Page last updated: 2024-11-12

fauc 213

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Cross-References

ID SourceID
PubMed CID10336538
CHEMBL ID310843
MeSH IDM0397006

Synonyms (37)

Synonym
CHEMBL310843 ,
gtpl974
2-[[4-(4-chlorophenyl)piperazin-1-yl]methyl]pyrazolo[1,5-a]pyridine
fauc 213, >=98% (hplc), solid
NCGC00165795-01
NCGC00165795-02
2-((4-(4-chlorophenyl)piperazin-1-yl)methyl)-pyrazolo[1,5-a]pyridine
4-(4-chloro-phenyl)-1-pyrazolo[1,5-a]pyridin-2-ylmethyl-piperazin-1-ium
2-[4-(4-chloro-phenyl)-piperazin-1-ylmethyl]-pyrazolo[1,5-a]pyridine
2-((4-(4-chlorophenyl)piperazin-1-yl)methyl)h-pyrazolo[1,5-a]pyridine
bdbm50102712
HMS3263F09
fauc 213
fauc213
fauc-213
2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine
337972-47-1
LP01144
CCG-222448
g8f040299r ,
unii-g8f040299r
pyrazolo(1,5-a)pyridine, 2-((4-(4-chlorophenyl)-1-piperazinyl)methyl)-
tox21_501144
NCGC00261829-01
DTXSID40187460
J-019326
2-((4-(4-chlorophenyl)piperazin-1-yl)methyl)pyrazolo[1,5-a]pyridine
Q27077288
SDCCGSBI-0633796.P001
NCGC00165795-04
MS-24880
EX-A5435
fauc213fauc 213
HY-14327
CS-0003283
F87660
AKOS040745787
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (14)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
GLS proteinHomo sapiens (human)Potency5.62340.35487.935539.8107AID624146
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency24.89700.001530.607315,848.9004AID1224819; AID1224820; AID1224821
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency0.15000.035520.977089.1251AID504332
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency33.80780.134610.395030.1313AID1347049
chromobox protein homolog 1Homo sapiens (human)Potency50.11870.006026.168889.1251AID488953
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency7.07950.251215.843239.8107AID504327
[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)
D(2) dopamine receptorHomo sapiens (human)Ki7.07850.00000.651810.0000AID1456758; AID1456759; AID238699; AID277677; AID319903; AID319904; AID320344; AID419541; AID419547; AID419553; AID62931; AID64333; AID64661; AID767067
D(1A) dopamine receptorHomo sapiens (human)Ki5.50000.00010.836310.0000AID1456727
D(4) dopamine receptorHomo sapiens (human)Ki0.00290.00000.436210.0000AID238274; AID277674; AID320346; AID419543; AID419715; AID63528; AID64031; AID767064
Substance-P receptorCavia porcellus (domestic guinea pig)Ki3.40000.00130.69133.4000AID320344
D(3) dopamine receptorHomo sapiens (human)Ki4.78130.00000.602010.0000AID1456729; AID238613; AID277673; AID319905; AID320345; AID419542; AID419556; AID419557; AID419558; AID419559; AID419560; AID419561; AID419562; AID419563; AID64976; AID767065
5-hydroxytryptamine receptor 2ASus scrofa (pig)Ki0.90000.03000.42700.9000AID319909; AID320343
D(1A) dopamine receptorSus scrofa (pig)Ki5.50000.00051.22238.8000AID320340
DBos taurus (cattle)Ki5.50000.00012.367610.0000AID63182
[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)
D(4) dopamine receptorHomo sapiens (human)EC50 (µMol)0.15400.00140.08892.2300AID65925
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (152)

Processvia Protein(s)Taxonomy
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
temperature homeostasisD(2) dopamine receptorHomo sapiens (human)
response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein phosphorylationD(2) dopamine receptorHomo sapiens (human)
response to amphetamineD(2) dopamine receptorHomo sapiens (human)
nervous system process involved in regulation of systemic arterial blood pressureD(2) dopamine receptorHomo sapiens (human)
regulation of heart rateD(2) dopamine receptorHomo sapiens (human)
regulation of sodium ion transportD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(2) dopamine receptorHomo sapiens (human)
positive regulation of neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
positive regulation of receptor internalizationD(2) dopamine receptorHomo sapiens (human)
autophagyD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
neuron-neuron synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
axonogenesisD(2) dopamine receptorHomo sapiens (human)
synapse assemblyD(2) dopamine receptorHomo sapiens (human)
sensory perception of smellD(2) dopamine receptorHomo sapiens (human)
long-term memoryD(2) dopamine receptorHomo sapiens (human)
grooming behaviorD(2) dopamine receptorHomo sapiens (human)
locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
adult walking behaviorD(2) dopamine receptorHomo sapiens (human)
protein localizationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell population proliferationD(2) dopamine receptorHomo sapiens (human)
