Inhibitory activity against Lp-PLA2 in whole human plasma
|
None
|
5.0
nM
|
|
Inhibitory activity against recombinant human Lp-PLA2
|
None
|
0.25
nM
|
|
Non specific binding effect against Lp-PLA2 was determined in human plasma at 10 nM
|
None
|
60.0
%
|
|
Inhibitory activity against recombinant human Lp-PLA2 by mechanistic studies
|
None
|
0.11
nM
|
|
Inhibition of Lp-PLA2 within the atherosclerotic plaque 2 hr after an oral dose of 30 mg/kg to the WHHL rabbit
|
Oryctolagus cuniculus
|
95.0
%
|
|
Non specific binding effect against Lp-PLA2 was determined in rabbit plasma at 100 nM
|
Oryctolagus cuniculus
|
79.0
%
|
|
Inhibition of human plasma Lp-PLA2 at 1 nM by liquid scintillation counting
|
Homo sapiens
|
80.0
%
|
|
Inhibition of human plasma Lp-PLA2 at 10 nM by liquid scintillation counting
|
Homo sapiens
|
95.0
%
|
|
Inhibition of rabbit plasma Lp-PLA2 at 10 nM by liquid scintillation counting
|
Oryctolagus cuniculus
|
82.0
%
|
|
Inhibition of rabbit plasma Lp-PLA2 at 100 nM by liquid scintillation counting
|
Oryctolagus cuniculus
|
99.0
%
|
|
Inhibition of recombinant human Lp-PLA2 using [3H]PAF as substrate at 10 nM incubated for 5 mins prior to substrate addition measured after 10 mins by liquid scintillation counting analysis
|
Homo sapiens
|
0.1
nM
|
|
Inhibition of Lp-PLA2 in human plasma using [3H]PAF as substrate at 10 nM incubated for 5 mins prior to substrate addition measured after 10 mins by liquid scintillation counting analysis relative to control
|
Homo sapiens
|
95.0
%
|
|
Inhibition of Lp-PLA2 in rabbit plasma using [3H]PAF as substrate at 10 nM incubated for 5 mins prior to substrate addition measured after 10 mins by liquid scintillation counting analysis relative to control
|
Oryctolagus cuniculus
|
82.0
%
|
|
Inhibition of Lp-PLA2 in rabbit plasma using [3H]PAF as substrate at 100 nM incubated for 5 mins prior to substrate addition measured after 10 mins by liquid scintillation counting analysis relative to control
|
Oryctolagus cuniculus
|
99.0
%
|
|
Inhibition of Lp-PLA2 (unknown origin)
|
Homo sapiens
|
0.25
nM
|
|
Invivo inhibition of Lp-PLA2 in mouse plasma at 100 nM after 24 hrs
|
Mus musculus
|
96.0
%
|
|
Inhibition of Lp-PLA2 in mouse plasma at 1 uM using 2-thio-PAF substrate after 10 mins
|
Mus musculus
|
99.0
%
|
|
Inhibition of Lp-PLA2 in Sprague-Dawley rat plasma at 10 nM using 2-thio-PAF substrate after 10 mins
|
Rattus norvegicus
|
84.0
%
|
|
Inhibition of Lp-PLA2 in Sprague-Dawley rat plasma at 100 nM using 2-thio-PAF substrate after 10 mins
|
Rattus norvegicus
|
98.0
%
|
|
Inhibition of Lp-PLA2 in human plasma at 10 nM using 2-thio-PAF substrate after 10 mins
|
Homo sapiens
|
93.0
%
|
|
Inhibition of Lp-PLA2 in human plasma at 100 nM using 2-thio-PAF substrate after 10 mins
|
Homo sapiens
|
100.0
%
|
|
Inhibition of recombinant human Lp-PLA2 using 2-thio-PAF substrate after 10 mins
|
Homo sapiens
|
0.7
nM
|
|
Inhibition of recombinant human Lp-PLA2 at 100 nM using 2-thio-PAF substrate after 10 mins
|
Homo sapiens
|
92.0
%
|
|
Inhibition of recombinant human Lp-PLA2 at 10 nM using 2-thio-PAF substrate after 10 mins
|
Homo sapiens
|
88.0
%
|
|
Inhibition of recombinant human Lp-PLA2 using 2-thio-PAF as substrate measured for 10 mins by plate reader analysis
|
Homo sapiens
|
0.7
nM
|
|
Inhibition of Lp-PLA2 in human plasma at 10 nM using 2-thio-PAF as substrate measured for 10 mins by plate reader analysis
|
Homo sapiens
|
94.0
%
|
|
Inhibition of Lp-PLA2 in human plasma at 1 nM using 2-thio-PAF as substrate measured for 10 mins by plate reader analysis
|
