( Improvement in the selectivity and metabolic stability of the serotonin 5-HT(1A) ligand, S 15535: a series of cis- and trans-2-(arylcycloalkylamine) 1-indanols.
Bertrand, M; Charlot, V; Dekeyne, A; Despaux, N; Genissel, P; Giraud, H; Goument, B; Millan, MJ; Newman-Tancredi, A; Nisole, C; Peglion, JL, 2002
)
0.31
" SAR studies, driven primarily by in vitro liver microsomal stability assessment, identified compound 10b, which displayed improved oral bioavailability and lower intrinsic clearance."( The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists.
Abou-Gharbia, MA; Adedoyin, A; Andree, TH; Aschmies, SH; Asselin, M; Bach, AC; Beyer, C; Bicksler, JJ; Childers, WE; Chong, DC; Comery, TA; Day, M; Grauer, SM; Grosu, GT; Harrison, BL; Havran, LM; Hirst, WD; Hughes, ZA; Huselton, C; Kagan, N; Kleintop, T; Magolda, R; Marathias, V; Platt, B; Pulicicchio, C; Robichaud, AJ; Rosenzweig-Lipson, S; Sabb, AL; Shen, Z; Smith, DE; Sukoff-Rizzo, SJ; Sullivan, KM; Zhang, MY, 2010
)
0.36
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
piperazines
[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 (38)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency4.53390.100020.879379.4328AID588453; AID588456
ATAD5 protein, partialHomo sapiens (human)Potency14.57500.004110.890331.5287AID493106
thyroid stimulating hormone receptorHomo sapiens (human)Potency39.81070.001318.074339.8107AID926
regulator of G-protein signaling 4Homo sapiens (human)Potency8.43680.531815.435837.6858AID504845
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency31.62280.00207.533739.8107AID891
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency3.98110.031610.279239.8107AID884; AID885
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency19.95260.00106.000935.4813AID944
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
[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)
5-hydroxytryptamine receptor 1AHomo sapiens (human)IC50 (µMol)0.00550.00010.666410.0000AID1409504; AID1704733; AID481371; AID597282
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki0.00080.00010.532610.0000AID1555771; AID1593198; AID339531; AID3803; AID3836; AID3922; AID408275; AID408276; AID422848; AID441123; AID481370; AID510391; AID597282; AID597314
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.05380.00010.949010.0000AID37309; AID510388
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)0.00420.00031.38338.4000AID1854988
D(4) dopamine receptorHomo sapiens (human)Ki0.01600.00000.436210.0000AID597310
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.08900.00000.575110.0000AID37309
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.00460.00000.360910.0000AID1555770; AID1593197; AID510390
5-hydroxytryptamine receptor 1BHomo sapiens (human)Ki0.02400.00010.54859.2100AID597315
Sodium-dependent serotonin transporterHomo sapiens (human)IC50 (µMol)4.50000.00010.86458.7096AID204069
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Ki0.66690.00000.705610.0000AID204533; AID408276
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki10.00000.00030.380610.0000AID597312
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.01900.00000.272610.0000AID1555768; AID1593195; AID510388; AID597313
Alpha-1B adrenergic receptorHomo sapiens (human)Ki0.13010.00000.471310.0000AID1555769; AID1593196; AID510389; AID597311
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.08900.00000.965010.0000AID37309
Sodium-dependent dopamine transporter Homo sapiens (human)Ki0.00030.00021.11158.0280AID6433
5-hydroxytryptamine receptor 1DMus musculus (house mouse)Ki0.00070.00033.333810.0000AID6432; AID6433
[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)
5-hydroxytryptamine receptor 1AHomo sapiens (human)EC50 (µMol)0.00710.00010.25718.0000AID3510; AID3513
5-hydroxytryptamine receptor 1AHomo sapiens (human)Kd0.00020.00010.95285.0119AID1854976
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)EC50 (µMol)0.00710.00132.612925.7000AID3513
D(4) dopamine receptorHomo sapiens (human)Kd0.00240.00020.00320.0050AID1854984
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 1AHomo sapiens (human)Kb0.00010.00000.00490.0271AID1393526
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (140)

Processvia Protein(s)Taxonomy
behavioral fear response5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
gamma-aminobutyric acid signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of serotonin secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of vasoconstriction5-hydroxytryptamine receptor 1AHomo sapiens (human)
exploration behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of dopamine metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of hormone secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1AHomo sapiens (human)
positive regulation of MAP kinase activityD(4) dopamine receptorHomo sapiens (human)
behavioral fear responseD(4) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(4) dopamine receptorHomo sapiens (human)
response to amphetamineD(4) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(4) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
dopamine receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
adult locomotory behaviorD(4) dopamine receptorHomo sapiens (human)
positive regulation of sodium:proton antiporter activityD(4) dopamine receptorHomo sapiens (human)
positive regulation of kinase activityD(4) dopamine receptorHomo sapiens (human)
response to histamineD(4) dopamine receptorHomo sapiens (human)
social behaviorD(4) dopamine receptorHomo sapiens (human)
regulation of dopamine metabolic processD(4) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(4) dopamine receptorHomo sapiens (human)
fear responseD(4) dopamine receptorHomo sapiens (human)
regulation of circadian rhythmD(4) dopamine receptorHomo sapiens (human)
positive regulation of MAP kinase activityD(4) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(4) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(4) dopamine receptorHomo sapiens (human)
rhythmic processD(4) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(4) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(4) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(4) dopamine receptorHomo sapiens (human)
inhibitory postsynaptic potentialD(4) dopamine receptorHomo sapiens (human)
regulation of postsynaptic neurotransmitter receptor internalizationD(4) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(4) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerD(4) dopamine receptorHomo sapiens (human)
chemical synaptic transmissionD(4) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-1D adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1D adrenergic receptorHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 1BHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of gamma-aminobutyric acid secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of serotonin secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of synaptic transmission, GABAergic5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to cocaine5-hydroxytryptamine receptor 1BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 1BHomo sapiens (human)
