|
Inhibition of specific binding of [125I]angiotensin-II to angiotensin 1 receptor in rat lung membrane preparation
|
None
|
3.0
nM
|
|
|
Displacement of [125I]SI-Ang2 from AT1 receptor in Sprague-Dawley rat liver membrane
|
Rattus norvegicus
|
0.23
nM
|
|
|
Inhibition of AT1 receptor
|
None
|
3.0
nM
|
|
|
Binding affinity to angiotensin AT1 receptor in rat lung membranes
|
Rattus norvegicus
|
3.7
nM
|
|
|
Displacement of [125I]Tyr4-Sar1,Ile8-Angiotensin II from human Angiotensin 1 receptor after 60 mins by scintillation counting
|
Homo sapiens
|
0.49
nM
|
|
|
Displacement of [125I]Sar1 Ile8-Ang 2 from angiotensin 2 AT1 receptor after 180 mins by gamma counting
|
None
|
1.0
nM
|
|
|
Displacement of [125I]Sar1 Ile8-Ang 2 from angiotensin 2 AT2 receptor after 180 mins by gamma counting
|
None
|
0.33
nM
|
|
|
Displacement of [125I]Sar1Ile8-Ang2 from angiotensin AT1 receptor after 180 mins by gamma counting
|
Homo sapiens
|
1.0
nM
|
|
|
Inhibition of angiotensin AT1 receptor
|
Homo sapiens
|
150.0
nM
|
|
|
HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells
|
Plasmodium berghei
|
25.0
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
|
109.4
%
|
|
|
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
|
91.5
%
|
|
|
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
|
94.9
%
|
|
|
Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation at 20 uM after 45 mins by spectrophotometric analysis relative to control
|
Mus musculus
|
55.0
%
|
|
|
Displacement of [125I]-SI-Ang-2 from AT1 receptor in Rattus norvegicus Sprague-Dawley (rat) liver membranes after 2 hr
|
Rattus norvegicus
|
0.23
nM
|
|
|
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells at 20 uM after 1.5 mins by fluorescence assay
|
Homo sapiens
|
38.0
%
|
|
|
Displacement of [125I]Tyr4-Sar1,Ile8-Angiotensin II from human Angiotensin 1 receptor after
|
Homo sapiens
|
0.49
nM
|
|
|
Displacement of [125I]-Sar1Ile8-angiotensin 2 from angiotensin 2 AT1 receptor (unknown origin) after 180 mins by gamma counting analysis
|
Homo sapiens
|
1.0
nM
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
77.57
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
41.88
%
|
|
|
Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells
|
Cricetulus griseus
|
960.0
nM
|
|
|
Inhibition of ACE (unknown origin) assessed as 3-Hydroxybutyril-glycil-glycil-glycine conversion to 3-hydroxybutyric acid at 500 uM after 60 mins by WST assay relative to control
|
Homo sapiens
|
97.0
%
|
|
|
Antagonist activity at human AT1 receptor expressed in CHO cells measured after overnight incubation by luciferase reporter gene assay
|
Homo sapiens
|
2.0
nM
|
|
|
Non-competitive inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method and Dixon plot
|
Homo sapiens
|
100.0
nM
|
|
|
Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method
|
Homo sapiens
|
420.0
nM
|
|
|
Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation reduction in astemizole O-demethylation after 30 mins by LC-MS/MS method in absence of 1 mM NADPH
|
Homo sapiens
|
540.0
nM
|
|
|
Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation after 30 mins by LC-MS/MS method in presence of 1 mM NADPH
|
Homo sapiens
|
540.0
nM
|
|
|
Mixed type inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method
|
Homo sapiens
|
190.0
nM
|
|
|
Displacement of [125I]-Sar1,Ile8-angiotensin 2 from AT1 receptor in Sprague-Dawley rat vascular smooth muscle cells after 150 mins by gamma counting analysis
|
Rattus norvegicus
|
3.8
nM
|
|
Displacement of [125I]-Sar1,Ile8-angiotensin 2 from AT1 receptor in Sprague-Dawley rat vascular smooth muscle cells after 150 mins by gamma counting analysis
|
Rattus norvegicus
|
2.75
nM
|
|
|
Displacement of Fluoromone from GST-tagged recombinant human PPARgamma ligand binding domain at 10 uM by LanthaScreen TR-FRET assay relative to control
|
Homo sapiens
|
61.3
%
|
|
|
Displacement of Fluoromone from GST-tagged recombinant human PPARgamma ligand binding domain at 10 uM by LanthaScreen TR-FRET assay relative to pioglitazone
|
Homo sapiens
|
91.0
%
|
|
|
Displacement of Fluoromone from GST-tagged recombinant human PPARgamma ligand binding domain by LanthaScreen TR-FRET assay
|
Homo sapiens
|
700.0
nM
|
|
|
Induction of mitochondrial dysfunction in Sprague-Dawley rat liver mitochondria assessed as inhibition of mitochondrial respiration per mg mitochondrial protein measured for 20 mins by A65N-1 oxygen probe based fluorescence assay
|
Rattus norvegicus
|
70.5
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
|
33.03
%
|
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
4.91
%
|
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
15.0
%
|
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
38.9
%
|
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
22.54
%
|
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
1.9
%
|
|
|
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
|
-31.0
%
|
|
|
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
|
1.27
%
|
|
|
Inhibition of AT1 receptor (unknown origin)
|
Homo sapiens
|
2.0
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
|
15.51
%
|
|
|
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
|
0.0
%
|
|
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
|
0.0
%
|
|
|
Modulation of cell death in imatinib-resistant human K562 cells assessed by increase in imatinib-mediated cell death in presence of presence of imatinib at 5 uM measured after 72 hrs by Propidium iodide stain based FACS assay (Rvb = 17%)
|
Homo sapiens
|
54.0
%
|
|
|
Modulation of cell death in imatinib-resistant human K562 cells assessed by increase in imatinib-mediated cell death in presence of presence of imatinib at 10 uM measured after 72 hrs by Propidium iodide stain based FACS assay (Rvb = 17%)
|
Homo sapiens
|
56.0
%
|
|
