|
Binding affinity was determined for human glucocorticoid receptor(hGR).
|
None
|
5.5
nM
|
|
|
Compound was evaluated for IL 4 production inhibition from mice splenocytes stimulated by anti-CD3 mAb
|
Mus musculus
|
4.7
nM
|
|
|
Compound was evaluated for IL 5 production inhibitio from mice splenocytes stimulated by anti-CD3 mAb
|
Mus musculus
|
3.5
nM
|
|
|
Inhibitory activity against production of nitric oxide induced by interferon-gamma in mouse macrophages
|
Mus musculus
|
0.1
nM
|
|
|
In vivo antiinflammatory activity of 0.04 uM concentration of compound was determined by inhibition of oxazolone-induced allergic contact dermatitis (ACD) in mouse up on tropical application
|
Mus musculus
|
16.0
%
|
|
|
In vivo antiinflammatory activity of 0.4 uM concentration of compound was determined by inhibition of oxazolone-induced allergic contact dermatitis (ACD) in mouse up on tropical application
|
Mus musculus
|
41.0
%
|
|
|
In vivo antiinflammatory activity of 40 uM concentration of compound was determined by inhibition of oxazolone-induced allergic contact dermatitis (ACD) in mouse up on tropical application
|
Mus musculus
|
35.0
%
|
|
|
In vivo antiinflammatory activity of compound was determined by inhibition of oxazolone-induced allergic contact dermatitis (ACD) in mouse up on tropical application
|
Mus musculus
|
42.0
%
|
|
|
Inhibitory activity against production of nitric oxide induced by interferon gamma in mouse macrophages
|
Mus musculus
|
0.1
nM
|
|
|
Inhibitory activity against TNF-alpha release in N9 cells in the supernatant
|
Mus musculus
|
74.0
nM
|
|
|
Inhibition of P-gp was determined using rhodamine-assay in human CaCo-2 cells
|
None
|
0.0
%
|
|
|
Inhibitory concentration against TNF-alpha production from human peripheral blood mononuclear cells stimulated by LPS
|
Homo sapiens
|
10.0
nM
|
|
|
Inhibitory concentration against growth of LPS stimulated human peripheral blood mononuclear cells
|
Homo sapiens
|
40.0
nM
|
|
|
In vivo antiinflammatory activity of 130 uM concentration of compound was determined by inhibition of oxazolone-induced allergic contact dermatitis (ACD) in pig up on tropical application
|
Sus scrofa
|
35.0
%
|
|
|
In vivo antiinflammatory activity of 40 uM concentration of compound was determined by inhibition of oxazolone-induced allergic contact dermatitis (ACD) in pig up on tropical application
|
Sus scrofa
|
20.0
%
|
|
|
In vivo antiinflammatory activity of 400 uM concentration of compound was determined by inhibition of oxazolone-induced allergic contact dermatitis (ACD) in pig up on tropical application
|
Sus scrofa
|
32.0
%
|
|
|
Inhibitory activity against TNF-alpha release in RAW 264.7 cells in the supernatant
|
Mus musculus
|
420.0
nM
|
|
|
In vitro inhibition of lipopolysaccharide stimulated tumor necrosis factor-alpha production in rat whole blood
|
Rattus norvegicus
|
20.0
nM
|
|
|
Evaluated for its ability to inhibit LPS stimulated production of TNF-alpha in rat whole blood
|
Rattus norvegicus
|
20.0
nM
|
|
|
Percent inhibition value on the Sephadex-induced lung eosinophilia model at an intraperitoneal (ip) dose of 0.1 mg/kg
|
Rattus norvegicus
|
95.0
%
|
|
|
Percentage inhibition of Carrageenan-induced rat paw edema at a concentration of 0.3 mg/kg
|
Rattus norvegicus
|
69.0
%
|
|
|
Radiographic change was judged in the area of the talus joint, using an arbitrary scoring system upon termination of the test (0.5 mg/kg 1-5 days dosing,0.25 mg/kg 6-15 days dosing)in a model of type II collagen arthritis in the rat.
|
Rattus norvegicus
|
95.0
%
|
|
Radiographic change was judged in the area of the talus joint, using an arbitrary scoring system upon termination of the test (0.5 mg/kg 1-5 days dosing,0.25 mg/kg 6-15 days dosing)in a model of type II collagen arthritis in the rat.
|
Rattus norvegicus
|
98.0
%
|
|
|
Tested for sephadex-induced lung Eosinophilia inhibition at 30 mg/kg in rat
|
Rattus norvegicus
|
95.0
%
|
|
|
Inhibitory concentration against T cell proliferation using concanavalin A stimulated mice spleen cells
|
Mus musculus
|
5.0
nM
|
|
|
Tested in vivo for inhibition of serum tumor necrosis factor alpha production in rats at 100 ug/kg subcutaneous dose
|
Rattus norvegicus
|
99.0
%
|
|
|
Compound was evaluated for inhibitory activity against production of nitric oxide (NO) induced by interferon-gamma (IFN-gamma) in mouse macrophages
|
Mus musculus
|
0.3
nM
|
|
|
Inhibition of nitric oxide (NO) production induced by interferon-gamma (IFN-gamma) in mouse macrophages
|
Mus musculus
|
0.1
nM
|
|
|
Inhibition of monocyte accumulation (DNA content) in a rat pleural exudate model of inflammation at 45 ug administered perorally
|
Rattus norvegicus
|
71.0
%
|
|
|
Inhibition of monocyte accumulation (exudate volume) in a rat pleural exudate model of inflammation at 45 ug administered perorally
|
Rattus norvegicus
|
80.0
%
|
|
|
Binding affinity for glucocorticoid receptor
|
None
|
7.943
nM
|
|
|
inhibition of acute TPA-induced ear swelling in mice on oral administration of 0.1 nmol/kg
|
Mus musculus
|
82.0
%
|
|
|
Percent inhibition of acute TPA-induced ear swelling in mice upon topical application at 2x 100 ug
|
Mus musculus
|
96.0
%
|
|
|
Effective agonist concentration for transcriptional repression of IL-6 production in IL-1 stimulated human foreskin fibroblasts
|
Homo sapiens
|
1.0
nM
|
|
|
Inhibition of fluorescent-labeled Dexamethasone binding to GR
|
Homo sapiens
|
7.943
nM
|
|
|
Agonist activity at GR assessed as NF-kappaB-mediated transrepression of secreted placental alkaline phosphatase gene in human A549 cells
|
Homo sapiens
|
1.175
nM
|
|
|
Agonist activity at GR assessed as MMTV-mediated transactivation of renilla luciferase gene in human A549 cells relative to Dexamethasone
|
Homo sapiens
|
5.012
nM
|
|
|
Inhibition of tetramethylrhodamine labeled dexamethasone binding to GR by FP assay
|
None
|
3.0
nM
|
|
|
Inhibition of tetramethylrhodamine labeled dexamethasone binding to MR by FP assay
|
None
|
33.0
nM
|
|
|
Inhibition of IL1-stimulated IL6 production in HFF cells
|
Homo sapiens
|
0.51
nM
|
|
|
Induction of aromatase activity in HFF cells assessed as production of beta estradiol by aromatase assay
|
Homo sapiens
|
1.9
nM
|
|
|
Activation of MMTV in HeLa cells measured by luciferase activity
|
Homo sapiens
|
17.0
nM
|
|
|
Inhibition of interferon gamma-stimulated NO production in RAW 264.7 cells after 24 hrs
|
Mus musculus
|
20.0
nM
|
|
|
Inhibition of peritoneal cell count in zymosan-induced Swiss mouse peritoneal fluid at 1 mg/kg, po
|
Mus musculus
|
36.0
%
|
|
|
Inhibition of peritoneal granulocyte count in zymosan-induced Swiss mouse peritoneal fluid at 1 mg/kg, po
|
Mus musculus
|
62.0
%
|
|
|
Inhibition of monocyte count in zymosan-induced Swiss mouse peritoneal fluid at 1 mg/kg, po
|
Mus musculus
|
14.0
%
|
|
|
Inhibition of lymphocyte count in zymosan-induced Swiss mouse peritoneal fluid at 1 mg/kg, po
|
Mus musculus
|
44.0
%
|
|
|
Inhibition of granulocyte count in zymosan-induced Swiss mouse peritoneal fluid at 1 mg/kg, po
|
Mus musculus
|
42.0
%
|
|
|
Inhibition of human GR
|
Homo sapiens
|
3.4
nM
|
|
|
Inhibition of human MR
|
Homo sapiens
|
33.0
nM
|
|
|
Agonist activity at human GR expressed in CV1 cells by GRE activation assay
|
Homo sapiens
|
0.2
nM
|
|
|
Activity at human GR expressed in NHDFneo cells assessed as inhibition of IL-6 production
|
Homo sapiens
|
1.4
nM
|
|
|
Antiproliferative activity against human RPMI8226 cells after 4 days
|
Homo sapiens
|
6.5
nM
|
|
|
Binding affinity to GR
|
None
|
2.1
nM
|
|
|
Binding affinity to MR
|
None
|
7.2
nM
|
|
|
Binding affinity to glucocorticoid receptor
|
None
|
7.586
nM
|
|
|
Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay
|
Homo sapiens
|
1.0
nM
|
|
|
Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay
|
Homo sapiens
|
5.37
nM
|
|
|
Antagonist activity at glucocorticoid receptor in human A549 cells transfected with MMTV luciferase reporter gene assessed as inhibition of dexamethasone-induced activation
|
Homo sapiens
|
7.0
%
|
|
|
Displacement of TAMRA labeled Dexamethasone at human glucocorticoid receptor in insect cell
|
Homo sapiens
|
3.0
nM
|
|
|
Displacement of TAMRA labeled mifepristone at human mineralocorticoid receptor in insect cell
|
Homo sapiens
|
33.0
nM
|
|
|
Antiinflammatory activity assessed as inhibition of IL1 stimulated IL6 production in HFF cells by transrepression assay
|
Homo sapiens
|
0.5
nM
|
|
|
Antiinflammatory activity assessed as upregulation of aromatase in HFF cells by transactivation assay
|
Homo sapiens
|
2.0
nM
|
|
|
Inhibition of LPS-induced TNFalpha production in mouse J774A.1 cells
|
Mus musculus
|
48.0
nM
|
|
|
Displacement of fluorescent labeled Dexamethasone from glucocorticoid receptor
|
None
|
7.943
nM
|
|
|
Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay
