|
Inhibitory activity against Angiotensin II receptor, type 1 in rabbit aorta
|
Oryctolagus cuniculus
|
28.0
nM
|
|
|
Inhibitory activity against Angiotensin II receptor, type 1 in rat adrenal membrane
|
Oryctolagus cuniculus
|
0.64
nM
|
|
|
Displacement of [125 I]-AII (0.2 nM) from bovine adrenal cortical membrane angiotensin II (AII) receptor at 10e-7 M
|
Bos taurus
|
110.0
nM
|
|
|
Concentration required to inhibit [125I]AII binding to Angiotensin II receptor from membrane fractions of bovine adrenal cortex
|
None
|
110.0
nM
|
|
|
Inhibition of specific binding of [125 I ] Angiotensin-II (0.2 nM) to bovine adrenal cortex
|
None
|
110.0
nM
|
|
|
Inhibition of specific binding of [125I]angiotensin II (0.2 nM) to angiotensin II receptor in bovine adrenal cortex
|
Bos taurus
|
110.0
nM
|
|
|
Inhibitory activity against angiotensin II type 1 induced contractions in rabbit aorta
|
Oryctolagus cuniculus
|
0.3
nM
|
|
|
Concentration required for inhibition of Angiotensin-II induced rabbit aorta strips contraction
|
Oryctolagus cuniculus
|
0.2
nM
|
|
|
Percent inhibition of angiotensin II (0.1 ug/kg iv) -induced pressor response 3h after administration of test compounds (1 mg/kg po) in conscious male Sprague-Dawley rats
|
None
|
100.0
%
|
|
|
Percent inhibition of AII (0.1 ug/kg iv) -induced pressor response at 7 hr after administration of test compounds (0.1 mg/kg po) in conscious male Sprague-Dawley rats.
|
Rattus norvegicus
|
67.0
%
|
|
|
Inhibitory activity against the pressor response induced by angiotensin II (AII) in conscious rats, at 1 mg/kg p.o. at 3h
|
Rattus norvegicus
|
100.0
%
|
|
|
Inhibitory activity against the pressor response induced by angiotensin II (AII) in conscious rats, at 1 mg/kg p.o. at 7 hr
|
Rattus norvegicus
|
92.0
%
|
|
|
Inhibitory activity on AII (100 ng/kg iv)-induced pressor response after administration at 0.1 mg/kg po in conscious male Sprague-Dawley rats at 2 h.
|
None
|
51.0
%
|
|
|
Inhibitory activity on AII (100 ng/kg iv)-induced pressor response after administration at 0.1 mg/kg po in conscious male Sprague-Dawley rats at 24 h.
|
None
|
43.0
%
|
|
|
Inhibitory activity on AII (100 ng/kg iv)-induced pressor response after administration at 0.1 mg/kg po in conscious male Sprague-Dawley rats at 3 h.
|
None
|
67.0
%
|
|
|
Inhibitory activity on AII (100 ng/kg iv)-induced pressor response after administration at 0.1 mg/kg po in conscious male Sprague-Dawley rats at 5 h.
|
None
|
85.0
%
|
|
|
Inhibitory activity on AII (100 ng/kg iv)-induced pressor response after administration at 0.1 mg/kg po in conscious male Sprague-Dawley rats at 7 h.
|
None
|
91.0
%
|
|
|
Inhibitory activity on AII (100 ng/kg iv)-induced pressor response at 0.1 mg/kg po in conscious male Sprague-Dawley rats at 1 h.
|
None
|
24.0
%
|
|
|
Inhibitory effect on AII (100 ng/kg iv)-induced pressor response after administration at 0.1 mg/kg po in conscious male Sprague-Dawley rats at 0.5 h.
