Binding affinity towards 5-hydroxytryptamine 2 receptor as antagonism of serotonin-induced contractions in rat jugular vein
|
Rattus norvegicus
|
60.0
nM
|
|
Binding affinity towards 5-hydroxytryptamine 2 receptor was measured using radioligand ([3H]spiperone) binding assay
|
None
|
18.0
nM
|
|
Binding affinity towards human 5-hydroxytryptamine 7 receptor
|
Homo sapiens
|
70.0
nM
|
|
Displacement of [3H]WB-4101 from alpha-1 adrenergic receptor in rat brain
|
Rattus norvegicus
|
17.0
nM
|
|
In vitro affinity for cortical alpha-1 adrenergic receptor labelled with [3H]WB-4101
|
None
|
65.0
nM
|
|
Inhibition of [3H]WB-4101 binding to rat cortical Alpha-1 adrenergic receptor in vitro
|
None
|
65.0
nM
|
|
Displacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brain
|
Rattus norvegicus
|
80.0
nM
|
|
Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1
|
None
|
17.3
nM
|
|
Compound was tested in vitro for its affinity towards rat striatal Dopamine receptor D2 labeled with [3H]- spiperone
|
None
|
60.0
nM
|
|
Displacement of [3H]haloperidol from Dopamine receptor D2 in rat brain
|
Rattus norvegicus
|
4.0
nM
|
|
Inhibition of [3H]spiperone binding to dopamine receptor from rat corpus striatal membranes
|
None
|
85.0
nM
|
|
Binding affinity towards Dopamine receptor D2
|
None
|
27.0
nM
|
|
In vitro binding affinity against Dopamine receptor D2 by displacement of [3H]haloperidol from rat striatal membranes.
|
None
|
2.8
nM
|
|
In vitro inhibitory against radioligand [3H]spiperone binding to rat striatal Dopamine receptor D2
|
None
|
60.0
nM
|
|
K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1
|
Homo sapiens
|
35.7
nM
|
|
Binding affinity against Histamine H1 receptor was measured using radioligand ([3H]pyrilamine) binding assay
|
None
|
99.0
nM
|
|
Compound was evaluated for the inhibition of Locomotion-Screen falloff test, at dose (mg/Kg) = 10; 60-100%
|
Mus musculus
|
60.0
%
|
|
Displacement of [3H]quinuclidinyl benzilate (QNB) from Muscarinic acetylcholine receptor in rat brain
|
Rattus norvegicus
|
2.0
nM
|
|
Binding affinity against Muscarinic acetylcholine receptor was measured using radioligand ([3H]QNB) binding assay
|
None
|
106.0
nM
|
|
Inhibition of human Potassium channel HERG expressed in mammalian cells
|
Homo sapiens
|
363.08
nM
|
|
Inhibitory activity against Potassium channel HERG
|
Homo sapiens
|
191.0
nM
|
|
Displacement of (+)-[3H]-3-PPP from rat cortical sigma site
|
Cavia porcellus
|
750.0
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
|
63.5
%
|
|
Inhibitory concentration against potassium channel HERG
|
None
|
190.55
nM
|
|
Inhibition of partially open human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel)
|
Homo sapiens
|
35.48
nM
|
|
Displacement of [3H]Astemizole from hERG expressed in HEK293 cells at 10 uM
|
Homo sapiens
|
869.0
nM
|
|
Inhibition of wild type androgen receptor expressed in CV1 cells assessed as dihydrotestosterone-stimulated transactivation at 500 nM by CAT reporter gene assay
|
None
|
2.4
%
|
|
Inhibition of human ERG channel
|
Homo sapiens
|
33.2
nM
|
|
Inhibition of human ERG channel
|
Homo sapiens
|
33.2
nM
|
|
Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique
|
Homo sapiens
|
363.08
nM
|
|
Inhibition of human ERG in MCF7 cells
|
Homo sapiens
|
35.48
nM
|
|
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 NorA in Staphylococcus aureus 1199B assessed as reduction in ethidium bromide efflux at 50 uM by fluorimetry after 5 mins
|
Staphylococcus aureus
|
88.0
%
|
|
Inhibition of human ERG
|
Homo sapiens
|
95.5
nM
|
|
DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
7.019
nM
|
|
DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
1.69
nM
|
|
DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
106.0
nM
|
|
DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
38.0
nM
|
|
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
90.0
nM
|
|
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
19.0
nM
|
|
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
80.0
nM
|
|
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
11.0
nM
|
|
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
9.246
nM
|
|
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
6.643
nM
|
|
DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine)
|
None
|
996.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
|
None
|
60.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
|
None
|
34.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
|
None
|
4.366
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
|
None
|
1.247
nM
|
|
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
5.093
nM
|
|
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
2.062
nM
|
|
DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
4.692
nM
|
|
DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
2.597
nM
|
|
DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
|
None
|
5.891
nM
|
|
DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
|
None
|