drinking behavior5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to ethanol5-hydroxytryptamine receptor 1BHomo sapiens (human)
bone remodeling5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to mineralocorticoid5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to alkaloid5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to xenobiotic stimulus5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 1BHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentration5-hydroxytryptamine receptor 1BHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferation5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of synaptic vesicle exocytosis5-hydroxytryptamine receptor 1BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1BHomo sapiens (human)
monoamine transportSodium-dependent serotonin transporterHomo sapiens (human)
response to hypoxiaSodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transportSodium-dependent serotonin transporterHomo sapiens (human)
response to nutrientSodium-dependent serotonin transporterHomo sapiens (human)
memorySodium-dependent serotonin transporterHomo sapiens (human)
circadian rhythmSodium-dependent serotonin transporterHomo sapiens (human)
response to xenobiotic stimulusSodium-dependent serotonin transporterHomo sapiens (human)
response to toxic substanceSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of gene expressionSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of serotonin secretionSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of cerebellar granule cell precursor proliferationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of synaptic transmission, dopaminergicSodium-dependent serotonin transporterHomo sapiens (human)
response to estradiolSodium-dependent serotonin transporterHomo sapiens (human)
social behaviorSodium-dependent serotonin transporterHomo sapiens (human)
vasoconstrictionSodium-dependent serotonin transporterHomo sapiens (human)
sperm ejaculationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of neuron differentiationSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of cell cycleSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of organ growthSodium-dependent serotonin transporterHomo sapiens (human)
behavioral response to cocaineSodium-dependent serotonin transporterHomo sapiens (human)
enteric nervous system developmentSodium-dependent serotonin transporterHomo sapiens (human)
brain morphogenesisSodium-dependent serotonin transporterHomo sapiens (human)
serotonin uptakeSodium-dependent serotonin transporterHomo sapiens (human)
membrane depolarizationSodium-dependent serotonin transporterHomo sapiens (human)
platelet aggregationSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to retinoic acidSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to cGMPSodium-dependent serotonin transporterHomo sapiens (human)
regulation of thalamus sizeSodium-dependent serotonin transporterHomo sapiens (human)
conditioned place preferenceSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion transmembrane transportSodium-dependent serotonin transporterHomo sapiens (human)
amino acid transportSodium-dependent serotonin transporterHomo sapiens (human)
smooth muscle contraction5-hydroxytryptamine receptor 7Homo sapiens (human)
circadian rhythm5-hydroxytryptamine receptor 7Homo sapiens (human)
blood circulation5-hydroxytryptamine receptor 7Homo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 7Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 7Homo sapiens (human)
MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
apoptotic processAlpha-1A adrenergic receptorHomo sapiens (human)
smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
activation of phospholipase C activityAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1A adrenergic receptorHomo sapiens (human)
adult heart developmentAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of cell population proliferationAlpha-1A adrenergic receptorHomo sapiens (human)
response to xenobiotic stimulusAlpha-1A adrenergic receptorHomo sapiens (human)
response to hormoneAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of autophagyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of action potentialAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
calcium ion transport into cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
cell growth involved in cardiac muscle cell developmentAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase C signalingAlpha-1A adrenergic receptorHomo sapiens (human)
pilomotor reflexAlpha-1A adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-1B adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of cardiac muscle contractionAlpha-1B adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1B adrenergic receptorHomo sapiens (human)
monoamine transportSodium-dependent dopamine transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent dopamine transporter Homo sapiens (human)
lactationSodium-dependent dopamine transporter Homo sapiens (human)
sensory perception of smellSodium-dependent dopamine transporter Homo sapiens (human)
locomotory behaviorSodium-dependent dopamine transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent dopamine transporter Homo sapiens (human)
response to iron ionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine transportSodium-dependent dopamine transporter Homo sapiens (human)
adenohypophysis developmentSodium-dependent dopamine transporter Homo sapiens (human)
response to nicotineSodium-dependent dopamine transporter Homo sapiens (human)
positive regulation of multicellular organism growthSodium-dependent dopamine transporter Homo sapiens (human)
regulation of dopamine metabolic processSodium-dependent dopamine transporter Homo sapiens (human)
response to cocaineSodium-dependent dopamine transporter Homo sapiens (human)
dopamine biosynthetic processSodium-dependent dopamine transporter Homo sapiens (human)
dopamine catabolic processSodium-dependent dopamine transporter Homo sapiens (human)
response to ethanolSodium-dependent dopamine transporter Homo sapiens (human)
cognitionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent dopamine transporter Homo sapiens (human)
response to cAMPSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent dopamine transporter Homo sapiens (human)
prepulse inhibitionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine uptakeSodium-dependent dopamine transporter Homo sapiens (human)
hyaloid vascular plexus regressionSodium-dependent dopamine transporter Homo sapiens (human)
amino acid transportSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine transportSodium-dependent dopamine transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent dopamine transporter Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (36)

Processvia Protein(s)Taxonomy
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
receptor-receptor interaction5-hydroxytryptamine receptor 1AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(4) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activityD(4) dopamine receptorHomo sapiens (human)
protein bindingD(4) dopamine receptorHomo sapiens (human)
