Binding affinity against 5-hydroxytryptamine 1A receptor from bovine hippocampus, used [3H]8-OH-DPAT as radioligand
|
None
|
1.8
nM
|
|
Binding affinity towards Serotonin 5-hydroxytryptamine 1A receptor by displacement of [3H]-(+)-8-OH-DPAT.
|
Homo sapiens
|
4.0
nM
|
|
In vitro affinity for alpha adrenergic receptor by displacement of 3[H]clonidine in calf cerebral cortex
|
Bos taurus
|
41.0
nM
|
|
Alpha-2 adrenergic receptor activity assessed in vitro for displacement of [3H]clonidine from specific binding sites on rat striatal membranes
|
None
|
41.0
nM
|
|
In vitro inhibitory activity against alpha-1 adrenergic receptor from whole rat brain using [3H]WB-4101 as radioligand
|
None
|
550.0
nM
|
|
In vitro inhibitory activity against alpha-2 adrenergic receptor from rat brain minus cerebellum using [3H]clonidine as radioligand
|
None
|
170.0
nM
|
|
Compound was tested for neuronal inhibition of postganglionic cardio accelerator nerve stimulation in anaesthetized cat at 2 Hz frequency at 10 mg/kg
|
Felis catus
|
59.0
%
|
|
Compound was tested for neuronal inhibition of postganglionic cardio accelerator nerve stimulation in anaesthetized cat at 2 Hz frequency at 30 mg/kg
|
Felis catus
|
80.0
%
|
|
Compound was tested for neuronal inhibition of postganglionic cardio accelerator nerve stimulation in anaesthetized cat at 2 Hz frequency at 3 mg/kg
|
Felis catus
|
23.0
%
|
|
Inhibitory activity against Dopamine receptor D2 in calf corpus striatum using [3H]spiperone as radioligand
|
None
|
48.0
nM
|
|
Dopamine receptor binding affinity by displacing the radioligand [3H]-dopamine from dopamine receptor.
|
Bos taurus
|
18.0
nM
|
|
Dopamine receptor binding affinity by displacing the radioligand [3H]spiroperidol from dopamine receptor.
|
Bos taurus
|
145.0
nM
|
|
In vitro inhibitory activity against dopamine receptor from calf caudate using [3H]dopamine as radioligand
|
None
|
18.0
nM
|
|
In vitro inhibitory activity against dopamine receptor from calf caudate using [3H]spiperone as radioligand
|
None
|
145.0
nM
|
|
Dopaminergic activity assessed in vitro for displacement of [3H]apomorphine from specific binding sites on rat striatal membranes
|
None
|
3.1
nM
|
|
In vitro affinity for dopamine receptor by displacement of [3H]- apomorphine in rat striatal membranes
|
Rattus norvegicus
|
3.1
nM
|
|
Affinity towards Dopamine receptor D2
|
None
|
50.0
nM
|
|
Binding affinity towards Dopamine receptor D2 by displacement of [3H]U-86170.
|
Homo sapiens
|
4.0
nM
|
|
Inhibitory activity against Dopamine receptor D2 in rat corpus striatum using [3H]Apomorphine as radioligand
|
None
|
1.6
nM
|
|
In vitro affinity at mutant D2 receptor (S194A) in C6 (glioma) cell membranes.
|
None
|
4.0
nM
|
|
In vitro affinity at mutant D2 receptor (S194A) in C6 (glioma) cell membranes.
|
None
|
45.0
nM
|
|
In vitro affinity at mutant D2 receptor (S197A) in C6 (glioma) cell membranes.
|
None
|
40.0
nM
|
|
In vitro affinity at wild type Dopamine receptor D2 on C6 (glioma) cell membranes.
|
None
|
30.0
nM
|
|
Compound was tested for antagonistic activity against D2 receptor from rat striatum, used [3H]raclopride as radioligand
|
None
|
1.0
nM
|
|
Binding affinity towards Dopamine receptor D3 by displacement of [3H](+)-7-OH-DPAT.
