|
Binding affinity to human CBG receptor (corticosteroid-binding globulins)
|
None
|
13.18
nM
|
|
|
Compound was measured for its inhibitory activity on IFN-gamma-induced nitric oxide production in mouse macrophage
|
Mus musculus
|
15.0
nM
|
|
|
Inhibitory activity against production of nitric oxide induced by interferon-gamma in mouse macrophages
|
Mus musculus
|
10.0
nM
|
|
|
In vitro inhibitory activity on the production of nitric oxide (NO) induced by LPS in mouse peritoneal macrophages at a concentration of 10e-4 M
|
Mus musculus
|
92.6
%
|
|
|
In vivo inhibitory activity on the increase of serum GOT induced by D-GalN / LPS (liver injury) in mice at 20 mg/kg peroral administration
|
Mus musculus
|
98.3
%
|
|
|
In vivo inhibitory activity on the increase of serum GPT induced by D-GalN / LPS (liver injury) in mice at 50 mg/kg peroral administration
|
Mus musculus
|
99.0
%
|
|
|
Inhibition of P-gp was determined using rhodamine-assay in human CaCo-2 cells
|
None
|
0.0
%
|
|
|
Compound evaluated for inhibition of rat paw swelling after ip administration at 0.30 mg/kg in acute phase
|
Rattus norvegicus
|
32.0
%
|
|
|
Compound evaluated for inhibition of rat paw swelling after ip administration at 0.30 mg/kg in delayed phase
|
Rattus norvegicus
|
36.0
%
|
|
|
Compound was evaluated for its inhibitory effects on passive cutaneous anaphylaxis in rats at a dose of 1 (mg / site).
|
Rattus norvegicus
|
6.99
%
|
|
|
Compound was evaluated for its inhibitory effects on passive cutaneous anaphylaxis in rats at a dose of 2.5 (mg / site).
|
Rattus norvegicus
|
-16.4
%
|
|
|
50 percent inhibitory concentration of compound to inhibit nitric oxide production induced by IFN-gamma in mouse macrophages
|
Mus musculus
|
10.0
nM
|
|
|
Inhibition of nitric oxide (NO) production induced by interferon-gamma (IFN-gamma) in mouse macrophages
|
Mus musculus
|
10.0
nM
|
|
|
Inhibitory activity against nitric oxide production induced by interferon-gamma (IFN-gamma) in mouse macrophages
|
Mus musculus
|
10.0
nM
|
|
|
Percent inhibition of nitric oxide production induced by IFN-uM concentration
|
Mus musculus
|
80.0
%
|
|
|
Inhibition of peribronchial eosinophilia in BALB/c mouse at 100 mg/kg, po relative to control
|
Mus musculus
|
94.0
%
|
|
|
Inhibition of D-galactosamine/LPS-induced liver injury in ddY mouse assessed as serum GOT level at 10 mg/kg, po
|
Mus musculus
|
94.2
%
|
|
|
Inhibition of D-galactosamine/LPS-induced liver injury in ddY mouse assessed as serum GPT level at 10 mg/kg, po
|
Mus musculus
|
97.7
%
|
|
|
Inhibition of D-galactosamine/LPS-induced TNFalpha level in ddY mouse serum at 10 mg/kg, po by ELISA
|
Mus musculus
|
92.1
%
|
|
|
Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin
|
Homo sapiens
|
630.96
nM
|
|
|
Hepatoprotective activity against D-galactosamine/LPS-induced liver injury in ddY mouse assessed as inhibition of serum alanine transaminase level at 20 mg/kg, ip administered 1 hr before D-galactosamine/LPS challenge by Reitman-Frankel method
|
Mus musculus
|
99.0
%
|
|
|
Hepatoprotective activity against D-galactosamine/LPS-induced liver injury in ddY mouse assessed as inhibition of serum aspartate transaminase level at 20 mg/kg, ip administered 1 hr before D-galactosamine/LPS challenge by Reitman-Frankel method
|
Mus musculus
|
97.0
%
|
|
|
Hepatoprotective activity in ddY mouse assessed as inhibition of D-galactosamine/LPS-induced liver injury by measuring serum aspartate aminotransferase activity at 10 mg/kg, po dosed 1 hr before D-GalN/LPS challenge relative to untreated control
|
Mus musculus
|
94.2
%
|
|
|
Hepatoprotective activity in ddY mouse assessed as inhibition of D-galactosamine/LPS-induced liver injury by measuring serum alanine aminotransferase activity at 10 mg/kg, po dosed 1 hr before D-GalN/LPS challenge relative to untreated control
|
Mus musculus
|
97.7
%
|
|
|
Hepatoprotective activity in ddY mouse assessed as inhibition of D-galactosamine/LPS-induced increase in serum TNFalpha level at 20 mg/kg, po dosed 1 hr before D-GalN/LPS challenge relative to untreated control
|
Mus musculus
|
92.1
%
|
|
|
Hepatoprotective activity against D-galactosamine/lipopolysaccharide-induced liver injury in ddY mouse assessed as inhibition of increase in sAST level at 10 mg/kg, po administered 1 hr before D-GalN/LPS challenge measured after 10 hrs
|
Mus musculus
|
94.2
%
|
|
|
Hepatoprotective activity against D-galactosamine/lipopolysaccharide-induced liver injury in ddY mouse assessed as inhibition of increase in sALT level at 10 mg/kg, po administered 1 hr before D-GalN/LPS challenge measured after 10 hrs
|
Mus musculus
|
97.7
%
|
|
|
Inhibition of human 17beta-HSD7 expressed in HEK293 cells assessed as inhibition of reduction of [14C]estrone into [14C]estradiol at 3 uM after 7 hrs