potassium channel regulator activityD(4) dopamine receptorHomo sapiens (human)
SH3 domain bindingD(4) dopamine receptorHomo sapiens (human)
dopamine bindingD(4) dopamine receptorHomo sapiens (human)
identical protein bindingD(4) dopamine receptorHomo sapiens (human)
metal ion bindingD(4) dopamine receptorHomo sapiens (human)
epinephrine bindingD(4) dopamine receptorHomo sapiens (human)
norepinephrine bindingD(4) dopamine receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityD(4) dopamine receptorHomo sapiens (human)
neurotransmitter receptor activityD(4) dopamine receptorHomo sapiens (human)
serotonin bindingD(4) dopamine receptorHomo sapiens (human)
protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
identical protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1D adrenergic receptorHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1BHomo sapiens (human)
voltage-gated calcium channel activity involved in regulation of presynaptic cytosolic calcium levels5-hydroxytryptamine receptor 1BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1BHomo sapiens (human)
integrin bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoatomic cation channel activitySodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
serotonin:sodium:chloride symporter activitySodium-dependent serotonin transporterHomo sapiens (human)
protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
antiporter activitySodium-dependent serotonin transporterHomo sapiens (human)
syntaxin-1 bindingSodium-dependent serotonin transporterHomo sapiens (human)
cocaine bindingSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion bindingSodium-dependent serotonin transporterHomo sapiens (human)
identical protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
nitric-oxide synthase bindingSodium-dependent serotonin transporterHomo sapiens (human)
actin filament bindingSodium-dependent serotonin transporterHomo sapiens (human)
serotonin bindingSodium-dependent serotonin transporterHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 7Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 7Homo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1B adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1B adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1B adrenergic receptorHomo sapiens (human)
protease bindingSodium-dependent dopamine transporter Homo sapiens (human)
signaling receptor bindingSodium-dependent dopamine transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent dopamine transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent dopamine transporter Homo sapiens (human)
protein bindingSodium-dependent dopamine transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent dopamine transporter Homo sapiens (human)
dopamine bindingSodium-dependent dopamine transporter Homo sapiens (human)
amine bindingSodium-dependent dopamine transporter Homo sapiens (human)
protein-containing complex bindingSodium-dependent dopamine transporter Homo sapiens (human)
metal ion bindingSodium-dependent dopamine transporter Homo sapiens (human)
protein phosphatase 2A bindingSodium-dependent dopamine transporter Homo sapiens (human)
heterocyclic compound bindingSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent dopamine transporter Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (33)

Processvia Protein(s)Taxonomy
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
centrosomeD(4) dopamine receptorHomo sapiens (human)
plasma membraneD(4) dopamine receptorHomo sapiens (human)
membraneD(4) dopamine receptorHomo sapiens (human)
postsynapseD(4) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(4) dopamine receptorHomo sapiens (human)
plasma membraneD(4) dopamine receptorHomo sapiens (human)
dendriteD(4) dopamine receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
endoplasmic reticulum5-hydroxytryptamine receptor 1BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
calyx of Held5-hydroxytryptamine receptor 1BHomo sapiens (human)
serotonergic synapse5-hydroxytryptamine receptor 1BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 1BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
focal adhesionSodium-dependent serotonin transporterHomo sapiens (human)
endosome membraneSodium-dependent serotonin transporterHomo sapiens (human)
endomembrane systemSodium-dependent serotonin transporterHomo sapiens (human)
presynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
membrane raftSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
postsynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
serotonergic synapseSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
neuron projectionSodium-dependent serotonin transporterHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
trans-Golgi network membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
synapse5-hydroxytryptamine receptor 7Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 7Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
nucleusAlpha-1A adrenergic receptorHomo sapiens (human)
nucleoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
caveolaAlpha-1A adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
nucleusAlpha-1B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
caveolaAlpha-1B adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
cytoplasmSodium-dependent dopamine transporter Homo sapiens (human)
plasma membraneSodium-dependent dopamine transporter Homo sapiens (human)
cell surfaceSodium-dependent dopamine transporter Homo sapiens (human)
membraneSodium-dependent dopamine transporter Homo sapiens (human)
axonSodium-dependent dopamine transporter Homo sapiens (human)
neuron projectionSodium-dependent dopamine transporter Homo sapiens (human)
neuronal cell bodySodium-dependent dopamine transporter Homo sapiens (human)
axon terminusSodium-dependent dopamine transporter Homo sapiens (human)
membrane raftSodium-dependent dopamine transporter Homo sapiens (human)
postsynaptic membraneSodium-dependent dopamine transporter Homo sapiens (human)
dopaminergic synapseSodium-dependent dopamine transporter Homo sapiens (human)
flotillin complexSodium-dependent dopamine transporter Homo sapiens (human)
axonSodium-dependent dopamine transporter Homo sapiens (human)
presynaptic membraneSodium-dependent dopamine transporter Homo sapiens (human)
plasma membraneSodium-dependent dopamine transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent dopamine transporter Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (203)

Assay IDTitleYearJournalArticle
AID1337900Analgesic activity in Swiss CD1 mouse assessed reduction in formalin-induced inflammatory pain by measuring reduction in time spent in licking or biting formalin injected hind paw at 3 mg/kg, ip pretreated for 30 mins followed by formalin injection measur
AID4418Compound was tested for inhibition constant against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes.1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Functional characteristics of a series of N4-substituted 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazines as 5-HT1A receptor ligands. Structure-activity relationships.