associative learningD(2) dopamine receptorHomo sapiens (human)
visual learningD(2) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(2) dopamine receptorHomo sapiens (human)
response to light stimulusD(2) dopamine receptorHomo sapiens (human)
response to toxic substanceD(2) dopamine receptorHomo sapiens (human)
response to iron ionD(2) dopamine receptorHomo sapiens (human)
response to inactivityD(2) dopamine receptorHomo sapiens (human)
Wnt signaling pathwayD(2) dopamine receptorHomo sapiens (human)
striatum developmentD(2) dopamine receptorHomo sapiens (human)
orbitofrontal cortex developmentD(2) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(2) dopamine receptorHomo sapiens (human)
adenohypophysis developmentD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell migrationD(2) dopamine receptorHomo sapiens (human)
peristalsisD(2) dopamine receptorHomo sapiens (human)
auditory behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of synaptic transmission, GABAergicD(2) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(2) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
response to histamineD(2) dopamine receptorHomo sapiens (human)
response to nicotineD(2) dopamine receptorHomo sapiens (human)
positive regulation of urine volumeD(2) dopamine receptorHomo sapiens (human)
positive regulation of renal sodium excretionD(2) dopamine receptorHomo sapiens (human)
positive regulation of multicellular organism growthD(2) dopamine receptorHomo sapiens (human)
response to cocaineD(2) dopamine receptorHomo sapiens (human)
negative regulation of circadian sleep/wake cycle, sleepD(2) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(2) dopamine receptorHomo sapiens (human)
drinking behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(2) dopamine receptorHomo sapiens (human)
response to morphineD(2) dopamine receptorHomo sapiens (human)
pigmentationD(2) dopamine receptorHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(2) dopamine receptorHomo sapiens (human)
negative regulation of innate immune responseD(2) dopamine receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IID(2) dopamine receptorHomo sapiens (human)
negative regulation of insulin secretionD(2) dopamine receptorHomo sapiens (human)
acid secretionD(2) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(2) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(2) dopamine receptorHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityD(2) dopamine receptorHomo sapiens (human)
response to axon injuryD(2) dopamine receptorHomo sapiens (human)
branching morphogenesis of a nerveD(2) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(2) dopamine receptorHomo sapiens (human)
epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(2) dopamine receptorHomo sapiens (human)
release of sequestered calcium ion into cytosolD(2) dopamine receptorHomo sapiens (human)
dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of synapse structural plasticityD(2) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(2) dopamine receptorHomo sapiens (human)
excitatory postsynaptic potentialD(2) dopamine receptorHomo sapiens (human)
positive regulation of growth hormone secretionD(2) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeD(2) dopamine receptorHomo sapiens (human)
regulation of locomotion involved in locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
negative regulation of cellular response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
positive regulation of glial cell-derived neurotrophic factor productionD(2) dopamine receptorHomo sapiens (human)
positive regulation of long-term synaptic potentiationD(2) dopamine receptorHomo sapiens (human)
hyaloid vascular plexus regressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of neuron migrationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(2) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
temperature homeostasisD(1A) dopamine receptorHomo sapiens (human)
conditioned taste aversionD(1A) dopamine receptorHomo sapiens (human)
behavioral fear responseD(1A) dopamine receptorHomo sapiens (human)
regulation of protein phosphorylationD(1A) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(1A) dopamine receptorHomo sapiens (human)
response to amphetamineD(1A) dopamine receptorHomo sapiens (human)
protein import into nucleusD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
activation of adenylate cyclase activityD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
