|
Binding affinity towards human cloned 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand
|
None
|
10.0
nM
|
|
|
Antagonistic affinity against Alpha-1B adrenergic receptor was determined in isolated spleen tissue from rat
|
None
|
1.023
nM
|
|
|
Antagonism of phenylephrine stimulated contraction of the rat isolated spleen.
|
None
|
1.023
nM
|
|
|
Compound was tested for binding Alpha-1B adrenergic receptor from rat liver using radioligand ([3H]prazosin) binding assay
|
None
|
0.3631
nM
|
|
|
Compound was tested for its binding affinity for alpha-1 adrenergic receptor site by displacement of [3H]clonidine at 10e-6 M concentration
|
None
|
0.19
nM
|
|
|
Compound was tested for the inhibition of [3H]prazosin binding Alpha-1 adrenergic receptor of crude rat brain membrane.
|
None
|
0.16
nM
|
|
|
Evaluated for binding affinity against alpha-1 adrenergic receptor
|
None
|
0.32
nM
|
|
|
Binding affinity was determined for the alpha-1D adrenergic receptor
|
None
|
0.33
nM
|
|
|
Ability to displace [3H]prazosin from cloned human Alpha-1D adrenergic receptor
|
None
|
0.3
nM
|
|
|
Binding affinity against human Alpha-1D adrenergic receptor (h alpha-1d)
|
None
|
0.33
nM
|
|
|
Compound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1D adrenergic receptor
|
None
|
0.2
nM
|
|
|
In vitro binding affinity against alpha-1D adrenergic receptor of human liver microsomes.
|
None
|
0.3
nM
|
|
|
Binding affinity against Alpha-1D adrenergic receptor, from human clones.
|
Homo sapiens
|
0.32
nM
|
|
|
The compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1D adrenergic receptor in CHO cells
|
None
|
0.29
nM
|
|
|
Antagonistic activity against presynaptic alpha-2 adrenergic receptor in isolated rat vas deferens using xylazine as agonist
|
None
|
144.54
nM
|
|
|
Intrinsic activity for displacement of [3H]- prazosin from Alpha-1 adrenergic receptor of rat cerebral cortex membrane in the absence of 1 nM GTP
|
None
|
0.26
nM
|
|
|
Intrinsic activity for displacement of [3H]- prazosin from Alpha-1 adrenergic receptor of rat cerebral cortex membrane in the presence of 1 nM GTP
|
None
|
0.32
nM
|
|
|
Intrinsic activity towards Alpha-1 adrenergic receptor by the displacement of [3H]prazosin from rat cerebral cortex membrane in absence of 1 nM GTP
|
None
|
0.26
nM
|
|
|
Intrinsic activity towards Alpha-1 adrenergic receptor by the displacement of [3H]prazosin from rat cerebral cortex membrane in presence of 1 nM GTP.
|
None
|
0.32
nM
|
|
|
In vitro binding affinity determined for alpha-1 adrenergic receptor by the displacement of [3H]- prazosin.
|
None
|
0.19
nM
|
|
|
The compound was tested for binding affinity on [3H]- prazosin as specific ligand on alpha-1 adrenergic receptor cells in rat cerebral cortex
|
None
|
0.74
nM
|
|
|
Binding affinity was tested on human Alpha-1D adrenergic receptor
|
None
|
0.3162
nM
|
|
|
Binding affinity measured in CHO cells expressing human cloned Alpha-1D adrenergic receptor expressed as pKi
|
Homo sapiens
|
0.2239
nM
|
|
|
Binding affinity at human cloned Alpha-1D adrenergic receptor in chinese hamster ovary cells by [3H]prazosin displacement.
|
None
|
0.2239
nM
|
|
|
Alpha-2 adrenergic receptor antagonistic activity in rat vas deferens vs clonidine
|
None
|
724.44
nM
|
|
|
The compound was evaluated for the alpha-2 adrenergic receptor antagonistic activity in rat vas deferens vs methoxamine alpha1 adrenoceptor antagonism
|
None
|
1.096
nM
|
|
|
Antagonistic affinity against native rat cortex Alpha-2 adrenergic receptor
|
None
|
158.49
nM
|
|
|
Binding affinity against native Alpha-2 adrenergic receptor from rat cerebral cortex using radioligand ([3H]rauwolscine) binding assay
|
None
|
147.91
nM
|
|
|
Antagonist activity for Alpha-1 adrenergic receptor against norepinephrine in rat vas deferences
|
Rattus norvegicus
|
2.884
nM
|
|
|
Displacement of [3H]prazosin (0.3 nM) from rat Alpha-1D adrenergic receptor expressed in CHO cells
|
None
|
0.2
nM
|
|
|
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1D adrenergic receptor
|
None
|
0.3
nM
|
|
|
Binding affinity against Alpha-1D adrenergic receptor, from rat clones.