|
Homo sapiens
|
1.175
nM
|
|
|
Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay
|
Homo sapiens
|
5.012
nM
|
|
|
Antiinflammatory activity in Swiss mouse assessed as inhibition of ethylphenylpropiolate-induced ear edema at 0.5 mg/ear administered tropically 16 hrs prior to ethylphenylpropiolate challenge
|
Mus musculus
|
82.0
%
|
|
|
Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as effect on TNFalpha formation pretreated 1 hr before LPS challenge measured after 24 hrs
|
Mus musculus
|
700.0
nM
|
|
|
Displacement of radiolabeled Dexamethasone from human glucocorticoid receptor
|
Homo sapiens
|
3.0
nM
|
|
Displacement of radiolabeled Dexamethasone from human glucocorticoid receptor
|
Homo sapiens
|
6.0
nM
|
|
|
Antiinflammatory activity in mouse ear edema model assessed as inhibition of PMA-induced ear edema at 1 mg/ear administered 2 times 30 mins before and 15 mins after PMA challenge measured after 6 hrs of PMA application relative to control
|
Mus musculus
|
72.0
%
|
|
|
Displacement of FITC-dexamethasone from human recombinant glucocorticoid receptor alpha by fluorescence polarization assay
|
Homo sapiens
|
1.1
nM
|
|
|
Transrepression activity at GR in PMA-stimulated human A549 cells assessed as inhibition of AP1 response element-induced luciferase reporter gene activity
|
Homo sapiens
|
2.5
nM
|
|
|
Transrepression activity at GR in IL-1-beta-stimulated human A549 cells assessed as inhibition of NF-kappaB-dependent E-selectin transcription by luciferase reporter gene assay
|
Homo sapiens
|
1.1
nM
|
|
|
Agonist activity at GR ligand binding domain expressed in human NP1 cells assessed as glucocorticoid response element transactivation by GAL4 luciferase reporter gene assay
|
None
|
4.2
nM
|
|
|
Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of TNFalpha formation at 10 uM pretreated 1 hr before LPS challenge measured after 24 hrs by enzyme immunoassay
|
Mus musculus
|
49.9
%
|
|
|
Antiinflammatory activity in LPS/IFN-gamma-stimulated mouse N9 cells assessed as inhibition of TNFalpha formation at 10 uM pretreated 1 hr before LPS/IFNgamma challenge measured after 24 hrs by enzyme immunoassay
|
Mus musculus
|
82.0
%
|
|
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha by ELISA
|
Homo sapiens
|
50.0
nM
|
|
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL6 by ELISA
|
Homo sapiens
|
7.0
nM
|
|
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha at 1 uM by ELISA
|
Homo sapiens
|
72.0
%
|
|
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL6 at 1 uM by ELISA
|
Homo sapiens
|
94.0
%
|
|
|
Cytotoxicity against human THP1 cells at 1 uM
|
Homo sapiens
|
0.0
%
|
|
|
Antiinflammatory activity in sc dosed mouse assessed as inhibition of LPS-induced TNFalpha upregulation measured 2 hrs after LPS challenge relative to control
|
Mus musculus
|
90.0
%
|
|
|
Antiinflammatory activity in mouse assessed as inhibition of LPS-induced TNFalpha upregulation at 300 pg, sc measured 2 hrs after LPS challenge
|
Mus musculus
|
24.0
%
|
|
|
Antiinflammatory activity in mouse assessed as inhibition of LPS-induced TNFalpha upregulation at 0.003 ug, sc measured 2 hrs after LPS challenge
|
Mus musculus
|
31.0
%
|
|
|
Antiinflammatory activity in mouse assessed as inhibition of LPS-induced TNFalpha upregulation at 0.03 ug, sc measured 2 hrs after LPS challenge
|
Mus musculus
|
33.0
%
|
|
|
Antiinflammatory activity in mouse assessed as inhibition of LPS-induced TNFalpha upregulation at 0.3 ug, sc measured 2 hrs after LPS challenge
|
Mus musculus
|
69.0
%
|
|
|
Antiinflammatory activity in mouse assessed as inhibition of LPS-induced TNFalpha upregulation at 0.003 mg, sc measured 2 hrs after LPS challenge
|
Mus musculus
|
75.0
%
|
|
|
Antiinflammatory activity in mouse assessed as inhibition of LPS-induced TNFalpha upregulation at 0.015 mg, sc measured 2 hrs after LPS challenge
|
Mus musculus
|
84.0
%
|
|
|
Antiinflammatory activity in mouse assessed as inhibition of LPS-induced TNFalpha upregulation at 0.03 mg, sc measured 2 hrs after LPS challenge
|
Mus musculus
|
90.0
%
|
|
|
Antiinflammatory activity in mouse assessed as inhibition of LPS-induced TNFalpha upregulation at 0.06 mg, sc measured 2 hrs after LPS challenge
|
Mus musculus
|
87.0
%
|
|
|
Antiinflammatory activity in mouse assessed as inhibition of LPS-induced TNFalpha upregulation at 0.12 mg, sc measured 2 hrs after LPS challenge
|
Mus musculus
|
88.0
%
|
|
|
Activity at glucocorticoid receptor in human A549 cells assessed as effect on GRE promoter response by luciferase reporter assay
|
Homo sapiens
|
1.0
nM
|
|
|
Antiinflammatory activity against Swiss mouse chronic dermatitis model assessed as inhibition of TPA-induced edema at 0.5 mg/ear applied twice daily for 4 days measured after 6 hrs
|
Mus musculus
|
92.0
%
|
|
|
Antiinflammatory activity against Swiss mouse chronic dermatitis model assessed as inhibition of TPA-induced tissue myeloperoxidase activity at 0.5 mg/ear applied twice daily for 4 days measured after 6 hrs
|
Mus musculus
|
92.0
%
|
|
|
Cytotoxicity against mouse RAW264.7 cells after 2 days by MTT assay
|
Mus musculus
|
25.0
ug.mL-1
|
|
|
Inhibition of iNOS production in LPS-activated mouse RAW264.7 cells after 20 hrs
|
Mus musculus
|
36.0
ug.mL-1
|
|
|
Inhibition of glucocorticoid receptor-glucocorticoid complex transfected in rat R1 cells assessed as down-regulation of TPA-responsive element proinflammatory gene expression at 10 uM after 24 hrs by beta-galactosidase assay
|
None
|
5.0
nM
|
|
|
Inhibition of glucocorticoid receptor
|
None
|
5.0
nM
|
|
|
Inhibition of pro-inflammatory cytokine IL5 production in ovalbumin-stimulated BALB/c mouse TH2 cells after 48 hrs by sandwich-ELISA
|
Mus musculus
|
5.0
nM
|
|
|
Inhibition of pro-inflammatory cytokine IL13 production in ovalbumin-stimulated BALB/c mouse TH2 cells after 48 hrs by sandwich-ELISA
|
Mus musculus
|
5.0
nM
|
|
|
Displacement of fluormone from human recombinant glucocorticoid receptor ligand binding domain by fluorescence polarization assay
|
Homo sapiens
|
5.0
nM
|
|
|
Agonist activity at GR in human A549 cells by NF-kappaB transrepression assay
|
Homo sapiens
|
1.0
nM
|
|
|
Displacement of GS-red from human glucocorticoid receptor by fluorescent polarization assay
|
Homo sapiens
|
1.2
nM
|
|
|
Transrepression activity at glucocorticoid receptor expressed in human A549 cells assessed as inhibition of PMA-induced AP1 activity after 6 hrs by luciferase reporter gene assay
|
None
|
2.5
nM
|
|
|
Transrepression activity at glucocorticoid receptor expressed in human A549 cells assessed as inhibition of IL-1-beta-induced NF-kappaB dependent E-selection promoter activation after 6 hrs by luciferase reporter gene based ELAM assay
|
None
|
1.1
nM
|
|
|
Transactivation of GAL-4 tagged glucocorticoid receptor ligand binding domain expressed in human HeLa cells assessed as NP1 activation by luciferase reporter gene assay
|
None
|
4.5
nM
|
|
|
Antagonist activity at mineralocorticoid receptor at 10 uM by antagonist mode functional assay
|
None
|
30.0
%
|
|
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha release at 1 uM/mL after 24 hrs by ELISA
|
Homo sapiens
|
69.0
%
|
|
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL6 release at 1 uM/mL after 24 hrs by ELISA
|
Homo sapiens
|
90.0
%
|
|
|
Cytotoxicity against human THP1 cells assessed as CCK8 release at 1 uM/mL after 24 hrs by ELISA
|
Homo sapiens
|
0.0
%
|
|
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha release at 1 uM by ELISA
|
Homo sapiens
|
89.0
%
|
|
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha release at 1 uM preincubated for 30 mins before LPS challenge by ELISA
|
Homo sapiens
|
73.0
%
|
|
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL6 release at 1 uM preincubated for 30 mins before LPS challenge by ELISA
|
Homo sapiens
|
84.0
%
|
|
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha release at 1 uM after 24 hrs by ELISA
|
Homo sapiens
|
73.0
%
|
|
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL6 release at 1 uM after 24 hrs by ELISA
|
Homo sapiens
|
84.0
%
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of 10 ng/ml LPS-induced TNFalpha release at 1.3 uM pretreated 24 hrs before inducer-challenge measured 24 hrs after LPS addition by ELISA
|
Homo sapiens
|
32.0
%
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of 10 ng/ml LPS-induced TNFalpha release at 5.1 uM pretreated 24 hrs before inducer-challenge measured 24 hrs after LPS addition by ELISA
|
Homo sapiens
|
25.0
%
|
|
|
Agonist activity at glucocorticoid receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay
|
None
|
7.2
nM
|
|
|
Displacement of fluoromone from human glucocorticoid receptor LBD assessed as reduction of maximum polarization by fluorescence polarization assay relative to control
|
