|
In vitro activation of human peroxisome proliferator activated receptor gamma (PPAR gamma)
|
None
|
570.0
nM
|
|
|
Inhibition of triglyceride level in Syrian golden hamster at 300 umol/kg after 10 days
|
Mesocricetus auratus
|
77.0
%
|
|
|
Inhibition of cholesterol level in Syrian golden hamster at 300 umol/kg after 10 days
|
Mesocricetus auratus
|
30.0
%
|
|
|
Inhibition of HDL level in Syrian golden hamster at 300 umol/kg after 10 days
|
Mesocricetus auratus
|
33.0
%
|
|
|
Inhibition of glucose level in Syrian golden hamster at 300 umol/kg after 10 days
|
Mesocricetus auratus
|
33.0
%
|
|
|
Inhibition of glycerol level in Syrian golden hamster at 300 umol/kg after 10 days
|
Mesocricetus auratus
|
52.0
%
|
|
|
Inhibition of free fatty acids level in Syrian golden hamster at 300 umol/kg after 10 days
|
Mesocricetus auratus
|
53.0
%
|
|
|
Inhibition of synthetic amyloid beta-42 fibrillation by ThT fluorescence analysis relative to control
|
None
|
0.9
%
|
|
|
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy
|
Homo sapiens
|
0.2
%
|
|
|
Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP high binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay
|
Rattus norvegicus
|
24.0
nM
|
|
|
Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP low binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay
|
Rattus norvegicus
|
405.0
nM
|
|
|
Binding affinity to rat recombinant L-FABP low affinity site expressed in Escherichia coli BL21(DE3) at 5 deg C by fluorimetric assay
|
Rattus norvegicus
|
130.0
nM
|
|
|
Binding affinity to rat recombinant L-FABP high affinity site expressed in Escherichia coli BL21(DE3) at 5 deg C by fluorimetric assay
|
Rattus norvegicus
|
18.0
nM
|
|
|
Binding affinity to rat recombinant L-FABP low affinity site expressed in Escherichia coli BL21(DE3) at 42 deg C by fluorimetric assay
|
Rattus norvegicus
|
360.0
nM
|
|
|
Binding affinity to rat recombinant L-FABP low affinity site expressed in Escherichia coli BL21(DE3) at 37 deg C by fluorimetric assay
|
Rattus norvegicus
|
320.0
nM
|
|
|
Binding affinity to rat recombinant L-FABP high affinity site expressed in Escherichia coli BL21(DE3) at 37 deg C by fluorimetric assay
|
Rattus norvegicus
|
62.0
nM
|
|
|
Binding affinity to rat recombinant L-FABP low affinity site expressed in Escherichia coli BL21(DE3) at 30 deg C by fluorimetric assay
|
Rattus norvegicus
|
270.0
nM
|
|
|
Binding affinity to rat recombinant L-FABP high affinity site expressed in Escherichia coli BL21(DE3) at 30 deg C by fluorimetric assay
|
Rattus norvegicus
|
41.0
nM
|
|
|
Binding affinity to rat recombinant L-FABP low affinity site expressed in Escherichia coli BL21(DE3) at 25 deg C by fluorimetric assay
|
Rattus norvegicus
|
250.0
nM
|
|
|
Binding affinity to rat recombinant L-FABP high affinity site expressed in Escherichia coli BL21(DE3) at 25 deg C by fluorimetric assay
|
Rattus norvegicus
|
32.0
nM
|
|
|
Binding affinity to rat recombinant L-FABP low affinity site expressed in Escherichia coli BL21(DE3) at 20 deg C by fluorimetric assay
|
Rattus norvegicus
|
200.0
nM
|
|
|
Binding affinity to rat recombinant L-FABP high affinity site expressed in Escherichia coli BL21(DE3) at 20 deg C by fluorimetric assay
|
Rattus norvegicus
|
27.0
nM
|
|
|
Binding affinity to rat recombinant L-FABP high affinity site expressed in Escherichia coli BL21(DE3) at 15 deg C by fluorimetric assay
|
Rattus norvegicus
|
24.0
nM
|
|
|
Binding affinity to rat recombinant L-FABP low affinity site expressed in Escherichia coli BL21(DE3) at 15 deg C by fluorimetric assay
|
Rattus norvegicus
|
160.0
nM
|
|
|
Binding affinity to rat recombinant L-FABP high affinity site expressed in Escherichia coli BL21(DE3) at 10 deg C by fluorimetric assay
|
Rattus norvegicus
|
23.0
nM
|
|
|
Binding affinity to rat recombinant L-FABP low affinity site expressed in Escherichia coli BL21(DE3) at 10 deg C by fluorimetric assay
|
Rattus norvegicus
|
150.0
nM
|
|
|
Inhibition of human FAAH at 1 uM
|
Homo sapiens
|
-12.0
%
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
|
None
|
605.0
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
|
5.4
%
|
|
|
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
|
-10.8
%
|
|
|
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