|
Rattus norvegicus
|
0.79
nM
|
|
|
Antagonistic affinity against Alpha-1D adrenergic receptor was determined in isolated thoracic aorta from rat
|
None
|
1.23
nM
|
|
|
Antagonism of norepinephrine induced contraction of rat isolated thoracic aorta.
|
None
|
1.23
nM
|
|
|
Binding affinity at native Alpha-2 adrenergic receptor in rat cerebral cortex by [3H]rauwolscine displacement.
|
None
|
158.49
nM
|
|
|
Alpha-1 adrenergic receptor antagonist activity against agonist (norepinephrine) in isolated rat vas deferens
|
None
|
1.82
nM
|
|
|
Compound was tested for binding affinity against cloned Alpha-1D adrenergic receptor from rat brain.
|
None
|
1.38
nM
|
|
|
Tested for functional alpha-antagonist activity against norepinephrine in rabbit aorta and pulmonary artery.
|
Oryctolagus cuniculus
|
10.0
nM
|
|
|
Alpha-1 Adrenoceptor blocking activity as antagonism of norepinephrine-induced contractions of epididymal portion of rat vas deferens
|
Rattus norvegicus
|
2.884
nM
|
|
|
Alpha-1 antagonistic activity against phenylephrine in rat aorta
|
None
|
4.571
nM
|
|
|
Alpha-1-adrenergic receptor antagonism was measured on ring segments of rat thoracic aorta contracted by phenylephrine
|
None
|
0.5012
nM
|
|
|
Antagonism against Alpha-1 adrenergic receptor of rat aorta
|
None
|
0.04169
nM
|
|
|
Antagonist potency for alpha 1 adrenoceptor
|
None
|
0.5754
nM
|
|
|
Antagonistic activity against postsynaptic Alpha-1 adrenergic receptor in isolated rat vas deferens using (-)-phenylephrine as agonist
|
None
|
0.4365
nM
|
|
|
Antagonistic potency of compound for Alpha-1 adrenergic receptor
|
None
|
1.995
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
|
None
|
106.0
nM
|
|
|
Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
|
None
|
210.0
nM
|
|
|
Binding affinity against native Alpha-1 adrenergic receptor from rat cerebral cortex using radioligand [3H]-prazosin binding assay
|
None
|
0.7413
nM
|
|
|
Ability to inhibit 50% specific binding of [3H]prazosin radioligand to alpha-1 adrenergic receptor in rat cerebrocortex
|
None
|
8.0
nM
|
|
|
pA2 for Alpha-1 adrenergic receptor from human prostate.
|
None
|
1.995
nM
|
|
|
Activity against Alpha-1 adrenergic receptor subtypes of human prostate tissue
|
None
|
1.995
nM
|
|
|
Partial affinity towards Alpha-1 adrenergic receptor was assessed on rat aortic strips
|
None
|
0.1549
nM
|
|
|
Affinity for alpha-1 adrenoceptor of rat cerebral cortex was determined by ligand binding using [3H]prazosin
|
None
|
0.6026
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in alpha-2 C2
|
None
|
108.0
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]-MK-91 to Alpha-2 adrenergic receptor in alpha-2 C4
|
None
|
40.0
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in human OK cells
|
None
|
34.0
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in human Y-79 cells
|
None
|
123.0
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in human platelets
|
None
|
540.0
nM
|
|
|
Ability to displace [3H]rauwolscine from cloned human Alpha-2B adrenergic receptor
|
None
|
13.0
nM
|
|
|
Binding affinity against Alpha-2B adrenergic receptor from human clones.
|
Homo sapiens
|
365.0
nM
|
|
|
Antagonistic activity against postsynaptic alpha-1 adrenergic receptor in rabbit pulmonary artery using l-norepinephrine as agonist
|
Oryctolagus cuniculus
|
1.738
nM
|
|
|
Antagonistic activity at Alpha-1 adrenergic receptor was performed on ring segments of rabbit thoracic aorta contracted by noradrenaline.
