|
Inhibition of beta-lactamase at 100 uM
|
None
|
5.0
%
|
|
|
Inhibition of chymotrypsin at 250 uM
|
unidentified
|
5.0
%
|
|
|
Inhibitory activity when administered intravenously in histamine-stimulated gastric fistula dog at 3 mg/kg, id
|
Canis lupus familiaris
|
97.0
%
|
|
|
Percent inhibition of histamine-stimulated gastric acid secretion in Heidenhain pouch dog after intraduodenal administration of compound (1 umol/kg)
|
Canis lupus familiaris
|
53.0
%
|
|
|
Evaluated for the inhibition of H+/K+ ATPase enzyme from fundic mucosa of white rabbits at 100 uM
|
Oryctolagus cuniculus
|
3.3
uM
|
|
|
In vitro evaluation for the inhibition of H+/K+ ATPase at pH < 3 in the gastric glands of isolated rabbit stomach.
|
Oryctolagus cuniculus
|
501.19
nM
|
|
|
Inhibition of H+/K+ ATPase activity in buffered solution (pH 7.4) at concentration 400 mM
|
None
|
95.0
%
|
|
|
Compound was evaluated for gastric acid suppression on intravenous administration of a single dose up to 7 hr
|
Equus caballus
|
90.0
%
|
|
|
Inhibition of malate dehydrogenase (MDH) at 400 uM
|
None
|
5.0
%
|
|
|
Inhibition of [14C]aminopyrine (AP) accumulation stimulated by dibutyryl cyclic AMP in isolated rabbit parietal cells
|
Oryctolagus cuniculus
|
370.0
nM
|
|
|
Antisecretory activity evaluated by the inhibition of 14C -AP uptake in isolated rabbit parietal cells stimulated by dibutyryl cyclic adenosine 3', 5' -monophosphate (dcAMP)
|
Oryctolagus cuniculus
|
280.0
nM
|
|
|
Antisecretory activity evaluated by the inhibition of 14C -AP uptake in isolated rabbit parietal cells stimulated by exogenous histamine
|
Oryctolagus cuniculus
|
250.0
nM
|
|
|
Percent inhibition of gastric lesions induced by endomethacin was measured, after administration of 10 mg/kg po in rats
|
Rattus norvegicus
|
98.2
%
|
|
|
Percent inhibition of gastric lesions induced by endomethacin was measured, after administration of 2.5 mg/kg po in rats
|
Rattus norvegicus
|
42.5
%
|
|
|
Percent inhibition of gastric lesions induced by endomethacin was measured, after administration of 5 mg/kg po in rats
|
Rattus norvegicus
|
58.9
%
|
|
|
Percent inhibition of gastric lesions induced by endomethacin was measured, after administration of 7.5 mg/kg po in rats
|
Rattus norvegicus
|
86.6
%
|
|
|
Percent inhibition of gastric lesions induced by ethanol was measured, after administration of 10 mg/kg po in rats
|
Rattus norvegicus
|
43.1
%
|
|
|
Percent inhibition of gastric lesions induced by ethanol was measured, after administration of 15 mg/kg po in rats
|
Rattus norvegicus
|
82.0
%
|
|
|
Percent inhibition of gastric lesions induced by ethanol was measured, after administration of 20 mg/kg po in rats
|
Rattus norvegicus
|
89.4
%
|
|
|
Gastric antisecretory activity was tested in rats at 30 mg/kg, po expressed as the percentage of inhibition against the acid output of the control group
|
None
|
100.0
%
|
|
|
Inhibition of gastric proton pump activity of gastric H(+)/K(+) ATPase in Sprague-Dawley rat microsomal vesicles before washing at 10 uM
|
Rattus norvegicus
|
60.0
%
|
|
|
Inhibition of gastric proton pump activity of gastric H(+)/K(+) ATPase in Sprague-Dawley rat microsomal vesicles after washing at 10 uM
|
Rattus norvegicus
|
90.0
%
|
|
|
Inhibition of gastric H+/K(+)-ATPase activity in Sprague-Dawley rat microsomal vesicles at 3 uM in presence of 0.3 mM of ATP
|
Rattus norvegicus
|
38.0
%
|
|
|