Homo sapiens
|
11.4
nM
|
|
|
Displacement of [3H]DEX from human glucocorticoid receptor
|
Homo sapiens
|
1.1
nM
|
|
|
Antiinflammatory activity in mouse assessed as inhibition of phorbol ester-induced ear edema at 1 mg/ear
|
Mus musculus
|
68.0
%
|
|
|
Binding affinity to glucocorticoid receptor
|
None
|
19.0
nM
|
|
|
Antiinflammatory activity in human primary synovial fibroblasts assessed as inhibition of IL1-induced IL6 release after 18 hrs by MSD technology
|
Homo sapiens
|
0.631
nM
|
|
|
Antiinflammatory activity in human primary synovial fibroblasts assessed as inhibition of IL1-induced IL8 release after 18 hrs by MSD technology
|
Homo sapiens
|
0.5012
nM
|
|
|
Antiinflammatory activity in human primary synovial fibroblasts assessed as inhibition of IL1-induced MMP1 release after 18 hrs by MSD technology
|
Homo sapiens
|
0.3162
nM
|
|
|
Inhibition of IL1-induced circulating IL6 release in mouse at 10 mg/kg, po
|
Mus musculus
|
83.0
%
|
|
|
Inhibition of IL1-induced circulating IL6 release in mouse at 1 mg/kg, po
|
Mus musculus
|
88.0
%
|
|
|
Inhibition of IL1-induced circulating IL6 release in mouse at 0.1 mg/kg, po
|
Mus musculus
|
67.0
%
|
|
|
Inhibition of IL1-induced circulating IL6 release in mouse at 0.01 mg/kg, po
|
Mus musculus
|
24.0
%
|
|
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha secretion at 10 uM treated 30 mins before LPS challenge measured after 24 hrs by ELISA relative to control
|
Homo sapiens
|
69.0
%
|
|
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL-6 secretion at 10 uM treated 30 mins before LPS challenge measured after 24 hrs by ELISA relative to control
|
Homo sapiens
|
90.0
%
|
|
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha production at 1 uM treated 30 mins before LPS challenge measured after 24 hrs by ELISA relative to control
|
Homo sapiens
|
69.0
%
|
|
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL-6 production at 1 uM treated 30 mins before LPS challenge measured after 24 hrs by ELISA relative to control
|
Homo sapiens
|
90.0
%
|
|
|
Binding affinity to glucocorticoid receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled Dexamethasone by fluorescence polarization microplate assay
|
None
|
3.4
nM
|
|
|
Binding affinity to mineralocorticoid receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled Dexamethasone by fluorescence polarization microplate assay
|
None
|
33.0
nM
|
|
|
Transrepression activity at glucocorticoid receptor in HFF assessed as inhibition of IL-1-induced IL-6 production after 18 to 24 hrs by ELISA
|
Homo sapiens
|
0.51
nM
|
|
|
Binding affinity to human recombinant glucocorticoid receptor expressed in baculovirus infected Sf9 cells
|
Homo sapiens
|
12.59
nM
|
|
|
Transrepression activity at glucocorticoid receptor-mediated antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL-8 production
|
Homo sapiens
|
2.512
nM
|
|
|
Transrepression activity at glucocorticoid receptor-mediated antiinflammatory activity in human HeLa cells assessed as inhibition of TPA-induced collagenase promoter activity by luciferase reporter gene assay
|
Homo sapiens
|
1.585
nM
|
|
|
Transactivation activity at glucocorticoid receptor in human HeLa cells assessed as induction of MMTV promoter activity by luciferase reporter gene assay
|
Homo sapiens
|
7.943
nM
|
|
|
Antagonist activity at glucocorticoid receptor-LBD in human U2OS cells transfected with Gal4-DBD assessed as inhibition of transactivation activity after 18 hrs by luciferase reporter gene assay
|
Homo sapiens
|
0.5082
nM
|
|
|
Inhibition of human glucocorticoid receptor
|
Homo sapiens
|
5.0
nM
|
|
|
Displacement of fluorescent-labelled Dexamethasone from glucocorticoid receptor
|
None
|
12.59
nM
|
|
|
Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay
|
Homo sapiens
|
1.0
nM
|
|
|
Agonist activity at GR in human A549 cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity
|
Homo sapiens
|
3.981
nM
|
|
|
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production treated 2 hrs before LPS challenge measured after 18 hrs by griess reaction
|
Mus musculus
|
860.0
nM
|
|
|
Displacement of [3H]dexamethasone from Sprague-Dawley rat GR by liquid scintillation counting
|
Rattus norvegicus
|
22.0
nM
|
|
|
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess method
|
Mus musculus
|
800.0
nM
|
|
|
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha secretion after 18 hrs
|
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
|
20.0
nM
|
|
|
Antiinflammatory activity in rat Polymorphonuclear leukocyte assessed as inhibition of LPS-induced nitric oxide production at 5 uM
|
Rattus norvegicus
|
74.7
%
|
|
|
Inhibition of LPS-induced nitric oxide production in C57BL/6J mouse peritoneal macrophages at 10 uM after 24 hrs by Griess reaction
|
Mus musculus
|
61.6
%
|
|
|
Displacement of GS-red from GRapha by fluorescence polarization assay
|
None
|
1.1
nM
|
|
|
Transrepression activity of glucocorticoid receptor in human A549 cells expressing AP-1 assessed as inhibition of PMA-induced AP-1 activity by luciferase reporter gene assay
|
Homo sapiens
|
2.5
nM
|
|
|
Transactivation activity of glucocorticoid receptor ligand binding domain expressed in human NP-1 Hela cells co-expressing GAL4 DNA binding domain by luciferase reporter gene assay
|
Homo sapiens
|
4.2
nM
|
|
|
Transrepression activity of glucocorticoid receptor in human A549 cells assessed as inhibition of IL1beta-stimulated NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay
|
Homo sapiens
|
1.1
nM
|
|
|
Transactivation activity at glucocorticoid receptor in human 13D3/Huh7 cells assessed as induction of tyrosine aminotransferase activity after 24 hrs
|
Homo sapiens
|
5.0
nM
|
|
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha production at 1 uM treated 30 mins before LPS challenge measured after 24 hrs by ELISA
|
Homo sapiens
|
71.0
%
|
|
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL6 production at 1 uM treated 30 mins before LPS challenge measured after 24 hrs by ELISA
|
Homo sapiens
|
84.0
%
|
|
|
Antiinflammatory activity in knockout-transgenic sickle cell mouse monocytes assessed as inhibition of LPS-induced TNFalpha production at 1 uM administered 30 mins before LPS challenge measured after 24 hrs by ELISA
|
Mus musculus
|
83.0
%
|
|
|
DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
|
None
|
8.06
nM
|
|
DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
|
None
|
3.664
nM
|
|
|
Displacement of tetramethylrhodamine-labeled Dexamethasone from human recombinant glucocorticoid receptor expressed in baculovirus infected insect cells by fluorescence polarization assay
|
Homo sapiens
|
3.0
nM
|
|
|
Displacement of tetramethylrhodamine-labeled Dexamethasone from human recombinant mineralocorticoid receptor expressed in baculovirus infected insect cells by fluorescence polarization assay
|
Homo sapiens
|
33.0
nM
|
|
|
Agonist activity at glucocorticoid receptor in HFF assessed as inhibition of IL1-induced IL-6 production after 18 to 24 hrs
|
Homo sapiens
|
0.51
nM
|
|
|
Transactivation activity of glucocorticoid receptor in HFF assessed as induction of aromatase activity by measuring beta-estradiol activity after 18 to 24 hrs by ELISA
|
Homo sapiens
|
1.8
nM
|
|
|
Agonist activity at glucocorticoid receptor in human HeLa cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity
|
Homo sapiens
|
17.0
nM
|
|
|
Displacement of [3H]Dex from glucocorticoid receptor in Sprague-Dawley rat liver after 2 hrs by liquid scintillation counting
|
Rattus norvegicus
|
22.0
nM
|
|
|
Antiinflammatory activity in human whole blood assessed as inhibition of LPS-induced TNFalpha production after overnight incubation by ELISA
|
Homo sapiens
|
6.9
nM
|
|
|
Antiinflammatory activity in human whole blood assessed as inhibition of IL-1beta-induced IL-8 production after overnight incubation by ELISA
|
Homo sapiens
|
5.1
nM
|
|
|
Antiinflammatory activity in BALB/c mouse model assessed as inhibition of ovalbumin-induced eosinophil accumulation in bronchoalveolar lavage fluid at 1 mg/kg, ip administered 1 hr prior to and 7 hrs after ovalbumin challenge for 3 days measured 8 hrs after final dose by cell counting
|
Mus musculus
|
90.0
%
|
|
|
Antihypersensitivity against TNCB-induced contact hypersensitivity in BALB/c mouse ear assessed as inhibition of edema at 0.025 mg/ear applied tropically after 30 mins, 24 hrs and 48 hrs of TNCB challenge measured after 24 hrs relative to control
|
Mus musculus
|
78.0
%
|
|
|
Antihypersensitivity against TNCB-induced contact hypersensitivity in BALB/c mouse ear assessed as inhibition of edema at 0.025 mg/ear applied tropically after 30 mins, 24 hrs and 48 hrs of TNCB challenge measured after 72 hrs relative to control
|
Mus musculus
|
83.0
%
|
|
|
