|
Displacement of [3H]clonidine from adrenergic alpha 2 receptor of rat cerebral cortical membranes
|
Rattus norvegicus
|
38.0
nM
|
|
|
Binding affinity against alpha 2-Adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]clonidine
|
Cavia porcellus
|
30.0
nM
|
|
|
Binding affinity against Alpha adrenergic receptor using [3H]dihydroergocryptine radioligand in rat brain homogenate
|
None
|
16.0
nM
|
|
|
Displacement of [3H]clonidine from Alpha-2 adrenergic receptor of rat brain membranes
|
Rattus norvegicus
|
17.0
nM
|
|
|
The compound was evaluated for the binding affinity towards alpha-2 adrenergic receptor from rat cortex
|
None
|
37.0
nM
|
|
|
The compound was evaluated for the inhibition of [3H]prazosin binding to alpha-1 adrenergic receptor from rat liver
|
None
|
390.0
nM
|
|
|
In vitro agonist potency towards Alpha-1D adrenergic receptor in rat aorta
|
None
|
12.02
nM
|
|
|
Binding affinity towards rat clonal Alpha-1D adrenergic receptor
|
None
|
22.39
nM
|
|
|
Tested for binding affinity against alpha-2 adrenergic receptor in rat brain using [3H]- rauwolscine as radioligand
|
None
|
4.8
nM
|
|
|
Binding affinity for human Alpha-2A adrenergic receptor
|
Homo sapiens
|
66.0
nM
|
|
|
Effective dose for contraction of reserpine-pretreated guinea pig aorta.
|
None
|
112.0
nM
|
|
|
Effective dose for inhibition of neurotransmission in field-stimulated, reserpine-pretreated guinea pig ileum.
|
None
|
30.0
nM
|
|
|
Binding affinity for rat Alpha-2B adrenergic receptor
|
Rattus norvegicus
|
78.0
nM
|
|
|
Alpha-1 adrenergic receptor activation causing vasoconstriction in the isolated rabbit ear artery
|
Oryctolagus cuniculus
|
150.0
nM
|
|
|
Binding affinity for human Alpha-2C adrenergic receptor
|
Homo sapiens
|
63.0
nM
|
|
|
Effective dose for contraction of rabbit aorta.
|
None
|
6.6
nM
|
|
|
Effective dose for contraction of rat aorta.
|
None
|
1.2
nM
|
|
|
Effective dose for on contraction of rat aorta.
|
None
|
200.0
nM
|
|
|
Tested for binding affinity against alpha-1 adrenergic receptor in rat brain using [3H]-Prazosin as radioligand
|
None
|
450.0
nM
|
|
|
Binding affinity towards bovine clonal Alpha-1A adrenergic receptor
|
None
|
446.68
nM
|
|
|
Displacement of [3H]rauwolscine from Alpha-2 adrenergic receptor of rat cortical membranes
|
Rattus norvegicus
|
750.0
nM
|
|
|
The compound was evaluated for the inhibition of [3H]rauwolscine binding to alpha-2-adrenergic receptor from rat cortex
|
None
|
33.0
nM
|
|
|
Binding of [3H]prazosin to alpha-1 adrenergic receptor of rat cerebral cortical membranes at 100 uM
|
None
|
18.0
%
|
|
|
Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands
|
None
|
281.84
nM
|
|
|
Binding affinity for alpha-2 adrenergic receptor in rat cortex using [3H]rauwolscine.
|
None
|
37.0
nM
|
|
|
Compound was evaluated for alpha adrenergic binding affinity towards Alpha-2 adrenergic receptor of rat brain
|
None
|
4.8
nM
|
|
|
Binding affinity towards hamster clonal Alpha-1B adrenergic receptor
|
Cricetulus griseus
|
263.03
nM
|
|
|
Binding affinity for alpha-1 adrenergic receptor in rat liver using [3H]prazosin.
|
None
|
390.0
nM
|
|
|
Binding affinity towards Alpha-1 adrenergic receptor of rat brain
|
Rattus norvegicus
|
450.0
nM
|
|
|
Compound was evaluated for inhibition of [3H]prazosin binding to Alpha-1 adrenergic receptor in rat forebrain homogenate.