Inhibition of gastric H+/K(+)-ATPase activity in Sprague-Dawley rat microsomal vesicles at 10 uM in presence of 0.3 mM of ATP
|
Rattus norvegicus
|
56.0
%
|
|
|
Inhibition of gastric H+/K(+)-ATPase activity in Sprague-Dawley rat microsomal vesicles at 30 uM in presence of 0.3 mM of ATP
|
Rattus norvegicus
|
75.0
%
|
|
|
Inhibition of gastric H+/K(+)-ATPase activity in Sprague-Dawley rat microsomal vesicles at 3 uM in presence of 1.0 mM of ATP
|
Rattus norvegicus
|
38.0
%
|
|
|
Inhibition of gastric H+/K(+)-ATPase activity in Sprague-Dawley rat microsomal vesicles at 10 uM in presence of 1.0 mM of ATP
|
Rattus norvegicus
|
51.0
%
|
|
|
Inhibition of gastric H+/K(+)-ATPase activity in Sprague-Dawley rat microsomal vesicles at 30 uM in presence of 1.0 mM of ATP
|
Rattus norvegicus
|
71.0
%
|
|
|
Inhibition of gastric H+/K(+)-ATPase activity in Sprague-Dawley rat microsomal vesicles at 3 uM in presence of 3.0 mM of ATP
|
Rattus norvegicus
|
34.0
%
|
|
|
Inhibition of gastric H+/K(+)-ATPase activity in Sprague-Dawley rat microsomal vesicles at 10 uM in presence of 3.0 mM of ATP
|
Rattus norvegicus
|
53.0
%
|
|
|
Inhibition of gastric H+/K(+)-ATPase activity in Sprague-Dawley rat microsomal vesicles at 30 uM in presence of 3.0 mM of ATP
|
Rattus norvegicus
|
76.0
%
|
|
|
Inhibition of p-NPPase in Sprague-Dawley rat microsomal vesicles at 3 uM in presence of 1.0 mM of p-NPP
|
Rattus norvegicus
|
28.0
%
|
|
|
Inhibition of p-NPPase in Sprague-Dawley rat microsomal vesicles at 10 uM in presence of 1.0 mM of p-NPP
|
Rattus norvegicus
|
54.0
%
|
|
|
Inhibition of p-NPPase in Sprague-Dawley rat microsomal vesicles at 30 uM in presence of 1.0 mM of p-NPP
|
Rattus norvegicus
|
77.0
%
|
|
|
Inhibition of p-NPPase in Sprague-Dawley rat microsomal vesicles at 3 uM in presence of 3.0 mM of p-NPP
|
Rattus norvegicus
|
28.0
%
|
|
|
Inhibition of p-NPPase in Sprague-Dawley rat microsomal vesicles at 10 uM in presence of 3.0 mM of p-NPP
|
Rattus norvegicus
|
52.0
%
|
|
|
Inhibition of p-NPPase in Sprague-Dawley rat microsomal vesicles at 30 uM in presence of 3.0 mM of p-NPP
|
Rattus norvegicus
|
78.0
%
|
|
|
Inhibition of p-NPPase in Sprague-Dawley rat microsomal vesicles at 10 uM in presence of 5.0 mM of p-NPP
|
Rattus norvegicus
|
48.0
%
|
|
|
Inhibition of p-NPPase in Sprague-Dawley rat microsomal vesicles at 30 uM in presence of 5.0 mM of p-NPP
|
Rattus norvegicus
|
79.0
%
|
|
|
Inhibition of p-NPPase in Sprague-Dawley rat microsomal vesicles at 100 uM in presence of 5.0 mM of p-NPP
|
Rattus norvegicus
|
96.0
%
|
|
|
Gastroprotective effect in ddY rat assessed as inhibition of ethanol-induced gastric mucosal lesions at 10 mg/kg, po administered 1 hr prior to ethanol challenge relative to control
|
Rattus norvegicus
|
43.1
%
|
|
|
Gastroprotective effect in ddY rat assessed as inhibition of ethanol-induced gastric mucosal lesions at 15 mg/kg, po administered 1 hr prior to ethanol challenge relative to control
|
Rattus norvegicus
|
82.0
%
|
|
|
Gastroprotective effect in ddY rat assessed as inhibition of ethanol-induced gastric mucosal lesions at 20 mg/kg, po administered 1 hr prior to ethanol challenge relative to control
|
Rattus norvegicus
|
89.4
%
|
|
|
Inhibition of H+/K+ATPase in pig gastric microsome assessed as liberation of inorganic phosphate using ATP at 10 uM relative to control
|
Sus scrofa
|
39.0
%
|
|
|