Antihypersensitivity activity against TNCB-induced acute contact hypersensitivity in BALB/c mouse ear assessed as inhibition of neutrophil infiltration by measuring MPO activity at 0.025 mg/ear measured after 24 to 72 hrs relative to control
|
Mus musculus
|
65.0
%
|
|
|
Antihypersensitivity activity against TNCB-induced acute contact hypersensitivity in BALB/c mouse ear assessed as inhibition of neutrophil infiltration by measuring MPO activity at 0.025 mg/ear measured after 22 days of repeated application of TNCB relative to control
|
Mus musculus
|
78.0
%
|
|
|
Antihypersensitivity activity against TNCB-induced contact hypersensitivity in BALB/c mouse ear assessed as decrease cytokines levels at 0.025 mg/ear measured at 24 hrs by ELISA relative to control
|
Mus musculus
|
50.0
%
|
|
|
Antihypersensitivity activity against TNCB-induced contact hypersensitivity in BALB/c mouse ear assessed as decreased COX2 expression at 0.025 mg/ear after at 24 hrs by Western blotting relative to control
|
Mus musculus
|
48.0
%
|
|
|
Antihypersensitivity activity against TNCB-induced contact hypersensitivity in BALB/c mouse ear assessed as decreased COX2 expression at 0.025 mg/ear after at 72 hrs by Western blotting relative to control
|
Mus musculus
|
43.0
%
|
|
|
Antihypersensitivity activity against TNCB-induced contact hypersensitivity in BALB/c mouse ear assessed as inhibition of MMP9 production at 0.025 mg/ear measured at 24 hrs by Western blot analysis relative to control
|
Mus musculus
|
81.0
%
|
|
|
Antihypersensitivity activity against TNCB-induced contact hypersensitivity in BALB/c mouse ear assessed as inhibition of MMP9 production at 0.025 mg/ear measured at 72 hrs by Western blot analysis relative to control
|
Mus musculus
|
69.0
%
|
|
|
Antiinflammatory activity in human PMA-stimulated THP1 cells assessed as inhibition of LPS-induced TNFalpha production at 1 uM treated 30 mins before LPS challenge measured after 24 hrs by ELISA
|
Homo sapiens
|
72.0
%
|
|
|
Antiinflammatory activity in human PMA-stimulated THP1 cells assessed as inhibition of LPS-induced IL-6 production at 1 uM treated 30 mins before LPS challenge measured after 24 hrs by ELISA
|
Homo sapiens
|
86.0
%
|
|
|
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production pretreated for 2 hrs before LPS challenge measured after 18 hrs by Griess method
|
Mus musculus
|
980.0
nM
|
|
|
Antiarthritic activity in B10/R3 mouse immunized with bovine type2 collagen in Freund's complete adjuvant assessed as inhibition of increase in clinical arthritic scores at 0.1 mg/kg, po administered bid for 10 days measured for 10 days
|
Mus musculus
|
63.0
%
|
|
|
Antiinflammatory activity in rat polymorphonuclear leukocytes assessed as inhibition of LPS-stimulated nitric oxide production after 20 mins by Griess method
|
Rattus norvegicus
|
2.3
nM
|
|
|
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated nitric oxide production pretreated for 2 hrs before LPS challenge measured after 18 hrs by Griess method
|
Mus musculus
|
470.0
nM
|
|
|
Antiinflammatory activity in ovalbumin-sensitised Balb/c mouse assessed as reduction in ovalbumin-induced eosinophil count in bronchoalveolar lavage fluid at 1 mg/kg, ip administered 1 hr before and 7 hrs after ovalbumin challenge measured after 8 hrs by haemocytometeric analysis
|
Mus musculus
|
83.0
%
|
|
|
TP_TRANSPORTER: inhibition of DHEAS uptake (DHEAS: 5 uM, Dexamethasone: 100 uM) in Xenopus laevis oocytes
|
Xenopus laevis
|
97.3
%
|
|
|
Antiinflammatory activity in human PMA-activated THP1 cells assessed as inhibition of LPS-induced TNFalpha production at 1 uM incubated for 30 mins prior to LPS-challenge measured after 24 hrs by ELISA relative to control
|
Homo sapiens
|
71.0
%
|
|
|
Antiinflammatory activity in human PMA-activated THP1 cells assessed as inhibition of LPS-induced IL6 production at 1 uM incubated for 30 mins prior to LPS-challenge measured after 24 hrs by ELISA relative to control
|
Homo sapiens
|
84.0
%
|
|
|
Antiarthritic activity in BALB/c mouse type 2 collagen antibody-induced arthritis model assessed as inhibition of disease burden at 3 mg/kg, po qd for 14 days measured on day 20 relative to control
|
Mus musculus
|
102.0
%
|
|
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-stimulated TNFalpha production at 1 uM incubated for 30 mins prior to LPS-challenge measured 24 hrs post LPS-challenge by ELISA
|
Homo sapiens
|
76.0
%
|
|
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-stimulated IL-6 production at 1 uM incubated for 30 mins prior to LPS-challenge measured 24 hrs post LPS-challenge by ELISA
|
Homo sapiens
|
84.0
%
|
|
|
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
|
10.7
%
|
|
|
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
|
34.2
%
|
|
|
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
|
-12.5
%
|
|
|
Anti-inflammatory activity in Homo sapiens (human) PMA-stimulated THP1 cells assessed as inhibition of LPS-induced IL6 production at 1 uM incubated for 30 min prior to LPS-challenge measured after 24 hr by ELISA
|
Homo sapiens
|
94.0
%
|
|
|
Anti-inflammatory activity in Homo sapiens (human) PMA-stimulated THP1 cells assessed as inhibition of LPS-induced TNFalpha production at 1 uM incubated for 30 min prior to LPS-challenge measured after 24 hr by ELISA
|
Homo sapiens
|
72.0
%
|
|
|
Anti-inflammatory activity in Homo sapiens (human) THP1 cells assessed as inhibition of LPS-induced IL6 production at 1 uM incubated for 30 min prior to LPS-challenge measured after 24 hr by ELISA
|
Homo sapiens
|
94.0
%
|
|
|
Anti-inflammatory activity in Homo sapiens (human) THP1 cells assessed as inhibition of LPS-induced TNFalpha production at 1 uM incubated for 30 min prior to LPS-challenge measured after 24 hr by ELISA
|
Homo sapiens
|
72.0
%
|
|
|
Anti-inflammatory activity in fasted Rattus norvegicus Wistar (rat) assessed as inhibition of carrageenan-induced paw edema at 1 mg/kg, ip administered 1 hr prior to carrageenan challenge measured at 5 hr relative to control
|
Rattus norvegicus
|
40.0
%
|
|
|
Anti-inflammatory activity in fasted Rattus norvegicus Wistar (rat) assessed as inhibition of carrageenan-induced paw edema at 1 mg/kg, ip administered 1 hr prior to carrageenan challenge measured at 3 hr relative to control
|
Rattus norvegicus
|
30.0
%
|
|
|
Anti-inflammatory activity in fasted Rattus norvegicus Wistar (rat) assessed as inhibition of carrageenan-induced paw edema at 1 mg/kg, ip administered 1 hr prior to carrageenan challenge measured at 1 hr relative to control
|
Rattus norvegicus
|
23.0
%
|
|
|
Anti-inflammatory activity in Homo sapiens (human) THP1 cells assessed as inhibition of LPS-induced IL-6 production preincubated at 1 uM for 30 min before LPS treatment measured after 24 hr by ELISA
|
Homo sapiens
|
84.0
%
|
|
|
Anti-inflammatory activity in Homo sapiens (human) THP1 cells assessed as inhibition of LPS-induced TNF-alpha production preincubated at 1 uM for 30 min before LPS treatment measured after 24 hr by ELISA
|
Homo sapiens
|
71.0
%
|
|
|
Anti-inflammatory activity in Homo sapiens (human) THP1 cells assessed as inhibition of LPS-induced IL6 production at 1 uM incubated for 30 min prior to LPS-challenge measured after 24 hr by ELISA
|
Homo sapiens
|
80.0
%
|
|
|
Anti-inflammatory activity in Homo sapiens (human) THP1 cells assessed as inhibition of LPS-induced TNFalpha production at 1 uM incubated for 30 min prior to LPS-challenge measured after 24 hr by ELISA
|
Homo sapiens
|
71.0
%
|
|
|
Anti-inflammatory activity in Homo sapiens (human) THP1 cells assessed as inhibition of LPS-induced IL6 production at 1 uM incubated for 30 min prior to LPS-challenge measured after 24 hr by ELISA relative to control
|
Homo sapiens
|
86.0
%
|
|
|
Anti-inflammatory activity in Homo sapiens (human) THP1 cells assessed as inhibition of LPS-induced TNFalpha production at 1 uM incubated for 30 min prior to LPS-challenge measured after 24 hr by ELISA relative to control
|
Homo sapiens
|
72.0
%
|
|
|
Anti-inflammatory activity in Wistar Rattus norvegicus (rat) assessed as inhibition of carrageenan-induced paw edema at 1 mg/kg, ip administered 30 min prior to carrageenan-challenge measured at 6 hr by plethysmometric analysis relative to control
|
Rattus norvegicus
|
89.0
%
|
|
|
Anti-inflammatory activity in Wistar Rattus norvegicus (rat) assessed as inhibition of carrageenan-induced paw edema at 1 mg/kg, ip administered 30 min prior to carrageenan-challenge measured at 5 hr by plethysmometric analysis relative to control
|
Rattus norvegicus
|
87.0
%
|
|
|
Anti-inflammatory activity in Wistar Rattus norvegicus (rat) assessed as inhibition of carrageenan-induced paw edema at 1 mg/kg, ip administered 30 min prior to carrageenan-challenge measured at 4 hr by plethysmometric analysis relative to control
|
Rattus norvegicus
|
71.0
%
|
|
|
