|
Binding affinity at 5-hydroxytryptamine 2 receptor by the inhibition of binding to [3H]ketanserin in rat cortical membranes
|
Rattus norvegicus
|
100.0
nM
|
|
|
Binding affinity for human alpha-2 adrenergic receptor expressed in CHO cell
|
Homo sapiens
|
6.31
nM
|
|
|
Binding affinity against rat cortical alpha-1 adrenergic receptor labeled with [3H]prazosin radioligand
|
None
|
605.0
nM
|
|
|
Binding affinity at dopamine receptor D2 by the inhibition of binding to [3H]spiperone in rat striatal membranes
|
None
|
100.0
nM
|
|
|
Binding affinity towards dopamine receptor D2 at 1.0 uM concentration
|
None
|
12.0
%
|
|
|
Tested in vitro for norepinephrine (NE) neuronal uptake inhibition
|
None
|
85.0
nM
|
|
|
Tested in vitro for serotonin(5-HT) neuronal uptake inhibition
|
None
|
10.8
nM
|
|
|
Ability to inhibit high affinity reuptake of [3H]-NE (Norepinephrine transporter) into nerve ending synaptosomes prepared from brain regions
|
None
|
167.0
nM
|
|
|
Inhibition of [3H]NE uptake by Norepinephrine transporter of rat occipital cortex synaptosomes
|
Rattus norvegicus
|
176.0
nM
|
|
|
Equilibrium dissociation constant (KD) for Competitive binding between [3H]- nisoxatine and the compound at human Norepinephrine transporter
|
None
|
240.0
nM
|
|
|
Inhibition of norepinephrine transporter by inhibition of [3H]NE uptake into rat nerve endings (synaptosomes)
|
None
|
176.0
nM
|
|
|
Evaluated for inhibition of 5-Hydroxytryptamine, biogenic amine reuptake in synaptosomal rat brain preparations
|
Rattus norvegicus
|
308.0
nM
|
|
|
In vitro inhibition of serotonin (5-HT) uptake in crude rat brain synaptosomes
|
Rattus norvegicus
|
70.0
nM
|
|
|
Compound was evaluated for its ability to antagonizing norepinephrine (NE) high affinity uptake was determined using [3H]NE on synaptosomes prepared from rat occipital cortices.
|
Rattus norvegicus
|
193.0
nM
|
|
|
Compound was evaluated for its ability to antagonizing serotonin high affinity uptake was determined using [3H]5-HT on synaptosomes prepared from rat midbrain or parietal cortices.
|
Rattus norvegicus
|
8.1
nM
|
|
|
Inhibition of [3H]- NE reuptake into rat hippocampal synaptosomes
|
None
|
143.0
nM
|
|
|
Inhibition of [3H]5-HT reuptake into rat frontal cortex synaptosomes
|
None
|
14.0
nM
|
|
|
Inhibition of serotonin uptake into rat synaptosomes
|
Rattus norvegicus
|
48.0
nM
|
|
|
Inhibition of neuronal uptake of 5 - Hydroxytryptamine in rat brain homogenate
|
None
|
130.0
nM
|
|
|
In vitro binding affinity was determined against NA (noradrenaline) reuptake site of rat in presence of [3H]nisoxetine radioligand
|
Rattus norvegicus
|
794.33
nM
|
|
|
In vitro binding affinity was determined against serotonin reuptake site of rat in presence of [3H]paroxetine radioligand
|
Rattus norvegicus
|
10.0
nM
|
|
|
Compound was evaluated for inhibition of 5-HT uptake by measuring its ability to inhibit [3H]paroxetine binding to rat cortical membranes
|
None
|
15.0
nM
|
|
|
Inhibition of [3H]peroxitine binding to rat cortical membranes as measure of inhibitory activity towards 5-HT uptake
|
None
|
15.0
nM
|
|
|
Inhibition of high affinity re-uptake of [3H]5-HT (serotonin) into nerve ending synaptosomes
|
None
|
7.3
nM
|
|
|
The compound was tested for affinity towards sigma-3 receptor
|
None
|
851.14
nM
|
|
|
Binding affinity towards serotonin S1 receptor at 1.0 uM