|
Homo sapiens
|
10.3
%
|
|
|
Antiinflammatory activity in CD-1 mouse Macrophage assessed as inhibition of IFN-gamma induced NO production after 48 hrs by Griess reaction
|
Mus musculus
|
10.0
nM
|
|
|
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFN-gamma induced NO production after 24 hrs by Griess reaction
|
Mus musculus
|
61.0
nM
|
|
|
DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
|
None
|
26.0
nM
|
|
DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
|
None
|
12.0
nM
|
|
|
TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical)(Digoxin: 5 uM, Cortisol: 100 uM) in Caco-2 cells
|
None
|
56.0
%
|
|
|
Antiinflammatory activity in CD1 mouse ear dermatitis model assessed as inhibition of Croton oil-induced ear edema at 0.10 umol administered topically per cm'2 of ear measured after induction of dermatitis relative to untreated control
|
Mus musculus
|
77.0
%
|
|
|
Antiinflammatory activity in CD1 mouse ear dermatitis model assessed as inhibition of Croton oil-induced ear edema at 0.04 umol administered topically per cm'2 of ear measured 6 hrs after induction of dermatitis relative to untreated control
|
Mus musculus
|
79.0
%
|
|
|
Antiinflammatory activity in CD1 mouse ear dermatitis model assessed as inhibition of Croton oil-induced ear edema at 0.04 umol administered topically per cm'2 of ear measured 12 hrs after induction of dermatitis relative to untreated control
|
Mus musculus
|
60.0
%
|
|
|
Antiinflammatory activity in CD1 mouse ear dermatitis model assessed as reduction in AUC of of Croton oil-induced ear edema response at 0.04 umol administered topically per cm'2 of ear measured 48 hrs after induction of dermatitis relative to untreated control
|
Mus musculus
|
69.0
%
|
|
|
Antiinflammatory activity in CD1 mouse ear dermatitis model assessed as reduction in leukocyte infiltration-based myeloperoxidase activity at 0.04 umol administered topically per cm'2 of ear measured 3 to 48 hrs post dermatitis induction relative to untreated control
|
Mus musculus
|
35.0
%
|
|
|
Antiinflammatory activity in CD1 mouse ear dermatitis model assessed as inhibition of Croton oil-induced ear edema at 0.01 umol administered topically per cm'2 of ear measured after induction of dermatitis relative to untreated control
|
Mus musculus
|
29.0
%
|
|
|
Antiinflammatory activity in CD1 mouse ear dermatitis model assessed as inhibition of Croton oil-induced ear edema at 0.03 umol administered topically per cm'2 of ear measured after induction of dermatitis relative to untreated control
|
Mus musculus
|
55.0
%
|
|
|
Antiinflammatory activity in CD1 mouse ear dermatitis model assessed as reduction in AUC of global leukocyte infiltration-based myeloperoxidase activity at 0.04 umol administered topically per cm'2 of ear measured 3 to 48 hrs post dermatitis induction relative to untreated control
|
Mus musculus
|
51.0
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
98.24
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
113.79
%
|
|
|
Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw swelling at 2 x 50 mg/kg, po administered 0.5 to 3 hrs prior to carrageenan challenge measured after 2.5 hrs by plethysmographic analysis relative to control
|
Rattus norvegicus
|
35.0
%
|
|
|
Antiinflammatory activity in rat assessed as reduction of carrageenan-induced foot edema at 50 mg/kg, po administered as two doses
|
Rattus norvegicus
|
51.0
%
|
|
|
Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 50 mg/kg, po administered as two doses 3 and 0.5 hr prior to challenge measured 2.5 hrs post challenge
|
Rattus norvegicus
|
42.0
%
|
|
|
Displacement of 1 x 10'-8 M of [1,2,3-3H]-triamcinolone acetonide from glucocorticoid receptor in soluble fraction of mouse L929 cells after 20 hrs
|
Mus musculus
|
43.0
nM
|
|
|
Antiinflammatory activity in Wistar rat assessed as inhibition of cotton pellet-induced granuloma formation at 10 mg/kg, po after 5 days relative to control
|
Rattus norvegicus
|
30.0
%
|
|
|
Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced thromboxane B2 production at 10 uM incubated for 48 hrs by ELISA method
|
Mus musculus
|
42.0
%
|
|
|
Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced prostaglandin E2 production at 10 uM incubated for 48 hrs by ELISA method
|
Mus musculus
|
21.0
%
|
|
|
Displacement of [3H]-dexamethasone from GR receptor in human IM-9 cytosolic extracts at 60 nM preincubated for 6 hrs followed by washout and second incubation with [3H]-dexamethasone for 1 hr relative to control
|
Homo sapiens
|
3.0
%
|
|
|
Displacement of [3H]-dexamethasone from GR receptor in human IM-9 cytosolic extracts at 60 nM preincubated for 6 hrs followed by washout and second incubation with [3H]-dexamethasone for 2 hrs relative to control
