|
Binding affinity for Angiotensin II receptor, type 1 measured by ability to displace [125I]- A II from its specific binding site in rat liver membrane
|
None
|
1.3
nM
|
|
|
Binding affinity towards Angiotensin II receptor, type 1 in rat liver membrane using [125I]-angiotensin II (0.1 nM)
|
Rattus norvegicus
|
1.3
nM
|
|
|
In vitro inhibition of specific binding of [125I]AII to Angiotensin II receptor, type 1 from rat liver membrane
|
None
|
1.3
nM
|
|
|
Compound was evaluated for its binding affinity towards rat Angiotensin II receptor, type 1
|
None
|
0.8
nM
|
|
|
Inhibitory activity against Angiotensin II receptor, type 1 in rat liver membrane
|
None
|
1.3
nM
|
|
|
Displacement of [125I]- Ang II from type 1 Angiotensin II receptor
|
Rattus norvegicus
|
0.9
nM
|
|
|
Inhibition of [125I]-AII binding to Angiotensin II receptor of rat uterine membrane
|
Rattus norvegicus
|
1.3
nM
|
|
|
Binding affinity against AT1 in human hepatoma cell line, PLC-PRF-5
|
None
|
2.0
nM
|
|
|
Compound was evaluated for its binding affinity towards human Angiotensin II receptor, type 1
|
None
|
1.1
nM
|
|
|
In vitro binding affinity towards Angiotensin II receptor, type 1 of human hepatoma cell line PLC-PRF-5
|
None
|
2.0
nM
|
|
|
Compound was evaluated for its binding affinity towards human Endothelin A receptor
|
None
|
0.0001
nM
|
|
|
Inhibitory activity against Ang II-induced proliferation of human aortic smooth muscle cells in a dose-dependent manner
|
Homo sapiens
|
320.0
nM
|
|
|
Inhibition of AII(50 nM) induced intracellular [Ca2+] increase in PLC-PRF cells
|
Homo sapiens
|
4.0
nM
|
|
|
In vitro antagonist activity, Inhibition of angiotensin II (50 nM) mediated increase in cytosolic [Ca2+] conc. in PLC-PRF-5 cells
|
None
|
3.0
nM
|
|
|
Inhibitory activity against contractile response to angiotensin II (10 nM) of rabbit aortic rings
|
Oryctolagus cuniculus
|
4.0
nM
|
|
|
Compound was tested for its antagonistic activity against angiotensin II-induced contractions in rabbit aorta
|
Oryctolagus cuniculus
|
4.0
nM
|
|
|
Antagonistic activity through inhibition of A II induced contractions on rabbit aortic strips
|
Oryctolagus cuniculus
|
4.0
nM
|
|
|
Inhibitory concentration against angiotensin II receptor, type 1
|
Homo sapiens
|
0.8
nM
|
|
|
Binding affinity to angiotensin AT1 receptor in rat liver membranes
|
Rattus norvegicus
|
1.3
nM
|
|
|
Binding affinity to angiotensin AT1 receptor
|
None
|
20.8
nM
|
|
|
Displacement of [I125]angiotensin2 from AT1 receptor in Sprague-Dawley rat VSMC after 2.5 hrs by gamma spectrophotometry
|
Rattus norvegicus
|
0.58
nM
|
|
Displacement of [I125]angiotensin2 from AT1 receptor in Sprague-Dawley rat VSMC after 2.5 hrs by gamma spectrophotometry
|
Rattus norvegicus
|
0.41
nM
|
|
|
Binding affinity to AT1 receptor
|
None
|
0.8
nM
|
|
|
Displacement of [125I]Angiotensin-2 from angiotensin AT1 receptor in Sprague-Dawley rat VSMC after 60 mins by gamma counting
|
Rattus norvegicus
|
2.75
nM
|
|
Displacement of [125I]Angiotensin-2 from angiotensin AT1 receptor in Sprague-Dawley rat VSMC after 60 mins by gamma counting
|
Rattus norvegicus
|
3.11
nM
|
|
|
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells at 20 uM after 1.5 mins by fluorescence assay
|
Homo sapiens
|
15.0
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
76.05
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
47.18
%
|
|
|
Displacement of 125I-Ang2 from AT1 receptor in SPF Sprague-Dawley rat vascular smooth muscle cell membranes after 150 mins by gamma counting method
|
Rattus norvegicus
|
1.05
nM
|
|
Displacement of 125I-Ang2 from AT1 receptor in SPF Sprague-Dawley rat vascular smooth muscle cell membranes after 150 mins by gamma counting method
|
Rattus norvegicus
|
1.46
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
|
6.34
%
|
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
-3.35
%
|
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
7.4
%
|
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
1.45
%
|
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
6.33
%
|
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
-0.2
%
|
|
|
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
|
0.28
%
|
|
|
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
|
-3.98
%
|
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
13.92
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
9.227
%
|
|
|
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
|
-0.15
%
|
|
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
|
0.11
%
|
|
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
|
-0.15
%
|
|
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
|
0.11
%
|
|
|
Inhibition of [3H]-U46619 binding to TxA2 receptor in human platelet suspension at 0.3 uM incubated for 30 mins by liquid scintillation counting method relative to control
|
Homo sapiens
|
50.0
%
|
|
|
Agonist activity at human BLT2 overexpressed in CHO-K1 cells assessed as accumulation of inositol monophosphate measured after 90 mins by HTRF assay
|
Homo sapiens
|
410.0
nM
|
|
|
Antagonist activity at human AT1 overexpressed in CHO-K1 cells in presence of 10 nM [Val5-angiotensin II measured after 90 mins by HTRF based IP-one assay
|
Homo sapiens
|
6.0
nM
|
|