|
Rattus norvegicus
|
13.0
%
|
|
|
Inhibition concentration against [3H]5-HT uptake by human serotonin transporter in JAR cells
|
None
|
32.4
nM
|
|
|
Equilibrium dissociation constant (KD) for Competitive binding between [3H]- imipramine and the compound at human transporter-hSERT
|
None
|
0.81
nM
|
|
|
Compound was evaluated for its binding affinity towards human serotonin transporter
|
None
|
3.5
nM
|
|
|
Binding affinity against serotonin transporter in rat cortical tissues using radioligand [3H]paroxetine
|
None
|
2.72
nM
|
|
|
Displacement of [3H]citalopram from rat cortical serotonin transporter (SERT)
|
Rattus norvegicus
|
22.13
nM
|
|
|
Inhibition of [3H]5-HT uptake by Serotonin transporter of rat midbrain or parietal synaptosomes
|
Rattus norvegicus
|
7.3
nM
|
|
|
Inhibition of [3H]citalopram binding to Serotonin transporter of rat cerebral cortex
|
Rattus norvegicus
|
22.13
nM
|
|
|
Inhibition of [3H]5-HT uptake into rat synaptosomes by Serotonin transporter
|
Rattus norvegicus
|
7.3
nM
|
|
|
Binding affinity against Serotonin transporter in rat cerebral cortex using [3H]paroxetine binding assay.
|
None
|
6.31
nM
|
|
|
Evaluated for affinity at 5-HT uptake site using [3H]paroxetine as radioligand in radioligand binding assay
|
None
|
3.17
nM
|
|
|
Binding affinity at alpha-1-adrenoceptor by the inhibition of binding to [3H]prazosin in rat cortical membranes
|
Rattus norvegicus
|
100.0
nM
|
|
|
Inhibition constant against serotonin transporter
|
Homo sapiens
|
48.0
nM
|
|
|
Binding inhibition towards human serotonin transporter
|
Homo sapiens
|
0.72
nM
|
|
|
Binding inhibition towards human norepinephrine transporter
|
Homo sapiens
|
440.0
nM
|
|
|
Displacement of [3H]paroxetine from 5-HT transporter in Sprague-Dawley rat cortical membranes
|
Rattus norvegicus
|
3.9
nM
|
|
|
Inhibition of [3H]5-HT uptake at human 5-HT transporter expressed in Jar cells
|
Homo sapiens
|
39.4
nM
|
|
|
Inhibition of [3H]5-HT reuptake at 5HT transporter in HEK293 cells
|
Homo sapiens
|
16.0
nM
|
|
|
Inhibition of [3H]5-HT uptake at 5HT transporter expressed in HEK293 cells
|
Homo sapiens
|
16.0
nM
|
|
|
Binding affinity to rat SERT
|
Rattus norvegicus
|
2.8
nM
|
|
|
Binding affinity to human SERT
|
Homo sapiens
|
2.0
nM
|
|
|
Displacement of [3H]citalopram from Sprague-Dawley rat SERT
|
Rattus norvegicus
|
8.7
nM
|
|
|
Binding affinity to rat SERT
|
Rattus norvegicus
|
2.9
nM
|
|
|
Binding affinity to human SERT
|
Homo sapiens
|
2.2
nM
|
|
|
Binding affinity at rat SERT
|
Rattus norvegicus
|
2.9
nM
|
|
|
Binding affinity at human SERT
|
Homo sapiens
|
2.2
nM
|
|
|
Binding affinity to rat SERT
|
Rattus norvegicus
|
2.9
nM
|
|
|
Binding affinity to human SERT
|
Homo sapiens
|
2.2
nM
|
|
|
Inhibition of SERT
|
None
|
180.0
nM
|
|
|
Inhibition of serotonin reuptake site of serotonin transporter at 1 nM
|
None
|
50.0
%
|
|
|
Inhibition of sigma opioid receptor at 100 nM
|
None
|
50.0
%
|
|
|
Inhibition of histamine H1 receptor at 100 nM
|
None
|
50.0
%
|
|
|
Inhibition of 5HT2 receptor at 100 nM
|
None
|
50.0
%
|
|
|
Inhibition of low conductance potassium channel at 100 nM
|
None
|
50.0
%
|
|
|
Inhibition of norepinephrine reuptake site of norepinephrine transporter at 100 nM
|
None
|
50.0
%
|
|
|
Inhibition of 5HT uptake at human SERT expressed in human JAR cells
|
Homo sapiens
|
9.4
nM
|