Anti-inflammatory activity in Wistar Rattus norvegicus (rat) assessed as inhibition of carrageenan-induced paw edema at 1 mg/kg, ip administered 30 min prior to carrageenan-challenge measured at 3 hr by plethysmometric analysis relative to control
|
Rattus norvegicus
|
45.0
%
|
|
|
Anti-inflammatory activity in Wistar Rattus norvegicus (rat) assessed as inhibition of carrageenan-induced paw edema at 1 mg/kg, ip administered 30 min prior to carrageenan-challenge measured at 2 hr by plethysmometric analysis relative to control
|
Rattus norvegicus
|
33.0
%
|
|
|
Anti-inflammatory activity in Wistar Rattus norvegicus (rat) assessed as inhibition of carrageenan-induced paw edema at 1 mg/kg, ip administered 30 min prior to carrageenan-challenge measured at 1 hr by plethysmometric analysis relative to control
|
Rattus norvegicus
|
29.0
%
|
|
|
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells at 20 uM after 1.5 mins by fluorescence assay
|
Homo sapiens
|
30.0
%
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of PHA-induced IL-5 production after 48 hrs
|
Homo sapiens
|
1.0
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of PHA-induced IL-10 production after 48 hrs
|
Homo sapiens
|
5.5
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of PHA-induced IL-3 production after 48 hrs
|
Homo sapiens
|
3.5
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of PHA-induced IL-2 production after 48 hrs
|
Homo sapiens
|
3.6
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of PHA-induced MCP-1 production after 24 hrs
|
Homo sapiens
|
200.0
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of PHA-induced IL-13 production after 24 hrs
|
Homo sapiens
|
1.2
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of PHA-induced IP-10 production after 24 hrs
|
Homo sapiens
|
2.4
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of PHA-induced IL-4 production after 24 hrs
|
Homo sapiens
|
0.92
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of PHA-induced IFNgamma production after 24 hrs
|
Homo sapiens
|
7.6
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of PHA-induced MIP1alpha production after 6 hrs
|
Homo sapiens
|
130.0
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of PHA-induced IL-8 production after 6 hrs
|
Homo sapiens
|
88.0
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of PHA-induced IL-6 production after 6 hrs
|
Homo sapiens
|
82.0
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of PHA-induced TNFalpha production after 6 hrs
|
Homo sapiens
|
6.1
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of PHA-induced IL-1beta production after 6 hrs
|
Homo sapiens
|
9.4
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of anti-CD3-induced GM-CSF production after 48 hrs
|
Homo sapiens
|
0.47
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of anti-CD3-induced IL-12p70 production after 48 hrs
|
Homo sapiens
|
4.1
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of anti-CD3-induced IL-1beta production after 48 hrs
|
Homo sapiens
|
2.1
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of anti-CD3-induced TNFalpha production after 48 hrs
|
Homo sapiens
|
1.9
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced MIP1alpha production after 6 hrs
|
Homo sapiens
|
66.0
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-8 production after 6 hrs
|
Homo sapiens
|
72.0
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha production after 6 hrs
|
Homo sapiens
|
10.0
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-6 production after 6 hrs
|
Homo sapiens
|
55.0
nM
|
|
|
Inhibition of glucocorticoid receptor in human H13 cells assessed as inhibition of glucocorticoid-induced cell proliferation after 3 hrs by [3H]-thymidine incorporation assay
|
Homo sapiens
|
9.7
nM
|
|
|
Displacement of [3H]-dexamethasone human glucocorticoid receptor alpha expressed in 293 MSR cells after 60 mins by scintillation counting
|
Homo sapiens
|
12.5
nM
|
|
|
Binding affinity to glucocorticoid receptor (unknown origin) by fluorescence polarization competitive binding assay
|
Homo sapiens
|
3.7
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-1beta production after 6 hrs
|
Homo sapiens
|
14.0
nM
|
|
|
Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells at 5 uM
|
Mus musculus
|
70.4
%
|
|
|
Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced IL6 release at 10 uM incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay relative to control
|
Homo sapiens
|
43.0
%
|
|
|
Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced IL1-beta release at 100 uM incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay relative to control
|
Homo sapiens
|
80.0
%
|
|
|
Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced TNFalpha release at 100 uM incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay relative to control
|
Homo sapiens
|
80.0
%
|
|
|
Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced IL1-beta release incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay
|
Homo sapiens
|
9.5
nM
|
|
|
Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced TNFalpha release incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay
|
Homo sapiens
|
17.0
nM
|
|
|
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production at 50 uM incubated for 2 hrs prior to LPS-challenge measured after 24 hrs by Griess method
|
Mus musculus
|
98.24
%
|
|
|
Binding affinity to human glucocorticoid receptor by radioligand displacement assay
|
Homo sapiens
|
2.5
nM
|
|
|
Displacement of [3H]Dexamethasone from glucocorticoid receptor in human HeLaS3 cells after 2 hrs
|
Homo sapiens
|
2.2
nM
|
|
Displacement of [3H]Dexamethasone from glucocorticoid receptor in human HeLaS3 cells after 2 hrs
|
Homo sapiens
|
4.1
nM
|
|
|
Displacement of [3H]Dexamethasone from glucocorticoid receptor in human HeLaS3 cells at 10 uM after 2 hrs relative to control
|
Homo sapiens
|
21.0
%
|
|
|
Binding affinity to human glucocorticoid receptor by radioligand displacement assay
|
Homo sapiens
|
1.5
nM
|
|
Binding affinity to human glucocorticoid receptor by radioligand displacement assay
|
Homo sapiens
|
3.0
nM
|
|
|
Antiinflammatory activity in LPS-stimulated human THP1 cells assessed as inhibition of IL-6 release at 1 ug/ml after 24 hrs by ELISA relative to control
|
Homo sapiens
|
85.0
%
|
|
|
Antiinflammatory activity in LPS-stimulated human THP1 cells assessed as inhibition of TNFalpha release at 1 ug/ml after 24 hrs by ELISA relative to control
|
Homo sapiens
|
72.0
%
|
|
|
Transactivation of glucocorticoid receptor ligand binding domain (unknown origin) transfected in human HeLa cells assessed as activation of NP-1 by GAL4 luciferase reporter gene assay
|
Homo sapiens
|
4.5
nM
|
|
|
Agonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-induced AP-1 activation by luciferase reporter gene assay
|
Homo sapiens
|
2.5
nM
|
|
|
Agonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of IL-1beta-induced NF-kappaB dependent E-selectin activation by luciferase reporter gene assay
|
Homo sapiens
|
1.1
nM
|
|
|
Binding affinity to glucocorticoid receptor (unknown origin) by fluorescence polarization assay
|
Homo sapiens
|
1.2
nM
|
|
|
Transactivation of GR-LBD expressed in human HeLa cells co-expressing GAL4-DBD by luciferase reporter gene assay
|
Homo sapiens
|
4.2
nM
|
|
|
Transrepression of glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-induced AP-1 activity by luciferase reporter gene assay
|
Homo sapiens
|
2.5
nM
|
|
|
Binding affinity to glucocorticoid receptor-LBD (unknown origin) by fluorescence polarization assay
|
Homo sapiens
|
1.1
nM
|
|
|
Transactivation activity at glucocorticoid receptor ligand binding domain (unknown origin) expressed in human Hela cells co-expressing GAL4 DNA binding domain assessed as NP-1-stimulated GRE activation by luciferase reporter gene assay
|
Homo sapiens
|
4.5
nM
|
|
|
Transrepression activity at glucocorticoid receptor in human A549 cells assessed as inhibition of IL1beta-stimulated NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay
|
Homo sapiens
|
1.1
nM
|
|
|
Transrepression activity at glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-stimulated AP1 response element by luciferase reporter gene assay
|
Homo sapiens
|
2.5
nM
|
|
|
Binding affinity to glucocorticoid receptor (unknown origin) by fluorescence assay
|
Homo sapiens
|
1.2
nM
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
103.89
%
|
|
|
Agonist activity at glucocorticoid receptor in HFF assessed as inhibition of IL-1-induced IL-6 production after 24 hrs
|
Homo sapiens
|
0.5
nM
|
|
|
Binding affinity to mineralocorticoid receptor (unknown origin) by fluorescence polarization competitive binding assay
|
Homo sapiens
|
33.0
nM
|
|
|