|
Homo sapiens
|
4.0
nM
|
|
Evaluated for the prolactin inhibition at the dose 50 ug/kg administered intraperitoneally
|
Rattus norvegicus
|
95.0
%
|
|
Evaluated for the prolactin inhibition at the dose 50 ug/kg administered intraperitoneally (treatment)
|
Rattus norvegicus
|
1.6
ng ml-1
|
|
Inhibition of serum prolactin concentration in rats when 5 mg/Kg was administered intraperitoneally
|
Rattus norvegicus
|
88.0
%
|
|
In vitro inhibitory activity against serotonin receptor from rat frontal cortex using [3H]spiperone as radioligand
|
Rattus norvegicus
|
140.0
nM
|
|
In vitro inhibitory activity against serotonin receptor from whole rat brain using [3H]5-HT as radioligand
|
Rattus norvegicus
|
385.0
nM
|
|
Inhibition of [3H]apomorphine binding to dopamine receptor of rat corpus striatum
|
None
|
1.6
nM
|
|
Inhibition of [3H]dopamine binding to dopamine receptor of rat corpus striatum
|
None
|
4.1
nM
|
|
Inhibition of [3H]spiperone binding to dopamine receptor of rat corpus striatum
|
None
|
48.0
nM
|
|
Inhibition constant against [3H]-spiperone binding to human Dopamine receptor D3 expressed in CHO cells
|
Homo sapiens
|
0.8511
nM
|
|
Inhibition of human ERG
|
Homo sapiens
|
120.23
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
|
None
|
15.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
|
None
|
8.468
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
|
Rattus norvegicus
|
87.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
|
Rattus norvegicus
|
40.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
|
None
|
14.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
|
None
|
3.904
nM
|
|
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
781.0
nM
|
|
DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
|
None
|
744.0
nM
|
|
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
|
None
|
264.0
nM
|
|
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
|
None
|
99.0
nM
|
|
DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
|
None
|
64.0
nM
|
|
DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
|
None
|
29.0
nM
|
|
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
|
None
|
205.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
76.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
49.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
|
None
|
379.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
|
None
|
199.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
39.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
18.0
nM
|
|
DRUGMATRIX: Calcium Channel Type L, Phenylalkylamine radioligand binding (ligand: [3H] (-)-Desmethoxyverapamil (D-888))
|
Rattus norvegicus
|
913.0
nM
|
|
DRUGMATRIX: Calcium Channel Type L, Phenylalkylamine radioligand binding (ligand: [3H] (-)-Desmethoxyverapamil (D-888))
|
Rattus norvegicus
|
887.0
nM
|
|
DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
None
|
200.0
nM
|
|
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
|
None
|
679.0
nM
|
|
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
|
None
|
339.0
nM
|
|
DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
|
None
|
111.0
nM
|
|
DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
|
None
|
37.0
nM
|
|
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
|
None
|
5.393
nM
|
|
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
|
None
|
1.832
nM
|
|
Agonist activity at Rattus norvegicus (rat) dopamine D2/D3 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 min
|
Rattus norvegicus
|
4.31
nM
|
|
Agonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 min
|
Rattus norvegicus
|
7.86
nM
|
|
Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
|
Rattus norvegicus
|
5.12
nM
|
|
Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
|
Rattus norvegicus
|
2.41
nM
|
|
Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D2 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
|
Rattus norvegicus
|
5.85
nM
|
|
Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D2 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
|
Rattus norvegicus
|
5.59
nM
|
|
Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D2 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
|
Rattus norvegicus
|
32.0
nM
|
|
Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D2 trunk/D2 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
|
Rattus norvegicus
|
27.5
nM
|
|
Displacement of [125]iodosulpride from human recombinant dopamine D2L receptor expressed in CHO cells after 30 mins
|
Homo sapiens
|
26.0
nM
|
|
Displacement of [125]iodosulpride from human recombinant dopamine D2L receptor expressed in CHO cells after 30 mins
|
Homo sapiens
|
25.7
nM
|
|
Agonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
|
Homo sapiens
|
0.3548
nM
|
|
Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
|
Homo sapiens
|
8.913
nM
|
|
Agonist activity at 5HT2C receptor VGV isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
|
Homo sapiens
|
218.78
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
|
17.72
%
|
|
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
|
0.27
%
|
|
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
|
0.27
%
|
|