|
Binding affinity towards 5-hydroxytryptamine 2 receptor
|
None
|
23.0
nM
|
|
|
Binding affinity towards 5-hydroxytryptamine 2A receptor using [3H]ketanserin
|
None
|
94.0
nM
|
|
|
Displacement of [3H]ketanserin from 5-hydroxytryptamine 2A receptor expressed NIH3T3 cells
|
None
|
160.0
nM
|
|
|
Binding affinity to 5-hydroxytryptamine 2C receptor using [3H]Mesulergine as radioligand in stably transfected NIH3T3 cells
|
None
|
160.0
nM
|
|
|
Binding affinity towards 5-hydroxytryptamine 2C receptor using [3H]mesulergine as radioligand
|
None
|
160.0
nM
|
|
|
Compound was tested for its inhibitory activity against 5-hydroxytryptamine receptor
|
Rattus norvegicus
|
44.0
nM
|
|
|
Compound was tested for its binding affinity towards brain (Hippocampus) Adenylate cyclase
|
Cavia porcellus
|
160.0
nM
|
|
|
Compound was tested for its binding affinity towards brain (neocortex) Adenylate cyclase
|
Cavia porcellus
|
160.0
nM
|
|
|
In vitro binding affinity at Alpha-1 adrenergic receptor by radioligand binding assay using [3H]prazosin
|
None
|
46.0
nM
|
|
|
Concentration of compound for 50% displacement of [3H]WB-4101 from Alpha-1 adrenergic receptor of rat brain
|
None
|
160.0
nM
|
|
|
In vitro binding affinity at Alpha-2 adrenergic receptor in rat cortex by radioligand binding assay using [3H]rauwolscine
|
None
|
255.0
nM
|
|
|
Binding affinity to Dopamine receptor D2 using [3H]spiperone as radioligand in stably transfected NIH3T3 cells
|
None
|
726.0
nM
|
|
|
Concentration of compound for 50% displacement of [3H]spiperone from Dopamine receptor in rat brain
|
None
|
645.0
nM
|
|
|
Binding affinity towards dopamine receptor D2 using [3H]spiperone as radioligand
|
None
|
726.0
nM
|
|
|
Binding affinity towards dopamine receptor D2 at 1.0 uM concentration
|
None
|
63.0
%
|
|
|
Concentration required to reducing the histamine induced contraction by 50% was measured
|
Cavia porcellus
|
0.032
ug.mL-1
|
|
|
Compound tested for its inhibitory activity against Histamine H1 receptor
|
None
|
0.06
nM
|
|
|
Binding affinity towards histamine receptor by inhibiting specific binding of [3H]-mepyramine (3 nM) in vitro to membranes of rat brain without cerebellum
|
None
|
30.0
nM
|
|
|
Inhibition of binding of [3H]imipramine to imipramine receptor in rat brain
|
None
|
1.7
nM
|
|
|
Binding affinity against imipramine receptor was determined in homogenized rat cortex tissue using [3H]-imipramine as radioligand
|
Rattus norvegicus
|
12.0
nM
|
|
|
Compound at an intraperitoneal dose of 10 mg/Kg was tested for the inhibition of abdominal constriction in mice
|
Mus musculus
|
100.0
%
|
|
|
In vitro activity for the ability to inhibit the uptake of Serotonin into mouse cortical slices.