Homo sapiens
|
59.0
%
|
|
Inhibition of Lp-PLA2 in rat plasma at 100 nM using 2-thio-PAF as substrate measured for 10 mins by plate reader analysis
|
Rattus norvegicus
|
98.0
%
|
|
Inhibition of Lp-PLA2 in rat plasma at 10 nM using 2-thio-PAF as substrate measured for 10 mins by plate reader analysis
|
Rattus norvegicus
|
84.0
%
|
|
Inhibition of human recombinant Lp-PLA2 using 2-thio-PAF as substrate after 20 mins by CPM-based fluorescence assay
|
Homo sapiens
|
0.049
nM
|
|
Inhibition of human recombinant PLA2-7B using 2-thio-PAF as substrate after 20 mins by CPM-based fluorescence assay
|
Homo sapiens
|
63.0
nM
|
|
Inhibition of Lp-PLA2 in human whole plasma using 2-thio-PAF as substrate preincubated for 15 mins followed by substrate addition measured after 3 mins by CPM-based fluorescence assay
|
Homo sapiens
|
35.0
nM
|
|
Binding affinity to human Lp-PLA2 by ITC assay
|
Homo sapiens
|
49.7
nM
|
|
Inhibition of Lp-PLA2 in whole human plasma pre-incubated for 15 mins before 2-thio-PAF substrate addition
|
Homo sapiens
|
0.035
nM
|
|
Inhibition of recombinant human Lp-PLA2 incubated for 20 mins by Thio-PAF assay
|
Homo sapiens
|
0.049
nM
|
|
Inhibition of recombinant human Lp-PLA2 pre-incubated for 30 mins before PED6 fluorogenic substrate
|
Homo sapiens
|
0.049
nM
|
|
Inhibition of recombinant human PLA2-VIIB by Thio-PAF assay
|
Homo sapiens
|
63.0
nM
|
|
Inhibition of human recombinant LpPLA2
|
Homo sapiens
|
0.0631
nM
|
|
Inhibition of Lp-PLA2 in rat plasma at 250 nM using 2-thio-PAF as substrate preincubated for 30 min followed by substrate addition measured every minute for 10 mins by DNTB reagent based assay by DNTB reagent based assay relative to control
|
Rattus norvegicus
|
97.0
%
|
|
Inhibition of Lp-PLA2 in human plasma at 250 nM using 2-thio-PAF as substrate preincubated for 30 min followed by substrate addition measured every minute for 10 mins by DNTB reagent based assay relative to control
|
Homo sapiens
|
100.0
%
|
|
Inhibition of human recombinant GST-tagged Lp-PLA2 (47 to 429 residues) expressed in Escherichia coli Rosetta(DE3) pLysS using 2-thio-PAF as substrate preincubated for 30 min followed by substrate addition measured every minute for 10 mins by DNTB reagent based assay
|
Homo sapiens
|
0.6
nM
|
|
Inhibition of Lp-PLA2 in human plasma at 50 nM using 2-thio-PAF as substrate preincubated for 30 min followed by substrate addition measured every minute for 10 mins by DNTB reagent based assay relative to control
|
Homo sapiens
|
93.0
%
|
|
Inhibition of Lp-PLA2 in rat plasma at 50 nM using 2-thio-PAF as substrate preincubated for 30 min followed by substrate addition measured every minute for 10 mins by DNTB reagent based assay relative to control
|
Rattus norvegicus
|
98.0
%
|
|
Inhibition of Lp-PLA2 in human plasma LDL fractions using 2-thio platelet-activating factor as substrate by TMB dye based spectrophotometry
|
Homo sapiens
|
0.1
nM
|
|
Inhibition of human Lp-PLA2
|
Homo sapiens
|
0.25
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
|
0.57
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
15.33
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
17.58
%
|
|
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
|
-0.38
%
|
|
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
|
-0.39
%
|
|
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
|
-0.39
%
|
|
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
|
-0.38
%
|
|
Inhibition of recombinant human Lp-PLA2 (47 to 429 residues) expressed in Escherichia coli RosettaTM2 (DE3) pLysS
|
Homo sapiens
|
0.7
nM
|
|