Displacement of TAMRA-labeled dexamethasone from glucocorticoid receptor (unknown origin) by fluorescence polarization competitive binding assay
|
Homo sapiens
|
3.5
nM
|
|
|
Displacement of [3H]-methyltrienolone from human progesterone receptor expressed in HEK293 cells
|
Homo sapiens
|
561.0
nM
|
|
|
Displacement of [3H]-dexamethasone from human glucocorticoid receptor expressed in HEK293 cells
|
Homo sapiens
|
0.69
nM
|
|
|
Displacement of [3H]-aldosterone from human mineralocorticoid receptor expressed in HEK293 cells
|
Homo sapiens
|
0.36
nM
|
|
|
Displacement of TAMRA-labeled dexamethasone from glucocorticoid receptor (unknown origin) by fluorescence polarization assay
|
Homo sapiens
|
3.0
nM
|
|
|
Displacement of TAMRA-labeled dexamethasone from mineralocorticoid receptor (unknown origin) by fluorescence polarization assay
|
Homo sapiens
|
33.0
nM
|
|
|
Agonist activity at glucocorticoid receptor in human foreskin fibroblasts assessed as inhibition of IL-1-induced IL-6 production by trans-repression assay
|
Homo sapiens
|
0.5
nM
|
|
|
Transactivation of glucocorticoid receptor in human HeLa cells harboring MMTV promoter by luciferase reporter gene assay
|
Homo sapiens
|
17.0
nM
|
|
|
Antiinflammatory activity in immature rat assessed as inhibition of cantharidin-induced inflammation at 5 ug administered topically to outer surface of ear after 72 hrs relative to control
|
Rattus norvegicus
|
17.0
%
|
|
|
Antiinflammatory activity in immature rat assessed as inhibition of cantharidin-induced inflammation at 10 ug administered topically to outer surface of ear after 72 hrs relative to control
|
Rattus norvegicus
|
25.0
%
|
|
|
Antiinflammatory activity in immature rat assessed as inhibition of cantharidin-induced inflammation at 20 ug administered topically to outer surface of ear after 72 hrs relative to control
|
Rattus norvegicus
|
30.0
%
|
|
|
Antiinflammatory activity in immature rat assessed as inhibition of cantharidin-induced inflammation at 40 ug administered topically to outer surface of ear after 72 hrs relative to control
|
Rattus norvegicus
|
53.0
%
|
|
|
Antiinflammatory activity in immature rat assessed as inhibition of cantharidin-induced inflammation at 80 ug administered topically to outer surface of ear after 72 hrs relative to control
|
Rattus norvegicus
|
76.0
%
|
|
|
Agonist activity at human GCR expressed in HEK293 cells by luciferase reporter gene assay
|
Homo sapiens
|
1.3
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-1beta expression pretreated 1 hr before LPS challenge followed by incubated for 16 hrs by flow cytometry
|
Homo sapiens
|
8.0
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-8 expression pretreated 1 hr before LPS challenge followed by incubated for 16 hrs by flow cytometry
|
Homo sapiens
|
9.0
nM
|
|
|
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha expression pretreated 1 hr before LPS challenge followed by incubated for 16 hrs by flow cytometry
|
Homo sapiens
|
2.0
nM
|
|
|
Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay relative to vehicle-treated control
|
Mus musculus
|
800.0
nM
|
|
|
Inhibition of LPS-induced TNFalpha production in mouse inflammatory model at 1 mg/kg
|
Mus musculus
|
97.0
%
|
|
|
Inhibition of LPS-induced IL6 production in mouse inflammatory model at 1 mg/kg
|
Mus musculus
|
83.0
%
|
|
|
Agonist activity at GR in HFF cells assessed as suppression of IL-1-induced IL-6 production
|
Homo sapiens
|
1.0
nM
|
|
|
Antiasthmatic activity in ovalbumin-induced asthma model in Hartley guinea pig assessed as suppression of immediate asthmatic response at 10 mg/kg, po administered 16 hr before and 2 hrs after ovalbumin challenge
|
Cavia porcellus
|
45.0
%
|
|
|
Antiasthmatic activity in ovalbumin-induced asthma model in Hartley guinea pig assessed as suppression of late asthmatic response at 10 mg/kg, po administered 16 hr before and 2 hrs after ovalbumin challenge
|
Cavia porcellus
|
88.0
%
|
|
|
Inhibition of sPLA2-V (unknown origin) using substrate 1,2-bis(heptanoylthio)-glycerophosphocholine by Ellman's method based photometric assay
|
Homo sapiens
|
610.0
nM
|
|
|
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha production at 20 ug/ml incubated for 1 hr prior to LPS challenge measured after 6 hrs by sandwich ELISA relative to control
|
Mus musculus
|
0.016
%
|
|
|
Antiinflammatory activity in mouse J774A1 cells assessed as inhibition of LPS-induced TNF-alpha production at 20 ug/ml incubated for 1 hr prior to LPS challenge measured after 6 hrs by sandwich ELISA relative to control
|
Mus musculus
|
0.165
%
|
|
|
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-1beta production at 20 ug/ml incubated for 1 hr prior to LPS challenge measured after 12 hrs by sandwich ELISA relative to control
|
Mus musculus
|
1.84
%
|
|
|
Antiinflammatory activity in mouse J774A1 cells assessed as inhibition of LPS-induced IL-1beta production at 20 ug/ml incubated for 1 hr prior to LPS challenge measured after 12 hrs by sandwich ELISA relative to control
|
Mus musculus
|
9.09
%
|
|
|
Binding affinity to glucocorticoid receptor (unknown origin) by fluorescence polarization assay
|
Homo sapiens
|
1.2
nM
|
|
|
Binding affinity to progesterone receptor (unknown origin) by fluorescence polarization assay
|
Homo sapiens
|
778.0
nM
|
|
|
Agonist activity at glucocorticoid receptor in human A549 cells assessed as AP-1 transrepression by luciferase reporter gene assay
|
Homo sapiens
|
2.5
nM
|
|
|
Agonist activity at glucocorticoid receptor in human A549 cells assessed as E-selectin transrepression by luciferase reporter gene assay
|
Homo sapiens
|
1.1
nM
|
|
|
Agonist activity at glucocorticoid receptor in human HeLa cells assessed as NP-1 transactivation by luciferase reporter gene assay
|
Homo sapiens
|
4.5
nM
|
|
|
Agonist activity at glucocorticoid receptor in human whole blood assessed as inhibition of LPS-induced TNF production incubated for 20 hrs prior to LPS challenge measured after 5 hrs by ELISA
|
Homo sapiens
|
6.9
nM
|
|
|
Inhibition of LPS-induced TNF-alpha release in mouse RAW264.7 cells compound preincubated for 1 hr before LPS treatment measured after 6 to 12 hrs by sandwich immunoassay
|
Mus musculus
|
0.016
ug.mL-1
|
|
|
Inhibition of LPS-induced TNF-alpha release in mouse J774A1 cells compound preincubated for 1 hr before LPS treatment measured after 6 to 12 hrs by sandwich immunoassay
|
Mus musculus
|
0.165
ug.mL-1
|
|
|
Inhibition of LPS-induced IL1-beta release in mouse RAW264.7 cells compound preincubated for 1 hr before LPS treatment measured after 6 to 12 hrs by sandwich immunoassay
|
Mus musculus
|
1.84
ug.mL-1
|
|
|
Inhibition of LPS-induced IL1-beta release in mouse J774A1 cells compound preincubated for 1 hr before LPS treatment measured after 6 to 12 hrs by sandwich immunoassay
|
Mus musculus
|
9.09
ug.mL-1
|
|
|
Antiinflammatory activity against ovalbumin-induced model of allergic inflammation in brown Norway rat assessed as inhibition of eosinophil infiltration in bronchoalveolar lavage fluid at 1 mg/kg, po bid 1 hr before and 6.5 hrs post ovalbumin challenge measured 24 hrs post challenge relative to vehicle-treated control
|
Rattus norvegicus
|
100.0
%
|
|
|
Inhibition of TNFalpha production in mouse RAW264.7 cells incubated for 6 hrs by sandwich immunoassay
|
Mus musculus
|
40.0
nM
|
|
|
Inhibition of TNFalpha production in mouse J774A.1 cells incubated for 6 hrs by sandwich immunoassay
|
Mus musculus
|
400.0
nM
|
|
|
Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition of LPS-induced IL-1beta production at 150 umol/kg, po pre-administered at interval of 12 hrs followed by LPS-stimulation 6 hrs after final dose and measured 2 hrs post LPS challenge by ELISA method
|
Rattus norvegicus
|
62.5
%
|
|
|
Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition of LPS-induced TNFalpha production at 150 umol/kg, po pre-administered at interval of 12 hrs followed by LPS-stimulation 2 hrs after final dose and measured 2 hrs post LPS challenge by ELISA method
|
Rattus norvegicus
|
73.4
%
|
|
|
Binding affinity to human GR
|
Homo sapiens
|
3.5
nM
|
|
|
Transrepression activity at glucocorticoid receptor in human SW1353 cells assessed as repression of IL-1-induced MMP-13 production after 24 hrs by ELISA
|
Homo sapiens
|
1.8
nM
|
|
|
Transrepression activity at glucocorticoid receptor in human whole blood assessed as repression of IL-1-induced TNF-alpha production after 4 hrs by ELISA
|
Homo sapiens
|
21.0
nM
|
|
|
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay
|
Mus musculus
|
630.0
nM
|
|
|
Antiinflammatory activity in C57BL6/J mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay
|
Mus musculus
|
25.0
nM
|
|
|
Antiinflammatory activity in ICR mouse assessed as inhibition of croton oil-induced ear edema at 1 mg/ml administered 1 hr prior to croton oil challenge measured after 4 hrs relative to control