AID192922Ability to counteract the 8-OH-DPAT (1 mg/kg sc)-induced Hypothermia in rats (n=4) and evaluated for the decrease in body temperature (degrees Celsius) at 0.1(micro mol/kg)2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635.
AID481374Half life in human liver microsomes at 1 uM after 20 mins2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists.
AID597359Octanol-water partition coefficient, log D of the compound at pH 7.4 by HPLC analysis2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID1830042Displacement of [3H]5-CT from human recombinant 5-HT7A receptor expressed in HEK cells by radioligand completion assay2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Activity of
AID597306Inhibition of adrenergic Alpha-2C receptor at 10 uM2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID17425Biodistribution of the [11C]-radiolabeled compound in rat cerebellum1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Development of fluorine-18-labeled 5-HT1A antagonists.
AID239801Binding affinity for alpha 1d adrenoceptor2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses.
AID79314Ability to antagonize the 8-OH-DPAT-induced contractions of a strip of guinea pig ileum tissue2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635.
AID17427Biodistribution of the [11C]-radiolabeled compound in rat cortex1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Development of fluorine-18-labeled 5-HT1A antagonists.
AID597314Inhibition of 5HT1A receptor2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID1601988Induction of hypothermia in CD-1 mouse assessed as change in body temperature at 0.1 mg/kg, sc measured after 30 mins by thermometric method (Rvb <= 0.4 deg C)2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT
AID726708Ratio of drug level in brain to plasma at steady state in rat at 1000 ng/g after 5 hrs2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Discovery of novel α₁-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands.
AID510389Displacement [3H]prazosin of human recombinant Alpha-1B adrenergic receptor expressed in CHO cells by rapid filtration technique2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors.
AID1713196Inhibition of 8-OH-DPAT-induced hypothermia in Swiss albino mouse assessed as change in rectal body temperature at 0.3 mg/kg, sc pretreated with compound for 45 mins followed by 8-OH-DPAT challenge and measured after 45 min by thermometer (Rvb = -1.3 degr2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Synthesis and biological investigation of new equatorial (β) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile.
AID1517951Induction of hypothermia in CD-1 mouse assessed as change in body temperature at 0.1 mg/kg, ip measured after 120 mins by thermometric method (Rvb = -0.1 to 0.3 deg C)
AID597302Inhibition of adrenergic beta3 receptor at 10 uM2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID1713195Inhibition of 8-OH-DPAT-induced hypothermia in Swiss albino mouse assessed as change in rectal body temperature at 0.3 mg/kg, sc pretreated with compound for 45 mins followed by 8-OH-DPAT challenge and measured after 30 min by thermometer (Rvb = -1.7 degr2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Synthesis and biological investigation of new equatorial (β) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile.
AID37309Binding affinity against rat cortical alpha-1 adrenergic receptor labeled with [3H]prazosin radioligand2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines.
AID726716Efflux ratio of apparent permeability from basolateral to apical side over apical to basolateral side in human Caco2 cells at 1 to 20 uM2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Discovery of novel α₁-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands.
AID1593196Displacement of [3H]Prazosin from human recombinant alpha 1B adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay
AID1365313In-vivo 5-HT1A receptor antagonist activity in Swiss albino mouse assessed as reduction in 8-OH-DPAT-stimulated induction of lower lip retraction by measuring lower lip retraction score at 0.3 mg/kg, ip dosed 15 mins before test (Rvb = 2.875 +/- 0.08183 N2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
New 5-HT
AID3922Binding affinity at human 5-hydroxytryptamine 1A receptor by inhibition of [3H]8-OH-DPAT binding in Chinese hamster ovary cell line2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
Improvement in the selectivity and metabolic stability of the serotonin 5-HT(1A) ligand, S 15535: a series of cis- and trans-2-(arylcycloalkylamine) 1-indanols.
AID17429Biodistribution of the [11C]-radiolabeled compound in rat hippocampus1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Development of fluorine-18-labeled 5-HT1A antagonists.
AID239800Binding affinity for alpha 1b adrenoceptor2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses.
AID193028Ability to counteract the 8-OH-DPAT (1 mg/kg sc)-induced Hypothermia in rats (n=4) and evaluated for the decrease in body temperature (degrees Celsius) at 10(micro mol/kg)2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635.
AID481370Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists.
AID309503Effect on 8-OH-DPAT-induced lower lip retraction in Wistar rat at 0.1 mg/kg2007Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22
The influence of modifications in imide fragment structure on 5-HT(1A) and 5-HT(7) receptor affinity and in vivo pharmacological properties of some new 1-(m-trifluoromethylphenyl)piperazines.
AID597310Inhibition of dopamine D4 receptor2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID1517941Induction of hypothermia in CD-1 mouse assessed as change in body temperature at 0.1 mg/kg, ip measured after 60 mins by thermometric method (Rvb = -0.2 to 0.5 deg C)
AID597320Inhibition of adrenergic alpha2B receptor at 10 uM2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID226695In vitro affinity against 5-HT1B/1D receptor using [3H]5-HT in calf striatum2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635.
AID17428Biodistribution of the [11C]-radiolabeled compound in rat cortex co-injected with 50 nM of WAY 100635.1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Development of fluorine-18-labeled 5-HT1A antagonists.
AID1555769Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1B expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counter2019European journal of medicinal chemistry, Aug-15, Volume: 1761,3-Dioxane as a scaffold for potent and selective 5-HT
AID510388Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors.
