|
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brain
|
None
|
90.0
nM
|
|
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brain
|
None
|
109.0
nM
|
|
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brain
|
None
|
140.0
nM
|
|
|
Binding affinity against norepinephrine transporter (NET) by displacement of [3H]nisoxetine in male wistar rats
|
None
|
719.0
nM
|
|
|
Inhibition of uptake of tritiated norepinephrine (NE) into rat brain synaptosomes
|
None
|
640.0
nM
|
|
Inhibition of uptake of tritiated norepinephrine (NE) into rat brain synaptosomes
|
None
|
760.0
nM
|
|
|
Inhibition of uptake of tritiated serotonin (5-HT) into rat brain synaptosomes
|
None
|
210.0
nM
|
|
Inhibition of uptake of tritiated serotonin (5-HT) into rat brain synaptosomes
|
None
|
100.0
nM
|
|
Inhibition of uptake of tritiated serotonin (5-HT) into rat brain synaptosomes
|
None
|
190.0
nM
|
|
|
Inhibition of [3H]- DA reuptake into rat striatal synaptosomes
|
None
|
360.0
nM
|
|
|
Inhibition of [3H]- NE reuptake into rat hippocampal synaptosomes
|
None
|
138.0
nM
|
|
|
Inhibition of [3H]5-HT reuptake into rat frontal cortex synaptosomes
|
None
|
37.0
nM
|
|
|
Equilibrium dissociation constant (KD) for Competitive binding between [3H]- imipramine and the compound at human transporter-hSERT
|
None
|
8.9
nM
|
|
|
Binding affinity to the serotonin transporter (SERT) measured by displacement of [3H]paroxetine in male wistar rats
|
None
|
52.0
nM
|
|
|
Displacement of [3H]nisoxetine from human norepinephrine transporter expressed in MDCK-Net6 cells
|
Homo sapiens
|
385.0
nM
|
|
|
Inhibition of norepinephrine uptake at human norepinephrine transporter expressed in MDCK-Net6 cells
|
Homo sapiens
|
535.0
nM
|
|
|
Inhibition of 5HT uptake at human SERT expressed in human JAR cells
|
Homo sapiens
|
31.0
nM
|
|
|
Inhibition of norepinephrine uptake at rat brain norepinephrine transporter
|
Rattus norvegicus
|
640.0
nM
|
|
|
Inhibition of 5HT uptake at rat brain SERT
|
Rattus norvegicus
|
210.0
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
|
0.0
%
|
|
|
Inhibition of [3H]5HT reuptake at rat brain frontal cortex serotonin transporter
|
Rattus norvegicus
|
350.0
nM
|
|
|
Inhibition of human NET transfected in MDCK-Net6 cells
|
Homo sapiens
|
535.0
nM
|
|
|
Inhibition of human SERT expressed in human JAR cells
|
Homo sapiens
|
27.0
nM
|
|
|
Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells
|
Homo sapiens
|
35.0
nM
|
|
|
Inhibition of norepinephrine reuptake at human NET expressed in MDCK cells
|
Homo sapiens
|
581.0
nM
|
|
|
Analgesic activity in mouse assessed as reduction of acetic acid-induced writhing at 30 mg/kg, po
|
Mus musculus
|
70.2
%
|
|
|
Anxiolytic activity in mouse assessed as inhibition of marble buried at 30 mg/kg, ip by marble burying test
|
Mus musculus
|
82.3
%
|
|
|
DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
|
None
|
7.18
nM
|
|
DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
|
None
|
3.814
nM
|
|
|
Inhibition of NET
|
None
|
149.0
nM
|
|
|
Inhibition of SERT
|
None
|
20.0
nM
|
|
|
Displacement of [3H]-nisoxetine from Sprague-Dawley rat brain NET after 1 hr
|
Rattus norvegicus
|
500.0
nM
|
|
|
Displacement of [3H]-citalopram from Sprague-Dawley rat brain SERT after 1 hr
|
Rattus norvegicus
|
25.0
nM
|
|
|
Displacement of [3H]WIN35428 from human DAT transfected in HEK293 cells after 3 hrs by Wallac counting analysis
|
Homo sapiens
|
890.0
nM
|
|
|
Displacement of [3H]Nisoxetine from human NET transfected in HEK293 cells after 3 hrs by Wallac counting analysis
|
Homo sapiens
|
680.0
nM
|
|
Displacement of [3H]Nisoxetine from human NET transfected in HEK293 cells after 3 hrs by Wallac counting analysis
|
Homo sapiens
|
553.0
nM
|
|
|
Displacement of [3H]citalopram from human SERT transfected in HEK293 cells after 3 hrs by Wallac counting analysis
|
Homo sapiens
|
20.0
nM
|
|
Displacement of [3H]citalopram from human SERT transfected in HEK293 cells after 3 hrs by Wallac counting analysis
|
Homo sapiens
|
11.0
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
|
113.0
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
|
323.59
nM
|
|
|
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
|
56.0
%
|
|
|
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
|
9.0
%
|
|
|
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
|
36.1
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
|
37.0
%
|
|
|
Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells at 1 uM after 15 mins by fluorescence neurotransmitter transporter assay
|
Homo sapiens
|
86.0
%
|
|
|
Inhibition of DA reuptake at human DAT expressed in HEK293 cells at 10 uM after 15 mins by fluorescence neurotransmitter transporter assay
|
Homo sapiens
|
56.0
%
|
|
|
Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells at 10 uM after 15 mins by fluorescence neurotransmitter transporter assay
|
Homo sapiens
|
92.0
%
|
|
|
Inhibition of norepinephrine reuptake at human NET expressed in HEK293 cells at 10 uM after 15 mins by fluorescence neurotransmitter transporter assay
|
Homo sapiens
|
81.0
%
|
|
|
Inhibition of DA reuptake at human DAT expressed in HEK293 cells at 1 uM after 15 mins by fluorescence neurotransmitter transporter assay
|
Homo sapiens
|
16.0
%
|
|
|
Antidepressant activity in rat assessed as reduction in immobility time at 30 mg/kg, po by forced swimming test relative to control
|
Rattus norvegicus
|
14.0
%
|
|
|
Binding affinity to human SERT expressed in HEK293 cells after 60 mins in presence of [3H]imipramine by liquid scintillation counting
|
Homo sapiens
|
39.0
nM
|
|
|
Binding affinity to human NET expressed in HEK293 cells after 60 mins in presence of [3H]imipramine by liquid scintillation counting
|
Homo sapiens
|
210.0
nM
|
|
|
Inhibition of human SERT expressed in HEK293 cells assessed as decrease in [3H]-serotonin reuptake after 10 mins by scintillation counting method
|
Homo sapiens
|
20.0
nM
|
|
|
Inhibition of human NET expressed in MDCK cells assessed as decrease in [3H]-noradrenaline reuptake after 10 mins by scintillation counting method
|
Homo sapiens
|
149.0
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
|
0.44
%
|
|
|
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
|
0.11
%
|
|
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
|
0.11
%
|
|
