|
Compound at 10E-5 M was tested in vitro for the inhibition of radioligand [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor in rat hippocampal membrane
|
None
|
50.0
%
|
|
|
Evaluated for norepinephrine as agonist.
|
Oryctolagus cuniculus
|
3.715
nM
|
|
|
Inhibitory concentration required for displacement of Alpha adrenergic receptor specific ligand, 2-[ [ [(2,6-dimethoxyphenoxy) ethyl]amino]methyl]benzodioxan ([3H]WB-4101) from rat brain cerebral cortical membranes
|
None
|
90.0
nM
|
|
|
Evaluated for norepinephrine as agonist.
|
None
|
4.786
nM
|
|
|
Evaluated for norepinephrine as agonist.
|
None
|
6.026
nM
|
|
|
In vitro postsynaptic antagonist activity against Alpha adrenergic receptor in rat anococcygeus muscle
|
None
|
19.95
nM
|
|
|
In vitro presynaptic antagonist activity against Alpha adrenergic receptor in rat vas deferens
|
None
|
12.59
nM
|
|
|
Tested for alpha adrenergic receptor agonistic activity on isolated rat vas deferens
|
None
|
138.04
nM
|
|
|
Displacement of [3H]clonidine from Alpha-2 adrenergic receptor of rat brain membranes
|
Rattus norvegicus
|
22.0
nM
|
|
|
Antagonistic activity against Alpha-2 adrenergic receptor in the prostatic portion of the rat vas deferens
|
None
|
9.333
nM
|
|
|
Antagonistic activity against presynaptic alpha-2 adrenergic receptor in isolated rat vas deferens using xylazine as agonist
|
None
|
16.6
nM
|
|
|
Antagonistic potency of compound for Alpha-2 adrenergic receptor
|
None
|
10.0
nM
|
|
|
Displacement of [3H]prazosin (0.3 nM) from rat Alpha-1D adrenergic receptor expressed in CHO cells
|
None
|
45.0
nM
|
|
|
Antagonistic activity against Alpha-1 adrenergic receptor in the epidermal portion of the rat vas deferens
|
None
|
11.48
nM
|
|
|
Antagonistic activity against postsynaptic Alpha-1 adrenergic receptor in isolated rat vas deferens using (-)-phenylephrine as agonist
|
None
|
9.55
nM
|
|
|
Antagonistic potency of compound for Alpha-1 adrenergic receptor
|
None
|
12.59
nM
|
|
|
Methoxamine antagonistic activity against alpha-1 adrenergic receptor in isolated, field -simulated vas deferens from rats
|
None
|
7.943
nM
|
|
|
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
|
None
|
0.93
nM
|
|
|
Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand
|
None
|
2.1
nM
|
|
|
The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.
|
None
|
2.6
nM
|
|
|
Antagonistic activity against adrenergic alpha-2 receptor in longitudinal muscle strip of the guinea pig ileum using l-norepinephrine as agonist
|
Rattus norvegicus
|
1.514
nM
|
|
|
Antagonistic activity against longitudinal muscle strip of the guinea pig ileum using xylazine as agonist
|
Cavia porcellus
|
15.49
nM
|
|
|
In vitro for relative blocking action (pA2) of Presynaptic Alpha-2 adrenergic receptor from guinea pig ileum.
|
Cavia porcellus
|
3.162
nM
|
|
|
The compound was tested for the concentration to inhibit 50% of Alpha-1 adrenergic receptor isolated from rat ventricle homogenates.
|
None
|
2.7
nM
|
|
|
Binding affinity against alpha-2-adrenergic receptor using 10 nM [3H]yohimbine in human platelet membranes from three separate experiments using 10 inhibitor concentrations
|
None
|
5.0
nM
|
|
|
Binding affinity against Alpha-2B adrenergic receptor from human clones.