AID6432Receptor-linked G protein activation at 5-hydroxytryptamine receptor was determined by measuring the stimulation of [35S]GTP-gamma-S, binding (Experiment 1)1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Development of fluorine-18-labeled 5-HT1A antagonists.
AID309481Decrease in body temperature in Swiss Albino mouse at 0.1 mg/kg after 90 mins2007Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22
The influence of modifications in imide fragment structure on 5-HT(1A) and 5-HT(7) receptor affinity and in vivo pharmacological properties of some new 1-(m-trifluoromethylphenyl)piperazines.
AID481372Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as maximal blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists.
AID87452Percent increase in the Forskolin-Stimulated cAMP formation, in HeLa cells transfected with the 5-HT 1A receptor at 1 uM concentration2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants.
AID231744Ratio of biodistribution of compound at cortex and cerebellum-1 in rat with 200 nmol of WAY 1006351999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Development of fluorine-18-labeled 5-HT1A antagonists.
AID1854976Binding affinity to 5-HT1A receptor (unknown origin) assessed as dissociation constant2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
AID87447Effect (1 uM) on Forskolin-Stimulated cAMP formation, in HeLa cells transfected with the 5-HT 1A receptor2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants.
AID597282Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in HEK293 EBNA cells after 1 hr by liquid scintillation counting2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID17431Biodistribution of the [11C]-radiolabeled compound in rat hypothalamus1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Development of fluorine-18-labeled 5-HT1A antagonists.
AID1517936Induction of hypothermia in CD-1 mouse assessed as change in body temperature at 0.1 mg/kg, ip measured after 30 mins by thermometric method (Rvb = -0.2 to 0.4 deg C)
AID1830038Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to control2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Activity of
AID3884Agonist efficacy of [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor compared to 5-HT2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
Improvement in the selectivity and metabolic stability of the serotonin 5-HT(1A) ligand, S 15535: a series of cis- and trans-2-(arylcycloalkylamine) 1-indanols.
AID597303Inhibition of adrenergic beta2 receptor at 10 uM2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID204533Binding affinity against serotonin transporter in rat cortical tissues using radioligand [3H]paroxetine2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines.
AID408276Displacement of [3H]WAY100635 from human recombinant 5HT1A receptor2008Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.
AID3752In vitro affinity against 5-hydroxytryptamine 1A receptor using [3H]-8-OH-DPAT in rat hippocampus2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635.
AID204069Inhibition concentration against [3H]5-HT uptake by human serotonin transporter in JAR cells2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines.
AID17430Biodistribution of the [11C]-radiolabeled compound in rat hippocampus co-injected with 50 nM of WAY 100635.1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Development of fluorine-18-labeled 5-HT1A antagonists.
AID1854984Binding affinity to D4 receptor (unknown origin) assessed as dissociation constant2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
AID17426Biodistribution of the [11C]-radiolabeled compound in rat cerebellum co-injected with 50 nM of WAY 100635.1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Development of fluorine-18-labeled 5-HT1A antagonists.
AID597309Inhibition of adrenergic Alpha-1D receptor2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID1704732Antagonist activity at human 5HT1A receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux at 10 uM incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4
AID1365297Inhibition of 8-OH-DPAT-induced hypothermia in Swiss albino mouse at 0.1 mg/kg, ip measured after 120 mins post dose co-treated with 8-OH-DPAT2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
New 5-HT
AID3758In vitro binding affinity to 5-hydroxytryptamine 1A receptor using [125I](R)-(+)-trans-8-OH-PIPAT as radioligand in rat hippocampal homogenate1994Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26
Derivatives of 4-(2'-methoxyphenyl)-1-[2'-(N-2"-pyridinyl-p-iodobenzamido)ethyl]pipera zine (p-MPPI) as 5-HT1A ligands.
AID597305Inhibition of 5HT5A receptor at 10 uM2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID1854988Displacement of [3H]-8-OH-DPAT from Sprague-Dawley rat hippocampal membrane 5HT1A receptor2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
AID510402Antagonist activity at human cloned 5HT1A receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced [34S]GTPgammaS binding by liquid scintillation counting2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors.
AID597321Inhibition of adrenergic alpha2A receptor at 10 uM2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID4140Antagonistic activity at postsynaptic 5-hydroxytryptamine 1A receptor was measured by its ability to inhibit hypothermia elicited by s.c. administration of 8-OH-DPAT in rat2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
Improvement in the selectivity and metabolic stability of the serotonin 5-HT(1A) ligand, S 15535: a series of cis- and trans-2-(arylcycloalkylamine) 1-indanols.
AID193027Ability to counteract the 8-OH-DPAT (1 mg/kg sc)-induced Hypothermia in rats (n=4) and evaluated for the decrease in body temperature (degrees Celsius) at 1.0(micro mol/kg)2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635.
AID597307Inhibition of 5HT1D receptor at 10 uM2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID1517946Induction of hypothermia in CD-1 mouse assessed as change in body temperature at 0.1 mg/kg, ip measured after 90 mins by thermometric method (Rvb = -0.3 to 0.3 deg C)
AID1593199Antagonist activity at cloned human 5-HT1A receptor transfected in human HeLa cell membranes preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 30 mins by liquid scintillation counting
AID87448Effect on Forskolin-Stimulated cAMP formation, in HeLa cells transfected with the 5-HT 1A receptor at 1 uM concentration2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants.
AID3510Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines.
AID510390Displacement [3H]prazosin of human recombinant Alpha-1D adrenergic receptor expressed in CHO cells by rapid filtration technique2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors.
