|
Concentration giving half of the maximal ATPase activity calculated for the high-affinity binding site of the CHO P-Glycoprotein (P-gp) in two-affinity model
|
Cricetulus griseus
|
100.0
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
|
100.0
%
|
|
|
Inhibition of dopamine uptake at VMAT in bovine chromaffin granule ghosts
|
Bos taurus
|
1.0
nM
|
|
|
Inhibition of NorA pump-mediated ethidium bromide efflux in Staphylococcus aureus K1199B at 50 uM by fluorimetric analysis
|
Staphylococcus aureus
|
81.6
%
|
|
|
Inhibition of MepA efflux pump in Staphylococcus aureus K2361 assessed as reduction of ethidium bromide efflux at 30 uM for 5 mins
|
Staphylococcus aureus
|
32.0
%
|
|
|
Inhibition of NorA efflux pump in Staphylococcus aureus K2361 assessed as reduction of ethidium bromide efflux at 30 uM for 5 mins
|
Staphylococcus aureus
|
81.0
%
|
|
|
Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay
|
Plasmodium falciparum 7G8
|
316.23
nM
|
|
|
Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay
|
Plasmodium falciparum
|
794.33
nM
|
|
|
Inhibition of NorA in Staphylococcus aureus 1199B assessed as reduction in ethidium bromide efflux at 50 uM by fluorimetry after 5 mins
|
Staphylococcus aureus
|
84.8
%
|
|
|
Inhibition of NorA in Staphylococcus aureus 1199B assessed as inhibition of ethidium bromide efflux at 50 uM by fluorimetry
|
Staphylococcus aureus
|
84.8
%
|
|
|
DRUGMATRIX: Calcium Channel Type L, Dihydropyridine radioligand binding (ligand: [3H] Nitrendipine)
|
Rattus norvegicus
|
821.0
nM
|
|
DRUGMATRIX: Calcium Channel Type L, Dihydropyridine radioligand binding (ligand: [3H] Nitrendipine)
|
Rattus norvegicus
|
528.0
nM
|
|
|
DRUGMATRIX: Sodium Channel, Site 2 radioligand binding (ligand: [3H] Batrachotoxin)
|
Rattus norvegicus
|
774.0
nM
|
|
DRUGMATRIX: Sodium Channel, Site 2 radioligand binding (ligand: [3H] Batrachotoxin)
|
Rattus norvegicus
|
706.0
nM
|
|
|
Inhibition of p-glycoprotein expression in vinblastine-sensitive human MCF7 cells at 5 ug/ml after 24 hrs by by immunofluorescence flow cytometry relative to control
|
Homo sapiens
|
38.0
%
|
|
|
Inhibition of norA-mediated EtBr efflux in Staphylococcus aureus SA1199B overexpressing norA and expressing A116E GrlA mutation at 50 uM by fluorometry
|
Staphylococcus aureus
|
84.8
%
|
|
|
TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells
|
None
|
500.0
nM
|
|
|
TP_TRANSPORTER: increase in Vinblastine intracellular accumulation in MDR1-expressing LLC-PK1 cells
|
None
|
970.0
nM
|
|
|
Inhibition of norA-mediated ethidium bromide efflux in methicillin-resistant Staphylococcus aureus SA-1199B at 2.5 ug/ml by spectrofluorometric analysis
|
Staphylococcus aureus
|
30.0
%
|
|
|
Inhibition of norA-mediated ethidium bromide efflux in methicillin-resistant Staphylococcus aureus SA-1199B at 5 ug/ml by spectrofluorometric analysis
|
Staphylococcus aureus
|
48.1
%
|
|
|
Inhibition of norA-mediated ethidium bromide efflux in methicillin-resistant Staphylococcus aureus SA-1199B at 10 ug/ml by spectrofluorometric analysis
|
Staphylococcus aureus
|
71.8
%
|
|
|
Inhibition of norA-mediated ethidium bromide efflux in methicillin-resistant Staphylococcus aureus SA-1199B at 20 ug/ml by spectrofluorometric analysis
|
Staphylococcus aureus
|
85.1
%
|
|
|
Inhibition of electric eel AChE at 2 mg/ml by Ellman's method
|
Electrophorus electricus
|
5.06
%
|
|
|
Inhibition of horse BChE at 2 mg/ml by Ellman's method
