|
Compound is evaluated for the inhibition of [125I]T3 uptake by H4 rat hepatoma cells at 0.1 mM
|
Rattus norvegicus
|
38.0
%
|
|
|
In vitro inhibitory activity against human whole blood Prostaglandin G/H synthase 1
|
None
|
150.0
nM
|
|
|
In vitro inhibitory activity against human whole blood Prostaglandin G/H synthase 2
|
Homo sapiens
|
50.0
nM
|
|
|
In vitro inhibition of prostaglandin synthesis was tested in rat
|
None
|
500.0
nM
|
|
|
Inhibitory activity was measured on carrageenan-induced paw edema at a dose of 25 mg/Kg at 4 hours after intraperitoneal administration in rats
|
Rattus norvegicus
|
31.0
%
|
|
|
Inhibition of carrageenan-induced 4 hours after 50 mg/kg i.p. administration in rats.
|
Rattus norvegicus
|
67.0
%
|
|
|
Antiinflammatory effect measured as % inhibition in carrageenan induced paw edema test in rat.
|
Rattus norvegicus
|
53.0
%
|
|
|
Analgesic effect measured as % inhibition in PBQ-induced writhing test in mice.
|
Mus musculus
|
84.0
%
|
|
Analgesic effect measured as % inhibition in PBQ-induced writhing test in mice.
|
Mus musculus
|
84.0
%
|
|
|
In vitro inhibitory activity against ovine cyclooxygenase-1 (COX-1) at 200 uM; Inactive
|
Ovis aries
|
50.0
%
|
|
|
Inhibitory concentration against COX-2; (valus obtained by Kato et al.)
|
Homo sapiens
|
26.0
nM
|
|
|
Inhibitory concentration against COX-2 upon incubation for 15 minutes at 37 degree C
|
Homo sapiens
|
5.0
nM
|
|
|
Inhibition of beta amyloid protein 42 in SH-SY5Y cell lines overexpressing SPA4CT at 100 uM
|
Homo sapiens
|
17.0
%
|
|
|
Inhibition of human COX1-mediated conversion of arachidonic acid to prostaglandin-E2
|
Homo sapiens
|
12.0
nM
|
|
|
Inhibition of mouse wild type COX2
|
Mus musculus
|
77.0
nM
|
|
|
Inhibition of mouse COX2 R120A mutant
|
Mus musculus
|
257.0
nM
|
|
|
Inhibition of mouse COX2 Y355F mutant
|
Mus musculus
|
137.0
nM
|
|
|
Inhibition of COX2
|
None
|
20.0
nM
|
|
|
Inhibition of COX1
|
None
|
70.0
nM
|
|
|
Inhibition of ovine COX1 for 17 mins pre-incubated before addition of [1-14C]arachidonic acid
|
Ovis aries
|
90.0
%
|
|
Inhibition of ovine COX1 for 17 mins pre-incubated before addition of [1-14C]arachidonic acid
|
Ovis aries
|
67.0
nM
|
|
|
Inhibition of mouse COX2 for 17 mins pre-incubated before addition of [1-14C]arachidonic acid
|
Mus musculus
|
85.0
%
|
|
Inhibition of mouse COX2 for 17 mins pre-incubated before addition of [1-14C]arachidonic acid
|
Mus musculus
|
22.0
nM
|
|
|
Inhibition of human COX2 for 17 mins pre-incubated before addition of [1-14C]arachidonic acid
|
Homo sapiens
|
90.0
%
|
|
Inhibition of human COX2 for 17 mins pre-incubated before addition of [1-14C]arachidonic acid
|
Homo sapiens
|
28.0
nM
|
|
|
Inhibition of mouse COX2 for 20 mins pre-incubated before addition of [1-14C]arachidonic acid
|
Mus musculus
|
22.0
nM
|
|
|
Inhibition of mouse COX2 V349A mutant at 4 uM 20 mins pre-incubated before addition of [1-14C]arachidonic acid
|
Mus musculus
|
40.0
%
|
|
|
Inhibition of mouse COX2 V349I mutant 20 mins preincubated before addition of [1-14C]arachidonic acid
|
Mus musculus
|
60.0
nM
|
|
|
Inhibition of mouse COX2 V349I mutant at 4 uM 20 mins pre-incubated before addition of [1-14C]arachidonic acid
|
Mus musculus
|
85.0
%
|
|
|
Inhibition of mouse COX2 V349L mutant at 4 uM 20 mins pre-incubated before addition of [1-14C]arachidonic acid
|
Mus musculus
|
20.0
%
|
|
|
Inhibition of mouse COX2 at 4 uM 20 mins pre-incubated before addition of [1-14C]arachidonic acid
|
Mus musculus
|
85.0
%
|
|
|
Inhibition of human cyclooxygenase 1
|
Homo sapiens
|
15.0
nM
|
|
|
Inhibition of COX1 in bovine platelets assessed as formation of 12-hydroxyheptadecatrienoic acid by HPLC
|
Bos taurus
|
3.0
nM
|
|
|
Inhibition of COX2 in LPS-stimulated human blood
|