|
Homo sapiens
|
7.6
nM
|
|
|
Antagonistic activity against postsynaptic alpha-1 adrenergic receptor in rabbit pulmonary artery using l-norepinephrine as agonist
|
Oryctolagus cuniculus
|
15.14
nM
|
|
|
Activity at alpha-1 adrenergic receptor in rabbit aorta rings
|
Oryctolagus cuniculus
|
15.85
nM
|
|
|
Binding affinity against Alpha-2C adrenergic receptor from human clones.
|
Homo sapiens
|
8.4
nM
|
|
|
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
|
Oryctolagus cuniculus
|
32.36
nM
|
|
|
In vitro relative blocking action (pA2) of the post-synaptic alpha-1-adrenoceptor from rat and rabbit aorta.
|
None
|
3.162
nM
|
|
|
Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
|
None
|
6.8
nM
|
|
|
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
|
None
|
0.7943
nM
|
|
|
The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.
|
Rattus norvegicus
|
4.7
nM
|
|
|
Compound was tested for the inhibition of [3H]prazosin binding Alpha-1 adrenergic receptor of crude rat brain membrane.
|
None
|
9.8
nM
|
|
|
Alpha-2 adrenergic receptor pA2 value against clonidine in vitro experiment in rat vas deferens
|
None
|
4.169
nM
|
|
|
Alpha-2 adrenergic receptor pA2 value against norepinephrine in vitro experiment in rat anococcygeus.
|
None
|
19.95
nM
|
|
|
Alpha-1-adrenolytic activity was assessed from the ability to inhibit [3H]prazosin binding to rat cerebral cortex preparation
|
None
|
10.0
nM
|
|
|
Alpha-1-adrenolytic activity was assessed in vitro from the ability to inhibit clonidine binding to rat aorta preparation
|
None
|
9.772
nM
|
|
|
In vitro inhibitory activity against Alpha-1 adrenergic receptor by using [3H]prazosin radioligand binding assay
|
Rattus norvegicus
|
12.0
nM
|
|
|
Alpha-2 adrenergic receptor activity was assessed from the ability to inhibit [3H]yohimbine binding to rat cerebral cortex preparation
|
None
|
10.0
nM
|
|
|
Concentration of compound for 50% displacement of [3H]WB-4101 from Alpha-1 adrenergic receptor of rat brain
|
None
|
5.2
nM
|
|
|
In vitro inhibitory concentration against radioligand [3H]prazosin binding to alpha-1 adrenergic receptor in rat cortical membrane.
|
None
|
36.0
nM
|
|
|
Inhibition of [3H]WB-4101 binding to alpha-1-adrenergic receptor from rat cerebral cortex membranes
|
None
|
9.0
nM
|
|
|
Inhibition of specific [3H]clonidine binding (0.4 nM) to rat brain membranes Alpha-2 adrenergic receptor
|
None
|
20.0
nM
|
|
|
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
|
Oryctolagus cuniculus
|
6.31
nM
|
|
|
Displacement of [3H]prazosin (0.5 nM) from hamster Alpha-1B adrenergic receptor expressed in rat-1 cells
|
mesocricetus auratus (golden hamster)
|
220.0
nM
|
|
|
Binding affinity towards Alpha-2 adrenergic receptor, using [3H]- atipamezole as radioligand from rat frontal cortex membranes
|
None
|
1.4
nM
|
|
|
Ability to displace [3H]prazosin (0.25 nM) from whole brain of rat alpha-1 adrenergic receptor
|
None
|
90.0
nM
|
|
|
Binding affinity towards Alpha-1 adrenergic receptor from rat cortical membranes
|
None
|
18.0
nM
|
|
|
Compound was tested for the inhibition of [3H]clonidine binding Alpha-2 adrenergic receptor of crude rat brain membrane
|
None
|
9.3
nM
|
|
|
Binding affinity towards alpha-1 adrenergic receptor in rat cortical membranes
|
None
|
18.0
nM
|
|
|
Percent inhibition of the pressor responses to 0.75 ug/kg iv norepinephrine in pentobarbital-anesthetized dogs for a dose of 1 mg/kg
|
Canis lupus familiaris
|
100.0
%
|
|
|
Percent inhibition of the pressor responses to 0.75 ug/kg iv norepinephrine in pentobarbital-anesthetized dogs for a dose of 10 mg/kg
|
Canis lupus familiaris
|
100.0
%
|
|
|
Percent inhibition of the pressor responses to 0.75 ug/kg iv norepinephrine in pentobarbital-anesthetized dogs for a dose of 5.0 mg/kg
|
Canis lupus familiaris
|
100.0
