|
In vitro affinity towards 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand in hippocampus
|
None
|
950.0
nM
|
|
|
Binding affinity towards human 5-hydroxytryptamine 1 receptor
|
None
|
21.0
nM
|
|
|
Affinity for 5-hydroxytryptamine 1 receptor
|
Rattus norvegicus
|
55.0
nM
|
|
|
The binding affinity was measured on serotonin 5-hydroxytryptamine 1 receptor in rat brain tissue
|
None
|
339.0
nM
|
|
|
Binding affinity towards serotonin 5-HT1A receptor was determined in rat hippocampus using [3H]8-OH-DPAT as ligand
|
None
|
950.0
nM
|
|
|
Affinity for 5-hydroxytryptamine 1A receptor labeled with [3H]8-OH-DPAT radioligand in hippocampus tissue
|
None
|
820.0
nM
|
|
|
Inhibitory activity against serotonin 5-hydroxytryptamine 1A receptor from mice.
|
None
|
430.0
nM
|
|
|
Binding affinity measured at the 5-hydroxytryptamine 1A receptor by the inhibition of [3H]8-OH-DPAT binding to rat cortex using unlabeled buspirone for nonspecific binding.
|
None
|
491.0
nM
|
|
|
Ability to displace [3H]-8-OH-DPAT from serotonergic 5-hydroxytryptamine 1A receptor
|
None
|
130.0
nM
|
|
|
Compound was evaluated for its binding affinity with 5-hydroxytryptamine 1A receptor using membranes prepared from rat cerebral cortex
|
None
|
253.0
nM
|
|
|
The compound was tested binding affinity against 5-hydroxytryptamine 1A receptor from rat brain using [3H]8-OH-DPAT as radioligand at 10e-6 M.
|
None
|
720.0
nM
|
|
|
Binding affinity for 5-hydroxytryptamine 1A receptor determined using [3H]8-OH-DPAT as radioligand
|
None
|
253.0
nM
|
|
|
Binding affinity towards serotonin 5-HT2 receptor was determined in rat cortex using [3H]spiperone as ligand
|
None
|
2.6
nM
|
|
|
Compound was measured for affinity at 5-hydroxytryptamine 2 receptor in rat cortical by [3H]spiroperidol displacement.
|
None
|
5.0
nM
|
|
|
Inhibition of [3H]ketanserin binding to dopamine 5-hydroxytryptamine 2 receptor
|
Rattus norvegicus
|
0.76
nM
|
|
|
Inhibitory activity against serotonin 5-hydroxytryptamine 2 receptor from mice.
|
None
|
1.5
nM
|
|
|
Affinity for 5-hydroxytryptamine 2 receptor binding sites by its ability to displace [3H]spiperone from rat frontal cortex.
|
None
|
2.6
nM
|
|
|
Binding affinity towards human serotonin 5-hydroxytryptamine 2A receptor
|
None
|
0.16
nM
|
|
|
Binding affinity for human 5-hydroxytryptamine 2A receptor
|
Homo sapiens
|
0.39
nM
|
|
|
Affinity for 5-hydroxytryptamine 2 receptor
|
Rattus norvegicus
|
0.2
nM
|
|
|
Ability to displace [3H]ketanserin from serotonergic 5-hydroxytryptamine 2 receptor
|
None
|
0.14
nM
|
|
|
The binding affinity was measured on 5-hydroxytryptamine 2 receptor in rat brain tissue
|
None
|
0.2
nM
|
|
|
In vitro affinity against serotonin 5-hydroxytryptamine 2A receptor
|
Rattus norvegicus
|
0.309
nM
|
|
|
Displacement of [3H]-ketanserin from rat brain 5-hydroxytryptamine 2A receptor
|
Rattus norvegicus
|
0.537
nM
|
|
|
Inhibitory constant on 5-hydroxytryptamine 2A receptor of Rat frontal cortex
|
None
|
0.309
nM
|
|
|
In vitro ability to displace [3H]ketanserin binding from 5-hydroxytryptamine 2A receptor in rat striatal membrane.
|
None
|
0.1995
nM
|
|
|
Binding affinity towards serotonin 5-hydroxytryptamine 2A receptor
|
None
|
0.5012
nM
|
|
|
In vitro affinity towards 5-hydroxytryptamine 2A receptor using [3H]spiroperidol as radioligand in cortex
|
None
|
2.6
nM
|
|
|
Inhibition of [3H]ketanserin binding to rat frontal cortex membrane 5-hydroxytryptamine 2A receptor
|
Rattus norvegicus
|
1.4
nM
|
|
|
Ability to inhibit the binding of iodine-125-labelled lysergic acid diethylamide([125I]-LSD) to the S-2A serotonin receptor.
|
None
|
0.16
nM
|
|
|
Binding affinity measured at the 5-hydroxytryptamine 2A receptor by the inhibition of [3H]ketanserin binding to rat cortex using unlabeled mianserin for nonspecific binding.
|
None
|
0.7
nM
|
|
|
Relative binding affinity for D2 receptor and 5-hydroxytryptamine 2A receptor, ratio of Ki
|
Rattus norvegicus
|
0.54
nM
|
|
|
Binding affinity towards human serotonin 5-hydroxytryptamine 2C receptor
|
None
|
63.0
nM
|
|
|
Binding affinity towards human 5-hydroxytryptamine 2C receptor
|
None
|
6.4
nM
|
|
|
In vitro affinity against serotonin (5-hydroxytryptamine 2C) receptor
|
Bos taurus
|
41.69
nM
|
|
|
Inhibitory constant was determined on 5-hydroxytryptamine 2C receptor of Bovine choroid plexus
|
Bos taurus
|
41.69
nM
|
|
|
In vitro ability to displace [3H]mesulergine binding from 5-hydroxytryptamine 2C receptor from bovine choroid plexus.