Homo sapiens
|
10.0
nM
|
|
|
Inhibition of COX1 assessed as inhibition of arachidonic acid conversion to prostaglandin-E2 release
|
None
|
12.0
nM
|
|
|
Antiinflammatory activity in albino rat acute inflammatory model assessed as inhibition of carrageenan-induced paw edema at 13.5 mg/kg, po dosed 1 hr before carrageenan challenge measured after 2 hrs relative to control
|
Rattus norvegicus
|
63.7
%
|
|
|
Antiinflammatory activity in albino rat acute inflammatory model assessed as inhibition of carrageenan-induced paw edema at 13.5 mg/kg, po dosed 1 hr before carrageenan challenge measured after 4 hrs relative to control
|
Rattus norvegicus
|
78.7
%
|
|
|
Antiinflammatory activity in albino rat chronic arthritis model assessed as inhibition of Freund's adjuvant-induced paw edema at 13.5 mg/kg, po administered on day 16 to 19 post Freund's adjuvant challenge measured on day 19 relative to control
|
Rattus norvegicus
|
53.0
%
|
|
|
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy
|
Homo sapiens
|
-3.7
%
|
|
|
Inhibition of cyclooxygenase 1
|
None
|
12.0
nM
|
|
|
Inhibition of human COX1 expressed in sf9 cells
|
Homo sapiens
|
30.0
nM
|
|
|
Inhibition of human COX2 expressed in sf9 cells
|
Homo sapiens
|
70.0
nM
|
|
|
Inhibition of CXCL8-induced chemotaxis in human polymorphonuclear leukocyte pretreated for 15 mins measured after 4 hrs by cell migration assay
|
Homo sapiens
|
8.0
nM
|
|
|
Inhibition of wild type CXCR1 transfected in mouse L1.2 cells assessed as inhibition of CXCL8-induced cell migration pretreated for 15 mins measured after 4 hrs
|
None
|
12.0
nM
|
|
|
Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po
|
Rattus norvegicus
|
65.6
%
|
|
|
Inhibition of lipid peroxidation assessed as malondialdehyde level per 100 mg of gastric mucosa isolated from albino mouse at dose 30 mg/kg, po
|
Mus musculus
|
8.9
%
|
|
|
Inhibition of human H-PGDS expressed in Escherichia coli BL21 assessed as rate of glutathione-chloro-dinitro benzene conjugation at 50 uM
|
Homo sapiens
|
0.0
%
|
|
|
Antiinflammatory activity against carrageenan-induced paw edema in rat at 10 mg/kg, po administered 1 hr before carrageenan challenge measured after 6 hrs by plethysmometer
|
Rattus norvegicus
|
21.0
%
|
|
|
Binding affinity to D10/DA24 ssDNA aptamer
|
None
|
100.64
nM
|
|
|
Binding affinity to D22 ssDNA aptamer
|
None
|
166.34
nM
|
|
|
Binding affinity to D16 ssDNA aptamer
|
None
|
148.73
nM
|
|
|
Binding affinity to D3 ssDNA aptamer
|
None
|
42.7
nM
|
|
|
Antiinflammatory activity against Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 0.5 hrs
|
Rattus norvegicus
|
83.0
%
|
|
|
Antiinflammatory activity against Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 1 hrs
|
Rattus norvegicus
|
59.0
%
|
|
|
Antiinflammatory activity against Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 1.5 hrs
|
Rattus norvegicus
|
70.0
%
|
|
|
Antiinflammatory activity against Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 2 hrs
|
Rattus norvegicus
|
87.0
%
|
|
|
Antiinflammatory activity against Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 2.5 hrs
|
Rattus norvegicus
|
69.0
%
|
|
|
Antiinflammatory activity against Wistar albino rat assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 3 hrs
|
Rattus norvegicus
|
65.0
%
|
|
|
Antiinflammatory activity in Albino rat assessed as inhibition of carrageenan-induced paw volume at 20 mg/kg, po administered 1 hr before carrageenan challenge measured after 1 hr
|
Rattus norvegicus
|
21.55
%
|
|
|
Antiinflammatory activity in Albino rat assessed as inhibition of carrageenan-induced paw volume at 20 mg/kg, po administered 1 hr before carrageenan challenge measured after 2 hrs
|
Rattus norvegicus
|
17.89
%
|
|
|