|
|
Displacement of [3H]paroxetine from rat cortical 5HTT reuptake site
|
Rattus norvegicus
|
2.7
nM
|
|
|
Inhibition of serotonin uptake at human SERT in human HEK293 cells
|
Homo sapiens
|
47.0
nM
|
|
|
Inhibition of norepinephrine uptake at human NET expressed in MDCK-Net6 cells
|
Homo sapiens
|
563.0
nM
|
|
|
Inhibition of serotonin uptake at human SERT expressed in human JAR cells
|
Homo sapiens
|
10.0
nM
|
|
|
Inhibition of serotonin uptake at human SERT expressed in HEK cells
|
Homo sapiens
|
47.0
nM
|
|
|
Inhibition of norepinephrine uptake at human NET expressed in MDCK cells
|
Homo sapiens
|
563.0
nM
|
|
|
Inhibition of serotonin uptake at human SERT expressed in JAR cells
|
Homo sapiens
|
10.0
nM
|
|
|
Displacement of [3H]paroxetine from serotonin transporter in Sprague-Dawley rat frontal cortical membrane
|
Rattus norvegicus
|
3.9
nM
|
|
|
Inhibition of 5-HT transporter-mediated [3H]5HT uptake in human Jar cells
|
Homo sapiens
|
39.4
nM
|
|
|
Displacement of [125I]RTI-55 from human recombinant SERT expressed in HEK293 cells by scintillation counting
|
Homo sapiens
|
1.1
nM
|
|
|
Displacement of [3H]serotonin from human recombinant SERT expressed in HEK293 cells by scintillation counting
|
Homo sapiens
|
7.3
nM
|
|
|
Inhibition of [3H]5-hydroxytryptamine reuptake at human SERT expressed in african green monkey COS7 cells at 100 nM
|
Homo sapiens
|
26.1
%
|
|
|
Inhibition of [3H]dopamine reuptake at human NET expressed in african green monkey COS7 cells at 100 nM
|
Homo sapiens
|
1.0
%
|
|
|
Inhibition of serotonin uptake at human SERT expressed in JAR cells
|
Homo sapiens
|
9.4
nM
|
|
|
Displacement of [3H]citalopram from SERT in Sprague-dawley rat frontal cortex by liquid scintillation spectrophotometry
|
Rattus norvegicus
|
48.0
nM
|
|
|
Displacement of [125I]RTI55 from human recombinant SERT expressed in HEK293 cells
|
Homo sapiens
|
1.1
nM
|
|
|
Inhibition of [3H]5HT from human recombinant SERT expressed in HEK293 cells
|
Homo sapiens
|
7.0
nM
|
|
|
Inhibition of human recombinant CYP2D6 at 5 uM assessed as blockade of O-demethylation of dextromethorphan in to dextrophan by nanoscale automated in-capillary assay
|
Homo sapiens
|
20.0
%
|
|
|
Antagonist activity at human 5HT3A receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced inward Na+ current at >= 10 uM
|
Homo sapiens
|
50.0
%
|
|
|
Displacement of [3H]paroxetine from 5HT transporter in rat cortical membrane
|
Rattus norvegicus
|
2.7
nM
|
|
|
Inhibition of [3H]hydroxytryptamine creatinine sulfate uptake at human SERT expressed in human JAR cells
|
Homo sapiens
|
9.4
nM
|
|
|
Inhibition of human SERT expressed in JAR cells
|
Homo sapiens
|
9.4
nM
|
|
|
Inhibition of serotonin uptake at human SERT expressed in JAR cells
|
Homo sapiens
|
9.4
nM
|
|
|
Displacement of [I125]RTI-55 from human SERT transfected in human HEK293 cells
|
Homo sapiens
|
2.5
nM
|
|
|
Inhibition of [3H]5HT uptake at SERT in rat brain hippocampal synaptosomes by liquid scintillation spectrophotometry
|
Rattus norvegicus
|
41.0
nM
|
|
|
Inhibition of serotonin uptake at human SERT expressed in human JAR cells
|
Homo sapiens
|
9.4
nM
|
|
|
Inhibition of human SERT expressed in human JAR cells
|
Homo sapiens
|
9.4
nM
|
|
|
Inhibition of AChE
|
None
|
130.0
nM
|
|
|
Inhibition of SERT-mediated serotonin uptake in human JAR cells
|
Homo sapiens
