Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
|
None
|
50.0
nM
|
|
Binding affinity towards 5-hydroxytryptamine 1A receptor by the displacement of [125I]trans-8-OH-PIPAT in membrane homogenates of hippocampal tissue of rat brain
|
Rattus norvegicus
|
113.0
nM
|
|
Inhibitory activity against 5-hydroxytryptamine 1A receptor of rat hippocampal tissue using [3H]OH-DPAT as radioligand.
|
None
|
90.0
nM
|
|
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
|
Cavia porcellus
|
1.738
nM
|
|
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparation
|
Cavia porcellus
|
1.995
nM
|
|
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)
|
None
|
2.399
nM
|
|
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
|
None
|
4.365
nM
|
|
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
|
None
|
4.365
nM
|
|
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
|
Canis lupus familiaris
|
17.0
nM
|
|
Inhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determined
|
Cavia porcellus
|
28.84
nM
|
|
Antagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig trachea
|
Cavia porcellus
|
43.65
nM
|
|
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
|
Cavia porcellus
|
3.388
nM
|
|
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
|
Cavia porcellus
|
3.02
nM
|
|
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
|
Cavia porcellus
|
0.9772
nM
|
|
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
|
Cavia porcellus
|
3.388
nM
|
|
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparation
|
Cavia porcellus
|
1.259
nM
|
|
Tested for Beta Adrenergic receptor binding inhibition from canine ventricular tissue, using [3H]dihydroalprenolol as the radioligand in anesthetized dogs
|
Canis lupus familiaris
|
12.0
nM
|
|
Concentration effective against displacing [3H]dihydroalprenolol from beta adrenergic receptor from canine ventricular tissue
|
Canis lupus familiaris
|
4.0
nM
|
|
In Vitro inhibition of the beta adrenergic receptor in guinea pig atria
|
Cavia porcellus
|
1.995
nM
|
|
In vitro blocking of beta adrenergic receptor in guinea pig trachea
|
Cavia porcellus
|
1.259
nM
|
|
Beta adrenergic receptor blocking activity measured by the chronotropic effect was determined 1 hr after pretreatment of the right atria in guinea pig
|
Cavia porcellus
|
3.631
nM
|
|
Beta adrenergic receptor blocking activity measured by the inotropic effect was determined 1 hr after pretreament of the right atria in guinea pig
|
Cavia porcellus
|
2.399
nM
|
|
Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)
|
None
|
1.778
nM
|
|
Inhibitory concentration required for displacement of Beta adrenergic receptor specific ligand [3H]dihydroalprenolol from rat brain cerebral cortical membranes
|
None
|
30.0
nM
|
|
The compound was tested for the concentration to inhibit 50% of Beta adrenergic receptor isolated from rat ventricle homogenates
|
None
|
3.0
nM
|
|
Inhibitory activity against beta adrenergic receptor of rat frontal cortex homogenate using (1.0 nM) [3H]- dihydroalprenolol
|
None
|
2.4
nM
|
|
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
|
Cavia porcellus
|
2.399
nM
|
|
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs
|
Canis lupus familiaris
|
18.0
nM
|
|
Inhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determined
|
Cavia porcellus
|
34.67
nM
|
|
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
|
Cavia porcellus
|
8.71
nM
|
|
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
|
Cavia porcellus
|
2.512
nM
|
|
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
|
Cavia porcellus
|
2.399
nM
|
|
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
|
Cavia porcellus
|
12.59
nM
|
|
Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)
|
Cavia porcellus
|
3.09
nM
|
|
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
|
Cavia porcellus
|
1.738
nM
|
|
In vivo beta-adrenoceptor blocking potency in cat (expressed as total dose infused over a period of 30 minutes causing 50% inhibition of the tachycardia by iv administration)
|
Felis catus
|
62.0
ug kg-1
|
|
Beta-adrenoceptor blocking potency in cat, measured as the degree (percent) of blockade of the vasopressor response at the dose level
|
Felis catus
|
85.0
%
|
|
In vivo beta adrenergic blocking potency was determined by inhibition of depressor response produced by isoproterenol (0.2 mg/kg iv) in cat preparation
|
Felis catus
|
85.0
%
|
|
In vivo beta-adrenergic blocking potency to inhibit vasopressor response in anesthetized cats
|
Felis catus
|
85.0
%
|
|
Percent inhibition of vasopressor response
|
Felis catus
|
85.0
%
|
|
The compound was evaluated for inhibition of depressor response.
|
Felis catus
|
85.0
%
|
|
Percent inhibition of isoproterenol induced tachycardia at a dose of 1.3 microg (3-h infusion period)
|
Canis lupus familiaris
|
68.0
%
|
|
Compound was tested for its ability to block isoproterenol-induced contractile force in anesthetized dogs.