Antiinflammatory activity in Albino rat assessed as inhibition of carrageenan-induced paw volume at 20 mg/kg, po administered 1 hr before carrageenan challenge measured after 3 hrs
|
Rattus norvegicus
|
20.85
%
|
|
|
Antiinflammatory activity in Albino rat assessed as inhibition of carrageenan-induced paw volume at 20 mg/kg, po administered 1 hr before carrageenan challenge measured after 4 hrs
|
Rattus norvegicus
|
6.94
%
|
|
|
PUBCHEM_BIOASSAY: Inhibitors of Bacterial Quorum Sensing Structure Activity Relationship (SAR) Analysis: Dose Response Assay. (Class of assay: confirmatory) [Related pubchem assays: 700, 527 ]
|
Staphylococcus aureus
|
943.0
nM
|
|
|
Antiinflammatory activity in bovine serum assessed as denaturation of albumin at 5 mM after 10 mins by spectrophotometry
|
Bos taurus
|
56.27
%
|
|
|
Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced hind paw edema at 100 mg/kg, po measured after 3 hrs of carrageenan challenge
|
Rattus norvegicus
|
38.19
%
|
|
|
Antiinflammatory activity in rat assessed as inhibition of complete Freund's adjuvant-induced paw swelling at 5 mg/kg, po administered on day 21 post induction of inflammation measured on day 35
|
Rattus norvegicus
|
35.27
%
|
|
|
Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, ip after 1 hr by plethysmometer
|
Rattus norvegicus
|
88.0
%
|
|
|
Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, ip after 2 hrs by plethysmometer
|
Rattus norvegicus
|
89.0
%
|
|
|
DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid)
|
Homo sapiens
|
13.0
nM
|
|
|
DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid)
|
None
|
37.0
nM
|
|
|
Antiinflammatory activity in Wistar rat pain model assessed as inhibition of DABK-induced paw oedema at 0.3 mg/kg, po administered 60 mins before DABK challenge
|
Rattus norvegicus
|
23.0
%
|
|
|
Antiinflammatory activity in Wistar rat pain model assessed as inhibition of DABK-induced paw oedema at 1 mg/kg, po administered 60 mins before DABK challenge
|
Rattus norvegicus
|
24.0
%
|
|
|
Antiinflammatory activity in Wistar rat pain model assessed as inhibition of DABK-induced paw oedema at 3 mg/kg, po administered 60 mins before DABK challenge
|
Rattus norvegicus
|
25.0
%
|
|
|
Inhibition of sheep placental cotyledons COX2
|
Ovis aries
|
60.0
nM
|
|
|
Inhibition of COX1
|
None
|
3.0
nM
|
|
|
Inhibition of COX2
|
None
|
5.0
nM
|
|
|
Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema dosed at 20 mg/kg in plantar region of paw administered 30 mins before carrageenan challenge measured 0.5 hrs post carrageenan-induced inflammation
|
Rattus norvegicus
|
61.0
%
|
|
|
Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema dosed at 20 mg/kg in plantar region of paw administered 30 mins before carrageenan challenge measured 1 hr post carrageenan-induced inflammation
|
Rattus norvegicus
|
69.0
%
|
|
|
Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema dosed at 20 mg/kg in plantar region of paw administered 30 mins before carrageenan challenge measured 1.5 hrs post carrageenan-induced inflammation
|
Rattus norvegicus
|
67.0
%
|
|
|
Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema dosed at 20 mg/kg in plantar region of paw administered 30 mins before carrageenan challenge measured 2 hrs post carrageenan-induced inflammation
|
Rattus norvegicus
|
78.0
%
|
|
|
Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema dosed at 20 mg/kg in plantar region of paw administered 30 mins before carrageenan challenge measured 2.5 hrs post carrageenan-induced inflammation
|
Rattus norvegicus
|
71.0
%
|
|
|
Antiinflammatory activity in Wistar albino rat assessed as inhibition of carrageenan-induced paw edema dosed at 20 mg/kg in plantar region of paw administered 30 mins before carrageenan challenge measured 3 hrs post carrageenan-induced inflammation