2.895
nM
|
|
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
|
None
|
133.0
nM
|
|
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
|
None
|
50.0
nM
|
|
DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
|
None
|
380.0
nM
|
|
DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
|
None
|
174.0
nM
|
|
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
|
None
|
171.0
nM
|
|
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
|
None
|
25.0
nM
|
|
DRUGMATRIX: Calcium Channel Type L, Benzothiazepine radioligand binding (ligand: [3H] Diltiazem)
|
Rattus norvegicus
|
469.0
nM
|
|
DRUGMATRIX: Calcium Channel Type L, Benzothiazepine radioligand binding (ligand: [3H] Diltiazem)
|
Rattus norvegicus
|
417.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
129.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
82.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
|
None
|
44.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
|
None
|
23.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
71.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
33.0
nM
|
|
DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
|
None
|
751.0
nM
|
|
DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
|
None
|
399.0
nM
|
|
DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
|
None
|
363.0
nM
|
|
DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
|
None
|
153.0
nM
|
|
DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
|
Rattus norvegicus
|
845.0
nM
|
|
DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
|
Rattus norvegicus
|
520.0
nM
|
|
DRUGMATRIX: Calcium Channel Type L, Phenylalkylamine radioligand binding (ligand: [3H] (-)-Desmethoxyverapamil (D-888))
|
Rattus norvegicus
|
443.0
nM
|
|
DRUGMATRIX: Calcium Channel Type L, Phenylalkylamine radioligand binding (ligand: [3H] (-)-Desmethoxyverapamil (D-888))
|
Rattus norvegicus
|
431.0
nM
|
|
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
|
None
|
194.0
nM
|
|
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
|
None
|
97.0
nM
|
|
DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
|
None
|
35.0
nM
|
|
DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
|
None
|
12.0
nM
|
|
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
|
None
|
9.892
nM
|
|
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
|
None
|
3.36
nM
|
|
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
|
None
|
515.0
nM
|
|
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
|
None
|
72.0
nM
|
|
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
|
None
|
8.412
nM
|
|
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
|
None
|
950.0
nM
|
|
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
|
None
|
934.0
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
|
26.1
%
|
|
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
|
25.2
%
|
|
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
|
21.5
%
|
|
Neuroleptic activity in Sprague-Dawley rat assessed as inhibition of Sidman avoidance at 20 mg/kg, ip relative to control
|
Rattus norvegicus
|
15.0
%
|
|
Cytotoxicity against african green monkey Vero cells assessed as reduction in cell viability by MTT assay
|
Chlorocebus sabaeus
|
5.3
ug.mL-1
|
|
Inhibition of hERG K channel
|
None
|
33.0
nM
|
|
Binding affinity to Wistar rat brain lipid by TRANSIL assay
|
Rattus norvegicus
|
369.0
nM
|
|
Cytotoxicity against human MDM assessed as cell viability after 3 days by Alamar blue dye-based fluorocytometric analysis relative to control
|
Homo sapiens
|
5.5
ug.mL-1
|
|
Cytotoxicity against human MRC5 cells assessed as decrease in cell viability after 24 hrs by resazurin reduction assay
|
Homo sapiens
|
8.2
ug.mL-1
|
|
Cytotoxicity against mouse J774 cells assessed as decrease in cell viability after 24 hrs by resazurin reduction assay
|
Mus musculus
|
4.1
ug.mL-1
|
|
Cytotoxicity against mouse L5178Y cells assessed as reduction in cell viability by MTT assay
|
Mus musculus
|
12.72
nM
|
|
Cytotoxicity against multidrug resistance mouse L5178Y cells expressing human MDR1 assessed as reduction in cell viability by MTT assay
|
Mus musculus
|
7.43
nM
|
|
Cytotoxicity against African green monkey Vero cells assessed as decrease in cell viability incubated for 72 hrs by resazurin assay
|
Chlorocebus sabaeus
|
17.79
ug.mL-1
|
|
Displacement of [3H]-Raclopride from human D2 receptor (unknown origin) expressed in HEK293 cell membranes
|
Homo sapiens
|
8.0
nM
|
|
Displacement of [3H]-Ketanserin from human 5HT2A receptor expressed in CHO-K1 cells
|
Homo sapiens
|
84.0
nM
|
|
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells
|
Homo sapiens
|
71.0
nM
|
|
Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells
|
Homo sapiens
|
181.0
nM
|
|
Inhibition of NF-kappaB (unknown origin) at 5 uM relative to control
|
Homo sapiens
|
85.0
%
|
|
Inhibition of NF-kappaB (unknown origin) assessed as reduction in IL-2 production at 5 uM by cell based assay relative to control
|
Homo sapiens
|
95.0
%
|
|