AID17432Biodistribution of the [11C]-radiolabeled compound in rat hypothalamus co-injected with 50 nM of WAY 100635.1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Development of fluorine-18-labeled 5-HT1A antagonists.
AID3772Inhibitory activity against 5-hydroxytryptamine 1A receptor of rat hippocampal homogenates1994Journal of medicinal chemistry, May-13, Volume: 37, Issue:10
Synthesis and evaluation of 4-(2'-methoxyphenyl)-1-[2'-[N-(2"-pyridinyl)-p- iodobenzamido]ethyl]piperazine (p-MPPI): a new iodinated 5-HT1A ligand.
AID1337901Analgesic activity in Swiss CD1 mouse assessed reduction in formalin-induced inflammatory pain by measuring reduction in time spent in licking or biting formalin injected hind paw at 3 mg/kg, ip pretreated for 30 mins followed by formalin injection measur
AID422848Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Synthesis, potency, and in vivo evaluation of 2-piperazin-1-ylquinoline analogues as dual serotonin reuptake inhibitors and serotonin 5-HT1A receptor antagonists.
AID239799Binding affinity for alpha 1a adrenoceptor2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses.
AID597284Inhibition of 5HT2A receptor at 10 uM2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID597301Inhibition of dopamine D2 receptor at 10 uM2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID597308Inhibition of 5HT1B receptor at 10 uM2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID3547Agonistic effect against 5-hydroxytryptamine 1A receptor using [35S]GTP-gamma-S as radioligand in CHO cells relative to 5-HT2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines.
AID3803Binding affinity against human 5-hydroxytryptamine 1A receptor in CHO cells labeled with [3H]8-OH-DPAT radioligand2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines.
AID87450Percent increase in the Forskolin-Stimulated cAMP formation, in HeLa cells transfected with the 5-HT 1A receptor [compound (1 uM)]2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants.
AID231742Ratio of biodistribution of compound at Hippocampus and cerebellum-1 in rat with 200 nmol of WAY 1006351999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Development of fluorine-18-labeled 5-HT1A antagonists.
AID309471Decrease in body temperature in Swiss Albino mouse at 0.1 mg/kg after 30 mins2007Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22
The influence of modifications in imide fragment structure on 5-HT(1A) and 5-HT(7) receptor affinity and in vivo pharmacological properties of some new 1-(m-trifluoromethylphenyl)piperazines.
AID3524Agonistic efficacy was evaluated by adenylyl cyclase assay in CHO cells stably expressing the human 5-HT1A receptor1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Functional characteristics of a series of N4-substituted 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazines as 5-HT1A receptor ligands. Structure-activity relationships.
AID1830041Displacement of [3H]LSD from human recombinant 5-HT2A receptor expressed in HEK cells by radioligand completion assay relative to control2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Activity of
AID231558Ratio of biodistribution of compound at Hippocampus and cerebellum-1 in rat1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Development of fluorine-18-labeled 5-HT1A antagonists.
AID309486Decrease in body temperature in Swiss Albino mouse at 0.1 mg/kg after 120 mins2007Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22
The influence of modifications in imide fragment structure on 5-HT(1A) and 5-HT(7) receptor affinity and in vivo pharmacological properties of some new 1-(m-trifluoromethylphenyl)piperazines.
AID597285Inhibition of 5HT2C receptor at 10 uM2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID441123Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in HEK293 cells after 120 mins2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and characterization of environment-sensitive fluorescent ligands for human 5-HT1A receptors with 1-arylpiperazine structure.
AID597304Inhibition of adrenergic beta1 receptor at 10 uM2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID339528Displacement of [3H]paroxetine from rat cortical 5HTT reuptake site2008Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
Studies toward the discovery of the next generation of antidepressants. Part 6: Dual 5-HT1A receptor and serotonin transporter affinity within a class of arylpiperazinyl-cyclohexyl indole derivatives.
AID597319Inhibition of sigma 1 receptor at 10 uM2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID1555768Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting2019European journal of medicinal chemistry, Aug-15, Volume: 1761,3-Dioxane as a scaffold for potent and selective 5-HT
AID221108Time-dependent effect on 8-OH-DPAT-induced hypothermia (change in body temperature) after 60 min, in mice at 1 mg/kg dose2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants.
AID1365310In-vivo 5-HT1A receptor agonist activity in Swiss albino mouse assessed as induction of lower lip retraction by measuring lower lip retraction score at 0.3 mg/kg, ip dosed 15 mins before test (Rvb = 0.0 +/- 0.0 No_unit)2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
New 5-HT
AID1713194Inhibition of 8-OH-DPAT-induced hypothermia in Swiss albino mouse assessed as change in rectal body temperature at 0.3 mg/kg, sc pretreated with compound for 45 mins followed by 8-OH-DPAT challenge and measured after 15 min by thermometer (Rvb = -1.8 degr2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Synthesis and biological investigation of new equatorial (β) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile.
AID1409504Antagonist activity at serotonin 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID597315Inhibition of 5HT1B receptor2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID1830039Displacement of [3H]LSD from human recombinant 5-HT2C receptor expressed in HEK cells by radioligand completion assay relative to control2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Activity of
AID3882Antagonistic efficacy was evaluated by adenylyl cyclase assay in CHO cells stably expressing the human 5-HT1A receptor1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Functional characteristics of a series of N4-substituted 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazines as 5-HT1A receptor ligands. Structure-activity relationships.
AID510394Selectivity for human recombinant adrenergic Alpha-1B receptor over human recombinant adrenergic alpha1A receptor2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors.