|
Rattus norvegicus
|
80.0
%
|
|
|
Antiinflammatory activity in Kunming mouse assessed as inhibition of xylene-induced auricle tumefaction at 0.2 mmol/kg, po qd administered prior to challenge for 5 days measured 30 mins post challenge
|
Mus musculus
|
41.92
%
|
|
|
TP_TRANSPORTER: inhibition of PAH uptake (PAH: 2 uM, Diclofenac: 1000 uM) in Xenopus laevis oocytes
|
Xenopus laevis
|
100.0
%
|
|
|
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
|
77.9
%
|
|
|
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
|
27.3
%
|
|
|
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
|
19.6
%
|
|
|
Anti-inflammatory activity in Rattus norvegicus Wistar albino (rat) assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 min before carrageenan challenge measured after 3 hr relative to control
|
Rattus norvegicus
|
75.0
%
|
|
|
Anti-inflammatory activity in Rattus norvegicus Wistar albino (rat) assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 min before carrageenan challenge measured after 2.5 hr relative to control
|
Rattus norvegicus
|
73.0
%
|
|
|
Anti-inflammatory activity in Rattus norvegicus Wistar albino (rat) assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 min before carrageenan challenge measured after 2 hr relative to control
|
Rattus norvegicus
|
76.0
%
|
|
|
Anti-inflammatory activity in Rattus norvegicus Wistar albino (rat) assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 min before carrageenan challenge measured after 1.5 hr relative to control
|
Rattus norvegicus
|
80.0
%
|
|
|
Anti-inflammatory activity in Rattus norvegicus Wistar albino (rat) assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 min before carrageenan challenge measured after 1 hr relative to control
|
Rattus norvegicus
|
65.0
%
|
|
|
Anti-inflammatory activity in Rattus norvegicus Wistar albino (rat) assessed as inhibition of carrageenan-induced paw edema at 20 mg/kg, po administered 30 min before carrageenan challenge measured after 0.5 hr relative to control
|
Rattus norvegicus
|
82.0
%
|
|
|
Acute Anti-inflammatory activity in Rattus norvegicus albino (rat) assessed as inhibition of carrageenan-induced paw edema at 13.5 mg/kg, po administered 1 hr after carrageenan challenge measured after 5 hr relative to control
|
Rattus norvegicus
|
75.0
%
|
|
|
Acute Anti-inflammatory activity in Rattus norvegicus albino (rat) assessed as inhibition of carrageenan-induced paw edema at 13.5 mg/kg, po administered 1 hr after carrageenan challenge measured after 3 hr relative to control
|
Rattus norvegicus
|
79.5
%
|
|
|
Anti-inflammatory activity in Rattus norvegicus Sprague-Dawley (rat) assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg administered 1 hr prior to carrageenan challenge measured at 4 hr relative to diclofenac
|
Rattus norvegicus
|
100.0
%
|
|
|
Anti-inflammatory activity in Rattus norvegicus Sprague-Dawley (rat) assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg administered 1 hr prior to carrageenan challenge measured at 4 hr relative to control
|
Rattus norvegicus
|
78.3
%
|
|
|
Anti-inflammatory activity in Rattus norvegicus Sprague-Dawley (rat) assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg administered 1 hr prior to carrageenan challenge measured at 2 hr relative to control
|
Rattus norvegicus
|
73.5
%
|
|
|
Anti-inflammatory activity in Rattus norvegicus Sprague-Dawley (rat) assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg administered 1 hr prior to carrageenan challenge measured at 1 hr relative to control
|
Rattus norvegicus
|
65.3
%
|
|
|
Anti-inflammatory activity in Rattus norvegicus Wistar (rat) assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip administered 30 min post carrageenan-challenge measured after 3 hr relative to control