|
9.4
nM
|
|
|
Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells
|
Homo sapiens
|
3.1
nM
|
|
|
Displacement of [3H]paroxetine from SERT in rat cerebral cortex
|
Rattus norvegicus
|
12.6
nM
|
|
|
Anxiolytic activity in mouse assessed as inhibition of marble buried at 10 mg/kg, ip by marble burying test
|
Mus musculus
|
60.3
%
|
|
|
Inhibition of [3H]serotonin reuptake at human SERT expressed in HEK293 cells by scintillation counting
|
Homo sapiens
|
5.2
nM
|
|
|
Inhibition of human ERG
|
Homo sapiens
|
457.09
nM
|
|
|
Inhibition of [3H]serotonin reuptake at human recombinant SERT expressed in LLC-PK1 cells by liquid scintillation counting
|
Homo sapiens
|
5.012
nM
|
|
|
Inhibition of NET in rat cerebral cortex assessed as [3H]norepinephrine accumulation
|
Rattus norvegicus
|
120.0
nM
|
|
|
Inhibition of SERT in rat cerebral cortex assessed as [3H]serotonin accumulation
|
Rattus norvegicus
|
12.2
nM
|
|
|
Inhibition of serotonin reuptake at SERT expressed in HEK293 cells
|
None
|
5.012
nM
|
|
|
Inhibition of human SERT expressed in JAR cells assessed as serotonin uptake
|
Homo sapiens
|
9.4
nM
|
|
|
DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
771.0
nM
|
|
|
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
762.0
nM
|
|
|
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
976.0
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
|
None
|
194.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
|
None
|
55.0
nM
|
|
|
DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
|
None
|
698.0
nM
|
|
|
DRUGMATRIX: Calcium Channel Type L, Benzothiazepine radioligand binding (ligand: [3H] Diltiazem)
|
Rattus norvegicus
|
827.0
nM
|
|
DRUGMATRIX: Calcium Channel Type L, Benzothiazepine radioligand binding (ligand: [3H] Diltiazem)
|
Rattus norvegicus
|
736.0
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
|
None
|
119.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
|
None
|
62.0
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
771.0
nM
|
|
|
DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
|
None
|
0.51
nM
|
|
DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
|
None
|
0.271
nM
|
|
|
DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
|
None
|
499.0
nM
|
|
DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
|
None
|
210.0
nM
|
|
|
DRUGMATRIX: Sodium Channel, Site 2 radioligand binding (ligand: [3H] Batrachotoxin)
|
Rattus norvegicus
|
90.0
nM
|
|
DRUGMATRIX: Sodium Channel, Site 2 radioligand binding (ligand: [3H] Batrachotoxin)
|
Rattus norvegicus
|
82.0
nM
|
|
|
DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
None
|
700.0
nM
|
|
|
Inhibition of human SERT-mediated serotonin reuptake in HEK293 cells
|
Homo sapiens
|
2.7
nM
|
|
|
TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: ? uM, Fluoxetine: 100 uM) in MDR1-expressing MDCKII cells
|
None
|
23.5
%
|
|
|
Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting
|
Homo sapiens
|
21.8
%
|
|
|
Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting
|
Homo sapiens
|
14.3
%
|
|
|
Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting
|
Homo sapiens
|
22.6
%
|
|
|
Antidepressant activity in Mus musculus Kunming (mouse) assessed as reduction in duration of immobility at 10 mg/kg, ip measured after 30 min by forced swim test
|
Mus musculus
|
39.36
%
|
|
|