synapse assemblyD(1A) dopamine receptorHomo sapiens (human)
memoryD(1A) dopamine receptorHomo sapiens (human)
mating behaviorD(1A) dopamine receptorHomo sapiens (human)
grooming behaviorD(1A) dopamine receptorHomo sapiens (human)
adult walking behaviorD(1A) dopamine receptorHomo sapiens (human)
visual learningD(1A) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(1A) dopamine receptorHomo sapiens (human)
astrocyte developmentD(1A) dopamine receptorHomo sapiens (human)
dopamine transportD(1A) dopamine receptorHomo sapiens (human)
transmission of nerve impulseD(1A) dopamine receptorHomo sapiens (human)
neuronal action potentialD(1A) dopamine receptorHomo sapiens (human)
dentate gyrus developmentD(1A) dopamine receptorHomo sapiens (human)
striatum developmentD(1A) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(1A) dopamine receptorHomo sapiens (human)
positive regulation of cell migrationD(1A) dopamine receptorHomo sapiens (human)
peristalsisD(1A) dopamine receptorHomo sapiens (human)
operant conditioningD(1A) dopamine receptorHomo sapiens (human)
synaptic transmission, glutamatergicD(1A) dopamine receptorHomo sapiens (human)
regulation of dopamine metabolic processD(1A) dopamine receptorHomo sapiens (human)
vasodilationD(1A) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(1A) dopamine receptorHomo sapiens (human)
maternal behaviorD(1A) dopamine receptorHomo sapiens (human)
positive regulation of potassium ion transportD(1A) dopamine receptorHomo sapiens (human)
glucose importD(1A) dopamine receptorHomo sapiens (human)
habituationD(1A) dopamine receptorHomo sapiens (human)
sensitizationD(1A) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(1A) dopamine receptorHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolD(1A) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(1A) dopamine receptorHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicD(1A) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(1A) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
long-term synaptic potentiationD(1A) dopamine receptorHomo sapiens (human)
long-term synaptic depressionD(1A) dopamine receptorHomo sapiens (human)
cellular response to catecholamine stimulusD(1A) dopamine receptorHomo sapiens (human)
modification of postsynaptic structureD(1A) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(1A) dopamine receptorHomo sapiens (human)
positive regulation of neuron migrationD(1A) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
dopamine receptor signaling pathwayD(1A) dopamine receptorHomo 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)
response to ethanolD(3) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(3) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
learning or memoryD(3) dopamine receptorHomo sapiens (human)
learningD(3) dopamine receptorHomo sapiens (human)
locomotory behaviorD(3) dopamine receptorHomo sapiens (human)
visual learningD(3) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(3) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(3) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(3) dopamine receptorHomo sapiens (human)
response to histamineD(3) dopamine receptorHomo sapiens (human)
social behaviorD(3) dopamine receptorHomo sapiens (human)
response to cocaineD(3) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(3) dopamine receptorHomo sapiens (human)
response to morphineD(3) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(3) dopamine receptorHomo sapiens (human)
positive regulation of mitotic nuclear divisionD(3) dopamine receptorHomo sapiens (human)
acid secretionD(3) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(3) dopamine receptorHomo sapiens (human)
negative regulation of oligodendrocyte differentiationD(3) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(3) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(3) dopamine receptorHomo sapiens (human)
musculoskeletal movement, spinal reflex actionD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(3) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(3) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(3) dopamine receptorHomo sapiens (human)
positive regulation of dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(3) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(3) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(3) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(3) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(3) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicDBos taurus (cattle)
vasodilationDBos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (20)

