|
Fold decrease in IC50 vs beta-lactamase on pre-incubation
|
Escherichia coli
|
5.0
|
|
|
Binding affinity was determined by displacement of [3H]P1075 from its binding sites in canine cardiac membranes
|
Canis lupus familiaris
|
130.0
nM
|
|
|
Fold increase in IC50 vs chymotrypsinogen with 1.0 mg/ml saponin
|
None
|
8.0
|
|
|
Fold decrease in IC50 vs chymotrypsinogen on pre-incubation
|
None
|
6.0
|
|
|
The inhibitory concentration was measured on guinea pig cardiomyocytes
|
Cavia porcellus
|
8.0
nM
|
|
|
Antiarrhythmic effect in Guinea pig papillary muscle KATP channel at 0.02 uM
|
Cavia porcellus
|
0.0
%
|
|
|
Antiarrhythmic effect in Guinea pig papillary muscle KATP channel at 0.2 uM
|
Cavia porcellus
|
76.0
%
|
|
|
Antiarrhythmic effect in Guinea pig papillary muscle KATP channel at 2 uM
|
Cavia porcellus
|
87.0
%
|
|
|
Fold increase in IC50 vs malate dehydrogenase (MDH) with 1 mg/ml saponin
|
None
|
24.0
|
|
|
Fold decrease in IC50 vs malate dehydrogenase (MDH) on pre-incubation
|
None
|
3.0
|
|
|
Inhibition of [125I]-I binding to ATP-inhibited Potassium channel receptor of Rat brain homogenate
|
Rattus norvegicus
|
0.608
nM
|
|
|
The inhibitory concentration was measured on the rat insulinoma cell line RIN-m5F
|
Rattus norvegicus
|
1.6
nM
|
|
|
Inhibition of human SUR1/Kir6.2 expressed in CHO cells
|
Homo sapiens
|
4.3
nM
|
|
|
Inhibition of human SUR2A/Kir6.2 expressed in Xenopus oocytes
|
Homo sapiens
|
220.0
nM
|
|
|
Fold increase in IC50 vs beta-lactamaase with 1 mg/mL saponin
|
Escherichia coli
|
49.0
|
|
|
Fold increase in IC50 vs beta-lactamase with 10x increased enzyme
|
Escherichia coli
|
50.0
|
|
|
Antiarrhythmic effect in hSUR1/hKir6.2 (pancreatic KATP channel) transfected in CHO cells at 10 nM
|
Homo sapiens
|
92.7
%
|
|
|
Antiarrhythmic effect in hSUR1/hKir6.2 (pancreatic KATP channel) transfected in CHO cells at 1 nM
|
Homo sapiens
|
24.0
%
|
|
|
Antiarrhythmic effect in hSUR1/hKir6.2 (pancreatic KATP channel) transfected in CHO cells at 3 nM
|
Homo sapiens
|
73.3
%
|
|
|
Antidiabetic activity in sucrose loaded albino Sprague-Dawley rat model assessed as decrease in blood glucose level at 100 mg/kg, po
|
Rattus norvegicus
|
33.9
%
|
|
|
Antidiabetic activity in streptozotocin-induced diabetic albino Sprague-Dawley rat model assessed as decrease in blood glucose level at 100 mg/kg, po
|
Rattus norvegicus
|
32.8
%
|
|
|
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy
|
Homo sapiens
|
0.3
%
|
|
|
Inhibition of CETP in rabbit serum at 10 uM after 1 hr by fluorescent cholesteryl esters transfer assay
|
Oryctolagus cuniculus
|
35.0
%
|
|
|
Inhibition of rat K+ATP channel
|
Rattus norvegicus
|
1.1
nM
|
|
|
Antihyperglycemic activity in Charles Foster/Wistar albino rat assessed as reduction in blood glucose level at 100 mg/kg, po administered 30 mins before sucrose challenge
|
Rattus norvegicus
|
33.9
%
|
|
|
Antihyperglycemic activity against sucrose challenged streptozotocin-induced diabetic Sprague-Dawley albino rat assessed as reduction in blood glucose level at 100 mg/kg, po administered 30 mins before sucrose challenge measured after 5 hrs
|
Rattus norvegicus
|
32.8
%
|
|
|
Antihyperglycemic activity in C57BL/Ks db/db mouse assessed as reduction in blood glucose level measured after 3 days relative to control
|
Mus musculus
|
13.6
%
|
|
|
Hypoglycemic activity in streptozotocin-induced diabetic rat model assessed as decrease in serum glucose level at 10 mg/kg/day, po dosed via gavage for 14 days administered 3 days after streptozotocin challenge by UV-spectrophotometry