%
|
|
|
Percent inhibition of the pressor responses to 1 ug/kg iv Epinephrine in pentobarbital-anesthetized dogs for a dose of 0.1 mg/kg
|
Canis lupus familiaris
|
41.0
%
|
|
|
Percent inhibition of the pressor responses to 1 ug/kg iv Epinephrine in pentobarbital-anesthetized dogs for a dose of 1 mg/kg
|
Canis lupus familiaris
|
100.0
%
|
|
|
Percent inhibition of the pressor responses to 1 ug/kg iv Epinephrine in pentobarbital-anesthetized dogs for a dose of 10 mg/kg
|
Canis lupus familiaris
|
100.0
%
|
|
|
Percent inhibition of the pressor responses to 7.5 ug/kg iv phenylephrine in pentobarbital-anesthetized dogs for a dose of 0.1 mg/kg
|
Canis lupus familiaris
|
42.0
%
|
|
|
Percent inhibition of the pressor responses to 7.5 ug/kg iv phenylephrine in pentobarbital-anesthetized dogs for a dose of 1 mg/kg
|
Canis lupus familiaris
|
86.0
%
|
|
|
Percent inhibition of the pressor responses to 7.5 ug/kg iv phenylephrine in pentobarbital-anesthetized dogs for a dose of 10 mg/kg
|
Canis lupus familiaris
|
100.0
%
|
|
|
Inhibition of specific [3H]-prazosin binding (0.2 nM) to rat brain membranes alpha1 adrenoceptor.
|
None
|
39.0
nM
|
|
|
Compound was tested for alpha-adrenoceptor blocking activity by its ability to antagonize norepinephrine contraction in the rat thoracic aorta
|
Rattus norvegicus
|
8.511
nM
|
|
|
Antagonist activity against phenylephrine-induced alpha1- adrenoceptor mediated vasoconstriction in pithed normotensive rats.
|
Rattus norvegicus
|
112.2
nM
|
|
|
Antagonist activity against B-HT 933-induced alpha-2-adrenoceptor-mediated vasoconstriction in pithed normotensive rats
|
Rattus norvegicus
|
338.84
nM
|
|
|
The compound was tested for affinity towards sigma-3 receptor
|
None
|
549.54
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
|
54.6
%
|
|
|
Compound was tested for its ability to inhibit specific binding of [3H]-clonidine to alpha-2-adrenoceptor.
|
None
|
37.5
nM
|
|
|
Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells
|
Homo sapiens
|
4.12
nM
|
|
|
Binding affinity towards human alpha-1B adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells
|
Homo sapiens
|
47.4
nM
|
|
|
Binding affinity towards human alpha-1D adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells
|
Homo sapiens
|
19.4
nM
|
|
|
Binding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells
|
Homo sapiens
|
55.9
nM
|
|
|
Binding affinity towards human alpha-2B adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells
|
Homo sapiens
|
48.0
nM
|
|
|
Binding affinity towards human alpha-2C adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells
|
Homo sapiens
|
80.3
nM
|
|
|
Displacement of [3H]prazosin from alpha1 adrenergic receptor
|
None
|
13.0
nM
|
|
|
Displacement of [3H]RX781094 from alpha2 adrenergic receptor
|
None
|
1.7
nM
|
|
|
Displacement of [125I]PIC from human alpha2 adrenoceptors expressed in CHO cells
|
Homo sapiens
|
57.03
nM
|
|
|
Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR
|
Homo sapiens
|
11.4
nM
|
|
Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR
|
Homo sapiens
|
11.4
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
|
None
|
359.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
|
None
|
103.0
nM
|
|
|
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
11.0
nM
|
|
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
4.655
nM
|
|
|
DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
82.0
nM
|
|
DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
45.0
nM
|
|
|
DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
|
None
|
22.0
nM
|
|
DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
|
None
|
11.0
nM
|
|
|
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
|
None
|
6.0
nM
|
|
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
|
None
|
2.25