|
Mus musculus
|
300.0
nM
|
|
|
In vitro inhibition of accumulation of [14C]5-HT (5-HT) in mouse brain slices
|
None
|
300.0
nM
|
|
|
Tested in vitro for norepinephrine (NE) neuronal uptake inhibition
|
None
|
12.0
nM
|
|
|
Tested in vitro for serotonin(5-HT) neuronal uptake inhibition
|
None
|
42.0
nM
|
|
|
Concentration of compound for 50% displacement of [3H]QNB from Muscarinic acetylcholine receptor in rat brain
|
None
|
269.0
nM
|
|
|
Binding affinity against Muscarinic acetylcholine receptor was determined in homogenized rat cortex tissue using [3H]N-methylscopolamine as radioligand
|
None
|
65.0
nM
|
|
|
Binding affinity towards muscarinic acetylcholine receptor by inhibiting specific binding of [3H]quinuclidinyl benzilate (0.8 nM) in vitro to membranes of rat brain without cerebellum
|
None
|
300.0
nM
|
|
|
Binding affinity to Norepinephrine transporter using [3H]-nisoxatine as radioligand in stably transfected NIH3T3 cells
|
None
|
16.0
nM
|
|
|
Binding affinity towards Norepinephrine transporter using [3H]nisoxitine as radioligand
|
None
|
16.0
nM
|
|
|
Compound was tested for its inhibitory activity against Noradrenaline receptor
|
Rattus norvegicus
|
46.0
nM
|
|
|
Concentration of compound to inhibit 50% of [3H]norepinephrine neurotransmitter uptake in rat brain
|
Rattus norvegicus
|
169.0
nM
|
|
|
Concentration of compound to inhibit 50% of [3H]-5-HT neurotransmitter uptake in rat brain
|
Rattus norvegicus
|
384.0
nM
|
|
|
Concentration required for its norepinephrine reuptake inhibitory activity in synaptosomal rat hyphalamic preparations
|
Rattus norvegicus
|
105.0
nM
|
|
|
In vitro inhibitory activity against [3H]5-HT uptake into crude synaptosomes from whole rat brain.
|
Rattus norvegicus
|
240.0
nM
|
|
|
Inhibition of 5-HT uptake in synaptosomal preparation from rat corpus striatum, using [3H]5-HT
|
Rattus norvegicus
|
810.0
nM
|
|
|
Inhibition of Norepinephrine uptake from rat diencephalon-midbrain
|
Rattus norvegicus
|
27.0
nM
|
|
|
Inhibition of norepinephrine uptake in synaptosomal preparation fro rat hypothalamus, using [3H]norepinephrine
|
None
|
60.0
nM
|
|
|
Inhibition of uptake of tritiated norepinephrine (NE) into rat brain synaptosomes
|
None
|
260.0
nM
|
|
|
Inhibition of uptake of tritiated serotonin (5-HT) into rat brain synaptosomes
|
None
|
120.0
nM
|
|
|
Inhibitory activity against uptake of [3H]norepinephrine into rat brain synaptosomes.
|
Rattus norvegicus
|
85.0
nM
|
|
|
In vitro inhibition of 5-HT uptake in rat brain synaptosomes using [3H]- 5-hydroxytryptamine
|
Rattus norvegicus
|
230.0
nM
|
|
|
Inhibition of GABA uptake from rat diencephalon-midbrain at 100 uM concentration
|
Rattus norvegicus
|
68.0
%
|
|
|
Maximum inhibition of immobility in the rat (Expressed as percentage of immobility observed in vehicle controls)
|
Rattus norvegicus
|
31.0
%
|
|
|
In vitro inhibition of norepinephrine (NE) uptake in synaptosomal preparation of rat brain
|
Rattus norvegicus
|
40.0
nM
|
|
|
In vitro inhibition of serotonin uptake in synaptosomal preparation of rat brain
|
Rattus norvegicus
|
500.0
nM
|
|
|
Inhibition of [3H]dopamine uptake into rat brain synaptosomes in vitro;Values ranges from: 0.09-0.18
|
Rattus norvegicus
|
130.0
nM
|
|
|
Inhibition of [3H]norepinephrine uptake into rat brain synaptosomes in vitro;Values ranges from: 0.01-0.07
|
Rattus norvegicus
|
30.0
nM
|
|
|
Inhibition of [3H]5-HT uptake into rat brain synaptosomes in vitro;Values ranges from: 0.14-0.22
|
Rattus norvegicus
|
180.0
nM
|
|
|
Inhibition of uptake of tritiated norepinephrine (NE) in rat synaptosomes
|
None
|
12.0
nM
|
|
|