Displacement of [3H]-citalopram from SERT in rat cerebral cortex after 1 hr by liquid scintillation counting analysis
|
Rattus norvegicus
|
12.7
nM
|
|
|
Inhibition of [3H]5-HT uptake at human SERT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay
|
Homo sapiens
|
98.0
nM
|
|
Inhibition of [3H]5-HT uptake at human SERT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay
|
Homo sapiens
|
281.84
nM
|
|
|
Displacement of [3H]Paroxetine from human recombinant SERT expressed in HEK293 cells after 60 mins
|
Homo sapiens
|
1.4
nM
|
|
Displacement of [3H]Paroxetine from human recombinant SERT expressed in HEK293 cells after 60 mins
|
Homo sapiens
|
8.6
nM
|
|
|
Displacement of [3H]Paroxetine from human recombinant SERT expressed in HEK293 cells at 10 uM after 60 mins relative to control
|
Homo sapiens
|
6.0
%
|
|
|
Displacement of [3H]imipramin from human recombinant SERT over-expressed in HEK293 cells
|
Homo sapiens
|
7.2
nM
|
|
|
Inhibition of human DAT-mediated dopamine uptake expressed in HEK293 cells at 10 uM after 15 mins by fluorescence plate reader analysis
|
Homo sapiens
|
31.0
%
|
|
|
Inhibition of human NET-mediated norepinephrine uptake expressed in HEK293 cells at 10 uM after 15 mins by fluorescence plate reader analysis
|
Homo sapiens
|
56.0
%
|
|
|
Inhibition of human SERT-mediated serotonin uptake expressed in HEK293 cells at 10 uM after 15 mins by fluorescence plate reader analysis
|
Homo sapiens
|
89.0
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
55.32
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
77.22
%
|
|
|
Inhibition of human ERG
|
Homo sapiens
|
10.0
nM
|
|
|
Displacement of [3H]-dopamine from rat cerebral cortex NET after 7 mins
|
Rattus norvegicus
|
158.0
nM
|
|
|
Displacement of [3H]5-HT from rat cerebral cortex SERT after 10 mins
|
Rattus norvegicus
|
12.2
nM
|
|
|
Cytotoxicity against human L02 cells assessed as inhibitory rate at 80 uM after 24 hrs by MTT assay
|
Homo sapiens
|
28.5
%
|
|
|
Cytotoxicity against human HEK293 cells assessed as inhibitory rate at 80 uM after 24 hrs by MTT assay
|
Homo sapiens
|
55.8
%
|
|
|
Displacement of [3H]citalopram from SERT in Sprague-Dawley rat whole brain membranes after 1 hr by liquid scintillation spectrophotometric analysis
|
Rattus norvegicus
|
5.6
nM
|
|
|
Displacement of [3H]mesulergine from 5-HT2C receptor in Sprague-Dawley rat choroid plexus membranes after 30 mins by liquid scintillation spectrophotometric analysis
|
Rattus norvegicus
|
109.0
nM
|
|
|
Cytotoxicity against human L02 cells as inhibition of cell viability at 80 uM after 24 hrs by MTT assay
|
Homo sapiens
|
28.5
%
|
|
|
Cytotoxicity against human HEK293 cells as inhibition of cell viability at 80 uM after 24 hrs by MTT assay
|
Homo sapiens
|
55.8
%
|
|
|
Antidepressant-like activity in C57 mouse assessed as reduction in immobility time at 32 mg/kg, ip administered from day 2 to 15 measured on 2nd and 15th day 30 mins after drug challenge by forced swim test
|
Mus musculus
|
50.7
%
|
|
|
Antidepressant activity in C57BL/6 mouse assessed as decrease in immobility duration at 10 mg/kg, ig by tail suspension test
|
Mus musculus
|
39.4
%
|
|
|
Antidepressant activity in C57BL/6 mouse assessed as decrease in immobility duration at 10 mg/kg, ig by forced swim test
|
Mus musculus
|
29.0
%
|
|
|
Inhibition of human SERT expressed in HEK293 cells at 0.1 uM incubated for 15 mins by neurotransmitter reuptake assay