|
Mus musculus
|
70.5
%
|
|
|
Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay
|
Mus musculus
|
800.0
nM
|
|
|
Displacement of [3H]dexamethasone from glucocorticoid receptor in human IM9 cells
|
Homo sapiens
|
3.8
nM
|
|
|
Antiinflammatory activity against mouse J774 cells assessed as inhibition of LPS-induced nitric oxide production at 10 uM by Griess assay
|
Mus musculus
|
85.0
%
|
|
|
Antiinflammatory activity against mouse J774 cells assessed as inhibition of LPS-induced COX-2 expression at 10 uM after 24 hrs by Western blot analysis
|
Mus musculus
|
90.0
%
|
|
|
Antiinflammatory activity against mouse J774 cells assessed as inhibition of LPS-induced IL-6 production at 10 uM after 24 hrs by ELISA
|
Mus musculus
|
86.0
%
|
|
|
Antiinflammatory activity against mouse J774 cells assessed as inhibition of LPS-induced MCP-1 production at 10 uM after 24 hrs by ELISA
|
Mus musculus
|
38.0
%
|
|
|
Antiinflammatory activity in C57BL/6 mouse assessed as inhibition of zymosan-induced knee joint edema formation at 10 mg/kg, ip administered 1 hr prior to zymosan challenge measured at 6 hrs relative to control
|
Mus musculus
|
42.0
%
|
|
|
Antiinflammatory activity in C57BL/6 mouse assessed as inhibition of zymosan-induced knee joint edema formation at 10 mg/kg, ip administered 1 hr prior to zymosan challenge measured at 24 hrs relative to control
|
Mus musculus
|
48.0
%
|
|
|
Binding affinity to GR (unknown origin) by FP assay
|
Homo sapiens
|
6.1
nM
|
|
|
Binding affinity to PR (unknown origin) by FP assay
|
Homo sapiens
|
440.0
nM
|
|
|
Displacement of 3H-aldosterone from MR (unknown origin) ligand binding domain by SPA assay
|
Homo sapiens
|
40.0
nM
|
|
|
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs in presence of LPS by Griess assay
|
Mus musculus
|
630.0
nM
|
|
|
Displacement of [3H]dexamethasone from GR receptor in human IM9 cells
|
Homo sapiens
|
3.8
nM
|
|
|
Inhibition of TNFalpha (unknown origin) at 1 uM relative to control
|
Homo sapiens
|
49.9
%
|
|
|
Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 production at 50 uM pretreated for 1 hr followed by LPS stimulation measured after 24 hrs by ELISA relative to control
|
Mus musculus
|
84.9
%
|
|
|
Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 production at 10 uM pretreated for 1 hr followed by LPS stimulation measured after 24 hrs by ELISA relative to control
|
Mus musculus
|
80.4
%
|
|
|
Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 production at 2 uM pretreated for 1 hr followed by LPS stimulation measured after 24 hrs by ELISA relative to control
|
Mus musculus
|
75.9
%
|
|
|
Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha production at 50 uM pretreated for 1 hr followed by LPS stimulation measured after 24 hrs by ELISA relative to control
|
Mus musculus
|
86.1
%
|
|
|
Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha production at 10 uM pretreated for 1 hr followed by LPS stimulation measured after 24 hrs by ELISA relative to control
|
Mus musculus
|
79.2
%
|
|
|
Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha production at 2 uM pretreated for 1 hr followed by LPS stimulation measured after 24 hrs by ELISA relative to control
|
Mus musculus
|
71.8
%
|
|
|
Inhibition of sEH in human HepG2 cells assessed as NF-kappaB mRNA expression at 1 uM after 8 to 16 hrs by SYBR green based qRT-PCR analysis relative to DMSO control
|
Homo sapiens
|
59.4
%
|
|
|
Invivo inhibition of IRAK4 in Lewis rat assessed as reduction in R848-stimulated serum IL-6 secretion at 3 mg/kg, po administered once daily pretreated for 1 hr followed by R848 challenge measured after 1.5 hrs relative to control
|
Rattus norvegicus
|
86.0
%
|
|
|
Transrepression activity at glucocorticoid receptorin human HeLa cells assessed as inhibition of TPA-induced collagenase promoter activity by luciferase reporter gene assay
|
Homo sapiens
|
1.585
nM
|
|
|
Transactivation activity at glucocorticoid receptor in human HeLa cells assessed as induction of MMTV promoter activity by luciferase reporter gene assay
|
Homo sapiens
|
7.943
nM
|
|
|
Transrepression activity at glucocorticoid receptor in human THP1 cells assessed as receptor-mediated anti-inflammatory activity by measuring inhibition of LPS-induced IL-8 production
|
Homo sapiens
|
2.512
nM
|
|
|
Binding affinity to recombinant human glucocorticoid receptor expressed in baculovirus infected sf9 cells
|
Homo sapiens
|
12.59
nM
|
|
|
Anti-inflammatory activity in Lewis rat mBSA-induced arthritis model assessed as inhibition of mBSA-induced knee swelling at 0.3 mg/kg, po, administered daily via gavage measured after 7 days post last dose relative to control
|
Rattus norvegicus
|
65.0
%
|
|
|
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production by griess assay
|
Mus musculus
|
800.0
nM
|
|
|
Antiproliferative activity against human RPMI18226 cells after 72 hrs by XTT assay
|
Homo sapiens
|
7.8
nM
|
|
|
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated nitric oxide production at 20 uM after 48 hrs by Griess assay relative to control
|
Mus musculus
|
60.9
%
|
|
|
Antiallergic activity in rat RBL2H3 cells assessed as inhibition of A23187-induced beta hexosaminidase release at 10 nM pretreated for 20 hrs followed by A23187 addition measured after 1 hr by p-NAG substrate based assay relative to control
|
Rattus norvegicus
|
80.7
%
|
|
|
Antiallergic activity in anti-DNP IgE-sensitized rat RBL2H3 cells assessed as inhibition of DNP-BSA-induced beta hexosaminidase release at 10 nM pretreated for 20 hrs followed by anti-DNP IgE-sensitization for 2 hrs and subsequent DNP-BSA addition measured after 1 hr by p-NAG substrate based assay relative to control
|
Rattus norvegicus
|
79.7
%
|
|
|
Anti-inflammatory activity in Balb/c mouse model of hypereosinophilia assessed as inhibition of eosinophil infiltration at 2.5 umol/kg, ip dosed 2 hrs before allergen challenge
|
Mus musculus
|
59.0
%
|
|
|
Antiinflammatory activity in Balb/c mouse ear edema model assessed as inhibition of croton oil-induced ear edema at 0.1 mg/ear administered topically immediately post croton oil treatment and measured after 4 hrs relative to control
|
Mus musculus
|
90.0
%
|
|
|
Antiinflammatory activity in BALB/c mouse J774 cells assessed as inhibition of LPS/IFNgamma-induced nitric oxide production at 20 uM after 24 hrs by Griess method relative to control
|
Mus musculus
|
69.8
%
|
|
|
Immunomodulatory activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A-induced lymphocyte proliferation by measuring [3H]-thymidine uptake after 48 to 72 hrs by scintillation counting analysis
|
Mus musculus
|
1.0
nM
|
|
|
Antiinflammatory activity against mouse J774.2 cells assessed as inhibition of LPS-induced TNFalpha release at 1 mM after 24 hrs by ELISA relative to control
|
Mus musculus
|
62.0
%
|
|
|
Antiinflammatory activity against mouse J774.2 cells assessed as inhibition of LPS-induced IL-6 release at 0.5 mM after 24 hrs by ELISA relative to control
|
Mus musculus
|
40.0
%
|
|
|
Antiinflammatory activity in PMA-differentiated human THP1 cells assessed as inhibition of LPS-induced TNF-alpha production at 1 uM after 24 hrs by ELISA relative to control
|
Homo sapiens
|
40.0
%
|
|
|
Antiinflammatory activity in PMA-differentiated human THP1 cells assessed as inhibition of LPS-induced IL-6 production at 1 uM after 24 hrs by ELISA relative to control
|
Homo sapiens
|
58.0
%
|
|
|
Agonist activity at GAL4 DNA-binding domain fused GR (unknown origin) ligand binding domain expressed in UAS-bla HEK 293T cells assessed as beta-lactamase transcriptional activation by FRET-based GeneBLAzer assay
|
Homo sapiens
|
2.35
nM
|
|
|
Inhibition of LPS-induced TNFalpha level in Sprague-Dawley rat serum at 25 mg/kg, po pretreated for 1 hr followed by LPS treatment measured after 90 mins by ELISA relative to control
|
Rattus norvegicus
|
91.0
%
|
|
|
Immunomodulatory activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A-induced lymphocyte proliferation by measuring [methyl-3H]-thymidine uptake at 50 uM after 48 hrs
|
Mus musculus
|
74.6
%
|
|
|
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
|
-14.23
%
|
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
5.83
%
|
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
-0.78
%
|
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
2.35
%
|
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
8.59
%
|
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
1.68
%
|
|
|
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
|
-1.2
%
|
|
|
Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production preincubated for 30 mins followed by LPS-stimulation and measured after 24 hrs by Griess assay
|
Mus musculus
|
10.0
nM
|
|
|
Inhibition of glucocorticoid receptor (unknown origin)
|
Homo sapiens