|
Bos taurus
|
91.2
nM
|
|
|
Binding affinity towards serotonin 5-hydroxytryptamine 2C receptor
|
None
|
7.413
nM
|
|
|
Binding affinity towards rat 5-hydroxytryptamine 7 receptor
|
None
|
1.4
nM
|
|
|
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in rat brain
|
Rattus norvegicus
|
0.74
nM
|
|
|
The binding affinity was measured on adrenergic alpha-1 receptor in rat brain tissue
|
None
|
3.0
nM
|
|
|
Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding.
|
None
|
25.0
nM
|
|
|
Displacement of [3H]prazosin from rat brain Alpha-1 adrenergic receptor
|
Rattus norvegicus
|
0.7413
nM
|
|
|
Binding affinity towards human alpha-1 adrenergic receptor
|
None
|
2.3
nM
|
|
|
Binding affinity towards human alpha-1 adrenergic receptor
|
None
|
0.69
nM
|
|
|
The compound was tested against Alpha-1 adrenergic receptor for percent displacement of radioligand at 10e-6 M
|
None
|
1.0
nM
|
|
|
Binding affinity towards human alpha-2 adrenergic receptor
|
None
|
1.8
nM
|
|
|
Binding affinity towards human alpha-2 adrenergic receptor
|
None
|
7.5
nM
|
|
|
Its affinity towards alpha-1 receptor using [3H]WB-4101 as radioligand in whole brain minus cerebellum
|
None
|
2.9
nM
|
|
|
Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding.
|
None
|
13.0
nM
|
|
|
Affinity for alpha-1 adrenergic receptor
|
Rattus norvegicus
|
3.0
nM
|
|
|
Compound was evaluated for its binding affinity with Alpha-1 adrenergic receptor using membranes prepared from rat cerebral cortex
|
None
|
0.81
nM
|
|
|
Inhibition of mouse Dopamine receptor D2
|
Mus musculus
|
23.0
nM
|
|
|
Ability to displace [3H]spiperone from D2 dopamine receptor isolated from the striata of male Wistar rats
|
None
|
1.8
nM
|
|
|
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
|
None
|
251.0
nM
|
|
|
Affinity for dopamine receptor D2 binding sites by its ability to displace [3H]spiperone from rat striatum.
|
None
|
37.5
nM
|
|
|
Affinity for Dopamine receptor D1
|
Rattus norvegicus
|
22.0
nM
|
|
|
Binding affinity towards Dopamine receptor D2 was determined in rat striatum using [3H]- spiperone as radioligand
|
None
|
37.0
nM
|
|
|
Compound was measured for affinity at dopamine receptor D2 labeled with [3H]spiroperidol radioligand in striatum tissue
|
None
|
30.0
nM
|
|
|
Binding affinity to the dopamine receptor D2L in rat brain membranes
|
None
|
5.1
nM
|
|
|
Binding affinity towards human dopamine-4.2 receptor
|
None
|
16.0
nM
|
|
|
Binding affinity towards human Dopamine receptor D2
|
None
|
3.3
nM
|
|
|
Binding affinity towards human D2 dopamine receptor.
|
None
|
0.44
nM
|
|
|
Binding affinity against dopamine receptor D1
|
None
|
21.0
nM
|
|
|
Binding affinity towards human Dopamine receptor D1
|
None
|
620.0
nM
|
|
|
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
|
None
|
6.2
nM
|
|
|
Binding affinity towards human dopamine receptor D4
|
None
|
16.0
nM
|
|
|
Affinity against Dopamine receptor D2
|
Rattus norvegicus
|
8.128
nM
|
|
|
Displacement of [3H]NPA from rat brain Dopamine receptor D2
|
Rattus norvegicus
|
3.715
nM
|
|
|
In vitro ability to displace [3H]spiperone binding from dopamine receptor D2 in rat striatal membrane.
|
None
|
8.128
nM
|
|
|
Binding affinity for dopamine receptor D2 determined using [3H]spiperone
|
None
|
3.1
nM
|
|
|
Compound was tested for the inhibition of [3H]spiperone binding to dopamine receptor D2
|
None
|
4.0
nM
|
|
|
Inhibition of [3H]methylspiperone binding to rat striatal membrane Dopamine receptor D2
|
Rattus norvegicus
|
27.4
nM
|
|
|
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D2L in COS7 cells
|
None
|
1.4
nM
|
|
|
Binding affinity measured at the Dopamine receptor D3 by the inhibition of [3H]YM-09151-2 binding to human recombinant CCL 1.3 cells using unlabeled 7-OH-DPAT for nonspecific binding.
|
None
|
31.0
nM
|
|
|
Binding affinity measured at the Dopamine receptor D2 by the inhibition of [3H]methylspiperone binding to rat striatum using unlabeled haloperidol for nonspecific binding.