Processvia Protein(s)Taxonomy
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(2) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(2) dopamine receptorHomo sapiens (human)
protein bindingD(2) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(2) dopamine receptorHomo sapiens (human)
dopamine bindingD(2) dopamine receptorHomo sapiens (human)
ionotropic glutamate receptor bindingD(2) dopamine receptorHomo sapiens (human)
identical protein bindingD(2) dopamine receptorHomo sapiens (human)
heterocyclic compound bindingD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(2) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via GsD(1A) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(1A) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activityD(1A) dopamine receptorHomo sapiens (human)
protein bindingD(1A) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(1A) dopamine receptorHomo sapiens (human)
dopamine bindingD(1A) dopamine receptorHomo sapiens (human)
arrestin family protein bindingD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(1A) dopamine receptorHomo 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)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(3) dopamine receptorHomo sapiens (human)
protein bindingD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(3) dopamine receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (27)

Processvia Protein(s)Taxonomy
Golgi membraneD(2) dopamine receptorHomo sapiens (human)
acrosomal vesicleD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
ciliumD(2) dopamine receptorHomo sapiens (human)
lateral plasma membraneD(2) dopamine receptorHomo sapiens (human)
endocytic vesicleD(2) dopamine receptorHomo sapiens (human)
axonD(2) dopamine receptorHomo sapiens (human)
dendriteD(2) dopamine receptorHomo sapiens (human)
synaptic vesicle membraneD(2) dopamine receptorHomo sapiens (human)
sperm flagellumD(2) dopamine receptorHomo sapiens (human)
dendritic spineD(2) dopamine receptorHomo sapiens (human)
perikaryonD(2) dopamine receptorHomo sapiens (human)
axon terminusD(2) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(2) dopamine receptorHomo sapiens (human)
ciliary membraneD(2) dopamine receptorHomo sapiens (human)
non-motile ciliumD(2) dopamine receptorHomo sapiens (human)
dopaminergic synapseD(2) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(2) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(2) dopamine receptorHomo sapiens (human)
presynaptic membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
nucleusD(1A) dopamine receptorHomo sapiens (human)
endoplasmic reticulum membraneD(1A) dopamine receptorHomo sapiens (human)
plasma membraneD(1A) dopamine receptorHomo sapiens (human)
ciliumD(1A) dopamine receptorHomo sapiens (human)
presynaptic membraneD(1A) dopamine receptorHomo sapiens (human)
dendritic spineD(1A) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(1A) dopamine receptorHomo sapiens (human)
ciliary membraneD(1A) dopamine receptorHomo sapiens (human)
non-motile ciliumD(1A) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(1A) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(1A) dopamine receptorHomo sapiens (human)
plasma membraneD(1A) dopamine receptorHomo sapiens (human)
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 membraneD(3) dopamine receptorHomo sapiens (human)
synapseD(3) dopamine receptorHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
endoplasmic reticulum membraneDBos taurus (cattle)
dendritic spineDBos taurus (cattle)
ciliary membraneDBos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (117)

Assay IDTitleYearJournalArticle
AID419549Displacement of [3H]spiperone from human cloned dopamine D2L receptor V2.61F mutant expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID419721Selectivity ratio of Ki for human cloned dopamine D2L receptor E181V/I183S mutant to Ki for wild type human cloned dopamine D2L receptor expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID1456729Inhibition of human dopamine D3 receptor2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Return of D
AID419546Selectivity ratio of Ki for human cloned dopamine D3 receptor to Ki for human cloned dopamine D4 receptor expressed in CHO cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID1456759Inhibition of human dopamine D2 (long) receptor (unknown origin)2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Return of D
AID277668Selectivity for dopamine D3 over dopamine D22007Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.