|
Canis lupus familiaris
|
25.12
nM
|
|
Compound was tested for its ability to block isoproterenol-induced increases in heart rate(HR) in anesthetized dogs.
|
Canis lupus familiaris
|
37.15
nM
|
|
Compound was tested for its ability to block isoproterenol-induced vasodilation in anesthetized dogs.
|
Canis lupus familiaris
|
11.22
nM
|
|
Evaluated for Adrenoceptor from guinea pig left atrium by using isoproterenol as agonist.
|
Cavia porcellus
|
1.549
nM
|
|
Evaluated for Adrenoceptor from guinea pig trachea by using isoproterenol as agonist.
|
Cavia porcellus
|
4.677
nM
|
|
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
|
Cavia porcellus
|
3.388
nM
|
|
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
|
Cavia porcellus
|
2.399
nM
|
|
Negative log concentration effecting 50% blockade of isoproterenol-induced rate responses in vitro in guinea pig right atria.
|
Cavia porcellus
|
1.995
nM
|
|
Positive chronotropic effect was evaluated on atrial muscles of the guinea pig
|
Cavia porcellus
|
7.586
nM
|
|
Positive inotropic effect was evaluated on atrial muscles of the guinea pig
|
Cavia porcellus
|
3.802
nM
|
|
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
|
Cavia porcellus
|
3.388
nM
|
|
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparation at a duration of 3h
|
Cavia porcellus
|
60.0
nM
|
|
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparation at a duration of 40 min
|
Cavia porcellus
|
46.0
nM
|
|
Ionotropic effect in electrically driven left atrial preparation (Atria isolated from guinea pig) and is expressed in pA2.
|
Cavia porcellus
|
7.943
nM
|
|
Chronotropic effect studied in right atria isolated from guinea pig and is expressed in pA2.
|
Cavia porcellus
|
5.012
nM
|
|
Inhibition of isoproterenol-induced responses in guinea pig trachea.
|
Cavia porcellus
|
1.259
nM
|
|
Beta blocking effect as percent inhibition of increased heart frequency induced by isoprenaline in 5-10 animals.
|
Rattus norvegicus
|
100.0
%
|
|
Beta-adrenergic receptor blockade activity in conscious normotensive rats at a dose of 1.25 mg/kg
|
Rattus norvegicus
|
26.0
%
|
|
The compound was tested for beta-adrenergic receptor blockade activity in conscious normotensive rats at a dose of 5 mg/kg
|
Rattus norvegicus
|
56.0
%
|
|
Evaluated for the percentage inhibition of the depressor response of isoproterenol (0.25 mg/kg, iv) by propranolol hydrochloride at dose of 10 mg/kg
|
Rattus norvegicus
|
100.0
%
|
|
Evaluated for beta-receptor affinity determined in rat brain membrane fraction with [3H]- dihydroalprenolol
|
None
|
6.5
nM
|
|
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
|
Meleagris gallopavo
|
2.3
nM
|
|
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
|
Rattus norvegicus
|
3.162
nM
|
|
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
|
Rattus norvegicus
|
31.62
nM
|
|
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
|
Rattus norvegicus
|
199.53
nM
|
|
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
|
Rattus norvegicus
|
10.0
nM
|
|
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
|
Rattus norvegicus
|
39.81
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
|
55.4
%
|
|
Binding affinity to human adrenergic beta2 receptor
|
Homo sapiens
|
0.79
nM
|
|
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cells
|
Homo sapiens
|
6.026
nM
|
|
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
|
Homo sapiens
|
0.6026
nM
|
|
Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells
|
Homo sapiens
|
213.8
nM
|
|
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
|
Homo sapiens
|
1.82
nM
|
|
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
|
Homo sapiens
|
199.53
nM
|
|
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
|
Homo sapiens
|
0.2399
nM
|
|
Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
|
Homo sapiens
|
162.18
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
|
None
|
243.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
|
None
|
139.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
|
None
|
419.0
nM
|
|
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
|
None
|
2.543
nM
|
|
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
|
None
|
1.468
nM
|
|
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
|
None
|
1.116
nM
|
|
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
|
None
|
0.767
nM
|
|
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
|
None
|
132.0
nM
|
|
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
|
None
|
99.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
342.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
218.0
nM
|
|
DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
|
None
|
380.0
nM
|
|
DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
|
None
|
202.0