|
None
|
19.0
nM
|
|
|
Binding affinity towards human dopamine receptor D3
|
None
|
14.0
nM
|
|
|
Affinity for Dopamine receptor D2
|
Rattus norvegicus
|
2.1
nM
|
|
|
Compound was evaluated for its binding affinity with Dopamine receptor D2 using membranes prepared from rat striatum
|
None
|
3.1
nM
|
|
|
Displacement of [3H]NPA from rat brain Dopamine receptor D2
|
Rattus norvegicus
|
3.7
nM
|
|
|
Binding affinity towards human Dopamine receptor D3
|
None
|
13.0
nM
|
|
|
The binding affinity was measured on dopamine receptor D2 in rat brain tissue
|
None
|
2.8
nM
|
|
|
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
|
None
|
7.0
nM
|
|
|
Binding affinity towards human histamine H1 receptor
|
None
|
2.6
nM
|
|
|
Binding affinity towards human H1 receptor
|
None
|
88.0
nM
|
|
|
Inhibition of human Potassium channel HERG expressed in mammalian cells
|
Homo sapiens
|
151.36
nM
|
|
|
Activity administered intraperitoneally was determined by social interaction of rat at 0.5 uM
|
Rattus norvegicus
|
27.0
%
|
|
|
The compound was measured at a dose 10 times the ED50 value for CAR block for production of catalepsy in the rat
|
Rattus norvegicus
|
0.32
nM
|
|
|
ED50 value for catalepsy indicates the dose required to produce a 50% of maximum catalepsy score
|
Rattus norvegicus
|
35.0
nM
|
|
|
In vitro affinity towards D2 receptor using [3H]spiroperidol as radioligand in striatum
|
None
|
37.0
nM
|
|
|
K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1
|
Homo sapiens
|
163.0
nM
|
|
|
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
|
Rattus norvegicus
|
147.0
nM
|
|
|
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
|
Homo sapiens
|
10.0
nM
|
|
|
Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor
|
Homo sapiens
|
3.2
nM
|
|
|
Inhibition of [3H]prazosin binding to rat Alpha-1 adrenergic receptor
|
Rattus norvegicus
|
2.5
nM
|
|
|
Inhibition of [125I]R91150 binding to human 5-hydroxytryptamine 2A receptor
|
Homo sapiens
|
0.81
nM
|
|
|
Inhibition of [3H]-spiperone binding to human Dopamine receptor D2
|
Homo sapiens
|
6.4
nM
|
|
|
Inhibition of [3H]mesulergine binding to human 5-hydroxytryptamine 2C receptor
|
Homo sapiens
|
12.0
nM
|
|
|
Inhibitory constant against dopamine D2 receptor using 0.2 nM [3H]-spiperone
|
Rattus norvegicus
|
6.65
nM
|
|
|
Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor
|
Homo sapiens
|
33.0
nM
|
|
|
Inhibition of [3H]5-HT binding to human 5-hydroxytryptamine 7 receptor
|
Homo sapiens
|
4.3
nM
|
|
|
Inhibition of [125I]iodosulpiride binding to human Dopamine receptor D3
|
Homo sapiens
|
16.0
nM
|
|
|
Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active
|
Homo sapiens
|
2.8
nM
|
|
|
Inhibitory concentration against IKr potassium channel
|
None
|
260.0
nM
|
|
|
Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open state
|
Homo sapiens
|
162.18
nM
|
|
|
Displacement of [3H]spiperone from human dopamine D2 receptor short form expressed in CHO cells
|
Homo sapiens
|
6.31
nM
|
|
|
Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells
|
Homo sapiens
|
10.0
nM
|
|
|
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
|
Homo sapiens
|
10.0
nM
|
|
|
Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells
|
Homo sapiens
|
251.19
nM
|
|
|
Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHO cells
|
Homo sapiens
|
1.0
nM
|
|
|
Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cells
|
Homo sapiens
|
19.95
nM
|
|
|
Displacement of [3H]mesulergine from 5HT2C receptor expressed in CHO cells
|
Homo sapiens
|
12.59
nM
|
|
|
Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells
|
Homo sapiens
|
1.0
nM
|
|
|
Displacement of [3H]prazosin from adrenergic alpha1 receptor in rat cerebral cortex
|
Rattus norvegicus
|
1.585
nM
|
|
|
Displacement of [3H]RX 821002 from adrenergic alpha-2 receptor in rat cerebral cortex
|
Rattus norvegicus
|
7.943
nM
|
|
|
Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum
|
Cavia porcellus
|
7.943
nM
|
|
|
Displacement of [3H]spiperone from dopamine D2 receptor in rat brain
|
Rattus norvegicus
|
3.105
nM
|
|
|
Displacement of [3H]ketanserin from 5HT2A receptor in rat brain
|
Rattus norvegicus
|
0.1603
nM
|
|
|
Displacement of [3H]ketanserin human cloned serotonin 5HT2A receptor
|
Homo sapiens
|
0.5012
nM
|
|
|
Displacement of [3H]mesulergine human cloned serotonin 5HT2C receptor
|
Homo sapiens
|
7.413
nM
|
|
|
Displacement of [3H]mepyramine from H1R in rat brain
|
Rattus norvegicus
|
80.0
nM
|
|
|
Binding affinity to human cloned dopamine D1 receptor
|
Homo sapiens
|
580.0
nM
|
|
|
Binding affinity to human cloned dopamine D2 receptor
|
Homo sapiens
|
2.2
nM
|
|
|
Binding affinity to human cloned dopamine D3 receptor
|
Homo sapiens
|
9.6
nM
|
|
|
Binding affinity to human cloned dopamine D4 receptor
|
Homo sapiens
|
8.5
nM
|
|
|
Binding affinity to human cloned 5HT2C receptor
|
Homo sapiens
|
10.0
nM
|
|
|
Binding affinity to human cloned histamine H1 receptor
|
Homo sapiens
|
19.0
nM
|
|
|
Binding affinity to human cloned 5HT1A receptor
|
Homo sapiens
|
210.0
nM
|
|
|