Inhibition the uptake of tritiated serotonin (5-HT) by the serotonin transporter SERT in rat synaptosomes
|
None
|
41.8
nM
|
|
|
Binding affinity towards serotonin S1 receptor at 1.0 uM
|
Rattus norvegicus
|
15.0
%
|
|
|
Binding affinity to Serotonin transporter using [3H]-paroxetine as radioligand in stably transfected NIH3T3 cells
|
None
|
5.0
nM
|
|
|
Binding affinity towards Serotonin transporter using [3H]paroxetine as radioligand
|
None
|
5.0
nM
|
|
|
Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM
|
Cavia porcellus
|
72.7
%
|
|
|
Binding affinity towards alpha-1 adrenergic receptor
|
None
|
220.0
nM
|
|
|
Percent inhibition against 5-hydroxytryptamine transporter at 1 uM nonselective
|
Homo sapiens
|
4.4
nM
|
|
|
Displacement of [3H]citalopram from serotonin transporter
|
None
|
20.3
nM
|
|
|
Displacement of radiolabeled imipramine from human SERT
|
Homo sapiens
|
6.9
nM
|
|
Displacement of radiolabeled imipramine from human SERT
|
Homo sapiens
|
3.2
nM
|
|
|
Inhibition of [3H]5HT uptake at human SERT expressed in HEK293 cells
|
Homo sapiens
|
8.0
nM
|
|
|
Inhibition of [3H]norepinephrine uptake at human NET expressed in HEK293 cells
|
Homo sapiens
|
74.0
nM
|
|
|
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy
|
Homo sapiens
|
82.8
%
|
|
|
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
%
|
|
|
Inhibition of [3H]serotonin reuptake at serotonin transporter
|
None
|
7.57
nM
|
|
|
Inhibition of human 5-HT transporter
|
Homo sapiens
|
7.3
nM
|
|
|
Displacement of [3H]imipramine from human 5HT transporter
|
Homo sapiens
|
0.77
nM
|
|
|
Inhibition of human OCT2 expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay
|
Homo sapiens
|
600.0
nM
|
|
|
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
|
26.9
%
|
|
|
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
|
-2.4
%
|
|
|
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
|
16.9
%
|
|
|
Inhibition of human SERT expressed in HEK293-MSR cells by 5-HT uptake assay
|
Homo sapiens
|
29.0
nM
|
|
|
Binding affinity to human serotonin 5-HT transporter by radioligand displacement assay
|
Homo sapiens
|
2.0
nM
|
|
|
Binding affinity to human 5-HT transporter by radioligand displacement assay
|
Homo sapiens
|
0.52
nM
|
|
Binding affinity to human 5-HT transporter by radioligand displacement assay
|
Homo sapiens
|
1.1
nM
|
|
|
Displacement of [3H]imipramin from human recombinant SERT over-expressed in HEK293 cells
|
Homo sapiens
|
6.8
nM
|
|
|
Binding affinity to SERT (unknown origin) by radioligand binding assay
|
Homo sapiens
|
3.5
nM
|
|
|
Binding affinity to 5HT2A receptor (unknown origin) by radioligand binding assay
|
Homo sapiens
|
220.0
nM
|
|
|
Binding affinity to dopamine D2 receptor (unknown origin) by radioligand binding assay
|
Homo sapiens
|
410.0
nM
|
|
|
Binding affinity to histamine H1 receptor (unknown origin) by radioligand binding assay
|
Homo sapiens
|
27.0
nM
|
|
|
Analgesic activity in mouse assessed as inhibition of acetic acid-induced writhing response at 30 mg/kg, po administered 30 mins prior to acetic acid-challenge relative to control
|
Mus musculus
|
50.0
%
|
|
|
Anticholinergic effect in guinea pig ileum assessed as inhibition of acetylcholine-induced contraction
|
Cavia porcellus
|
1.259
nM
|
|
|
Displacement of [3H]imipramine from human recombinant SERT expressed in CHO cells
|
Homo sapiens
|
2.1
nM
|
|
|
Displacement of [3H]imipramine from human SERT expressed in CHO cells
|
Homo sapiens
|
2.1
nM
|
|
|
Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
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 CYP2C19 in human liver microsomes at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2D6 (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
