|
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
|
53.0
nM
|
|
|
Compound was tested for its binding affinity towards brain (neocortex) Adenylate cyclase
|
Cavia porcellus
|
60.0
nM
|
|
|
Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptor
|
None
|
0.02
nM
|
|
|
Concentration required to reducing the histamine induced contraction by 50% was measured
|
Cavia porcellus
|
0.0083
ug.mL-1
|
|
|
Compound tested for its inhibitory activity against Histamine H1 receptor
|
None
|
0.02
nM
|
|
|
Inhibitory activity against brain adenylate cyclase Histamine H2 receptor
|
Cavia porcellus
|
660.0
nM
|
|
|
Inhibition of radioligand [3H]QNB binding to muscarinic acetylcholine receptor in the rat forebrain in the presence of zinc
|
None
|
300.0
nM
|
|
|
Compound was tested for its inhibitory activity against Noradrenaline receptor
|
Rattus norvegicus
|
41.0
nM
|
|
|
In vitro inhibition of the accumulation of (-)-[3H]-5-HT in synaptosomes from the rat brain cortex
|
Rattus norvegicus
|
320.0
nM
|
|
|
In vitro inhibition of the accumulation of (-)-[3H]Norepinephrine in synaptosomes from the rat brain cortex
|
Rattus norvegicus
|
61.0
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
|
73.8
%
|
|
|
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy
|
Homo sapiens
|
78.5
%
|
|
|
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells
|
Homo sapiens
|
1.12
nM
|
|
|
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
|
Homo sapiens
|
89.0
nM
|
|
|
Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells
|
Homo sapiens
|
170.0
nM
|
|
|
Displacement of [3H]spiperone from human dopamine D2 receptor expressed in CHO cells
|
Homo sapiens
|
196.0
nM
|
|
|
Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells
|
Homo sapiens
|
206.0
nM
|
|
|
DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
11.0
nM
|
|
DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
2.724
nM
|
|
|
DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
81.0
nM
|
|
DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
29.0
nM
|
|
|
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
26.0
nM
|
|
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
5.436
nM
|
|
|
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
5.297
nM
|
|
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
0.739
nM
|
|
|
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
8.02
nM
|
|
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
5.762
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
|
None
|
15.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
|
None
|
4.374
nM
|
|
|
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
14.0
nM
|
|
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
5.599
nM
|
|
|
DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
76.0
nM
|
|
DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
42.0
nM
|
|
|
DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
|
None
|
105.0
nM
|
|
DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
|
None
|
52.0
nM
|
|
|
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
|
None
|
351.0
nM
|
|
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
|
None
|
132.0
nM
|
|
|
DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
|
None
|
8.076
nM
|
|
DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
|
None
|
3.687
nM
|
|
|
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
|
None
|
59.0
nM
|
|
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
|
None
|
8.599
nM
|
|
|
DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
|
None
|
23.0
nM
|
|
DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
|
None
|
22.0
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
70.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
45.0
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
|
None
|
6.048
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
|
None
|
3.168
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
140.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
65.0
nM
|
|
|
DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
|
None
|
1.661
nM
|
|
DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
|
None
|
0.882
nM
|
|
|
DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
|
None
|
433.0
nM
|
|
|
DRUGMATRIX: Calcium Channel Type L, Phenylalkylamine radioligand binding (ligand: [3H] (-)-Desmethoxyverapamil (D-888))
|
Rattus norvegicus
|
840.0
nM
|
|
DRUGMATRIX: Calcium Channel Type L, Phenylalkylamine radioligand binding (ligand: [3H] (-)-Desmethoxyverapamil (D-888))
|
Rattus norvegicus
|
816.0
nM
|
|
|
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
|
None
|
355.0
nM
|
|
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
|
None
|
178.0
nM
|
|
|
DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
|
None
|
336.0
nM
|
|
|
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
|
None
|
182.0
nM
|
|
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
|
None
|
62.0
nM
|
|
|
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
|
None
|
4.782
nM
|
|
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
|
None
|
0.555
nM
|
|
|
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
|
None
|
730.0
nM
|
|
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
|
None
|
718.0
nM
|
|
|
TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: ? uM, Amitriptyline: 100 uM) in MDR1-expressing MDCKII cells
|
None
|
25.5
%
|
|
|
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
|
10.5
%
|
|
|
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
|
22.0
%
|
|
|
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
|
-8.9
%
|
|
|
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
|
141.0
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
|
549.54
nM
|
|
|
Inhibition of [3H]norepinephrine uptake at human NET expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay
|
Homo sapiens
|
333.0
nM
|
|
|
Displacement of [3H]Citalopram from serotonin transporter (unknown origin)
|
Homo sapiens
|
9.55
nM
|
|
Displacement of [3H]Citalopram from serotonin transporter (unknown origin)
|
Homo sapiens
|
4.3
nM
|
|
|
Antiplasmodial activity against Plasmodium falciparum K1 at 0.002 to 100 ug/ml by serial drug dilution assay
|
Plasmodium falciparum K1
|
500.0
nM
|
|
|
Inhibition of human ERG expressed in HEK293 cells at 10 uM by automated patch clamp method relative to control
|
Homo sapiens
|
97.7
%
|
|
|
Displacement of [3H]citalopram from human SERT expressed in HEK293 cells measured after 30 mins
|
Homo sapiens
|
5.4
nM
|
|
|
Displacement of [3H]citalopram from human SERT expressed in HEK293 cells at 10 uM measured after 30 mins
|
Homo sapiens
|
50.0
%
|
|
|
Inhibition of human ERG expressed in CHO cells at 1 uM by manual patch-clamp electrophysiology
|
Homo sapiens
|
23.15
%
|
|
|
Inhibition of human ERG expressed in CHO cells at 10 uM by manual patch-clamp electrophysiology
|
Homo sapiens
|
76.13
%
|
|
|
Displacement of [3H]-scopolamine from human recombinant muscarinic M1 receptor expressed in human recombinant CHO-K1 cells at 1 uM incubated for 120 mins by solid scintillation counting method relative to control
|
Homo sapiens
|
78.0
%
|
|
|
Displacement of [3H]-pyrilamine from human recombinant histamine H1 receptor expressed in human recombinant CHO-K1 cells at 1 uM incubated for 60 mins by solid scintillation counting method relative to control
|
Homo sapiens
|
99.0
%
|
|
|
Displacement of [3H]-prazosin from rat cortex membrane alpha1 adrenergic receptor expressed in human recombinant CHO-K1 cells at 1 uM after 30 mins by solid scintillation counting method relative to control
|
Rattus norvegicus
|
82.0
%
|
|
|
Displacement of [3H]-citalopram from human SERT expressed in HEK cell membrane assessed as inhibition constant by radioligand binding assay
|
Homo sapiens
|
9.2
nM
|
|