|
Homo sapiens
|
44.0
%
|
|
|
Inhibition of human NET expressed in HEK293 cells at 0.1 uM incubated for 15 mins by neurotransmitter reuptake assay
|
Homo sapiens
|
5.0
%
|
|
|
Inhibition of human DAT expressed in HEK293 cells at 0.1 uM incubated for 15 mins by neurotransmitter reuptake assay
|
Homo sapiens
|
6.0
%
|
|
|
Inhibition of human SERT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay
|
Homo sapiens
|
150.0
nM
|
|
|
Antidepressant-like activity in Swiss albino mouse assessed as decrease in immobility time at 20 mg/kg, ip measured for 5 mins by forced swimming test relative to control
|
Mus musculus
|
69.82
%
|
|
|
Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells at 0.1 uM after 15 mins by fluorescence neurotransmitter transporter assay
|
Homo sapiens
|
44.0
%
|
|
|
Inhibition of norepinephrine reuptake at human NET expressed in HEK293 cells at 0.1 uM after 15 mins by fluorescence neurotransmitter transporter assay
|
Homo sapiens
|
5.0
%
|
|
|
Inhibition of DA reuptake at human DAT expressed in HEK293 cells at 0.1 uM after 15 mins by fluorescence neurotransmitter transporter assay
|
Homo sapiens
|
6.0
%
|
|
|
Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
|
Homo sapiens
|
150.0
nM
|
|
|
Inhibition of norepinephrine reuptake at human NET expressed in HEK293 cells at 1 uM after 15 mins by fluorescence neurotransmitter transporter assay
|
Homo sapiens
|
8.0
%
|
|
|
Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells at 1 uM after 15 mins by fluorescence neurotransmitter transporter assay
|
Homo sapiens
|
84.0
%
|
|
|
Inhibition of DA reuptake at human DAT expressed in HEK293 cells at 10 uM after 15 mins by fluorescence neurotransmitter transporter assay
|
Homo sapiens
|
31.0
%
|
|
|
Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells at 10 uM after 15 mins by fluorescence neurotransmitter transporter assay
|
Homo sapiens
|
89.0
%
|
|
|
Inhibition of norepinephrine reuptake at human NET expressed in HEK293 cells at 10 uM after 15 mins by fluorescence neurotransmitter transporter assay
|
Homo sapiens
|
56.0
%
|
|
|
Inhibition of DA reuptake at human DAT expressed in HEK293 cells at 1 uM after 15 mins by fluorescence neurotransmitter transporter assay
|
Homo sapiens
|
5.0
%
|
|
|
Binding affinity to Wistar rat brain lipid by TRANSIL assay
|
Rattus norvegicus
|
323.0
nM
|
|
|
Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
12.0
%
|
|
|
Time dependent inhibition of CYP2B6 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2C9 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP3A4 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2C8 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2C19 in human liver microsomes at 30 uM by LC/MS system
|
Homo sapiens
|
36.0
%
|
|
|
Time dependent inhibition of CYP2D6 (unknown origin) at 10 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Inhibition of CYP2C19 (unknown origin) using luciferin tagged substrate preincubated for 10 mins before substrate addition
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibition of of human TREK1 expressed in tsA201 cells assessed as reduction in channel currents at 100 uM
|
Homo sapiens
|
84.0
%
|
|
|
Inhibition of of human TASK3 expressed in HEK293 cells assessed as reduction in channel currents at 10 uM