AID419726Selectivity ratio of Ki for human cloned dopamine D3 receptor L2.64F mutant to Ki for wild type human cloned dopamine D3 receptor expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID319911Selectivity for human dopamine D4.4 receptor over human dopamine D2L receptor2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET.
AID419728Selectivity ratio of Ki for human cloned dopamine D3 receptor V2.61F/FV3.28,3.29LM mutant to Ki for wild type human cloned dopamine D3 receptor expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID419555Displacement of [3H]spiperone from human cloned dopamine D2L receptor H6.55F mutant expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID767067Displacement of [3H]spiperone from human dopamine D2 receptor2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Discovery of highly potent and selective D4 ligands by interactive SAR study.
AID419733Selectivity ratio of Ki for wild type human cloned dopamine D2L receptor to Ki for human cloned dopamine D2L receptor V2.61F/FV3.28,3.29LM mutant expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID419547Displacement of [3H]spiperone from wild type human cloned dopamine D2L receptor expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID320345Binding affinity to human D3 receptor2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Discovery of a dopamine D4 selective PET ligand candidate taking advantage of a click chemistry based REM linker.
AID64179Ability to displace [3H]spiperone from dopamine receptor D4.4 expressed in CHO-K1 cells2001Journal of medicinal chemistry, Apr-12, Volume: 44, Issue:8
Comparative molecular field analysis of dopamine D4 receptor antagonists including 3-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 113), 3-[4-(4-chlorophenyl)piperazin-1-ylmethyl]-1H-pyrrolo-[2,3-b]pyridine (L-745,870), and clozapi
AID319908Displacement of [3H]8-OH-DPAT from 5HT1A receptor in pig cortical membranes2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET.
AID277677Binding affinity to dopamine D22007Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.
AID63528Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning.
AID419554Displacement of [3H]spiperone from human cloned dopamine D2L receptor H6.55A mutant expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID242945Ratio of dopamine receptor D2 long and D4 ki values2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.
AID277673Displacement of [3H]spiperone from human dopamine D3 expressed in CHO cell membrane2007Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.
AID419550Displacement of [3H]spiperone from human cloned dopamine D2L receptor L2.64F mutant expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID319904Displacement of [3H]spiperone from cloned human dopamine D2S receptor expressed in CHO cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET.
AID319915Agonist activity at rat dopamine D4.2 receptor expressed in CHO10001A cells assessed as incorporation of [3H]thymidine2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET.
AID65921Intrinsic activity was measured in the human Dopamine receptor D4 calcium flux assay wiht co-transfected G-alpha-qo5 protein2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning.
AID64976Binding affinity against dopamine receptor D3 using radioligand [3H]spiperone2001Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213).
AID320346Binding affinity to human dopamine D4.4 receptor2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Discovery of a dopamine D4 selective PET ligand candidate taking advantage of a click chemistry based REM linker.
AID226201Rate of incorporation of [3H]thymidine as evidence of mitogenetic activity2001Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213).
AID238699Binding affinity for human dopamine receptor D2 long2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.
AID419715Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID238274Binding affinity for Dopamine receptor D42005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.
AID419557Displacement of [3H]spiperone from human cloned dopamine D3 receptor D3.32E mutant expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID419724Selectivity ratio of Ki for human cloned dopamine D3 receptor D3.32E mutant to Ki for wild type human cloned dopamine D3 receptor expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID419730Selectivity ratio of Ki for human cloned dopamine D3 receptor H6.55A mutant to Ki for wild type human cloned dopamine D3 receptor expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID419551Displacement of [3H]spiperone from human cloned dopamine D2L receptor FV3.28,3.29LM mutant expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID419553Displacement of [3H]spiperone from human cloned dopamine D2L receptor E181V/I183S mutant expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID419563Displacement of [3H]spiperone from human cloned dopamine D3 receptor H6.55A mutant expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID419717Selectivity ratio of Ki for human cloned dopamine D2L receptor V2.61F mutant to Ki for wild type human cloned dopamine D2L receptor expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID319912Selectivity for human dopamine D4.4 receptor over human dopamine D2S receptor2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET.