AID231743Ratio of biodistribution of compound at cortex and cerebellum-1 in rat1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Development of fluorine-18-labeled 5-HT1A antagonists.
AID339531Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells2008Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
Studies toward the discovery of the next generation of antidepressants. Part 6: Dual 5-HT1A receptor and serotonin transporter affinity within a class of arylpiperazinyl-cyclohexyl indole derivatives.
AID1593197Displacement of [3H]Prazosin from human recombinant alpha 1D adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay
AID1555772Agonist activity at human recombinant 5HT1A receptor expressed in human HeLa cells assessed as increase in [35S]GTPgammaS binding incubated for 20 mins by liquid scintillation counter2019European journal of medicinal chemistry, Aug-15, Volume: 1761,3-Dioxane as a scaffold for potent and selective 5-HT
AID597317Inhibition of sigma 2 receptor at 10 uM2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID1409503Antagonist activity at serotonin 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux at 10 uM after 15 mins by calcium 4-dye based FLIPR assay relative to control2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID597283Inhibition of 5HT1E receptor at 10 uM2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID4398Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes.1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Functional characteristics of a series of N4-substituted 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazines as 5-HT1A receptor ligands. Structure-activity relationships.
AID1601994Induction of hypothermia in CD-1 mouse assessed as change in body temperature at 0.1 mg/kg, sc measured after 60 mins by thermometric method (Rvb = 0.1 deg C)2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT
AID1555770Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1D expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counter2019European journal of medicinal chemistry, Aug-15, Volume: 1761,3-Dioxane as a scaffold for potent and selective 5-HT
AID597318Inhibition of SERT at 10 uM2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID597313Inhibition of adrenergic alpha1A receptor2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID1602006Induction of hypothermia in CD-1 mouse assessed as change in body temperature at 0.1 mg/kg, sc measured after 120 mins by thermometric method (Rvb = -0.1 to 0.1 deg C)2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT
AID510393Selectivity for human recombinant adrenergic Alpha-1B receptor over human recombinant adrenergic alpha1D receptor2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors.
AID1602000Induction of hypothermia in CD-1 mouse assessed as change in body temperature at -0.1 to 0.1 mg/kg, sc measured after 90 mins by thermometric method (Rvb = -0.1 to 0.1 deg C)2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT
AID221103Time-dependent effect on 8-OH-DPAT-induced hypothermia (change in body temperature) after 30 min, in mice at 1 mg/kg dose2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants.
AID1593195Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay
AID597311Inhibition of adrenergic Alpha-1B receptor2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID408280Intrinsic activity at human recombinant 5HT1A receptor expressed in HEK293 cells by [35S]GTPgammaS binding relative to 5 hydroxytryptamine2008Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.
AID4198In vitro binding affinity for 5-hydroxytryptamine 1A receptor was determined by measuring specific inhibition of [125I]-binding to rat hippocampal membrane preparations1998Journal of medicinal chemistry, Jan-15, Volume: 41, Issue:2
Isoindol-1-one analogues of 4-(2'-methoxyphenyl)-1-[2'-[N-(2"-pyridyl)-p-iodobenzamido]ethyl]pipera zine (p-MPPI) as 5-HT1A receptor ligands.
AID6433Receptor-linked G protein activation at 5-hydroxytryptamine receptor was determined by measuring the stimulation of [35S]GTP-gamma-S, binding (Experiment 2)1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Development of fluorine-18-labeled 5-HT1A antagonists.
AID1555771Displacement of [3H]8-OH-DPAT from human cloned 5HT-1AR transfected in HeLa cells incubated for 30 mins by liquid scintillation counter2019European journal of medicinal chemistry, Aug-15, Volume: 1761,3-Dioxane as a scaffold for potent and selective 5-HT
AID3513Effective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cells2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines.
AID597312Inhibition of 5HT7 receptor2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID1830043Displacement of [3H]8-OH-DAPT from human recombinant 5-HT1A receptor expressed in COS7 cells measured after 60 to 90 mins by radioligand completion assay relative to control2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Activity of
AID726771Apparent permeability across apical to basolateral side in human Caco2 cells at 1 to 20 uM by LC-MS/MS analysis2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Discovery of novel α₁-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands.
AID597286Inhibition of 5HT3 receptor at 10 uM2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID4326Inhibition of binding of [125I]8-OH-PIPAT ligand to 5-hydroxytryptamine 1A receptor of rat hippocampal homogenates1994Journal of medicinal chemistry, May-13, Volume: 37, Issue:10
Synthesis and evaluation of 4-(2'-methoxyphenyl)-1-[2'-[N-(2"-pyridinyl)-p- iodobenzamido]ethyl]piperazine (p-MPPI): a new iodinated 5-HT1A ligand.
AID309476Decrease in body temperature in Swiss Albino mouse at 0.1 mg/kg after 60 mins2007Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22
The influence of modifications in imide fragment structure on 5-HT(1A) and 5-HT(7) receptor affinity and in vivo pharmacological properties of some new 1-(m-trifluoromethylphenyl)piperazines.
AID221098Time-dependent effect on 8-OH-DPAT-induced hypothermia (change in body temperature) after 15 min, in mice at 1 mg/kg dose2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants.
AID1593198Displacement of [3H]-8-OH-DPAT from human recombinant 5-HT1A receptor expressed in human HeLa cells incubated for 30 mins by radioligand competition binding assay
AID1713201Effect on 8-OH-DPAT-induced lower lip retraction in Wistar rat at 0.2 mg/kg, sc pretreated with compound for 45 mins followed by 8-OH-DPAT challenge and measured after 15 mins (Rvb = 2.7 to 2.8 No_unit)2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Synthesis and biological investigation of new equatorial (β) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile.