|
Rattus norvegicus
|
80.4
%
|
|
|
Anti-inflammatory activity assessed as inhibition of albumin denaturation incubated for 15 min at 27 degC followed by incubation at 60 degC for 10 min by UV-Vis spectrophotometric analysis
|
None
|
71.0
ug.mL-1
|
|
|
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells at 20 uM after 1.5 mins by fluorescence assay
|
Homo sapiens
|
12.0
%
|
|
|
Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw oedema at 50 mg/kg after 180 mins relative to untreated control
|
Rattus norvegicus
|
45.76
%
|
|
|
Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw oedema at 50 mg/kg after 60 mins relative to untreated control
|
Rattus norvegicus
|
44.52
%
|
|
|
Analgesic activity in Swiss albino mouse assessed as inhibition of acetic acid-induced writhing at 50 mg/kg administered 30 mins followed by acetic acid challenge measured for 20 mins relative to control
|
Mus musculus
|
53.65
%
|
|
|
Inhibition of UGT in human liver microsomes using 4-methylumbelliferone as substrate after 10 mins by fluorescence analysis
|
Homo sapiens
|
56.0
%
|
|
|
Inhibition of purified mouse COX-2 assessed as inhibition of PGE2/PGD2 formation preincubated at 10 uM for 15 mins before arachidonic acid substrate addition measured after 30 seconds by LC-MS-MS method
|
Mus musculus
|
85.0
%
|
|
|
Inhibition of purified mouse COX-2 assessed as inhibition of PGE2/PGD2 formation preincubated for 15 mins before arachidonic acid substrate addition measured after 30 seconds by LC-MS-MS method
|
Mus musculus
|
100.0
nM
|
|
|
Inhibition of purified mouse COX-2 assessed as inhibition of PGE2-G/PGD2-G formation preincubated for 15 mins before 2-AG substrate addition measured after 30 seconds by LC-MS-MS method
|
Mus musculus
|
30.0
nM
|
|
|
Inhibition of human recombinant TTR Y78F mutant-mediated fibrillogenesis at 40 uM after 30 mins by turbidimetric assay relative to control
|
Homo sapiens
|
74.0
%
|
|
|
Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 10 mins prior to substrate addition measured after 2 mins by spectrophotometry
|
Ovis aries
|
70.0
nM
|
|
|
Inhibition of human recombinant COX2 using arachidonic acid as substrate incubated for 10 mins prior to substrate addition measured after 2 mins by spectrophotometry
|
Homo sapiens
|
20.0
nM
|
|
|
Inhibition of human recombinant COX-2 assessed as PGF2-alpha formation using arachidonic acid as substrate at 20 uM by enzyme immunoassay
|
Homo sapiens
|
100.0
%
|
|
|
Inhibition of ovine COX1 after 2 mins by EIA
|
Ovis aries
|
180.0
nM
|
|
|
Acute antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 13.5 mg/kg, po administered 1 hr followed by carrageenan challenge measured at 2 hrs by plethysmometric analysis relative to control
|
Rattus norvegicus
|
65.5
%
|
|
|
Acute antiinflammatory activity in albino rat assessed as inhibition of carrageenan-induced paw edema at 13.5 mg/kg, po administered 1 hr followed by carrageenan challenge measured at 4 hrs by plethysmometric analysis relative to control
|
Rattus norvegicus
|
66.2
%
|
|
|
Inhibition of ovine COX1 peroxidase activity assessed as reduction of PGG2 to PGH2 by measuring oxidized TMPD level at 10 ug/ml by colorimetric assay relative to control
|
Ovis aries
|
90.64
%
|
|
|
Inhibition of ovine COX2 peroxidase activity assessed as reduction of PGG2 to PGH2 by measuring oxidized TMPD level at 10 ug/ml by colorimetric assay relative to control
|
Ovis aries
|
48.58
%
|
|
|
Antiinflammatory activity in Wistar albino rat assessed as reduction in carrageenan-induced hind paw volume at 12.5 mg/kg, ip administered 10 mins after carrageenan-challenge measured up to 3 hrs
|
Rattus norvegicus
|
67.31
%
|
|
|