|
Oryctolagus cuniculus
|
0.3802
nM
|
|
|
pA2 value for phenylephrine antagonist towards at alpha-1 adrenergic receptor was determined in rabbit aorta
|
Oryctolagus cuniculus
|
1.0
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]-MK-91 to Alpha-2 adrenergic receptor in Malpha-2 4H
|
None
|
97.0
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]-MK-91 to Alpha-2 adrenergic receptor in mouse NG-108 cells
|
None
|
13.0
nM
|
|
|
Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor
|
None
|
24.0
nM
|
|
|
Binding affinity against Alpha-2C adrenergic receptor from human clones.
|
Homo sapiens
|
95.0
nM
|
|
|
Alpha-1 adrenergic receptor binding affinity was evaluated by its ability to displace [3H]prazosin in rat brain synaptosomes
|
None
|
0.3
nM
|
|
|
Displacement of [3H]prazosin binding to Alpha-1 adrenergic receptor sites on rat cerebral cortical membranes at 100 nM concentration
|
Rattus norvegicus
|
0.1622
nM
|
|
|
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
|
None
|
0.93
nM
|
|
|
Binding affinity against Alpha-1A adrenergic receptor from bovine clone
|
Bos taurus
|
0.17
nM
|
|
|
Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay
|
None
|
0.7244
nM
|
|
|
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
|
None
|
0.1259
nM
|
|
|
Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor
|
None
|
0.27
nM
|
|
|
Binding affinity against human Alpha-1A adrenergic receptor
|
None
|
0.58
nM
|
|
|
Binding affinity was determined for the alpha-1A adrenergic receptor
|
None
|
0.58
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in opossum kidney
|
opossum
|
36.0
nM
|
|
|
Compound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor
|
None
|
0.39
nM
|
|
|
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
|
None
|
0.6
nM
|
|
|
Binding affinity against Alpha-1A adrenergic receptor from human clone
|
Homo sapiens
|
0.51
nM
|
|
|
The compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1A adrenergic receptor expressed in CHO cells
|
None
|
0.58
nM
|
|
|
Alpha-2 adrenergic receptor pA2 value against norepinephrine in vitro experiment in rat anococcygeus.
|
None
|
6.607
nM
|
|
|
Affinity for alpha-2 adrenergic receptor of rat cerebral cortex was determined by ligand binding using [3H]yohimbine
|
None
|
645.65
nM
|
|
|
Alpha-1-adrenolytic activity was assessed from the ability to inhibit [3H]prazosin binding to rat cerebral cortex preparation
|
None
|
0.6
nM
|
|
|
Alpha-1-adrenolytic activity was assessed in vitro from the ability to inhibit clonidine binding to rat aorta preparation
|
None
|
0.01023
nM
|
|
|
Binding affinity towards rat Alpha-1 adrenergic receptor was evaluated using [3H]- prazosin as radioligand
|
None
|
1.4
nM
|
|
|
Binding affinity against Alpha-1 adrenergic receptor in rat brain membrane using [3H]prazosin as radioligand
|
None
|
1.4
nM
|
|
|
Binding affinity was tested on human Alpha-1A adrenergic receptor
|
None
|
0.1995
nM
|
|
|
Binding affinity measured in CHO cells expressing human cloned Alpha-1A adrenergic receptor expressed as pKi
|
Homo sapiens
|
0.5888
nM
|
|
|
Binding affinity at human cloned Alpha-1A adrenergic receptor in chinese hamster ovary cells by [3H]-prazosin displacement.
|
None
|
0.5888
nM
|
|
|
Alpha-2 adrenergic receptor activity was assessed from the ability to inhibit [3H]yohimbine binding to rat cerebral cortex preparation
|
None
|
140.0
nM
|
|
|
In vitro binding affinity measured on alpha-1 adrenergic receptor using [3H]prazosin as radioligand.