|
Equus caballus
|
15.34
%
|
|
|
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
|
67.2
%
|
|
|
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
|
25.4
%
|
|
|
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
|
72.3
%
|
|
|
Inhibition of NorA in Staphylococcus aureus 1199B harboring grlA A116E mutant assessed as inhibition of ethidium bromide efflux at 50 uM measured for 5 mins by fluorometric analysis relative to control
|
Staphylococcus aureus
|
82.0
%
|
|
|
Inhibition of NorA efflux pump in Staphylococcus aureus SA-1199B assessed as inhibition of EtBr efflux at 50 uM
|
Staphylococcus aureus
|
85.0
%
|
|
|
Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay
|
Homo sapiens
|
0.037
ug.mL-1
|
|
|
Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay in presence of vinblastine
|
Homo sapiens
|
0.31
ug.mL-1
|
|
|
Cytotoxicity against vinblastin-sensitive human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay
|
Homo sapiens
|
0.003
ug.mL-1
|
|
|
Inhibition of NorA in fluoroquinolone-resistant Staphylococcus aureus 1199B assessed as increase in ethidium bromide uptake at 5 to 20 ug/ml after 20 mins by fluorimetry
|
Staphylococcus aureus
|
73.0
%
|
|
|
Inhibition of NorA in Staphylococcus aureus SA-1199B expressing GrlA A116E mutant assessed as reduction in EtBr efflux at 50 uM incubated for 5 mins by fluorescence based assay
|
Staphylococcus aureus
|
84.8
%
|
|
|
Inhibition of Staphylococcus aureus SA-1199B NorA assessed as reduction in EtBr efflux at 50 uM measured over 5 mins by fluorescence assay relative to control
|
Staphylococcus aureus
|
82.0
%
|
|
|
Displacement of [3H]reserpine from human VMAT2 expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
|
Homo sapiens
|
5.26
nM
|
|
|
Displacement of [3H]DHTB from human VMAT2 expressed in HEK293 cell membranes incubated for 90 mins by microbeta scintillation counting method
|
Homo sapiens
|
630.0
nM
|
|
|
Binding affinity to human VMAT2 expressed in HEK293 cell membranes by scintillation counting method based saturation binding assay
|
Homo sapiens
|
8.0
nM
|
|
|
Displacement of [3H](+)-syn-Ethyl 1-(2-(2,4-Dioxo-1,2-dihydroquinazolin-3(4H)-yl)ethyl)-4-(4-fluorophenyl)piperidine-3-carboxylate from human VMAT2 expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
|
Homo sapiens
|
410.0
nM
|
|
|
Inhibition of human VMAT2 expressed in HEK293 cell membranes assessed as reduction in [3H[-5HT uptake pre-incubated for 10 mins before [3H[-5HT addition and measured after 6 mins
|
Homo sapiens
|
13.2
nM
|
|
|
Inhibition of VMAT2 in C57Bl/6J mouse striatal membranes assessed as reduction in [3H[-5HT uptake pre-incubated for 10 mins before [3H[-5HT addition and measured after 8 mins
|
Mus musculus
|
1.79
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
|
64.21
%
|
|
|
Inhibition of NorA in Staphylococcus aureus 1199B assessed as reduction in ethidium bromide efflux at 50 uM measured over 5 mins interval for 30 mins by fluorescence assay relative to control
|
Staphylococcus aureus
|
83.06
%
|
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
16.08
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
21.65
%
|
|
|
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
|
2.65
%
|
|
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
|
0.79
%
|
|
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
|
0.79
%
|
|
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
|
2.65
%
|
|