Binding affinity to human cloned 5HT2A receptor
|
Homo sapiens
|
0.29
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
|
39.3
%
|
|
|
Inhibition of human ERG channel
|
Homo sapiens
|
148.0
nM
|
|
Inhibition of human ERG channel
|
Homo sapiens
|
148.0
nM
|
|
|
Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique
|
Homo sapiens
|
151.36
nM
|
|
|
Inhibition of dopamine D2 receptor-mediated apomorphine-induced cage climbing behavior in Swiss albino mouse at 10 mg/kg measured on 10 mins
|
Mus musculus
|
91.0
%
|
|
|
Inhibition of dopamine D2 receptor-mediated apomorphine-induced cage climbing behavior in Swiss albino mouse at 10 mg/kg measured on 20 mins
|
Mus musculus
|
91.0
%
|
|
|
Inhibition of dopamine D2 receptor-mediated apomorphine-induced cage climbing behavior in Swiss albino mouse at 10 mg/kg measured on 30 mins
|
Mus musculus
|
90.0
%
|
|
|
Inhibition of 5HT2A receptor-mediated quipazine-induced head twitches in Swiss albino mouse at 10 mg/kg
|
Mus musculus
|
100.0
%
|
|
|
Inhibition of dopamine D2 receptor-mediated apomorphine-induced cage climbing behavior in Swiss albino mouse at 10 mg/kg
|
Mus musculus
|
91.0
%
|
|
|
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
|
Rattus norvegicus
|
50.0
nM
|
|
|
Displacement of [3H]spiperone from dopamine D2 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
|
Rattus norvegicus
|
3.8
nM
|
|
|
Displacement of [3H]7OH-DPAT from dopamine D3 receptor expressed in Sf9 cells by scintillation spectrometry
|
None
|
6.7
nM
|
|
|
Displacement of [3H]8OH-DPAT from 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus by scintillation spectrometry
|
Rattus norvegicus
|
190.0
nM
|
|
|
Displacement of [3H]ketanserin from 5HT2A receptor in CRL:CD(SD)BR-COBS rat cortex by scintillation spectrometry
|
Rattus norvegicus
|
0.15
nM
|
|
|
Displacement of [3H]mesulergine from 5HT2C receptor in CRL:(HA) BR albino guinea pig cortex by scintillation spectrometry
|
Cavia porcellus
|
32.0
nM
|
|
|
Binding affinity to human ERG expressed in HEK293 cells by whole cell patch clamp method
|
Homo sapiens
|
920.0
nM
|
|
|
Inhibition of human ERG in MCF7 cells
|
Homo sapiens
|
162.18
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
%
|
|
|
Binding affinity to 5HT1A receptor
|
None
|
398.11
nM
|
|
|
Displacement of [3H]spiperone from human cloned dopamine D2 receptor
|
Homo sapiens
|
6.166
nM
|
|
|
Displacement of [3H]ketanserin from human cloned 5HT2A receptor
|
Homo sapiens
|
0.5012
nM
|
|
|
Displacement of [3H]SCH23390 from human dopamine D1 receptor
|
Homo sapiens
|
147.91
nM
|
|
|
Displacement of [3H]spiperone from human dopamine D3 receptor
|
Homo sapiens
|
16.22
nM
|
|
|
Displacement of [3H]mesulergine from human 5HT2C receptor
|
Homo sapiens
|
7.413
nM
|
|
|
Inhibition of human ERG
|
Homo sapiens
|
147.91
nM
|
|
|
Displacement of [3H]mesulergine from human 5HT2C receptor in human tsA201 cells
|
Homo sapiens
|
33.0
nM
|
|
|
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
|
Homo sapiens
|
224.0
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
|
None
|
799.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
|
None
|
457.0
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
|
None
|
0.346
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
|
None
|
0.099
nM
|
|
|
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
0.989
nM
|
|
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
0.4
nM
|
|
|
DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
1.949
nM
|
|
DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
1.079
nM
|
|
|
DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
|
None
|
9.995
nM
|
|
DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
|
None
|
4.913
nM
|
|
|
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
|
None
|
9.674
nM
|
|
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
|
None
|
3.628
nM
|
|
|
DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
|
None
|
26.0
nM
|
|
DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
|
None
|
12.0
nM
|
|
|
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
|
None
|
9.557
nM
|
|
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
|
None
|
1.389
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
23.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
15.0
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
|
None
|
15.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
|
None
|
7.639
nM
|
|
|
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
|
None
|
479.0
nM
|
|
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
|
None
|
240.0
nM
|
|
|
DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
|
None
|
20.0
nM
|
|
DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
|
None
|
6.545
nM
|
|
|
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
|
None
|
24.0
nM
|
|
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
|
None
|
8.036
nM
|
|
|
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
|
None
|
25.0
nM
|
|
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
|
None
|
2.87
nM
|
|
|
