|
Binding affinity against 5-hydroxytryptamine 3 receptor using [3H]BRL-43694 in rat posterior cortex
|
Rattus norvegicus
|
443.0
nM
|
|
|
Binding affinity against 5-hydroxytryptamine 3 receptor using [3H]BRL-43694 as radioligand in rat posterior cortex
|
None
|
443.0
nM
|
|
|
Displacement of the 5-hydroxytryptamine 3 receptor ligand [3H]GR-65630 from rat brain cortical membranes.
|
None
|
995.0
nM
|
|
|
Binding affinity at 5-hydroxytryptamine 3 receptor in rat entorhinal cortex by [3H]BRL-43694 displacement.
|
None
|
490.0
nM
|
|
|
Compound was evaluated for its binding affinity for 5-hydroxytryptamine 3 receptor by measuring displacement [3H]GR-65630 in rat cerebral cortex
|
None
|
348.0
nM
|
|
|
Inhibitory activity against 5-hydroxytryptamine 3 receptor in rat cortical membranes using [3H]- 1-Methyl-1H-indazole-3-carboxylic acid (8-methyl-8-aza-bicyclo[3.2.1]oct-3-yl)-amide as a radioligand
|
None
|
502.0
nM
|
|
|
Inhibition of [3H]GR-65630 binding to 5-hydroxytryptamine 3 receptor
|
Rattus norvegicus
|
240.0
nM
|
|
|
Compound was evaluated for the binding affinity at 5- HT3 receptor subtype
|
None
|
200.0
nM
|
|
|
Potency at neuronal 5-hydroxytryptamine 3 receptors in the rabbit heart
|
Oryctolagus cuniculus
|
50.12
nM
|
|
|
Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 3 receptor in isolated perfused rabbit heart (RH)
|
Oryctolagus cuniculus
|
79.43
nM
|
|
|
Antagonistic activity against Serotonin 5-hydroxytryptamine 3 receptor in isolated rabbit vagus nerve (RVN)
|
Oryctolagus cuniculus
|
50.12
nM
|
|
|
Inhibition of [3H]GR-65630 binding to rat cortical membrane 5-hydroxytryptamine 3 receptor
|
Rattus norvegicus
|
880.0
nM
|
|
|
Binding affinity against 5-hydroxytryptamine 3 receptor in rat cortical membrane using [3H]GR-65630 as radioligand
|
None
|
880.0
nM
|
|
|
Concentration required to inhibit the binding of radioligand [3H]GR-65630 to serotonin 5-hydroxytryptamine-3 receptor (5-HT 3 receptor)in rat brain cortical membrane
|
None
|
228.0
nM
|
|
|
Inhibition of [3H]GR-65630 binding to rat cortical membrane serotonin 5-hydroxytryptamine 3 receptor
|
Rattus norvegicus
|
210.0
nM
|
|
|
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
|
Cavia porcellus
|
5.7
nM
|
|
|
Concentration of compound required to inhibit the binding of radioligand [3H]GR-113808 to serotonin 5-hydroxytryptamine 4 receptor in guinea-pig striatum
|
Cavia porcellus
|
912.0
nM
|
|
|
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
|
Cavia porcellus
|
546.0
nM
|
|
|
Tested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosae
|
None
|
794.33
nM
|
|
|
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
|
Rattus norvegicus
|
975.0
nM
|
|
|
Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum
|
None
|
974.0
nM
|
|
|
Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatum by [3H]GR-113808 displacement.