|
Rattus norvegicus
|
52.0
%
|
|
|
Antihyperlipidemic activity in high-cholesterol diet-induced hypercholesterolemia Swiss albino rat model assessed as reduction in serum cholesterol level at 10 mg/kg/day, po administered via gavage simultaneously with diet cocktail for 14 days by UV-spectrophotometry relative to untreated control
|
Rattus norvegicus
|
11.0
%
|
|
|
DRUGMATRIX: Potassium Channel [KATP] radioligand binding (ligand: [3H] Glyburide)
|
None
|
3.804
nM
|
|
DRUGMATRIX: Potassium Channel [KATP] radioligand binding (ligand: [3H] Glyburide)
|
None
|
0.432
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
|
92.4
%
|
|
|
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
|
49.3
%
|
|
|
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
|
77.4
%
|
|
|
Displacement of [3H]Glyburide from ATP-sensitive potassium channel in hamster pancreatic HIT-T15 cells after 2 hrs
|
Mesocricetus auratus
|
0.65
nM
|
|
Displacement of [3H]Glyburide from ATP-sensitive potassium channel in hamster pancreatic HIT-T15 cells after 2 hrs
|
Mesocricetus auratus
|
5.7
nM
|
|
|
Displacement of [3H]Glyburide from ATP-sensitive potassium channel in hamster pancreatic HIT-T15 cells at 10 uM after 2 hrs relative to control
|
Mesocricetus auratus
|
10.0
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
72.34
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
59.94
%
|
|
|
Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 0.1 mM glucose
|
Rattus norvegicus
|
7.0
nM
|
|
|
Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 5 mM glucose
|
Rattus norvegicus
|
3.0
nM
|
|
|
In-vivo hypoglycemic activity in alloxan-pretreated diabetic BALB/c mouse assessed as blood glucose level at 10 mg/kg after 8 hrs by glucometer analysis
|
Mus musculus
|
60.92
%
|
|
|
PubChem BioAssay. insulin secretion from INS-1E cells in the presence of 5 mM glucose-IC50. (Class of assay: confirmatory)
|
None
|
8.08
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
|
14.24
nM
|
|
|
Displacement of Fluormone-Pan-PPAR Green from human GST-tagged PPARgamma LBD at 10 uM by TR-FRET assay relative to control
|
Homo sapiens
|
77.5
%
|
|
|
Displacement of Fluormone-Pan-PPAR Green from human GST-tagged PPARdelta LBD at 10 uM by TR-FRET assay relative to control
|
Homo sapiens
|
21.5
%
|
|
|
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
|
-3.01
%
|
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
-12.57
%
|
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
8.21
%
|
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
-8.45
%
|
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
12.14
%
|
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
-0.39
%
|
|
|
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
|
1.86
%
|
|
|
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
|
-1.61
%
|
|
|
Inhibition of human TASK3 expressed in Xenopus oocytes at 100 uM by whole cell patch clamp assay relative to control
|
Homo sapiens
|
3.6
%
|
|
|
Binding affinity to PPARgamma (unknown origin) by TR-FRET assay
|
Homo sapiens
|
660.0
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
|
7.89
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
13.62
%
|
|
|
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
|
-0.07
%
|
|
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
|
-0.23
%
|
|
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
|
-0.23
%
|
|
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
|
-0.07
%
|
|