DRUGMATRIX: Imidazoline I2, Central radioligand binding (ligand: [3H] Idazoxan)
|
Rattus norvegicus
|
20.0
nM
|
|
DRUGMATRIX: Imidazoline I2, Central radioligand binding (ligand: [3H] Idazoxan)
|
Rattus norvegicus
|
13.0
nM
|
|
|
Displacement of [3H]methylspiperone from human low affinity Dopamine D2S receptor by competition binding assay
|
Homo sapiens
|
2.7
nM
|
|
|
In vivo inhibition of 5-HT2A receptor in Swiss albino Mus musculus (mouse) at 10 mg/kg, ip relative to vehicle-treated control
|
Mus musculus
|
100.0
%
|
|
|
Antagonist activity at central serotonergic 5-HT2A receptor in Swiss albino Mus musculus (mouse) assessed as inhibition of quipazine meleate-induced head twiches at 0.6 mg/kg, ip administered 1 hr prior to quipazine meleate challenge measured after 30 to 40 min relative to vehicle-treated control
|
Mus musculus
|
100.0
%
|
|
|
Antagonist activity at mesolimbic dopaminergic D2 receptor in Swiss albino Mus musculus (mouse) assessed as inhibition of apomorphine-induced cage climbing behavior at 0.6 mg/kg, ip administered 1 hr prior to apomorphine challenge measured after 30 min relative to vehicle-treated control
|
Mus musculus
|
90.0
%
|
|
|
Antagonist activity at mesolimbic dopaminergic D2 receptor in Swiss albino Mus musculus (mouse) assessed as inhibition of apomorphine-induced cage climbing behavior at 0.6 mg/kg, ip administered 1 hr prior to apomorphine challenge measured after 20 min relative to vehicle-treated control
|
Mus musculus
|
91.0
%
|
|
|
Antagonist activity at mesolimbic dopaminergic D2 receptor in Swiss albino Mus musculus (mouse) assessed as inhibition of apomorphine-induced cage climbing behavior at 0.6 mg/kg, ip administered 1 hr prior to apomorphine challenge measured after 10 min relative to vehicle-treated control
|
Mus musculus
|
91.0
%
|
|
|
Inhibition of human ERG expressed in HEK293 cells by electrophysiology assay
|
Homo sapiens
|
581.0
nM
|
|
|
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis
|
Cavia porcellus
|
21.7
nM
|
|
|
Displacement of [3H]7-OH-DPAT from dopamine D3 receptor in rat olfactory tubercle after 60 mins by liquid scintillation counting analysis
|
Rattus norvegicus
|
9.7
nM
|
|
|
Displacement of [3H]ketanserin from 5HT2A receptor in rat cerebral cortex after 15 mins by liquid scintillation counting analysis
|
Rattus norvegicus
|
0.18
nM
|
|
|
Displacement of [3H]8-OH-DPAT from 5HT1A receptor in rat cerebral cortex after 30 mins by liquid scintillation counting analysis
|
Rattus norvegicus
|
180.0
nM
|
|
|
Displacement of [3H]spiperone from dopamine D2 receptor in rat striatum after 15 mins by liquid scintillation counting analysis
|
Rattus norvegicus
|
3.7
nM
|
|
|
Displacement of [3H]mesulergine from 5HT2C receptor in rat cerebral cortex after 15 mins by liquid scintillation counting analysis
|
Rattus norvegicus
|
14.5
nM
|
|
|
Displacement of [3H]prazosin from alpha-1 adrenergic receptor in rat cerebral cortex after 60 mins by liquid scintillation counting analysis
|
Rattus norvegicus
|
2.9
nM
|
|
|
Displacement of [3H]rauwolscine from alpha-2 adrenergic receptor in rat cerebral cortex after 60 mins by liquid scintillation counting analysis
|
Rattus norvegicus
|
29.5
nM
|
|
|
Antipsychotic activity in Sprague-Dawley rat psychosis model assessed as inhibition of MK-801-induced hyperlocomotion at 1 mg/kg, ip administered 5 mins prior to MK-801-challenge measured after 15 mins up to 1 hr
|
Rattus norvegicus
|
72.0
%
|
|
|
Displacement of [3H]spiperone from human D2 receptor
|
Homo sapiens
|
6.166
nM
|
|
|
Displacement of [3H]ketanserin from human 5-HT2A receptor
|
Homo sapiens
|
0.5012
nM
|
|
|
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting
|
Cavia porcellus
|
22.9
nM
|
|
|
Displacement of [3H]7-OH-DPA from dopamine D3 receptor in Sprague-Dawley rat olfactory tubercle homogenate after 60 mins by liquid scintillation counting
|
Rattus norvegicus
|
10.1
nM
|
|
|
Displacement of [3H]spiperone from dopamine D2 receptor in Sprague-Dawley rat striatum homogenate after 30 mins by liquid scintillation counting
|
Rattus norvegicus
|
2.8
nM
|
|
|
Displacement of [3H]Ketanserin from 5HT2A receptor in Sprague-Dawley rat brain cortex homogenate after 30 mins by liquid scintillation counting
|
Rattus norvegicus
|
0.25
nM
|
|
|
Displacement of [3H]8-OH-DPAT from 5HT1A receptor in Sprague-Dawley rat brain cortex homogenate after 30 mins by liquid scintillation counting
|
Rattus norvegicus
|
190.2
nM
|
|
|
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
|
Homo sapiens
|
10.0
nM
|
|
|
Binding affinity to serotonin 5-HT2A receptor (unknown origin) by PDSP assay
|
Homo sapiens
|
1.0
nM
|
|
|
Binding affinity to serotonin 5-HT2C receptor (unknown origin) by PDSP assay
|
Homo sapiens
|
100.0
nM
|
|
|
Binding affinity to serotonin 5-HT7 receptor (unknown origin) by PDSP assay
|
Homo sapiens
|
10.0
nM
|
|
|
Binding affinity to dopamine D2 receptor (unknown origin) by PDSP assay
|
Homo sapiens
|
10.0
nM
|
|
|
Binding affinity to dopamine D3 receptor (unknown origin) by PDSP assay
|
Homo sapiens
|
100.0
nM
|
|
|