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
|
8.9
%
|
|
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
|
12.8
%
|
|
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
|
10.1
%
|
|
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
|
Rattus norvegicus
|
3.0
nM
|
|
Inhibition of beta-adrenergic receptor in Rattus norvegicus albino (rat) aortic ring assessed as norepinephrine-induced contraction at 1 uM measured for 1 to 2 min (Rvb = 51.18%)
|
Rattus norvegicus
|
63.91
%
|
|
Inhibition of beta-adrenergic receptor in Rattus norvegicus albino (rat) norepinephrine-contracted aortic ring assessed as change in isoprenaline-induced relaxation at 1 uM measured for 1 to 2 min (Rvb = 19.75%)
|
Rattus norvegicus
|
-1.16
%
|
|
Antagonist activity at beta1 adrenoreceptor in Sprague-Dawley rat left atrium assessed as inhibition of isoprenaline-induced contraction at 1 uM incubated for 5 mins prior to isoprenaline-induction
|
Rattus norvegicus
|
73.8
%
|
|
Antagonist activity at beta1 adrenoreceptor in Sprague-Dawley rat left atrium assessed as inhibition of isoprenaline-induced contraction at 0.1 uM incubated for 5 mins prior to isoprenaline-induction
|
Rattus norvegicus
|
49.7
%
|
|
Displacement of [3H]CGP-12177 from beta1-adrenergic receptor in rat cerebral cortex after 60 mins by scintillation counting
|
Rattus norvegicus
|
7.0
nM
|
|
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
|
Homo sapiens
|
3.69
nM
|
|
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
|
Homo sapiens
|
0.46
nM
|
|
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rate
|
Cavia porcellus
|
9.55
nM
|
|
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile force
|
Cavia porcellus
|
14.13
nM
|
|
Competitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxation
|
Cavia porcellus
|
14.79
nM
|
|
Antagonist activity at guinea pig atrial beta adrenergic receptor assessed as isometric contractions by force displacement transducer
|
Cavia porcellus
|
6.31
nM
|
|
In vivo inhibition of beta-2 adrenergic receptor in cat assessed as inhibition of isoproterenol-induced vasodepressor response at ED50 administered as 30 mins of infusion measured at 30 mins relative to control
|
Felis catus
|
85.0
%
|
|
Inhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 mins
|
Cavia porcellus
|
240.88
nM
|
|
Inhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effect
|
Cavia porcellus
|
253.4
nM
|
|
In vivo inhibition of beta-adrenoceptor in Wistar rat assessed as inhibition of isoproterenol-induced tachycardia at 4 mg/kg, iv relative to control
|
Rattus norvegicus
|
95.0
%
|
|
In vivo inhibition of beta-adrenoceptor in Wistar rat assessed as decrease in heart rate at 4 mg/kg, iv relative to control
|
Rattus norvegicus
|
32.0
%
|
|
In vivo inhibition of beta-adrenoceptor in cat assessed as inhibition of isoproterenol-induced tachycardia at 0.1 mg/kg, iv relative to control
|
Felis catus
|
87.0
%
|
|
In vivo inhibition of beta-adrenoceptor in cat assessed as inhibition of isoproterenol-induced tachycardia at 1 mg/kg, iv relative to control
|
Felis catus
|
100.0
%
|
|
In vivo inhibition of beta-adrenoceptor in cat assessed as inhibition of isoproterenol-induced hypotension at 0.1 mg/kg, iv relative to control
|
Felis catus
|
85.0
%
|
|
In vivo inhibition of beta-adrenoceptor in cat assessed as inhibition of isoproterenol-induced hypotension at 1 mg/kg, iv relative to control
|
Felis catus
|
100.0
%
|
|
In vivo inhibition of beta-adrenoceptor in histamine-treated guinea pig assessed as inhibition of isoproterenol-induced bronchodilator effect at 0.1 mg/kg, iv administered 3 mins prior to histamine/isoproterenol challenge relative to control
|
Cavia porcellus
|
100.0
%
|
|
Local anesthetic activity in ICR Swiss mouse assessed as inhibition of pain reflex response at 0.5%, id relative to control
|
Mus musculus
|
93.0
%
|
|
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 mins
|
Cavia porcellus
|
1.995
nM
|
|
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
|
Cavia porcellus
|
1.38
nM
|
|
Inhibition of beta-adrenergic receptor in isoproterenol-stimulated guinea pig atrial muscle
|
Cavia porcellus
|
0.01
ug.mL-1
|
|
Inhibition of isoproterenol-induced decrease in diastolic blood pressure in bilaterally vagotomized open chest mongrel dog model at 1.45 mg/kg, iv administered 10 to 20 mins prior to and following isoproterenol challenge
|
Canis lupus familiaris
|
90.7
%
|
|
Inhibition of isoproterenol-induced decrease in diastolic blood pressure in bilaterally vagotomized open chest mongrel dog model at 4.61 mg/kg, iv administered 10 to 20 mins prior to and following isoproterenol challenge
|
Canis lupus familiaris
|
96.6
%
|
|
Inhibition of isoproterenol-induced increase in heart rate in bilaterally vagotomized open chest mongrel dog model at 0.03 mg/kg, iv administered 10 to 20 mins prior to and following isoproterenol challenge