AID64661Binding affinity against dopamine receptor D2S using radioligand [3H]spiperone2001Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213).
AID320340Binding affinity to pig cortical membrane dopamine D1 receptor2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Discovery of a dopamine D4 selective PET ligand candidate taking advantage of a click chemistry based REM linker.
AID232502Selectivity ratio of D2 receptor to that of D4 receptor2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning.
AID419729Selectivity ratio of Ki for human cloned dopamine D3 receptor V180E/S182I mutant to Ki for wild type human cloned dopamine D3 receptor expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID1456758Inhibition of human dopamine D2 (short) receptor2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Return of D
AID419723Selectivity ratio of Ki for human cloned dopamine D2L receptor H6.55F mutant to Ki for wild type human cloned dopamine D2L receptor expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID419722Selectivity ratio of Ki for human cloned dopamine D2L receptor H6.55A mutant to Ki for wild type human cloned dopamine D2L receptor expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID419545Selectivity ratio of Ki for human cloned dopamine D2L receptor to Ki for human cloned dopamine D4 receptor expressed in CHO cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID419731Selectivity ratio of dopamine D2L receptor V2.61F/FV3.28,3.29LM mutant over wild type dopamine D2L receptor2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID419559Displacement of [3H]spiperone from human cloned dopamine D3 receptor L2.64F mutant expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID242944Ratio of dopamine receptor D2 long and D3 ki values2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.
AID767065Binding affinity to human dopamine D3 receptor by radioligand binding assay2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Discovery of highly potent and selective D4 ligands by interactive SAR study.
AID419543Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID419544Selectivity ratio of Ki for human cloned dopamine D2L receptor to Ki for human cloned dopamine D3 receptor expressed in CHO cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID238613Binding affinity for human dopamine receptor D32005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.
AID63182Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 233902001Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213).
AID419542Displacement of [3H]spiperone from human cloned dopamine D3 receptor expressed in CHO cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID767064Binding affinity to human dopamine D4 receptor by radioligand binding assay2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Discovery of highly potent and selective D4 ligands by interactive SAR study.
AID419552Displacement of [3H]spiperone from human cloned dopamine D2L receptor V2.61F/FV3.28,3.29LM mutant expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID320344Binding affinity to human dopamine D2 long receptor2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Discovery of a dopamine D4 selective PET ligand candidate taking advantage of a click chemistry based REM linker.
AID62931Binding affinity against human Dopamine receptor D2 using [3H]spiperone as radioligand2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning.
AID320341Binding affinity to pig cortical membrane 5HT1A receptor2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Discovery of a dopamine D4 selective PET ligand candidate taking advantage of a click chemistry based REM linker.
AID277674Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane2007Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.
AID419718Selectivity ratio of Ki for human cloned dopamine D2L receptor L2.64F mutant to Ki for wild type human cloned dopamine D2L receptor expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID64333Binding affinity against dopamine receptor D2L using radioligand [3H]-spiperone2001Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213).
AID419556Displacement of [3H]spiperone from wild type human cloned dopamine D3 receptor expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID419734Selectivity ratio of Ki for wild type human cloned dopamine D3 receptor to Ki for human cloned dopamine D3 receptor V2.61F/FV3.28,3.29LM mutant expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID767062Modulation of human dopamine D4 receptor by fluorescent calcium assay2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Discovery of highly potent and selective D4 ligands by interactive SAR study.
AID419725Selectivity ratio of Ki for human cloned dopamine D3 receptor V2.61F mutant to Ki for wild type human cloned dopamine D3 receptor expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID419541Displacement of [3H]spiperone from human cloned dopamine D2L receptor expressed in CHO cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID419732Selectivity ratio of dopamine D3 receptor V2.61F/FV3.28,3.29LM mutant over wild type dopamine D3 receptor2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID1456726Inhibition of human dopamine D4.4 receptor2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Return of D
AID1456727Inhibition of human dopamine D1 receptor2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Return of D
AID64031Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone2001Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213).