|
Homo sapiens
|
6.0
%
|
|
|
Displacement of [3H]-dexamethasone from GR receptor in human IM-9 cytosolic extracts at 60 nM preincubated for 6 hrs followed by washout and second incubation with [3H]-dexamethasone for 3 hrs relative to control
|
Homo sapiens
|
4.0
%
|
|
|
Displacement of [3H]-dexamethasone from GR receptor in human IM-9 cytosolic extracts at 60 nM preincubated for 6 hrs followed by washout and second incubation with [3H]-dexamethasone for 4 hrs relative to control
|
Homo sapiens
|
-1.0
%
|
|
|
Displacement of [3H]-dexamethasone from GR receptor in human IM-9 cytosolic extracts at 60 nM preincubated for 6 hrs followed by washout and second incubation with [3H]-dexamethasone for 16 hrs relative to control
|
Homo sapiens
|
5.0
%
|
|
|
Displacement of [3H]-dexamethasone from GR receptor in human IM-9 cytosolic extracts at 60 nM preincubated for 6 hrs followed by washout and second incubation with [3H]-dexamethasone for 24 hrs relative to control
|
Homo sapiens
|
12.0
%
|
|
|
Displacement of [3H]-dexamethasone from GR receptor in human IM-9 cytosolic extracts at 60 nM preincubated for 6 hrs followed by [3H]-dexamethasone addition relative to control
|
Homo sapiens
|
69.0
%
|
|
|
Displacement of [3H]-dexamethasone from GR receptor in human IM-9 cytosolic extracts using buffer solution without beta-mercaptoethanol at 60 nM preincubated for 6 hrs followed by washout and second incubation with [3H]-dexamethasone for 1 hr relative to control
|
Homo sapiens
|
-16.0
%
|
|
|
Displacement of [3H]-dexamethasone from GR receptor in human IM-9 cytosolic extracts using buffer solution without beta-mercaptoethanol at 60 nM preincubated for 6 hrs followed by washout and second incubation with [3H]-dexamethasone for 2 hrs relative to control
|
Homo sapiens
|
-15.0
%
|
|
|
Displacement of [3H]-dexamethasone from GR receptor in human IM-9 cytosolic extracts using buffer solution without beta-mercaptoethanol at 60 nM preincubated for 6 hrs followed by washout and second incubation with [3H]-dexamethasone for 3 hrs relative to control
|
Homo sapiens
|
-23.0
%
|
|
|
Displacement of [3H]-dexamethasone from GR receptor in human IM-9 cytosolic extracts using buffer solution without beta-mercaptoethanol at 60 nM preincubated for 6 hrs followed by washout and second incubation with [3H]-dexamethasone for 4 hrs relative to control
|
Homo sapiens
|
-12.0
%
|
|
|
Displacement of [3H]-dexamethasone from GR receptor in human IM-9 cytosolic extracts using buffer solution without beta-mercaptoethanol at 60 nM preincubated for 6 hrs followed by washout and second incubation with [3H]-dexamethasone for 16 hrs relative to control
|
Homo sapiens
|
16.0
%
|
|
|
Displacement of [3H]-dexamethasone from GR receptor in human IM-9 cytosolic extracts using buffer solution without beta-mercaptoethanol at 60 nM preincubated for 6 hrs followed by washout and second incubation with [3H]-dexamethasone for 24 hrs relative to control
|
Homo sapiens
|
-8.0
%
|
|
|
Displacement of [3H]-dexamethasone from GR receptor in human IM-9 cytosolic extracts using buffer solution without beta-mercaptoethanol at 60 nM preincubated for 6 hrs followed by [3H]-dexamethasone addition relative to control
|
Homo sapiens
|
69.0
%
|
|
|
Antiinflammatory activity in BALB/c mouse assessed as inhibition of TPA-induced ear edema applied topically pretreated for 30 mins followed by TPA exposure measured after 4 hrs
|
Mus musculus
|
56.33
%
|
|
|
Binding affinity to MR (unknown origin)
|
Homo sapiens
|
0.5
nM
|
|
|
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
|
7.72
%
|
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
3.33
%
|
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
5.06
%
|
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
10.83
%
|
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
3.9
%
|
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
1.65
%
|
|
|
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
|
-3.64
%
|
|
|
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
|
52.93
%
|
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
14.45
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
1.1
%
|
|
|
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
|
-0.09
%
|
|
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
|
0.1
%
|
|
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
|
-0.09
%
|
|
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
|
0.1
%
|
|
|
Agonist activity at glucocorticoid receptor in rat INS-1 832/13 cells transfected with CCL2-promoter luciferase plasmid construct assessed as reduction in IL-1 beta induced inflammation by luciferase reporter gene assay
|
Rattus norvegicus
|
25.12
nM
|
|