|
None
|
0.44
nM
|
|
|
Inhibition of [3H]prazosin binding to alpha-1 adrenergic receptor from rat cortical membranes
|
None
|
0.36
nM
|
|
|
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor
|
None
|
0.3
nM
|
|
|
Compound was tested for its binding affinity towards Alpha-1A adrenergic receptor using [3H]prazosin from rat submaxillary gland
|
None
|
1.05
nM
|
|
|
Inhibition of [3H]- prazosin binding against Alpha-1A adrenergic receptor from rat submaxillary gland
|
None
|
0.07
nM
|
|
|
Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat
|
None
|
2.512
nM
|
|
|
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
|
None
|
2.512
nM
|
|
|
Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay
|
None
|
0.9333
nM
|
|
|
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
|
Oryctolagus cuniculus
|
5.012
nM
|
|
|
Displacement of [3H]prazosin (0.5 nM) from hamster Alpha-1B adrenergic receptor expressed in rat-1 cells
|
mesocricetus auratus (golden hamster)
|
0.83
nM
|
|
|
Binding affinity against alpha-2 adrenergic receptor was determined by the displacement of [3H]prazosin from rat brain cortical membranes
|
None
|
0.4
nM
|
|
|
Ability to displace [3H]prazosin (0.25 nM) from whole brain of rat alpha-1 adrenergic receptor
|
None
|
0.29
nM
|
|
|
Alpha-1 adrenergic receptor binding affinity of the compound, value taken from literature
|
None
|
0.74
nM
|
|
|
Binding affinity against Alpha-1B adrenergic receptor from hamster clones.
|
hamster
|
0.32
nM
|
|
|
Compound was tested for binding affinity against cloned Alpha-1B adrenergic receptor from hamster smooth muscle using radioligand ([3H]prazosin) binding assay
|
Cricetulus griseus
|
0.4571
nM
|
|
|
Ability to displace [3H]prazosin from cloned human Alpha-1B adrenergic receptor
|
None
|
0.21
nM
|
|
|
Binding affinity against human Alpha-1B adrenergic receptor
|
None
|
0.55
nM
|
|
|
Compound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1B adrenergic receptor
|
None
|
0.21
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in neonatal rat lung
|
None
|
5.0
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in rat RG10 clone
|
None
|
53.0
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in rat RNG clone
|
None
|
46.0
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in rat kidney
|
None
|
51.0
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in rat submaxillary
|
None
|
457.0
nM
|
|
|
Binding affinity against Alpha-1 adrenergic receptor by displacing [3H]prazosin radioligand in rat cortex membrane.
|
None
|
0.24
nM
|
|
|
Binding affinity against alpha-1 adrenergic receptor by measuring displacement of [3H]prazosin from rat brain cortex membranes (in vitro).
|
None
|
0.19
nM
|
|
|
Binding affinity for alpha-1 adrenergic receptor by displacement of [3H]-prazosin from rat brain homogenate preparation
|
None
|
0.15
nM
|
|
|
Binding affinity for Alpha-1 adrenergic receptor in rat cortex membranes using [3H]-prazosin as radioligand
|
None
|
0.24
nM
|
|
|
Binding affinity by its ability to displace [3H]prazosin radioligand from Alpha-1 adrenergic receptor on rat cerebral cortex
|
None
|
0.24
nM
|
|
|
In vitro binding affinity against Alpha-1B adrenergic receptor of human liver microsomes.
|
None
|
0.6
nM
|
|
|
Binding affinity against Alpha-1B adrenergic receptor from human clone
|
Homo sapiens
|
0.32
nM
|
|
|
The compound was tested for binding affinity on [3H]- prazosin as specific ligand on Human cloned alpha-1B adrenergic receptor in CHO cells
|
None
|
0.28
nM
|
|
|
Binding affinity against alpha-1 adrenergic receptor on rat cortex using [3H]-prazosin as radioligand.
|
None
|
0.097
nM
|
|
|
Binding affinity to Alpha-1 adrenergic receptor by displacement of [3H]prazosin
|
None
|
0.19
nM
|
|
|
Binding affinity towards Alpha-1 adrenergic receptor in rat cerebral cortex using [3H]prazosin
|
Rattus norvegicus
|
0.24
nM
|
|
|
Binding affinity towards alpha-1 adrenergic receptor from rat brain homogenate preparation by displacement of [3H]prazosin
|
None
|
0.19
nM
|
|
|
Binding affinity towards alpha-1 adrenergic receptor in rat cortex membrane using [3H]-prazosin radioligand
|
None
|
0.24
nM
|
|
|
Binding affinity was tested on human Alpha-1B adrenergic receptor
|
None
|
0.2512
nM
|
|
|
Binding affinity measured in CHO cells expressing human cloned Alpha-1B adrenergic receptor expressed as pKi
|
Homo sapiens
|
0.4074
nM
|
|
|
Binding affinity at human cloned Alpha-1B adrenergic receptor in chinese hamster ovary cells by [3H]prazosin displacement.
