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Paroxetine (CID 43815) - Compound BioActivity Data
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BioActivity Outcomes:
Active(100)
 
 
Inactive(129)
 
 
Inconclusive(73)
 
 
Unspecified(220)
 
 
Top Targets:
7TM GPCR Srx(21)
 
 
 
 
 
p450(19)
 
 
 
 
7TM GPCR Srsx(18)
 
 
 
SLC6sbd SERT(16)
 
 
 
NR LBD ER(9)
 
 
 
 
BioAssay Types:
Literature(170)
 
 
 
 
 
Confirmatory(163)
 
 
 
 
Summary(24)
 
 
 
Screening(16)
 
 
BioActivity Types:
Potency(180)
 
 
 
 
IC50(153)
 
 
 
 
 
Ki(28)
 
 
 
Kd(5)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 498    Data Row: 522   Total Pages: 11   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID104234151]
Ki 4e-05Binding inhibition towards human serotonin transporter [AID254322, Type: Literature]Sodium-dependent serotonin transporter [gi:400630]
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2
[SID104234151]
Ki 7.7e-05Evaluated for affinity at 5-HT uptake site using [3H]paroxetine as radioligand in radioligand binding assay [AID205020, Type: other]
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3
[SID104234151]
IC50 8e-05DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) [AID625222, Type: other]Sodium-dependent serotonin transporter [gi:400630]
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4
[SID104234151]
Ki 9e-05Displacement of [3H]paroxetine from SERT receptor in human platelet membrane [AID302140, Type: Literature]Sodium-dependent serotonin transporter [gi:400630]
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5
[SID104234151]
Kd 0.00013Equilibrium dissociation constant (KD) for Competitive binding between [3H]- imipramine and the compound at human transporter-hSERT [AID204080, Type: Literature]
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6
[SID104234151]
Kd 0.00015The potency of the [3H]paroxetine for 5-HT transporters [AID204516, Type: Literature]
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7
[SID104234151]
IC50 0.0002Displacement of [125I]RTI-55 from human recombinant SERT expressed in HEK293 cells after 1 hr by scintillation counting analysis [AID739022, Type: Literature]Sodium-dependent serotonin transporter [gi:400630]
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8
[SID104234151]
IC50 0.00028Inhibition of [3H]paroxetine (0.2 nM) binding to 5-HT transporter [AID205038, Type: Literature]Sodium-dependent serotonin transporter [gi:400629]
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9
[SID104234151]
Ki 0.00031Displacement of [3H]-paroxetine from SERT in rabbit cortical membrane [AID587249, Type: Literature]
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10
[SID104234151]
Ki 0.00038Displacement of [3H]paroxetine from human SERT expressed in HEK293 cells [AID361596, Type: Literature]Sodium-dependent serotonin transporter [gi:400630]
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11
[SID104234151]
Ki 0.00038Displacement of [3H]paroxetine from human SERT expressed in HEK293 cells [AID408802, Type: Literature]Sodium-dependent serotonin transporter [gi:400630]
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12
[SID104234151]
Ki 0.00042Displacement of [3H]citalopram from human SERT expressed in HEK293 cells [AID361595, Type: Literature]Sodium-dependent serotonin transporter [gi:400630]
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13
[SID104234151]
Ki 0.00042Displacement of [3H]citalopram from human SERT expressed in HEK293 cells [AID408801, Type: Literature]Sodium-dependent serotonin transporter [gi:400630]
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14
[SID104234151]
Ki 0.00044Tested in vitro for serotonin(5-HT) neuronal uptake inhibition [AID134217, Type: Literature]
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15
[SID104234151]
Ki 0.00053Displacement of [3H]citalopram from rat cortical serotonin transporter (SERT) [AID204695, Type: Literature]Sodium-dependent serotonin transporter [gi:400629]
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16
[SID104234151]
Ki 0.00053Inhibition of [3H]citalopram binding to Serotonin transporter of rat cerebral cortex [AID204703, Type: Literature]Sodium-dependent serotonin transporter [gi:400629]
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17
[SID104234151]
Ki 0.0007Binding affinity to the serotonin transporter (SERT) measured by displacement of [3H]paroxetine in male wistar rats [AID204534, Type: Literature]
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18
[SID104234151]
Ki 0.00073Inhibition of [3H]5-HT reuptake into rat frontal cortex synaptosomes [AID186981, Type: Literature]
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19
[SID104234151]
IC50 0.002Inhibition of serotonin uptake at human SERT expressed in JAR cells [AID387488, Type: Literature]Sodium-dependent serotonin transporter [gi:400630]
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20
[SID104234151]
IC50 0.00643Inhibition of uptake of [3H]5-HT in synaptosomes from rat cortex [AID196387, Type: Literature]Sodium-dependent serotonin transporter [gi:400629]
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21
[SID104234151]
IC50 0.00643Evaluated for inhibition of 5-Hydroxytryptamine, biogenic amine reuptake in synaptosomal rat brain preparations [AID179549, Type: other]
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22
[SID104234151]
Ki 0.02Tested in vitro for norepinephrine (NE) neuronal uptake inhibition [AID134216, Type: Literature]
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23
[SID104234151]
Ki 0.033Inhibition of [3H]- NE reuptake into rat hippocampal synaptosomes [AID186980, Type: Literature]
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24
[SID104234151]