|
None
|
500.0
nM
|
|
|
Compound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brain
|
None
|
126.0
nM
|
|
|
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligand
|
None
|
126.0
nM
|
|
|
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
|
Cavia porcellus
|
213.0
nM
|
|
|
Agonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atria
|
Cavia porcellus
|
350.0
nM
|
|
|
Effective concentration for Beta-1 adrenergic receptor mediated inhibition of neurotransmission in field-stimulated reserpine pretreated guinea pig ileum.
|
Cavia porcellus
|
30.0
nM
|
|
|
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
|
Cavia porcellus
|
400.0
nM
|
|
|
Stimulation of cyclic AMP accumulation in C6 glioma cells expressing adrenergic beta receptor
|
Rattus norvegicus
|
52.0
nM
|
|
|
Agonist required to inhibit Dopamine receptor D2 photoinactivation by 50% with Iodazidoclebopride using [3H]-Spiperone
|
Canis lupus familiaris
|
8e-05
nM
|
|
|
Binding of [3H]clonidine to alpha-2-adrenergic receptor of rat cerebral cortical membranes
|
None
|
30.0
nM
|
|
Binding of [3H]clonidine to alpha-2-adrenergic receptor of rat cerebral cortical membranes
|
None
|
340.0
nM
|
|
Binding of [3H]clonidine to alpha-2-adrenergic receptor of rat cerebral cortical membranes
|
None
|
20.0
nM
|
|
|
Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
|
Homo sapiens
|
794.33
nM
|
|
|
Agonist activity at human adrenergic alpha-2B receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
|
Homo sapiens
|
61.66
nM
|
|
|
Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
|
Homo sapiens
|
371.54
nM
|
|
|
Agonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
|
Homo sapiens
|
371.54
nM
|
|
|
Agonistic potency at human adrenergic alpha-2B receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
|
Homo sapiens
|
61.66
nM
|
|
|
Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation
|
Homo sapiens
|
794.33
nM
|
|
|
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
|
Homo sapiens
|
5.5
nM
|
|
|
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay
|
Homo sapiens
|
6.3
nM
|
|
|
Agonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidification
|
Homo sapiens
|
371.54
nM
|
|
|
Agonist activity at human recombinant adrenergic alpha2B receptor expressed in CHO cells
|
Homo sapiens
|
61.66
nM
|
|
|
Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidification
|
Homo sapiens
|
794.33
nM
|
|
|
Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
|
Homo sapiens
|
794.33
nM
|
|
|
Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry
|
Homo sapiens
|
371.54
nM
|
|
|
Inhibition of adipogenesis in mouse 3T3L1 cells assessed as triglyceride accumulation after 7 days
|
Mus musculus
|
69.0
ug.mL-1
|
|
|
Cytotoxicity against mouse 3T3L1 cells assessed as cell viability after 7 days
|
Mus musculus
|
100.0
ug.mL-1
|
|
|
Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
|
Homo sapiens
|
110.0
nM
|
|
|
Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting
|
Homo sapiens
|
118.0
nM
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
112.9
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
102.31
%
|
|
|
Agonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assay
|
Homo sapiens
|
128.82
nM
|
|
|
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
|
Homo sapiens
|
9.1
nM
|
|
|
Agonist activity at human recombinant Alpha-2 adrenergic receptor expressed in CHOK1 cells after 30 mins by [35S]GTPgammaS binding assay
|
Homo sapiens
|
166.0
nM
|
|
|
Binding affinity to mouse alpha-2C receptor expressed in COS7 cells
|
Mus musculus
|
650.0
nM
|
|
|
Agonist activity at recombinant human alpha1A adrenergic receptor expressed in HEK293 cells assessed as intercellular Ca mobilization by Fura-2AM dye-based fluorescence assay
|
Homo sapiens
|
9.1
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
|
-31.86
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
-11.01
%
|
|
|
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
|
-0.21
%
|
|
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
|
-0.04
%
|
|
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
|
-0.04
%
|
|
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
|
-0.21
%
|
|