Antiinflammatory activity in Wistar albino rat assessed as reduction in carrageenan-induced hind paw volume at 25 mg/kg, ip administered 10 mins after carrageenan-challenge measured up to 3 hrs
|
Rattus norvegicus
|
84.62
%
|
|
|
Inhibition of purified ovine COX1 pre-treated for 1 hr before 10-acetyl-3,7-dihydroxyphenoxazin substrate addition in absence of porcine liver esterase by fluorescence assay
|
Ovis aries
|
320.0
nM
|
|
|
Inhibition of purified ovine COX1 at saturation drug level pre-treated for 1 hr before 10-acetyl-3,7-dihydroxyphenoxazin substrate addition in absence of porcine liver esterase by fluorescence assay
|
Ovis aries
|
100.0
%
|
|
|
Inhibition of human recombinant COX2 at saturation drug level pre-treated for 1 hr before 10-acetyl-3,7-dihydroxyphenoxazin substrate addition in absence of porcine liver esterase by fluorescence assay
|
Homo sapiens
|
100.0
%
|
|
|
Analgesic activity in Swiss albino mouse assessed as decrease in capsaicin-induced paw lickings at 25 mg/kg, ip administered 30 mins before capsaicin injection
|
Mus musculus
|
68.0
%
|
|
|
Inhibition of ovine COX1 assessed as inhibition of PGF2alpha production from PGH2 preincubated for 5 mins before arachidonic acid addition measured after 2 mins by enzyme immunoassay
|
Ovis aries
|
250.0
nM
|
|
|
Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2B6 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2C9 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2C19 in human liver microsomes at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2D6 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP3A4 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2C8 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Anti-inflammatory activity against Swiss albino mouse assessed as reduction in paw thickness at 10 mg/kg, ip administered 30 mins prior to dextran injection measured after 4 hrs by vernier calliper analysis relative to control
|
Mus musculus
|
42.0
%
|
|
|
Anti-hyperalgesic activity against Swiss albino mouse assessed as reduction in paw lickings at 10 mg/kg, ip administered 30 mins prior to capsaicin injection relative to control
|
Mus musculus
|
90.0
%
|
|
|
Inhibition of ovine COX-1 assessed as PGF2alpha formation using arachidonic acid as substrate pretreated with compound for 20 mins prior to substrate addition by spectrophotometric analysis
|
Ovis aries
|
610.0
nM
|
|
|
Inhibition of human recombinant COX-2 assessed as PGF2 alpha formation using arachidonic acid as substrate pretreated with compound for 20 mins prior to substrate addition by spectrophotometric analysis
|
Homo sapiens
|
630.0
nM
|
|
|
Antiinflammatory activity in rat assessed as reduction of carrageenan-induced paw oedema at 0.15 mmol/kg, ip administered 5 mins before carrageenan challenge measured after 3.5 hrs
|
Rattus norvegicus
|
37.0
%
|
|
|
Anti-inflammatory activity in rat assessed as reduction of carrageenan-induced paw edema at 150 umol/kg, ip after 3.5 hrs relative to control
|
Rattus norvegicus
|
37.0
%
|
|
|
Anti-inflammatory activity in albino Wistar rat assessed as inhibition of carrageenan-induced paw edema at 30 mg/kg, po measured every one hour for 5 hrs
|
Rattus norvegicus
|
85.33
%
|
|
|
Inhibition of ovine COX1 assessed as reduction in PGH2-derived PGF2alpha using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 2 mins by enzyme immunoassay
|
Ovis aries
|
70.0
nM
|
|
|
Inhibition of human recombinant COX2 assessed as reduction in PGH2-derived PGF2alpha using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 2 mins by enzyme immunoassay
|
Homo sapiens
|
20.0
nM
|
|
|
Antiinflammatory activity in rat carrageenan-induced paw edema model assessed as inhibition of paw swelling at 25 mg/kg, ip administered 30 mins prior to carrageenan challenge measured after 3 hrs