|
34.2
%
|
|
|
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
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
82.56
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
90.21
%
|
|
|
Antihyperlipidemic activity in triton WR-1339 induced Charles Foster rat hyperlipidemia model assessed as inhibition of total cholesterol level in serum at 100 mg/kg, po administered simultaneously with triton WR-1339 after 18 hrs by enzymatic method relative to control
|
Rattus norvegicus
|
35.0
%
|
|
|
Antihyperlipidemic activity in triton WR-1339 induced Charles Foster rat hyperlipidemia model assessed as inhibition of phospholipid level in serum at 100 mg/kg, po administered simultaneously with triton WR-1339 after 18 hrs by enzymatic method relative to control
|
Rattus norvegicus
|
37.0
%
|
|
|
Antihyperlipidemic activity in triton WR-1339 induced Charles Foster rat hyperlipidemia model assessed as inhibition of triglyceride level in serum at 100 mg/kg, po administered simultaneously with triton WR-1339 after 18 hrs by enzymatic method relative to control
|
Rattus norvegicus
|
35.0
%
|
|
|
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
|
7.76
%
|
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
-2.44
%
|
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
13.99
%
|
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
12.37
%
|
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
15.83
%
|
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
1.23
%
|
|
|
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
|
-1.95
%
|
|
|
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
|
9.91
%
|
|
|
Antihyperlipidemic activity in high fat diet-induced hyperlipidemic mouse model assessed as reduction in serum triglyceride level at 13 mg/kg, po administered for last 30 days during 60 days of high fat diet feeding relative to control
|
Mus musculus
|
19.0
%
|
|
|
Antihyperlipidemic activity in high fat diet-induced hyperlipidemic mouse model assessed as reduction in total cholesterol level at 13 mg/kg, po administered for last 30 days during 60 days of high fat diet feeding relative to control
|
Mus musculus
|
1.6
%
|
|
|
Antihyperlipidemic activity in high fat diet-induced hyperlipidemic mouse model assessed as reduction in atherosclerosis index at 13 mg/kg, po administered for last 30 days during 60 days of high fat diet feeding relative to control
|
Mus musculus
|
25.7
%
|
|
|
Antihyperlipidemic activity in high fat diet-induced hyperlipidemic mouse model assessed as LDL level at 13 mg/kg, po administered for last 30 days during 60 days of high fat diet feeding relative to control
|
Mus musculus
|
15.3
%
|
|
|
Antioxidant activity in high fat diet-induced hyperlipidemic mouse model assessed as reduction in MDA level at 13 mg/kg, po administered for last 30 days during 60 days of high fat diet feeding relative to control
|
Mus musculus
|
8.0
%
|
|
|
In vivo anti-inflammatory activity in high fat diet-induced hyperlipidemic mouse model assessed as reduction in TNF-alpha level at 13 mg/kg, po administered for last 30 days during 60 days of high fat diet feeding relative to control
|
Mus musculus
|
24.6
%
|
|
|
In vivo anti-inflammatory activity in high fat diet-induced hyperlipidemic mouse model assessed as reduction in IL-6 level at 13 mg/kg, po administered for last 30 days during 60 days of high fat diet feeding relative to control
|
Mus musculus
|
16.9
%
|
|
|
Hepatoprotective activity in high fat diet-induced hyperlipidemic mouse model assessed as reduction in AST level at 13 mg/kg, po administered for last 30 days during 60 days of high fat diet feeding relative to control
|
Mus musculus
|
26.7
%
|
|
|
Hepatoprotective activity in high fat diet-induced hyperlipidemic mouse model assessed as reduction in ALT level at 13 mg/kg, po administered for last 30 days during 60 days of high fat diet feeding relative to control
|
Mus musculus
|
10.0
%
|
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
17.79
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
3.672
%
|
|
|
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
|
-0.17
%
|
|
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
|
-0.17
%
|
|
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
%
|
|