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
|
Homo sapiens
|
100.0
nM
|
|
|
Binding affinity to adrenergic alpha1A receptor (unknown origin) by PDSP assay
|
Homo sapiens
|
10.0
nM
|
|
|
Binding affinity to adrenergic alpha1B receptor (unknown origin) by PDSP assay
|
Homo sapiens
|
10.0
nM
|
|
|
Binding affinity to adrenergic alpha2C receptor (unknown origin) by PDSP assay
|
Homo sapiens
|
10.0
nM
|
|
|
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assay
|
Homo sapiens
|
100.0
nM
|
|
|
Displacement of [3H]spiperone from human cloned D2 receptor by in vitro binding assay
|
Homo sapiens
|
6.166
nM
|
|
|
Displacement of [3H]ketanserin from human cloned 5-HT2A receptor by in vitro binding assay
|
Homo sapiens
|
0.5012
nM
|
|
|
Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in CHO-K1 cell membrane after 60 mins by liquid scintillation counting analysis
|
Homo sapiens
|
1.0
nM
|
|
|
Binding affinity to dopamine D2 receptor (unknown origin)
|
Homo sapiens
|
3.8
nM
|
|
|
Binding affinity to dopamine D3 receptor (unknown origin)
|
Homo sapiens
|
6.7
nM
|
|
|
Binding affinity to 5HT1A receptor (unknown origin)
|
Homo sapiens
|
190.0
nM
|
|
|
Binding affinity to 5HT2A receptor (unknown origin)
|
Homo sapiens
|
0.15
nM
|
|
|
Binding affinity to 5HT2C receptor (unknown origin)
|
Homo sapiens
|
32.0
nM
|
|
|
Potentiation of human GlyR-alpha1 expressed in Xenopus laevis oocytes assessed as induction of glycine-activated currents after 1 to 4 days by two-electrode voltage clamp assay
|
Homo sapiens
|
320.0
nM
|
|
|
Inhibition of hERG K channel
|
None
|
150.0
nM
|
|
|
Displacement of [3H]spiperone from dopaminergic D2 receptor in rat striatum homogenates after 60 mins by liquid scintillation counting
|
Rattus norvegicus
|
3.6
nM
|
|
|
Displacement of [3H]8-OH-DPAT from 5-HT1A receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting
|
Rattus norvegicus
|
211.0
nM
|
|
|
Displacement of [3H]ketanserine from 5-HT2A receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting
|
Rattus norvegicus
|
0.31
nM
|
|
|
Displacement of [3H]-5-CT from 5-HT7 receptor in rat hypothalamus homogenates after 120 mins by liquid scintillation counting
|
Rattus norvegicus
|
3.2
nM
|
|
|
Displacement of [3H]prazosin from adrenergic alpha1 receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting
|
Rattus norvegicus
|
11.9
nM
|
|
|
Displacement of [3H]-rauwolscine from adrenergic alpha2 receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting
|
Rattus norvegicus
|
28.2
nM
|
|
|
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation counting
|
Cavia porcellus
|
38.3
nM
|
|
|
Displacement of [3H]mesulergine from 5-HT2C receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting
|
Rattus norvegicus
|
30.1
nM
|
|
|
Antipsychotic activity in Sprague Dawley rat psychosis model assessed as inhibition of 0.2 mg/kg dizocilpine-induced hyperlocomotion at 1 mg/kg, ip administered 30 mins prior to dizocilpine challenge measured every 5 mins for 1 hr starting from the 15th min of post dizocilpine challenge
|
Rattus norvegicus
|
82.0
%
|
|
|
Antipsychotic activity in Sprague Dawley rat psychosis model assessed as inhibition of 0.2 mg/kg dizocilpine-induced stereotypy at 1 mg/kg, ip administered 30 mins prior to dizocilpine challenge measured every 5 mins for 1 hr starting from the 15th min of post dizocilpine challenge
|
Rattus norvegicus
|
68.0
%
|
|
|
Antipsychotic activity in Sprague Dawley rat psychosis model assessed as inhibition of 0.2 mg/kg dizocilpine-induced ataxia at 1 mg/kg, ip administered 30 mins prior to dizocilpine challenge measured every 5 mins for 1 hr starting from the 15th min of post dizocilpine challenge
|
Rattus norvegicus
|
78.0
%
|
|
|
Antipsychotic activity in Sprague Dawley rat assessed as inhibition of 1 mg/kg quipazine-induced head twitches at 1 mg/kg, ip administered 30 mins prior to dizocilpine challenge measured for 30 mins
|
Rattus norvegicus
|
83.0
%
|
|
|
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
|
Homo sapiens
|
0.5
nM
|
|
|
Receptor Binding Assay: Alpha-1 receptor binding studies were performed according to the methods described by Greengrass and Bremner (Eur. J. Pharmacol., 55:323-326, 1979) on rat cortical membrane preparation using [3H]-prazosine (0.22-0.37 nM) as ligand. The non-specific binding was determined in the presence of 10 μM phentolamine.
|
None
|
0.88
nM
|
|
|
Receptor Binding Assay: D2 receptor binding was determined as described by Creese et al. (Eur. J. Pharmacol., 60:55-66, 1979) on rat brain striatal membrane preparation using [3H]spiperone (0.4-1.3 nM) as ligand. Non-specific binding was determined in the presence of 1 μM (+) butaclamol.
|
Rattus norvegicus
|
13.0
nM
|
|
|
Receptor Binding Assay: Binding assays were carried out on rat recombinant D3 receptors (Perkin-Elmer, Cat. No. 6110139) expressed in Sf9 cells using [3H]spiperone (0.44-1.49 nM) as ligand and haloperidol (10 μM) for determination of non-specific binding. The assay was performed according to the supplier's assay protocol (Cat. No.: 3110139).