|
Homo sapiens
|
31.0
%
|
|
|
Binding Assay: 5-HT transporter binding assay for evaluating binding of the compound to the serotonin transporter was carried out using human recombinant serotonin transporter membrane (PerkinElmer Life and Analytical Sciences, USA) expressed in HEK293 cells and radioisotope [3H]Imipramine (PerkinElmer).That is, the test drug, 2 nM [3H]Imipramine, serotonin transporter membrane (9 ug/well), 120 mM NaCl and 50 mM Tris-HCl buffer (pH 7.4) containing 5 mM KCl were added to obtain a reaction mixture with a final volume of 0.25 ml. After incubation for 30 minutes at 27° C., the mixture was quickly passed through a Filtermat A glass fiber filter (PerkinElmer) pre-soaked with 0.5% (w/v) PEI (polyethyleneimine) using Inotech Harvester (Inotech) to terminate the reaction. After washing with cold washing buffer (50 mM Tris-HCl, pH 7.4, 154 mM NaCl) solution, the filter was covered with MeltiLex and sealed in a sample bag. After drying in an oven, radioactivity was counted using MicroBeta Plus (Wallac).
|
Homo sapiens
|
3.58
nM
|
|
|
Antibacterial activity against Staphylococcus aureus MRSA ATCC 43300 (CO-ADD:GP_020); MIC in CAMBH media, using NBS plates, by OD(600)
|
Staphylococcus aureus subsp. aureus
|
7.53
%
|
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
3.0
%
|
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
7.93
%
|
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
5.21
%
|
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
-2.58
%
|
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
1.88
%
|
|
|
Antifungal activity against Cryptococcus neoformans H99 ATCC 208821 (CO-ADD:FG_002); MIC in YNB media using NBS plates, by Resazurin OD(600-570)
|
Cryptococcus neoformans
|
2.51
%
|
|
|
Inhibition of rat synaptosome SERT
|
Rattus norvegicus
|
180.0
nM
|
|
|
Antiviral activity against DENV2 infected in human Huh7 cells by qRT-PCR analysis
|
Dengue virus 2
|
380.0
nM
|
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
7.92
%
|
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
0.26
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
0.26
%
|
|
|
Growth inhibiting activity of Naegleria gruberi in vitro
|
Naegleria gruberi
|
7.5
%
|
|
|
Displacement of [3H]ketanserin from 5HT2A receptor (unknown origin) by cell based radioligand competitive binding analysis
|
Homo sapiens
|
710.0
nM
|
|
|
Displacement of [3H]mesulergine from 5-HT2C receptor (unknown origin) by cell based radioligand competitive binding analysis
|
Homo sapiens
|
160.0
nM
|
|
|
Displacement of [3H]imipramine from SERT receptor (unknown origin) by cell based radioligand competitive binding analysis
|
Homo sapiens
|
4.0
nM
|
|
|
Inhibition of CYP2C19 (unknown origin)
|
Homo sapiens
|
65.0
nM
|
|
|
Antidepressant activity in mouse assessed as reduction in duration of immobility at 3 mg/kg, ip relative to control
|
Mus musculus
|
48.9
%
|
|
|
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth
|
Homo sapiens
|
10.0
nM
|
|
|
Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in Sprague-Dawley rat brain membranes by scintillation counting method
|
Rattus norvegicus
|
240.0
nM
|
|
|
Inhibition of SERT (unknown origin)
|
Homo sapiens
|
3.58
nM
|
|
|
Displacement of [3H]citalopram from human SERT in HEK293 cells by Topcount scintillation analysis
|
Homo sapiens
|
31.0
nM
|
|