|
None
|
900.0
nM
|
|
|
Binding affinity to 5-hydroxytryptamine 3 receptor using [3H]GR-65630 as radioligand in rat cortex
|
None
|
199.53
nM
|
|
|
Binding affinity to 5-hydroxytryptamine 3 receptor using [3H]quipazine as radioligand in rat cortex
|
None
|
229.09
nM
|
|
|
Tested for its binding affinity by measuring its ability to displace [3H]granisetron from 5-hydroxytryptamine 3 receptor in rat cortex
|
None
|
158.49
nM
|
|
|
pKi value for inhibition of [3H]LY-278584 binding to 5-hydroxytryptamine 3 receptor
|
Rattus norvegicus
|
501.19
nM
|
|
|
Percent inhibition of apomorphine (0.3 mg/kg) induced emesis in dogs when 1 mg/kg of compound administered perorally
|
Canis lupus familiaris
|
100.0
%
|
|
|
Binding affinity against dopamine D2 receptor in rat brain synaptic membrane using [3H]-spiperone as radioligand
|
None
|
480.0
nM
|
|
|
Inhibition of [3H]- spiperone binding to rat brain Dopamine receptor D2
|
Rattus norvegicus
|
480.0
nM
|
|
|
Compound was evaluated for the binding affinity at Dopamine receptor D2
|
None
|
80.0
nM
|
|
|
Evaluated for the dopamine D2 receptor antagonistic activity (antagonism of apomorphine-induced emesis in dogs) at a dose of 3.0 mg/kg administered perorally
|
Canis lupus familiaris
|
100.0
%
|
|
|
Concentration of compound required to inhibit the binding of radioligand [3H]spiperone to Dopamine receptor D2 in rat brain synaptic membrane
|
None
|
444.0
nM
|
|
|
In vitro antagonistic activity against Dopamine receptor D2 was evaluated for the inhibition of [3H]spiperone binding
|
None
|
565.0
nM
|
|
|
Inhibitory activity against dopamine receptor D2 by 3H ligand binding experiments.
|
None
|
630.0
nM
|
|
|
Inhibitory concentration required for displacing radioligand [3H]SPI from DA D-2 receptor
|
None
|
820.0
nM
|
|
|
Affinity towards Dopamine receptor D2 in rat striatum using [3H]spiperone as radioligand
|
Rattus norvegicus
|
303.0
nM
|
|
|
Binding affinity to dopamine receptor D2
|
None
|
113.0
nM
|
|
|
Binding affinity against Dopamine receptor D2 using [3H]spiperone as radioligand in rat striatum
|
None
|
285.0
nM
|
|
|
Displacement of [125I]iodosulpiride from human Dopamine receptor D3 expressed in CHO cells
|
Homo sapiens
|
27.0
nM
|
|
|
Compound was evaluated for binding affinity towards DA D-2 receptor using radioligand [3H]SPI
|
None
|
104.0
nM
|
|
Compound was evaluated for binding affinity towards DA D-2 receptor using radioligand [3H]SPI
|
None
|
235.0
nM
|
|
|
Concentration of compound required to inhibit the binding of radioligand [3H](R)-7-OH-DPAT to Dopamine receptor D3 in rat striatum
|
None
|
61.3
nM
|
|
|
Tested for PCA activity of compound in rat at 10 mg/kg intravenous dose
|
Rattus norvegicus
|
84.0
%
|
|
|
PCA activity of compound in rat at 100 mg/kg dose
|
Rattus norvegicus
|
14.0
%
|
|
|
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
|
Rattus norvegicus
|
794.33
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
|
52.3
%
|
|
|
Mechanism based inhibition of human cytochrome P450 2D6 measured by dextromethorphan O-demethylation
|
Homo sapiens
|
960.0
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
630.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
401.0
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT3 radioligand binding (ligand: [3H] GR-65630)
|
None
|
902.0
nM
|
|
|
DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
None
|
800.0
nM
|
|
|
DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
|
None
|
127.0
nM
|
|
DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
|
None
|
42.0
nM
|
|
|
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
|
None
|
200.0
nM
|
|
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
|
None
|
68.0
nM
|
|
|
DRUGMATRIX: Imidazoline I2, Central radioligand binding (ligand: [3H] Idazoxan)
|
Rattus norvegicus
|
708.0
nM
|
|
DRUGMATRIX: Imidazoline I2, Central radioligand binding (ligand: [3H] Idazoxan)
|
Rattus norvegicus
|
472.0
nM
|
|
|
Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.
|
Homo sapiens
|
64.0
nM
|
|
|
Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.
|
Homo sapiens
|
16.0
nM
|
|
|
Inhibition of recombinant MPO (unknown origin) assessed as reduction in taurine chloramine production preincubated with enzyme and taurine followed by H2O2 addition measured after 5 mins
|
Homo sapiens
|
350.0
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
|
15.65
%
|
|
|
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
|
-0.09
%
|
|
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
|
-0.09
%
|
|