|
None
|
13.0
nM
|
|
|
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
|
Homo sapiens
|
63.0
nM
|
|
|
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
|
Homo sapiens
|
14.0
nM
|
|
|
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
|
Homo sapiens
|
5.9
nM
|
|
|
Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
|
Homo sapiens
|
2.3
nM
|
|
|
Displacement of [3H]spiperone from dopamine D2 receptor in rat striatum
|
Rattus norvegicus
|
2.8
nM
|
|
|
Displacement of [3H]8-OH-DPAT from 5HT1A receptor in rat brain cortex
|
Rattus norvegicus
|
190.2
nM
|
|
|
Displacement of [3H]ketanserin from 5HT2A receptor in rat brain cortex
|
Rattus norvegicus
|
0.25
nM
|
|
|
Displacement of [3H]7-OH-DPAT from dopamine D3 receptor in rat olfactory tubercle
|
Rattus norvegicus
|
15.1
nM
|
|
|
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum
|
Cavia porcellus
|
41.2
nM
|
|
|
Displacement of [3H]mesulergine from 5HT2C receptor in rat brain cortex
|
Rattus norvegicus
|
125.9
nM
|
|
|
Displacement of [3H]prazosin from adrenergic alpha1 receptor in rat brain cortex
|
Rattus norvegicus
|
7.8
nM
|
|
|
Displacement of [3H]rauwolscine from adrenergic alpha2 receptor in rat brain cortex
|
Rattus norvegicus
|
56.8
nM
|
|
|
Inhibition of human ERG
|
Homo sapiens
|
778.0
nM
|
|
|
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
|
Homo sapiens
|
10.0
nM
|
|
|
Antagonistic activity at histamine1 receptor (unknown origin) after 10 mins by FLIPR assay
|
Homo sapiens
|
868.0
nM
|
|
|
Antagonistic activity at 5-HT2c receptor (unknown origin) after 10 mins by FLIPR assay
|
Homo sapiens
|
7.0
nM
|
|
|
Displacement of [3H]mesulergine from 5-HT2C receptor in Sprague-Dawley rat cerebral cortex incubated for 15 mins in presence of spiperone by liquid scintillation counting analysis
|
Rattus norvegicus
|
26.7
nM
|
|
|
Displacement of [3H]spiperone from dopamine D2 receptor in Sprague-Dawley rat striatum incubated for 30 mins by liquid scintillation counting analysis
|
Rattus norvegicus
|
3.7
nM
|
|
|
Displacement of [3H]8-OH-DPAT from 5-HT1A receptor in Sprague-Dawley rat cerebral cortex incubated for 30 mins by liquid scintillation counting analysis
|
Rattus norvegicus
|
182.0
nM
|
|
|
Displacement of [3H] ketanserin from 5-HT2A receptor in Sprague-Dawley rat cerebral cortex incubated for 30 mins by liquid scintillation counting analysis
|
Rattus norvegicus
|
0.18
nM
|
|
|
Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum incubated for 60 mins by liquid scintillation counting analysis
|
Cavia porcellus
|
42.6
nM
|
|
|
Displacement of [3H]prazosin from adrenergic alpha1 receptor in Sprague-Dawley rat cerebral cortex incubated for 60 mins by liquid scintillation counting analysis
|
Rattus norvegicus
|
57.8
nM
|
|
|
Antagonist activity at dopamine D2 receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
|
Homo sapiens
|
7.09
nM
|
|
|
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
|
Homo sapiens
|
4.67
nM
|
|
|
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
|
Homo sapiens
|
10.9
nM
|
|
|
Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
|
Homo sapiens
|
454.0
nM
|
|
|
Antagonist activity at 5-HT2C receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
|
Homo sapiens
|
1.81
nM
|
|
|
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
|
Homo sapiens
|
10.0
nM
|
|
|
Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay
|
Homo sapiens
|
454.0
nM
|
|
|
Antagonistic activity at 5-HT2c receptor (unknown origin) after 10 mins by FLIPR assay
|
Homo sapiens
|
7.0
nM
|
|
|
Displacement of [3H]-ketanserin from human 5-HT2AR expressed in CHO-K1 cell membranes after 1.5 hrs by microbeta counting method
|
Homo sapiens
|
0.5
nM
|
|
|
Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
|
Homo sapiens
|
0.4
nM
|
|
|
Displacement of [3H]-raclopride from human D2LR expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
|
Homo sapiens
|
0.6
nM
|
|
|
Antagonist activity at 5-HT2C receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
|
Homo sapiens
|
1.81
nM
|
|
|
Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
|
Homo sapiens
|
454.0
nM
|
|
|
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
|
Homo sapiens
|
10.9
nM
|
|
|
Displacement of [3H]-spiperone from dopamine D2 receptor in rat striatum homogenates after 30 mins by liquid scintillation counting
|
Rattus norvegicus
|
3.7
nM
|
|
|
Displacement of [3H]-8-OH-DPAT from serotonin 5-HT1A receptor in rat brain cortex homogenates incubated for 30 mins by liquid scintillation counting
|
Rattus norvegicus
|
181.9
nM
|
|
|
Displacement of [3H]-ketanserine from serotonin 5-HT2A receptor in rat brain cortex homogenates incubated for 30 mins by liquid scintillation counting
|
Rattus norvegicus
|
0.18
nM
|
|
|
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation counting
|
Cavia porcellus
|
46.2
nM
|
|
|
Displacement of [3H]-mesulergine from serotonin 5-HT2C receptor in rat brain cerebral cortex homogenates incubated for 15 mins by liquid scintillation counting
|
Rattus norvegicus
|
28.2
nM
|
|
|
Displacement of [3H]-prazosin from alpha-1 adrenergic receptor in rat cerebral cortex homogenates incubated for 60 mins by liquid scintillation counting
|
Rattus norvegicus