Kd 0.04Equilibrium dissociation constant (KD) for Competitive binding between [3H]- nisoxatine and the compound at human Norepinephrine transporter [AID145563, Type: Literature]
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25
[SID104234151]
Ki 0.08Displacement of [3H]-Nisoxetine from NET in rabbit cortical membrane [AID587250, Type: Literature]
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26
[SID104234151]
IC50 0.086DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) [AID625207, Type: other]Sodium-dependent noradrenaline transporter [gi:128616]
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27
[SID104234151]
Ki 0.09Binding inhibition towards human norepinephrine transporter [AID254338, Type: Literature]Sodium-dependent noradrenaline transporter [gi:128616]
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28
[SID104234151]
IC50 0.1Inhibition of norepinephrine uptake at human NET expressed in MDCK cells [AID387487, Type: Literature]Sodium-dependent noradrenaline transporter [gi:128616]
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29
[SID104234151]
IC50 0.123DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625155, Type: other]Muscarinic acetylcholine receptor M5 [gi:543761]
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30
[SID104234151]
IC50 0.145DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625151, Type: other]Muscarinic acetylcholine receptor M1 [gi:113118]
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31
[SID104234151]
IC50 0.16Evaluated for inhibition of norepinephrine, biogenic amine reuptake in synaptosomal rat brain preparations [AID179551, Type: other]
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32
[SID104234151]
IC50 0.179DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625153, Type: other]Muscarinic acetylcholine receptor M3 [gi:113125]
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33
[SID104234151]
IC50 0.244DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625154, Type: other]Muscarinic acetylcholine receptor M4 [gi:23503039]
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34
[SID104234151]
IC50 0.373DRUGMATRIX: Calcium Channel Type L, Benzothiazepine radioligand binding (ligand: [3H] Diltiazem) [AID625215, Type: other]
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35
[SID104234151]
Ki 0.4Inhibitory constant towards reuptake of [125I]-12 from dopamine transporter in rat striatal membranes [AID65494, Type: Literature]
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36
[SID104234151]
Ki 0.4Binding inhibition towards human dopamine transporter [AID254319, Type: Literature]Sodium-dependent dopamine transporter [gi:266667]
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37
[SID104234151]
Ki 0.46Tested in vitro for dopamine(DA) neuronal uptake inhibition [AID134215, Type: Literature]
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38
[SID104234151]
Kd 0.49Equilibrium dissociation constant (KD) for Competitive binding between [3H]WIN-35428 and the compound at human transporter-hDAT [AID64372, Type: Literature]
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39
[SID104234151]
IC50 0.532DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) [AID625152, Type: other]Muscarinic acetylcholine receptor M2 [gi:113122]
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40
[SID104234151]
IC50 0.535Inhibition of [3H]nisoxetine (0.5 nM) binding to Noradrenaline transporter [AID147593, Type: Literature]Norepinephrine transporter b (RNETb) [gi:81907603]
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41
[SID104234151]
IC50 0.623Displacement of [3H]WIN-35428(0.5 nM) from Dopamine transporter [AID64686, Type: Literature]Sodium-dependent dopamine transporter [gi:128613]
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42
[SID104234151]
Ki 0.6596Binding affinity against norepinephrine transporter (NET) by displacement of [3H]nisoxetine in male wistar rats [AID147740, Type: Literature]
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43
[SID104234151]
IC50 0.672DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) [AID625256, Type: other]Sodium-dependent dopamine transporter [gi:266667]
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44
[SID104234151]
IC50 0.747DRUGMATRIX: Calcium Channel Type L, Phenylalkylamine radioligand binding (ligand: [3H] (-)-Desmethoxyverapamil (D-888)) [AID625234, Type: other]
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45
[SID104234151]
Ki 0.769Displacement of [3H]-WIN 35,428 from DAT in rabbit striatal membrane [AID587251, Type: Literature]
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46
[SID104234151]
IC50 0.9Displacement of [125I]substance P from human recombinant NK1 receptor expressed in human U373 cells after 1 hr by scintillation counting analysis [AID739023, Type: Literature]Substance-P receptor [gi:128359]
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47
[SID104234151]
IC50 1DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) [AID625249, Type: other]Cytochrome P450 2D6 [gi:84028191]
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48
[SID104234151]
IC50 1.476DRUGMATRIX: Calcium Channel Type L, Dihydropyridine radioligand binding (ligand: [3H] Nitrendipine) [AID625216, Type: other]
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49
[SID104234151]
Ki 1.7Inhibition of [3H]- DA reuptake into rat striatal synaptosomes [AID186979, Type: Literature]
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50
[SID104234151]
IC50 1.87Antagonist activity at human P2X4 receptor expressed in 1321N1 cells assessed as inhibition of ATP-induced cytosolic calcium influx compound preincubated for 30 mins before ATP treatment by Fluo-4 AM fluorescence method [AID709142, Type: Literature]P2X purinoceptor 4 [gi:116242696]
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