|
19.0
nM
|
|
|
Agonist activity at recombinant human glucocorticoid receptor expressed in African green monkey CV1 cells by MMTV luciferase reporter gene assay
|
Homo sapiens
|
0.1
nM
|
|
|
Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated NO production at 15 uM preincubated with LPS and measured after 20 hrs by Griess reagent-based assay relative to control
|
Mus musculus
|
34.25
%
|
|
|
Binding affinity to GR (unknown origin)
|
Homo sapiens
|
2.0
nM
|
|
|
Inhibition of anti-CD3-induced IL-17A level in Balb/c mouse plasma at 5 mg/kg, po treated prior to stimulation with anti-CD3 for 3 hrs relative to control
|
Mus musculus
|
51.0
%
|
|
|
Anti-inflammatory activity in mouse peritoneal macrophages assessed as inhibition of LPS-induced NO production incubated for 22 hrs by Griess reagent based colorimetric assay
|
Mus musculus
|
150.0
nM
|
|
|
Antiinflammatory activity in DNFB-induced ICR mouse model of auricle edema assessed as inhibition of ear swelling at 0.5 mg/kg, ig administered once daily for 6 days followed by 1% DNFB solution applied on right ear measured after 24 hrs relative to untreated control
|
Mus musculus
|
46.8
%
|
|
|
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitirc oxide production preincubated for 1 hr followed by LPS-stimulation and measured after 18 hrs by Griess assay
|
Mus musculus
|
10.0
nM
|
|
|
Inhibition of TNFalpha expression in LPS-induced macrophages (unknown origin) at 10 uM incubated for 24 hrs by ELISA relative to control
|
Not specified
|
82.5
%
|
|
|
Inhibition of TNFalpha expression in LPS-induced macrophages (unknown origin) incubated for 24 hrs by ELISA
|
Not specified
|
134.0
nM
|
|
|
Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production preincubated for 1 hr followed by LPS-stimulation and measured after 18 hrs by Griess reagent-based assay
|
Mus musculus
|
130.0
nM
|
|
|
Immunosuppressive activity against BALB/C mouse B lymphocytes assessed as reduction in LPS-induced cell proliferation by measuring [3H]-thymidine uptake incubated for 8 hrs by Beta scintillation counting method
|
Mus musculus
|
800.0
nM
|
|
|
Inhibition of carrageenan-induced paw edema in Swiss mouse at 0.5 mg/kg, sc pretreated for 1 hr followed by carrageenan-stimulation and measured after 6 hrs relative to control
|
Mus musculus
|
82.0
%
|
|
|
Inhibition of carrageenan-induced thermal allodynia in Swiss mouse at 0.5 mg/kg, sc pretreated for 1 hr followed by carrageenan-stimulation and measured after 6 hrs relative to control
|
Mus musculus
|
72.0
%
|
|
|
Inhibition of zymosan-induced TLR2/Dectin-1 Signaling Pathway assessed as reduction in paw edema in Swiss mouse at 0.5 mg/kg, sc pretreated for 1 hr followed by LPS-stimulation and measured after 48 hrs relative to control
|
Mus musculus
|
45.0
%
|
|
|
Inhibition of collagenase (unknown origin) transfected in human HeLa cells by luciferase reporter gene assay
|
Homo sapiens
|
7.943
nM
|
|
|
Immunomodulatory activity in human THP1 cells assessed as reduction in LPS-induced IL-8 production
|
Homo sapiens
|
2.512
nM
|
|
|
Inhibition of LPS-induced TNFalpha release in human PBMC cells
|
Homo sapiens
|
6.4
nM
|
|
|
Inhibition of LPS-induced IL12p40 release in human PBMC cells
|
Homo sapiens
|
4.3
nM
|
|
|
Inhibition of PHA-induced IL2 release in human PBMC cells
|
Homo sapiens
|
4.6
nM
|
|
|
Inhibition of PHA-induced IFNgamma release in human PBMC cells
|
Homo sapiens
|
3.8
nM
|
|
|
Inhibition of PHA-induced IL4 release in human PBMC cells
|
Homo sapiens
|
2.3
nM
|
|
|
Protection against imiquimod-induced psoriasis in C57BL/6 mouse assessed as inhibition of skin scaling at 3 mg/kg, po dosed via gavage once daily and measured on day 6 relative to control
|
Mus musculus
|
45.0
%
|
|
|
Protection against imiquimod-induced psoriasis in C57BL/6 mouse assessed as inhibition of skin erythema level at 3 mg/kg, po dosed via gavage once daily and measured on day 6 relative to control
|
Mus musculus
|
37.0
%
|
|
|
Antiinflammatory activity in mouse J774 cells assessed as inhibition of LPS/IFNgamma-induced IL-1beta level at 10 uM incubated for 24 hrs by ELISA relative to control
|
Mus musculus
|
87.1
%
|
|
|
Induction of translocation of human glucocorticoid receptor expressed in HEK293T cells transduced with lentiviral vector expressing H2B-mCherry and GFP-GR assessed as effective dissociation constant measured every 130 sec for 22 mins by fluorescence imaging analysis
|
Homo sapiens
|
2.8
nM
|
|
|
Cytotoxicity against human REH cells overexpressing GR assessed as reduction in cell viability measured after 3 days by resazurin based assay
|
Homo sapiens
|
6.7
nM
|
|
|
Antiinflammatory activity in Wistar rat model of LPS-induced uveitis assessed as reduction in infiltrating cells in aqueous humor at 10 ug/10ul/eye administered 24 hrs after LPS stimulation and measured after 1 hr by hemocytometry relative to control
|
Rattus norvegicus
|
79.1
%
|
|
|
Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced neutrophil level in BALF at 0.5 mg/kg, INH administered 18 hrs before LPS-stimulation and measured after 24 hrs by FACS analysis relative to control
|
Mus musculus
|
72.9
%
|
|
|
Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced macrophage level in BALF at 0.5 mg/kg, INH administered 18 hrs before LPS-stimulation and measured after 24 hrs by FACS analysis relative to control
|
Mus musculus
|
40.9
%
|
|
|
Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced lymphocyte level in BALF at 0.5 mg/kg, INH administered 18 hrs before LPS-stimulation and measured after 24 hrs by FACS analysis relative to control
|
Mus musculus
|
30.6
%
|
|
|
Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced neutrophil level in BALF at 0.5 mg/kg, ip administered 18 hrs before LPS-stimulation and measured after 24 hrs by FACS analysis relative to control
|
Mus musculus
|
66.9
%
|
|
|
Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced macrophage level in BALF at 0.5 mg/kg, ip administered 18 hrs before LPS-stimulation and measured after 24 hrs by FACS analysis relative to control
|
Mus musculus
|
75.1
%
|
|
|
Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced lymphocyte level in BALF at 0.5 mg/kg, ip administered 18 hrs before LPS-stimulation and measured after 24 hrs by FACS analysis relative to control
|
Mus musculus
|
46.1
%
|
|
|
Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced neutrophil infiltration in lungs at 0.5 mg/kg, INH administered 18 hrs before LPS-stimulation and measured after 24 hrs by H and E staining based imaging analysis relative to control
|
Mus musculus
|
55.9
%
|
|
|
Antiinflammatory activity in ICR mouse assessed as reduction in LPS-induced neutrophil infiltration in lungs at 0.5 mg/kg, ip administered 18 hrs before LPS-stimulation and measured after 24 hrs by H and E staining based imaging analysis relative to control
|
Mus musculus
|
58.7
%
|
|
|
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production at 10 uM preincubated for 1 hrs followed by LPS stimulation and measured after 24 hrs by Griess assay relative to control
|
Mus musculus
|
51.81
%
|
|
|
Inhibition of NFkappaB transcriptional activity in LPS-stimulated mouse RAW264.7 cells
|
Mus musculus
|
920.0
nM
|
|
|
Inhibition of activation of T cell in C57BL/6 mouse Staphylococcal enterotoxin B (SEB)-mediated acute T cell activation model assessed as inhibition of IL-2 release in plasma at 10 mg/kg, po measured after 2.5 hrs of SEB challenge
|
Mus musculus
|
81.0
%
|
|
|
Inhibition of activation of T cell in C57BL/6 mouse Staphylococcal enterotoxin B (SEB)-mediated acute T cell activation model assessed as inhibition of IL-2 release in spleen at 10 mg/kg, po measured after 2.5 hrs of SEB challenge
|
Mus musculus
|
68.0
%
|
|
|
Inhibition of LPS-induced NO production in C57BL/6J mouse peritoneal macrophages at 1 uM measured after 24 hrs in presence of LPS by Griess reagent based assay relative to control
|
Mus musculus
|
62.8
%
|
|
|
Cytotoxicity against C57BL/6J mouse peritoneal macrophages assessed as reduction of cell viability at 1 uM incubated for 24 hrs in presence of LPS by MTT assay
|
Mus musculus
|
17.0
%
|
|
|
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production preincubated for 3 hrs followed by LPS-stimulation and measured after 24 hrs by Griess reagent based assay
|
Mus musculus
|
580.0
nM
|
|
|
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
|
6.31
nM
|
|
|
Agonist activity at glucocorticoid receptor in rat INS-1 832/13 cells transfected with 3XGRE-promoter luciferase plasmid construct assessed as induction of receptor transactivation by luciferase reporter gene assay
|
Rattus norvegicus
|
1.995
nM
|
|
|
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production at 20 uM after 24 hrs by Griess assay
|
Mus musculus
|
93.62
%
|
|