|
None
|
0.4074
nM
|
|
|
Binding affinity was determined for the alpha-1B adrenergic receptor
|
None
|
0.55
nM
|
|
|
Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1B adrenergic receptor
|
None
|
0.2
nM
|
|
|
Compound was tested for its binding affinity towards Alpha-1B adrenergic receptor using [3H]prazosin from rat liver
|
None
|
2.93
nM
|
|
|
Inhibition of [3H]- prazosin binding against Alpha-1B adrenergic receptor from rat liver
|
None
|
0.15
nM
|
|
|
Inhibition of beta-lactamase at 100 uM
|
None
|
13.0
%
|
|
|
Inhibition of chymotrypsin at 250 uM
|
unidentified
|
5.0
%
|
|
|
Compound was tested for the inhibition of malate dehydrogenase (MDH) at 100 uM
|
None
|
14.0
%
|
|
|
In vitro antagonist activity against (-)-phenylephrine or (-)-norepinephrine-induced alpha1-adrenoceptor-mediated vasoconstriction of rabbit isolated pulmonary artery.
|
Oryctolagus cuniculus
|
1.995
nM
|
|
|
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha1 adrenoceptor.
|
None
|
0.58
nM
|
|
|
In vitro specific binding activity against [3H]prazosin.
|
Rattus norvegicus
|
0.13
|
|
|
Antagonist activity against phenylephrine-induced alpha1- adrenoceptor mediated vasoconstriction in pithed normotensive rats.
|
Rattus norvegicus
|
4.677
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
|
58.6
%
|
|
|
Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand
|
None
|
0.61
nM
|
|
|
Binding affinity towards human cloned alpha-1B-adrenoceptor using [3H]prazosin as radioligand
|
None
|
0.42
nM
|
|
|
Binding affinity towards human cloned alpha-1D-adrenoceptor using [3H]prazosin as radioligand
|
None
|
0.23
nM
|
|
|
Binding affinity against alpha-1-adrenoceptor was determined by displacement of [3H]-prazosin in rat brain homogenates.
|
None
|
0.19
nM
|
|
|
Equilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1b expressed in CHO cells
|
Homo sapiens
|
0.4074
nM
|
|
|
Equilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1d expressed in CHO cells
|
Homo sapiens
|
0.2239
nM
|
|
|
Blocking activity was assessed by antagonism of (-)-phenylephrine induced contraction of rat spleen (alpha1B adrenoceptor)
|
Rattus norvegicus
|
0.9772
nM
|
|
|
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat thoracic aorta (Alpha-1D adrenoceptor)
|
Rattus norvegicus
|
0.9772
nM
|
|
|
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
|
Rattus norvegicus
|
1.047
nM
|
|
|
Equilibrium dissociation constant was evaluated by radio-receptor binding assays using [3H]prazosin to label cloned human alpha 1a expressed in CHO cells
|
Homo sapiens
|
0.5888
nM
|
|
|
Antagonistic activity for Alpha-1 adrenergic receptor was measured as inhibition of phenylephrine-reduced contractions in isolated Sprague-Dawley rat anacoccygeal muscles
|
Rattus norvegicus
|
1.514
nM
|
|
|
Percent inhibition against Alpha-1 adrenergic receptor at 1 uM
|
Homo sapiens
|
0.86
nM
|
|
|
Displacement of [3H]prazosin from adrenergic alpha-1A receptor in rat submaxillary gland membranes
|
Rattus norvegicus
|
0.23
nM
|
|
|
Displacement of [3H]prazosin from adrenergic alpha-1B receptor in rat liver membranes
|
Rattus norvegicus
|
0.1
nM
|
|
|
Inhibition of alpha 1 adrenergic receptor
|
None
|
1.6
nM
|
|
|
Displacement of radiolabeled prazosin from adrenergic alpha1 receptor
|
None
|
0.68
nM
|
|
Displacement of radiolabeled prazosin from adrenergic alpha1 receptor
|
None
|
0.18
nM
|
|
|
Antagonist activity at alpha1 adrenoceptor in Wistar rat aorta assessed as inhibition of norepinephrine-induced contraction treated 30 mins before norepinephrine challenge
|
Rattus norvegicus
|
0.3548
nM
|
|
|
Inhibition of MT3 melatonin binding site from hamster brain membrane
|
Cricetinae
|
7.8
nM
|
|
|
Antagonistic activity at alpha 1-adrenoceptor in rat
|
Rattus norvegicus
|
10.0
nM
|
|
|
Binding affinity to adrenergic alpha1 receptor