Antiulcerogenic activity in Kunming mouse assessed as inhibition of ethanol-induced gastric ulcer at 13.4 mg/kg, po qd for 5 days measured 1 hr post last dose relative to control
|
Mus musculus
|
36.74
%
|
|
|
Antiprotozoan activity against Trichomonas vaginalis GT3 trophozoites compound treated for 48 hrs measured after 48 hrs washout period
|
Trichomonas vaginalis
|
121.6
nM
|
|
|
Antiprotozoan activity against Giardia intestinalis IMSS:0989:1 trophozoites compound treated for 48 hrs measured after 48 hrs washout period
|
Giardia intestinalis
|
95.5
nM
|
|
|
Antiprotozoan activity against Entamoeba histolytica HM1-IMSS trophozoites compound treated for 48 hrs measured after 48 hrs washout period
|
Entamoeba histolytica
|
492.2
nM
|
|
|
HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells
|
Plasmodium berghei
|
680.0
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
|
15.9
%
|
|
|
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
|
29.5
%
|
|
|
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
|
11.3
%
|
|
|
Antiulcerogenic activity in ethanol-induced gastric ulcer Swiss albino mouse model assessed as inhibition of ulceration at 3.6 mg/kg administered intragastrically for 3 days relative to control
|
Mus musculus
|
68.3
%
|
|
|
Inhibition of CYP2C19 (unknown origin) at 24 uM by luminescent readout-based method
|
Homo sapiens
|
93.4
%
|
|
|
Inhibition of CYP2C19 (unknown origin) at 24 uM by P450-glo assay
|
Homo sapiens
|
93.4
%
|
|
|
Anti-Trichomonas activity against Trichomonas vaginalis JT assessed as reduction in parasite growth after 24 hrs by haemocytometry
|
Trichomonas vaginalis
|
121.6
nM
|
|
|
Inhibition of hydrogen potassium ATPase in goat stomach mucosal membrane assessed as decrease in inorganic phosphate production using ATP as substrate after 10 to 15 mins by spectrophotometric analysis
|
Capra hircus
|
980.0
nM
|
|
|
Inhibition of hydrogen potassium ATPase in goat stomach mucosal membrane assessed as decrease in inorganic phosphate production using ATP as substrate after 10 to 15 mins by spectrophotometric analysis relative to omeprazole
|
Capra hircus
|
82.12
%
|
|
|
Inhibition of H+/K+-ATPase in sheep stomach parietal cells assessed as reduction in inorganic phosphate liberation using ATP as substrate measured after 10 to 15 mins
|
Ovis aries
|
46.14
ug.mL-1
|
|
|
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
|
3.38
%
|
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
-0.65
%
|
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
7.63
%
|
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
9.59
%
|
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
7.26
%
|
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
27.0
%
|
|
|
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
|
-26.65
%
|
|
|
Inhibition of human recombinant IDE expressed in Escherichia coli BL21 (DE3) cells using ATTO 655- Cys-Lys-Leu-Val-Phe-Phe-Ala-Glu-Asp-Trp as substrate at 100 uM preincubated for 10 mins followed by substrate addition and measured after 30 mins by spectrophotometric analysis relative to control
|
Homo sapiens
|
41.0
%
|
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
99.38
%
|
|
|
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
|
-0.08
%
|
|
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
|
-0.08
%
|
|
|
Giardicidal activity against Giardia intestinalis incubated for 48 hrs by hemocytometric counting method
|
Giardia intestinalis
|
95.5
nM
|
|