|
Rattus norvegicus
|
64.4
%
|
|
|
Antiinflammatory activity in rat carrageenan-induced paw edema model assessed as inhibition of paw swelling at 25 mg/kg, ip administered 30 mins prior to carrageenan challenge measured after 5 hrs
|
Rattus norvegicus
|
54.4
%
|
|
|
Analgesic activity in Dunkin Hartley guinea pig hyperalgesia pain model assessed as inhibition of LPS-induced thermal hyperalgesia at 10 mg/kg, po administered 1 hr prior to LPS stimulation measured after 4.5 hrs
|
Cavia porcellus
|
93.0
%
|
|
|
Anti-inflammatory activity against carrageenan-induced paw edema in albino rat assessed as inhibition of paw edema at 60 mg/kg, po pretreated for 1 hr followed by carrageenan challenge measured after 1 to 7 hrs relative to control
|
Rattus norvegicus
|
84.52
%
|
|
|
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
|
100.0
nM
|
|
|
Analgesic activity in Dunkin Hartley guinea pig hyperalgesia pain model assessed as inhibition of LPS-induced thermal hyperalgesia at 10 mg/kg, po qd administered 1 hr prior to LPS stimulation measured after 4.5 hrs by plantar test relative to control
|
Cavia porcellus
|
80.0
%
|
|
|
Anti inflammatory activity in carrageenan-induced Wistar rat paw edema model assessed as inhibition of left hind paw edema size at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge measured after 2 hrs by plethysmometry method (Rvb = 0%)
|
Rattus norvegicus
|
74.6
%
|
|
|
Inhibition of ovine COX-1 preincubated for 5 mins followed by arachidonic acid substrate addition by colorimetric enzyme immunoassay
|
Ovis aries
|
150.0
nM
|
|
|
Anti inflammatory activity in carrageenan-induced Wistar rat paw edema model assessed as inhibition of left hind paw edema size at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge measured after 4 hrs by plethysmometry method (Rvb = 0%)
|
Rattus norvegicus
|
91.6
%
|
|
|
Anti inflammatory activity in carrageenan-induced Wistar rat paw edema model assessed as inhibition of left hind paw edema size at 10 mg/kg, po pretreated for 1 hr followed by carrageenan challenge measured after 6 hrs by plethysmometry method (Rvb = 0%)
|
Rattus norvegicus
|
90.9
%
|
|
|
Inhibition of human COX-2 preincubated for 5 mins followed by arachidonic acid substrate addition by colorimetric enzyme immunoassay
|
Homo sapiens
|
50.0
nM
|
|
|
Antioxidant activity assessed as DPPH free radical scavenging activity at 20 ug/ml after 15 mins by spectrophotometric method
|
None
|
97.14
%
|
|
|
Inhibition of recombinant human COX2 at 20 uM using arachidonic acid as substrate by ELISA
|
Homo sapiens
|
100.0
%
|
|
|
Anti inflammatory activity in rat assessed as inhibition of carrageenan-induced hind paw edema at 50 mg/kg measured after 1 to 4 hrs by plethysmographic method relative to control
|
Rattus norvegicus
|
86.72
%
|
|
|
Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 5 mins followed by substrate addition measured after 2 mins by enzyme immunoassay
|
Ovis aries
|
250.0
nM
|
|
|
Inhibition of ovine COX2 using arachidonic acid as substrate incubated for 5 mins followed by substrate addition measured after 2 mins by enzyme immunoassay
|
Ovis aries
|
260.0
nM
|
|
|
Anti-inflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 1 hr relative to control
|
Rattus norvegicus
|
41.0
%
|
|
|
Anti-inflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 3 hrs relative to control
|
Rattus norvegicus
|
77.0
%
|
|
|
Anti-inflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins prior to carrageenan challenge measured after 5 hrs relative to control
|
Rattus norvegicus
|
48.0
%
|
|
|
Anti-inflammatory activity in human RBC assessed as membrane stabilization
|
Homo sapiens
|
942.0
nM
|
|
|