|
54.7
nM
|
|
|
Displacement of [3H] 7-OH-DPAT from dopamine D3 receptor in rat olfactory tubercle homogenates after 60 mins by liquid scintillation counting
|
Rattus norvegicus
|
31.9
nM
|
|
|
Inhibition of human ERG expressed in HEK293 cells at -50 mV holding potential by patch clamp assay
|
Homo sapiens
|
167.1
nM
|
|
|
Antibacterial activity against Staphylococcus aureus MRSA ATCC 43300 (CO-ADD:GP_020); MIC in CAMBH media, using NBS plates, by OD(600)
|
Staphylococcus aureus subsp. aureus
|
4.53
%
|
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
2.58
%
|
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
4.8
%
|
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
4.12
%
|
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
8.1
%
|
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
0.09
%
|
|
|
Antifungal activity against Cryptococcus neoformans H99 ATCC 208821 (CO-ADD:FG_002); MIC in YNB media using NBS plates, by Resazurin OD(600-570)
|
Cryptococcus neoformans
|
-0.58
%
|
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging
|
Homo sapiens
|
1.52
%
|
|
|
Displacement of [3H]ketanserin from human 5HT2A receptor expressed in HEK293 cell membranes measured after 30 mins
|
Homo sapiens
|
0.37
nM
|
|
|
Antagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assay
|
Homo sapiens
|
0.7079
nM
|
|
Antagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assay
|
Homo sapiens
|
0.72
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
|
14.83
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
14.66
%
|
|
|
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
|
0.42
%
|
|
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
|
0.42
%
|
|
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
%
|
|
|
Antagonist activity at alpha-1a adrenergic receptor (unknown origin)
|
Homo sapiens
|
10.9
nM
|
|
|
Cytotoxicity against human Chang cells assessed as reduction in cell viability
|
Homo sapiens
|
238.8
ug.mL-1
|
|
|
Cytotoxicity against human HEK293 cells assessed as reduction in cell viability
|
Homo sapiens
|
600.0
ug.mL-1
|
|
|
Antagonist activity at 5-HT2C receptor (unknown origin)
|
Homo sapiens
|
1.81
nM
|
|
|
Antagonist activity at H1 receptor (unknown origin)
|
Homo sapiens
|
454.0
nM
|
|
|
Binding affinity to H1 histamine receptor (unknown origin)
|
Homo sapiens
|
20.0
nM
|
|
|
Binding affinity to adrenergic alpha1 receptor (unknown origin)
|
Homo sapiens
|
0.7
nM
|
|
|
Antagonist activity at D2 receptor (unknown origin)
|
Homo sapiens
|
3.57
nM
|
|
|
Antagonist activity at 5HT2A receptor (unknown origin)
|
Homo sapiens
|
0.17
nM
|
|
|
Displacement of [3H]spiperone from D2 receptor in rat striatum measured after 15 mins by liquid scintillation counting method
|
Rattus norvegicus
|
3.7
nM
|
|
|
Displacement of [3H](+)8-OH-DPAT from rat cerebral cortex 5HT1A receptor measured after 30 mins by liquid scintillation counting method
|
Rattus norvegicus
|
182.0
nM
|
|
|
Displacement of [3H]ketanserin from rat cerebral cortex 5HT2A receptor measured after 15 mins by liquid scintillation counting method
|
Rattus norvegicus
|
0.19
nM
|
|
|
Displacement of [3H]prazosin from rat cerebral cortex alpha1 adrenergic receptor measured after 60 mins by liquid scintillation counting method
|
Rattus norvegicus
|
3.2
nM
|
|
|
Displacement of [3H]mesulergine from rat cerebral cortex 5HT2C receptor measured after 15 mins by liquid scintillation counting method
|
Rattus norvegicus
|
20.9
nM
|
|
|
Displacement of [3H]pyrilamine from guinea pig cerebellum histamine H1 receptor measured after 60 mins by liquid scintillation counting method
|
Cavia porcellus
|
32.6
nM
|
|
|
Displacement of [3H]5-CT from rat cerebral cortex 5HT7 receptor measured after 30 mins by liquid scintillation counting method
|
Rattus norvegicus
|
40.7
nM
|
|
|
Inhibition of human ERG expressed in HEK293 cells by whole-cell patch clamp method
|
Homo sapiens
|
167.0
nM
|
|
|
Binding affinity to D2 receptor (unknown origin)
|
Homo sapiens
|
3.8
nM
|
|
|
Binding affinity to 5HT1A receptor (unknown origin)
|
Homo sapiens
|
271.0
nM
|
|
|
Binding affinity to 5HT2A receptor (unknown origin)
|
Homo sapiens
|
0.39
nM
|
|
|
Binding affinity to alpha2 adrenergic receptor (unknown origin)
|
Homo sapiens
|
28.2
nM
|
|
|
Binding affinity to H1 receptor (unknown origin)
|
Homo sapiens
|
49.3
nM
|
|
|
Binding affinity to 5HT2C receptor (unknown origin)
|
Homo sapiens
|
39.1
nM
|
|
|
Binding affinity to alpha1 adrenergic receptor (unknown origin)
|
Homo sapiens
|
21.9
nM
|
|
|
Binding affinity to dopamine D2 receptor (unknown origin)
|
Homo sapiens
|
3.9
nM
|
|
|
Binding affinity to dopamine D3 receptor (unknown origin)
|
Homo sapiens
|
14.3
nM
|
|
|
Binding affinity to 5-HT1A receptor (unknown origin)
|
Homo sapiens
|
182.0
nM
|
|
|
Binding affinity to 5-HT2A receptor (unknown origin)
|
Homo sapiens
|
0.19
nM
|
|
|
Binding affinity to 5-HT2C receptor (unknown origin)
|
Homo sapiens
|
20.9
nM
|
|
|
Binding affinity to alpha1 adrenoceptor (unknown origin)
|
Homo sapiens
|
3.2
nM
|
|
|
Binding affinity to histamine H1 receptor (unknown origin)
|
Homo sapiens
|
32.6
nM
|
|
|
Inhibition of human ERG by automated patch method relative to control
|
Homo sapiens
|
167.0
nM
|
|