|
None
|
7.0
%
|
|
|
Percent inhibition of the Angiotensin-II (0.1micro g/kg, iv) induced pressor response after 3 hours of administration (10 mg/kg po) in rats
|
Rattus norvegicus
|
100.0
%
|
|
|
Percent inhibition of the Angiotensin-II (0.1micro g/kg, iv) induced pressor response after 7 hours of administration (10 mg/kg po) in rats
|
Rattus norvegicus
|
100.0
%
|
|
|
Percent inhibition of the Angiotensin-II (0.1micro g/kg, iv) induced pressor response after 7 hours of administration (3 mg/kg po) in rats
|
Rattus norvegicus
|
100.0
%
|
|
|
Percent inhibition of the Angiotensin-II (0.1ug/kg, iv) induced pressor response after 3 hours of administration (1 mg/kg po) in rats
|
None
|
100.0
%
|
|
|
Percent inhibition of the Angiotensin-II (0.1ug/kg, iv) induced pressor response after 3 hours of administration (3 mg/kg po) in rats
|
None
|
100.0
%
|
|
|
Percent inhibition of the Angiotensin-II (0.1ug/kg, iv) induced pressor response after 7 hours of administration (1 mg/kg po) in rats
|
None
|
92.0
%
|
|
|
Competitive antagonism of Angiotensin II receptor in endothelium removed isolated rat aortic ring; (n = 5)
|
Rattus norvegicus
|
9.55
nM
|
|
|
Antagonist activity at AT1 receptor in rat aorta
|
Rattus norvegicus
|
10.0
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
|
6.3
%
|
|
|
Antagonist activity at AT1 receptor in rat aortic rings
|
Rattus norvegicus
|
3.162
nM
|
|
|
Binding affinity to angiotensin AT1 receptor
|
None
|
110.0
nM
|
|
|
DRUGMATRIX: Phosphodiesterase PDE4 enzyme inhibition (substrate: [3H]cAMP + cAMP)
|
None
|
276.1
nM
|
|
|
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
|
None
|
689.5
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
|
52.1
%
|
|
|
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
|
28.6
%
|
|
|
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
|
28.4
%
|
|
|
Displacement of 125I-[Sar1,Leu8] angiotensin-2 from rat type 1 angiotensin-2 receptor expressed in African green monkey COS7 cells after 24 hrs
|
Rattus norvegicus
|
0.17
nM
|
|
|
Displacement of [3H]-Asp-{Nomega-[N-(4-propanoylaminobutyl)aminocarbonyl]}Arg-ValTyr-Ile-His-Pro-Phe-OH Tris(hydrotrifluoroacetate) from human AT1 receptor transfected in CHO cells co-expressing Galpha16-mtAEQ after 2 hrs by liquid scintillation counting
|
Homo sapiens
|
3.5
nM
|
|
Displacement of [3H]-Asp-{Nomega-[N-(4-propanoylaminobutyl)aminocarbonyl]}Arg-ValTyr-Ile-His-Pro-Phe-OH Tris(hydrotrifluoroacetate) from human AT1 receptor transfected in CHO cells co-expressing Galpha16-mtAEQ after 2 hrs by liquid scintillation counting
|
Homo sapiens
|
10.72
nM
|
|
|
Displacement of [3H]-Angiotensin 2 from human AT1 receptor transfected in CHOK1 cells preincubated for 30 mins with bovine serum albumin followed by radioligand addition by liquid scintillation counting
|
Homo sapiens
|
0.69
nM
|
|
|
Displacement of [125I-Sar1-Ile8]-Ang2 from human angiotensin 2 receptor type 1 receptor expressed in HEK293 cells after 1 hr by gamma counting analysis
|
Homo sapiens
|
10.4
nM
|
|
|
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
|
-4.34
%
|
|
|
Inhibition of Escherichia coli GroEL expressed in Escherichia coliDH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured soluble pig heart MDH refolding by measuring MDH enzyme activity using sodium mesoxalate as substrate after 20 to 40 mins by malachite green dye based spectrometric analysis relative to untreated control
|
Escherichia coli
|
98.0
%
|
|
|
Inhibition of Escherichia coli GroEL expressed in Escherichia coli DH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured rhodanese refolding by measuring rhodanese enzyme activity after 45 mins by Fe(SCN)3 dye based spectrometric analysis relative to untreated control
|
Escherichia coli
|
100.0
%
|
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
20.0
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
9.71
%
|
|
|
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
|
-0.2
%
|
|
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
|
-0.2
%
|
|