%
|
|
|
Displacement of [3H]imipramine from human recombinant 5-HT transporter expressed in CHO cells
|
Homo sapiens
|
0.88
nM
|
|
|
Inhibition of wild-type human SERT expressed in HEK293 MSR cells assessed as [3H]-5-HT uptake preincubated for 30 mins followed addition of [3H]-5HT and compound for 10 mins by micro-scintillation counter
|
Homo sapiens
|
31.0
nM
|
|
|
Inhibition of human SERT W103A mutant expressed in HEK293 MSR cells assessed as [3H]-5-HT uptake preincubated for 30 mins followed addition of [3H]-5HT and compound for 10 mins by micro-scintillation counter
|
Homo sapiens
|
2.6
nM
|
|
|
Inhibition of human SERT I179C mutant expressed in HEK293 MSR cells assessed as [3H]-5-HT uptake preincubated for 30 mins followed addition of [3H]-5HT and compound for 10 mins by micro-scintillation counter
|
Homo sapiens
|
5.7
nM
|
|
|
Inhibition of human SERT expressed in CHO cell membranes assessed as reduction in [3H]serotonin uptake preincubated for 10 mins followed by [3H]serotonin addition measured after 20 mins by liquid scintillation counting method
|
Homo sapiens
|
5.1
nM
|
|
|
Displacement of [3H]citalopram from human SERT expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting method
|
Homo sapiens
|
2.0
nM
|
|
|
Displacement of [3H]imipramine from human recombinant 5HT transporter expressed in CHO cells measured after 60 mins by scintillation counting method
|
Homo sapiens
|
0.88
nM
|
|
|
Displacement of [3H]-imipramine from human serotonin transporter expressed in HEK-293 cell membranes after 30 mins by scintillation counting
|
Homo sapiens
|
1.0
nM
|
|
|
Inhibition of SERT expressed in rat brain synaptosomes assessed as decrease in incorporation of [3H]serotonin measured after 15 mins by scintillation counting method
|
Rattus norvegicus
|
61.0
nM
|
|
|
Displacement of [3H]-imipramine from human serotonin transporter expressed in HEK293 cells membranes incubated for 30 mins by microbeta scintillation counting analysis
|
Homo sapiens
|
2.5
nM
|
|
|
Displacement of [3H]-citalopram from SERT in rat cortex tissue incubated for 60 mins by microbeta scintillation counting method
|
Rattus norvegicus
|
29.0
nM
|
|
|
Displacement of [3H] imipramine from human recombinant 5-HT transporter measured after 60 mins by scintillation counter method
|
Homo sapiens
|
1.9
nM
|
|
Displacement of [3H] imipramine from human recombinant 5-HT transporter measured after 60 mins by scintillation counter method
|
Homo sapiens
|
4.1
nM
|
|
|
Displacement of [3H]-citalopram from SERT in rat cortex tissue measured after 60 mins by microbeta scintillation counting analysis
|
Rattus norvegicus
|
29.0
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
|
13.63
%
|
|
|
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
|
0.02
%
|
|
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
|
0.02
%
|
|
|
Binding affinity to SERT (unknown origin)
|
Homo sapiens
|
20.0
nM
|
|
|
Binding affinity to H1 receptor (unknown origin)
|
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
|
343.0
nM
|
|
|
Inhibition of SERT (unknown origin)
|
Homo sapiens
|
29.0
nM
|
|
|
Displacement of SGRG-K(Ac)-GG-K(Ac)-GLG-K(Ac)-GGA-K(Ac)-RHRKVGG-K(Biotin) from Europium chelated human BRD4 bromodomain 1 (49 to 170 residues) measured after 2 hrs by TR-FRET assay
|
Homo sapiens
|
10.2
10^2 uM
|
|
|
Displacement of SGRG-K(Ac)-GG-K(Ac)-GLG-K(Ac)-GGA-K(Ac)-RHRKVGG-K(Biotin) from Europium chelated human BRD4 bromodomain 2 (342 to 460 residues) measured after 2 hrs by TR-FRET assay
|
Homo sapiens
|
6.47
10^2 uM
|
|