|
Canis lupus familiaris
|
24.7
%
|
|
Inhibition of isoproterenol-induced increase in heart rate in bilaterally vagotomized open chest mongrel dog model at 0.13 mg/kg, iv administered 10 to 20 mins prior to and following isoproterenol challenge
|
Canis lupus familiaris
|
62.0
%
|
|
Inhibition of isoproterenol-induced increase in heart rate in bilaterally vagotomized open chest mongrel dog model at 0.45 mg/kg, iv administered 10 to 20 mins prior to and following isoproterenol challenge
|
Canis lupus familiaris
|
85.2
%
|
|
Inhibition of isoproterenol-induced increase in heart rate in bilaterally vagotomized open chest mongrel dog model at 1.45 mg/kg, iv administered 10 to 20 mins prior to and following isoproterenol challenge
|
Canis lupus familiaris
|
95.8
%
|
|
Inhibition of isoproterenol-induced increase in heart rate in bilaterally vagotomized open chest mongrel dog model at 4.61 mg/kg, iv administered 10 to 20 mins prior to and following isoproterenol challenge
|
Canis lupus familiaris
|
98.4
%
|
|
Inhibition of isoproterenol-induced decrease in diastolic blood pressure in bilaterally vagotomized open chest mongrel dog model at 0.03 mg/kg, iv administered 10 to 20 mins prior to and following isoproterenol challenge
|
Canis lupus familiaris
|
40.5
%
|
|
Inhibition of isoproterenol-induced decrease in diastolic blood pressure in bilaterally vagotomized open chest mongrel dog model at 0.13 mg/kg, iv administered 10 to 20 mins prior to and following isoproterenol challenge
|
Canis lupus familiaris
|
63.5
%
|
|
Inhibition of isoproterenol-induced decrease in diastolic blood pressure in bilaterally vagotomized open chest mongrel dog model at 0.45 mg/kg, iv administered 10 to 20 mins prior to and following isoproterenol challenge
|
Canis lupus familiaris
|
80.8
%
|
|
Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
25.0
%
|
|
Time dependent inhibition of CYP2B6 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
Time dependent inhibition of CYP2C9 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
Time dependent inhibition of CYP2C19 in human liver microsomes at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
Time dependent inhibition of CYP2D6 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
Time dependent inhibition of CYP3A4 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
Time dependent inhibition of CYP2C8 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
Antagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assay
|
Homo sapiens
|
50.12
nM
|
|
Antagonist activity at human beta1 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assay
|
Homo sapiens
|
251.19
nM
|
|
Displacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting method
|
Rattus norvegicus
|
7.0
nM
|
|
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
|
Cavia porcellus
|
2.692
nM
|
|
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
|
Homo sapiens
|
1.738
nM
|
|
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation counting
|
Homo sapiens
|
11.75
nM
|
|
Displacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting method
|
Rattus norvegicus
|
15.0
nM
|
|
Inhibition of Streptococcus pyogenes SrtA deltaN81 mutant expressed in Escherichia coli BL21(DE3) at 100 uM using Abz-LPETA-Dap(Dnp) as substrate preincubated for 10 mins followed by substrate addition measured every min for 2.5 hrs by fluorimetric assay relative to control
|
Streptococcus pyogenes
|
-4.2
%
|
|
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
|
Mus musculus
|
2.4
nM
|
|
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
|
Homo sapiens
|
0.32
nM
|
|
Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranes
|
Homo sapiens
|
1.4
nM
|
|
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
|
Homo sapiens
|
0.1
nM
|
|
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
|
Homo sapiens
|
150.0
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
|
8.37
%
|
|
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
|
0.22
%
|
|
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
|
0.22
%
|
|
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assay
|
Homo sapiens
|
0.55
nM
|
|
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assay
|
Homo sapiens
|
0.48
nM
|
|
Inhibition of NE-induced lipolysis in adipocytes (unknown origin) assessed as reduction in glycerol release at 1 uM pre-incubated for 30 mins before NE stimulation for 90 mins by glycerol reagent based assay relative to control
|
Not specified
|
92.4
%
|
|
Binding affinity to TLX LBD expressed in His6-tagged Escherichia coli Rosetta assessed as binding constant measured after 300 sec at 200 mM by isothermal titration calorimetry
|
Homo sapiens
|
500.0
nM
|
|