|
None
|
0.32
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
|
55.6
%
|
|
|
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 10 uM by confocal microscopy
|
Homo sapiens
|
55.6
%
|
|
|
Displacement of [3H]prazosin from alpha1 adrenoceptor in rat cortex membrane
|
Rattus norvegicus
|
0.24
nM
|
|
|
Displacement of [3H]prazosin from alpha-1-adrenoceptor in Wistar rat cerebral cortex membrane
|
Rattus norvegicus
|
0.24
nM
|
|
|
Inhibition of rat alpha1 adrenoceptor
|
Rattus norvegicus
|
0.52
nM
|
|
|
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in rat cerebral cortex membranes after 30 mins by scintillation counting
|
Rattus norvegicus
|
0.24
nM
|
|
|
Antagonist activity at alpha1-adrenoceptor in rat anococcygeal muscle assessed as inhibition of phenylephrine-induced contraction
|
Rattus norvegicus
|
0.7727
nM
|
|
|
Binding affinity to low affinity melatonin (MT3) site of quinone reductase 2
|
None
|
7.8
nM
|
|
|
Displacement of [3H]prazosin from adrenergic alpha1 receptor
|
None
|
0.071
nM
|
|
|
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
0.218
nM
|
|
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
0.088
nM
|
|
|
DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
0.178
nM
|
|
DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
0.099
nM
|
|
|
DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
|
None
|
0.656
nM
|
|
DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
|
None
|
0.323
nM
|
|
|
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
|
None
|
989.0
nM
|
|
|
DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
|
None
|
290.0
nM
|
|
DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
|
None
|
133.0
nM
|
|
|
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
|
None
|
647.0
nM
|
|
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
|
None
|
94.0
nM
|
|
|
DRUGMATRIX: Imidazoline I2, Central radioligand binding (ligand: [3H] Idazoxan)
|
Rattus norvegicus
|
949.0
nM
|
|
DRUGMATRIX: Imidazoline I2, Central radioligand binding (ligand: [3H] Idazoxan)
|
Rattus norvegicus
|
633.0
nM
|
|
|
Antagonist activity at adrenergic alpha 1D receptor in rat thoracic aorta assessed as inhibition of noradrenaline-induced contraction after 1 hr
|
Rattus norvegicus
|
0.1698
nM
|
|
|
Displacement of [3H]prazosin from rat liver adrenergic alpha1B receptor after 45 mins by liquid scintillation counter
|
Rattus norvegicus
|
0.8511
nM
|
|
Displacement of [3H]prazosin from rat liver adrenergic alpha1B receptor after 45 mins by liquid scintillation counter
|
Rattus norvegicus
|
0.55
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
|
25.1
%
|
|
|
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
|
36.1
%
|
|
|
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
|
1.0
%
|
|
|
Binding affinity to adrenergic alpha1A receptor (unknown origin)
|
Homo sapiens
|
0.5888
nM
|
|
Binding affinity to adrenergic alpha1A receptor (unknown origin)
|
Homo sapiens
|
0.588
nM
|
|
|
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells at 20 uM after 1.5 mins by fluorescence assay
|
Homo sapiens
|
74.0
%
|
|
|
Binding affinity to adrenergic alpha1 receptor (unknown origin) by radioligand displacement assay
|
Homo sapiens
|
0.17
nM
|
|
|
Displacement of [3H]Prazosin from alpha1B adrenergic receptor in Wistar rat liver after 60 mins
|
Rattus norvegicus
|
0.15
nM
|
|
Displacement of [3H]Prazosin from alpha1B adrenergic receptor in Wistar rat liver after 60 mins
|
Rattus norvegicus
|
0.27
nM
|
|
|
Displacement of [3H]Prazosin from human recombinant alpha1D adrenergic receptor expressed in HEK293 cells after 60 mins
|
Homo sapiens
|
0.43
nM
|
|
Displacement of [3H]Prazosin from human recombinant alpha1D adrenergic receptor expressed in HEK293 cells after 60 mins
|
Homo sapiens
|
0.88
nM
|
|
|
Displacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 mins
|
Rattus norvegicus
|
0.28
nM
|
|
Displacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland after 60 mins
|
Rattus norvegicus
|
0.69
nM
|
|
|
Displacement of [3H]Prazosin from human recombinant alpha1D adrenergic receptor expressed in HEK293 cells at 10 uM after 60 mins relative to control
|
Homo sapiens
|
-1.0
%
|
|
|
Displacement of [3H]Prazosin from alpha1B adrenergic receptor in Wistar rat liver at 10 uM after 60 mins relative to control
|
Rattus norvegicus
|
11.0
%
|
|
|
Displacement of [3H]Prazosin from alpha1A adrenergic receptor in Wistar rat submaxillary gland at 10 uM after 60 mins relative to control
|
Rattus norvegicus
|
5.0
%
|
|
|
Binding affinity to adrenergic alpha1 receptor (unknown origin) by radioligand displacement assay
|
Homo sapiens
|
0.054
nM
|
|
Binding affinity to adrenergic alpha1 receptor (unknown origin) by radioligand displacement assay
|
Homo sapiens
|
0.2
nM
|
|
|
Antagonist activity at angiotensin-2 receptor in Wistar rat endothelium denuded thoracic aorta assessed as inhibition of angiotensin 2-induced contraction preincubated for 30 mins prior to angiotensin 2-challenge
|
Rattus norvegicus
|
5.495
nM
|
|
|
Antagonist activity at alpha1-adrenergic receptor in Wistar rat endothelium denuded thoracic aorta assessed as inhibition of phenylephrine-induced contraction preincubated for 30 mins prior to phenylephrine-challenge
|
Rattus norvegicus
|
8.318
nM
|
|
|
Displacement of [125I]HEAT from adrenergic alpha1D receptor (unknown origin)
|
Homo sapiens
|
0.4571
nM
|
|
Displacement of [125I]HEAT from adrenergic alpha1D receptor (unknown origin)
|
Homo sapiens
|
0.42
nM
|
|
|
Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)
|
Homo sapiens
|
1.862
nM
|
|
Displacement of [125I]HEAT from adrenergic alpha1A receptor (unknown origin)
|
Homo sapiens
|
0.59
nM
|
|
|
Displacement of [125I]HEAT from adrenergic alpha1B receptor (unknown origin)
|
Homo sapiens
|
7.943
nM
|
|
Displacement of [125I]HEAT from adrenergic alpha1B receptor (unknown origin)
|
Homo sapiens
|
1.0
nM
|
|
|
Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells
|
Homo sapiens
|
0.04
nM
|
|
|
Displacement of [3H]prazosin from rat cerebral cortex alpha-1 adrenergic receptor by liquid scintillation counting analysis
|
Rattus norvegicus
|
0.302
nM
|
|
|
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in CHO cells
|
Homo sapiens
|
0.04
nM
|
|
|
Displacement of [3H]prazosin from rat cerebral cortex Alpha-1 adrenergic receptor
|
Rattus norvegicus
|
0.25
nM
|
|
|
Displacement of [3H]prazosin from rat cerebral cortex alpha-1 adrenergic receptor measured after 60 mins by scintillation counting method
|
Rattus norvegicus
|
0.25
nM
|
|
|
Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins
|
Homo sapiens
|
0.5888
nM
|
|
|
Displacement of [3H]prazosin from human alpha1B adrenoceptor expressed in CHO cell membranes after 30 mins
|
Homo sapiens
|
0.4074
nM
|
|
|
Displacement of [3H]prazosin from human alpha1D adrenoceptor expressed in CHO cell membranes after 30 mins
|
Homo sapiens
|
0.2239
nM
|
|
|
Displacement of [3H]prazosin from alpha1-adrenoceptor (unknown origin) in cerebral cortex membranes after 60 mins by TopCount scintillation counting method
|
Homo sapiens
|
0.15
nM
|
|
|
Compound was evaluated for binding affinity towards alpha-1 adrenergic receptors from combinatorial peptoid library
|
Rattus norvegicus
|
0.2
nM
|
|
|
Displacement of [3H]prazosin from human recombinant adrenergic alpha-1D receptor expressed in CHO cell membranes incubated for 60 mins
|
Homo sapiens
|
0.17
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
|
7.68
%
|
|
|
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
|
0.08
%
|
|
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
|
0.08
%
|
|