AID221164In vitro oral metabolic bioavailability after incubation with hepatic microsomes.2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
Improvement in the selectivity and metabolic stability of the serotonin 5-HT(1A) ligand, S 15535: a series of cis- and trans-2-(arylcycloalkylamine) 1-indanols.
AID726714Unbound fraction in rat plasma at 1000 ng/g after 5 hrs by equilibrium dialysis method2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Discovery of novel α₁-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands.
AID481373Half life in rat liver microsomes at 1 uM after 20 mins2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists.
AID408275Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor2008Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.
AID726709Ratio of drug level in brain to plasma in rat at 1 hr2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Discovery of novel α₁-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands.
AID481371Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists.
AID510392Selectivity for human recombinant adrenergic alpha1A receptor over human recombinant adrenergic Alpha-1D receptor2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors.
AID1393526Antagonist activity at human 5-HT1AR expressed in HEK293 cells assessed as inhibition of 8-OH-DPAT-induced calcium flux by fluorimetric method
AID3836In vitro inhibition of [3H]- 8-OH-DPAT binding to cloned cell line containing human 5-hydroxytryptamine 1A receptor1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Development of fluorine-18-labeled 5-HT1A antagonists.
AID1713197Inhibition of 8-OH-DPAT-induced hypothermia in Swiss albino mouse assessed as change in rectal body temperature at 0.3 mg/kg, sc pretreated with compound for 45 mins followed by 8-OH-DPAT challenge and measured after 60 min by thermometer (Rvb = -1.3 degr2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Synthesis and biological investigation of new equatorial (β) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile.
AID597287Inhibition of 5HT6 receptor at 10 uM2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID3540Agonistic effect against 5-hydroxytryptamine 1A receptor using cAMP as radioligand relative to 5-HT in inhibiting forskolin-stimulated adenylate cyclase activity in CHO cells2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines.
AID726710Unbound fraction in rat brain at 1000 ng/g after 5 hrs by equilibrium dialysis method2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Discovery of novel α₁-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands.
AID197200Evaluated for the inhibition of footshock-evoked ultrasonic vocalization in rats after administration of 8-OH-DPAT (0.1 mg/kg sc) alone or in combination with WAY-1006352000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635.
AID1704733Antagonist activity at human 5HT1A receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based
AID309496Effect on lower lip retraction in Wistar rat at 0.1 mg/kg2007Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22
The influence of modifications in imide fragment structure on 5-HT(1A) and 5-HT(7) receptor affinity and in vivo pharmacological properties of some new 1-(m-trifluoromethylphenyl)piperazines.
AID510395Selectivity for human recombinant adrenergic alpha1 receptor over human cloned 5HT1A receptor2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors.
AID1713200Effect on 8-OH-DPAT-induced lower lip retraction in Wistar rat at 0.1 mg/kg, sc pretreated with compound for 45 mins followed by 8-OH-DPAT challenge and measured after 15 mins (Rvb = 2.7 to 2.8 No_unit)2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Synthesis and biological investigation of new equatorial (β) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile.
AID510391Displacement [3H]8-OH-DPAT of human cloned 5HT1A receptor expressed in human HeLa cells by rapid filtration technique2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors.
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.
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.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
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.
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.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
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.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347159Primary screen GU Rhodamine 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.
AID1347160Primary screen NINDS Rhodamine 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.
AID624215Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1A1998European journal of pharmacology, Aug-21, Volume: 355, Issue:2-3
Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study.
AID624215Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1A1998Naunyn-Schmiedeberg's archives of pharmacology, Mar, Volume: 357, Issue:3
Labelling of recombinant human and native rat serotonin 5-HT1A receptors by a novel, selective radioligand, [3H]-S 15535: definition of its binding profile using agonists, antagonists and inverse agonists.
AID1345814Human D4 receptor (Dopamine receptors)2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A recepto
AID1345615Human 5-HT1A receptor (5-Hydroxytryptamine receptors)1998Naunyn-Schmiedeberg's archives of pharmacology, Mar, Volume: 357, Issue:3
Labelling of recombinant human and native rat serotonin 5-HT1A receptors by a novel, selective radioligand, [3H]-S 15535: definition of its binding profile using agonists, antagonists and inverse agonists.
AID1345615Human 5-HT1A receptor (5-Hydroxytryptamine receptors)1998European journal of pharmacology, Aug-21, Volume: 355, Issue:2-3
Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS 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.
AID624215Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1A1997Life sciences, , Volume: 60, Issue:9
Pharmacological characterization of recombinant human 5-hydroxytryptamine1A receptors using a novel antagonist radioligand, [3H]WAY-100635.
AID1345615Human 5-HT1A receptor (5-Hydroxytryptamine receptors)1997Life sciences, , Volume: 60, Issue:9
Pharmacological characterization of recombinant human 5-hydroxytryptamine1A receptors using a novel antagonist radioligand, [3H]WAY-100635.
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.
AID493017Wombat Data for BeliefDocking2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (46)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's8 (17.39)18.2507
2000's11 (23.91)29.6817
2010's18 (39.13)24.3611
2020's9 (19.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.83

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

MetricThis Compound (vs All)
Research Demand Index10.83 (24.57)
Research Supply Index3.85 (2.92)
Research Growth Index4.68 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.83)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (2.17%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other45 (97.83%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]