AID319913Selectivity for human dopamine D4.4 receptor over human dopamine D3 receptor2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET.
AID277669Selectivity for dopamine D3 over dopamine D42007Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.
AID320343Displacement of [3H]ketanserin from pig cortical membrane 5HT2 receptor2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Discovery of a dopamine D4 selective PET ligand candidate taking advantage of a click chemistry based REM linker.
AID319910Displacement of [3H]prazosin from adrenergic alpha1 receptor in pig cortical membranes2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET.
AID419558Displacement of [3H]spiperone from human cloned dopamine D3 receptor V2.61F mutant expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID242943Ratio of dopamine receptor D3 and D4 ki values2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.
AID419562Displacement of [3H]spiperone from human cloned dopamine D3 receptor V180E/S182I mutant expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID419719Selectivity ratio of Ki for human cloned dopamine D2L receptor FV3.28,3.29LM mutant to Ki for wild type human cloned dopamine D2L receptor expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID419561Displacement of [3H]spiperone from human cloned dopamine D3 receptor V2.61F/FV3.28,3.29LM mutant expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID419716Selectivity ratio of Ki for human cloned dopamine D2L receptor D3.32E mutant to Ki for wild type human cloned dopamine D2L receptor expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID319907Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET.
AID419720Selectivity ratio of Ki for human cloned dopamine D2L receptor V2.61F/FV3.28,3.29LM mutant to Ki for wild type human cloned dopamine D2L receptor expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID319903Displacement of [3H]spiperone from cloned human dopamine D2L receptor expressed in CHO cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET.
AID319918Displacement of 2-[4-(2-(2-[18F]fluoroethoxy)phenyl)piperazin-1-ylmethyl]pyrazolo[1,5-alpha]pyridine from dopamine D4 receptor in Sprague-Dawley rat brain2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET.
AID419560Displacement of [3H]spiperone from human cloned dopamine D3 receptor FV3.28,3.29LM mutant expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID319914Agonist activity at rat dopamine D4.2 receptor expressed in CHO10001A cells assessed as incorporation of [3H]thymidine relative to quinpirole2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET.
AID319905Displacement of [3H]spiperone from cloned human dopamine D3 receptor expressed in CHO cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET.
AID419548Displacement of [3H]spiperone from human cloned dopamine D2L receptor D3.32E mutant expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID419727Selectivity ratio of Ki for human cloned dopamine D3 receptor FV3.28,3.29LM mutant to Ki for wild type human cloned dopamine D3 receptor expressed in HEK293 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.
AID319909Displacement of [3H]ketanserin from 5HT2 receptor in pig cortical membranes2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET.
AID319906Displacement of [3H]spiperone from cloned human dopamine D4.4 receptor expressed in CHO cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET.
AID320342Displacement of [3H]prazosin from pig cortical membrane adrenergic alpha-1 receptor2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Discovery of a dopamine D4 selective PET ligand candidate taking advantage of a click chemistry based REM linker.
AID65925Effective concentration against human Dopamine receptor D42004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning.
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.
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.
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
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.
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.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
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.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1347024Rat D4 receptor (Dopamine receptors)2004Molecular pharmacology, Dec, Volume: 66, Issue:6
Certain 1,4-disubstituted aromatic piperidines and piperazines with extreme selectivity for the dopamine D4 receptor interact with a common receptor microdomain.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (23)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's10 (43.48)29.6817
2010's7 (30.43)24.3611
2020's6 (26.09)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.32

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 Index11.32 (24.57)
Research Supply Index3.18 (2.92)
Research Growth Index4.50 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.32)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (4.35%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other22 (95.65%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]