nM
|
|
|
DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
|
None
|
18.0
nM
|
|
DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
|
None
|
8.228
nM
|
|
|
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
|
None
|
110.0
nM
|
|
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
|
None
|
16.0
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
|
None
|
396.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
|
None
|
207.0
nM
|
|
|
DRUGMATRIX: Calcium Channel Type L, Phenylalkylamine radioligand binding (ligand: [3H] (-)-Desmethoxyverapamil (D-888))
|
Rattus norvegicus
|
746.0
nM
|
|
DRUGMATRIX: Calcium Channel Type L, Phenylalkylamine radioligand binding (ligand: [3H] (-)-Desmethoxyverapamil (D-888))
|
Rattus norvegicus
|
725.0
nM
|
|
|
DRUGMATRIX: Imidazoline I2, Central radioligand binding (ligand: [3H] Idazoxan)
|
Rattus norvegicus
|
58.0
nM
|
|
DRUGMATRIX: Imidazoline I2, Central radioligand binding (ligand: [3H] Idazoxan)
|
Rattus norvegicus
|
39.0
nM
|
|
|
Displacement of [3H]prazosin from alpha1 adrenoceptor in rat cerebral cortex after 30 mins by beta scintillation counting
|
Rattus norvegicus
|
10.2
nM
|
|
|
Displacement of [3H]prazoin from rat cerebral cortex adrenergic alpha1 receptor
|
Rattus norvegicus
|
16.0
nM
|
|
|
Displacement of [3H]prazosin from alpha1-adrenergic receptor in rat cerebral cortex after 30 mins by scintillation counting
|
Rattus norvegicus
|
18.0
nM
|
|
|
Displacement of [3H]prazosin from alpha1 adrenergic receptor in rat cerebral cortex after 30 mins by Microbeta scintillation counting analysis
|
Rattus norvegicus
|
10.3
nM
|
|
|
Displacement of [3H]prazosin from rat cerebral cortex alpha-1 adrenergic receptor by liquid scintillation counting analysis
|
Rattus norvegicus
|
23.44
nM
|
|
|
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
|
Homo sapiens
|
1.1
nM
|
|
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
|
Homo sapiens
|
0.6
nM
|
|
|
Displacement of [3H]-Prazosin from human alpha-1B adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
|
Homo sapiens
|
10.8
nM
|
|
Displacement of [3H]-Prazosin from human alpha-1B adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
|
Homo sapiens
|
4.8
nM
|
|
|
Displacement of [3H]-Prazosin from human alpha-1D adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
|
Homo sapiens
|
12.5
nM
|
|
Displacement of [3H]-Prazosin from human alpha-1D adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
|
Homo sapiens
|
7.6
nM
|
|
|
Displacement of [3H]prazosin from alpha1 adrenergic receptor in rat brain cerebral cortex after 30 mins by microbeta scintillation counting method
|
Rattus norvegicus
|
18.0
nM
|
|
|
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in rat brain cortex after 30 mins by Microbeta scintillation counting method
|
Rattus norvegicus
|
16.0
nM
|
|
|
Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
|
Homo sapiens
|
12.0
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
|
2.09
%
|
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
-2.29
%
|
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
6.34
%
|
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
4.16
%
|
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
34.66
%
|
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
2.06
%
|
|
|
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
|
-2.31
%
|
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
14.21
%
|
|
|
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
|
0.13
%
|
|
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
|
0.13
%
|
|
|
Displacement of [3H]-pyrilamine from human recombinant histamine H1 receptor expressed in human recombinant CHO-K1 cells at 1 uM incubated for 60 mins by solid scintillation counting method relative to control
|
Homo sapiens
|
91.0
%
|
|