Analgesic activity in Dunkin-Hartley guinea pig hyperalgesia pain model assessed as inhibition of LPS-induced hyperalgesia at 10 mg/kg, po administered 2 hrs prior to LPS challenge measured after 4.5 hrs relative to control
|
Cavia porcellus
|
85.0
%
|
|
|
Anti-inflammatory activity in rat acute inflammation model assessed as inhibition of formalin-induced paw edema at 5 mg/kg, po measured after 4 hrs relative to control
|
Rattus norvegicus
|
66.67
%
|
|
|
Anti-inflammatory activity in rat acute inflammation model assessed as inhibition of formalin-induced paw edema at 5 mg/kg, po measured after 4 hrs relative to celecoxib
|
Rattus norvegicus
|
208.33
%
|
|
|
Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 50 mg/kg, ip administered 1 hr before carrageenan stimulation and measured after 3 hrs relative to control
|
Rattus norvegicus
|
71.26
%
|
|
|
Inhibition of ovine COX -2 by colorimetric inhibitor screening assay kit method
|
Ovis aries
|
800.0
nM
|
|
|
Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg , po and measured after 4 hrs of carrageenan addition relative to control
|
Rattus norvegicus
|
78.57
%
|
|
|
Analgesic activity in albino mouse assessed as inhibition of acetic acid induced writhing at 10 mg/kg , po
|
Mus musculus
|
67.7
%
|
|
|
Inhibition of COX1 in human platelet rich plasma in assessed as inhibition of ADP-induced platelet aggregation at 10 uM incubated for 5 mins by turbidimetry based Born's method relative to control
|
Homo sapiens
|
15.0
%
|
|
|
Anti-inflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins before carrageenan challenge measured after 5 hrs relative to control
|
Rattus norvegicus
|
50.0
%
|
|
|
Anti-inflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins before carrageenan challenge measured after 3 hrs relative to control
|
Rattus norvegicus
|
79.0
%
|
|
|
Anti-inflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 30 mins before carrageenan challenge measured after 1 hr relative to control
|
Rattus norvegicus
|
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
|
3.36
%
|
|
|
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
|
-0.11
%
|
|
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
|
-0.11
%
|
|
|
Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 10 mins followed by substrate addition and measured after 2 mins by EIA assay
|
Ovis aries
|
70.0
nM
|
|
|
Inhibition of human COX2 using arachidonic acid as substrate incubated for 10 mins followed by substrate addition and measured after 2 mins by EIA assay
|
Homo sapiens
|
20.0
nM
|
|
|
Binding affinity to wild type TTR (unknown origin) expressed in Escherichia coli BL21/DE3 by Circular dichroism spectroscopy
|
Homo sapiens
|
60.0
nM
|
|
|
Inhibition of sheep COX1 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by UV-visible spectrophotometric method
|
Ovis aries
|
480.0
nM
|
|
|
Antiinflammatory activity in Sprague-Dawley rat chronic model of formalin-induced paw edema assessed as inhibition of rat paw edema at 7.5 mg/kg, po pre treated for 1 hr followed by formalin-stimulation and measured after 5 days by plethysmometeric method relative to control
|
Rattus norvegicus
|
72.0
%
|
|
|
Antiinflammatory activity in rat model of carrageenan-induced paw edema assessed as inhibition of hind paw swelling at 10 mg/kg, ip measured after 1 hr relative to control
|
Rattus norvegicus
|
53.9
%
|
|
|
Antiinflammatory activity in rat model of carrageenan-induced paw edema assessed as inhibition of hind paw swelling at 10 mg/kg, ip measured after 3 hrs relative to control
|
Rattus norvegicus
|
61.8
%
|
|
|
Inhibition of ovine COX-1 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by EIA
|
Ovis aries
|
70.0
nM
|
|
|
Inhibition of human COX-2 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by EIA
|
Homo sapiens
|
20.0
nM
|
|
