|
Ability to induce human IL-6 assay in A549 lung carcinoma cell line.
|
Homo sapiens
|
4.5
nM
|
|
|
Transcriptional activation in CV-1 cells expressing human glucocorticoid receptor
|
None
|
8.0
nM
|
|
|
Inhibition of transcriptional activation in CV-1 cells expressing glucocorticoid receptor
|
Homo sapiens
|
8.0
nM
|
|
|
Inhibition of transcriptional repression in CV-1 cells expressing glucocorticoid receptor
|
Homo sapiens
|
2.1
nM
|
|
|
The effective concentration in CV-1 cells for glucocorticoid response element activation (GRE).
|
None
|
3.3
nM
|
|
|
Binding affinity to human CBG receptor (corticosteroid-binding globulins)
|
None
|
30.9
nM
|
|
|
Glucocorticoid-induced aromatase activity in human skin fibroblasts
|
Homo sapiens
|
41.0
nM
|
|
|
Concentration of compound required to inhibit the binding of 28 nM [3H]dexamethasone by 50% to rat hepatic cytosolic receptors
|
Rattus norvegicus
|
196.3
nM
|
|
|
Inhibition of human Glucocorticoid receptor
|
Homo sapiens
|
13.8
nM
|
|
|
Transcriptional activation in CV-1 cells expressing glucocorticoid receptor
|
Homo sapiens
|
8.0
nM
|
|
|
Binding affinity towards glucocorticoid receptor (GR) by displacing [3H]dexamethasone
|
None
|
2.4
nM
|
|
|
Binding affinity towards human glucocorticoid receptor (GR) was determined using [3H]dexamethasone as radioligand in SF-1 cells
|
None
|
2.4
nM
|
|
|
Binding affinity for glucocorticoid receptor
|
Homo sapiens
|
2.4
nM
|
|
|
Ability to induce human glutamine synthetase in skeletal muscle cells
|
None
|
32.0
nM
|
|
|
Inhibitory concentration against interleukin-1 beta production in HL-60 cells stimulated with lipopolysaccharide (LPS).
|
Homo sapiens
|
760.0
nM
|
|
|
Inhibitory concentration against interleukin-1 beta production in HL-60 cells stimulated with lipopolysaccharide (LPS).
|
Homo sapiens
|
760.0
nM
|
|
|
Transcriptional repression in HepG2 cells expressing human glucocorticoid receptor
|
Homo sapiens
|
2.1
nM
|
|
|
Effective concentration in HepG2 cells transfected with LUC gene (E-sel-Luc).
|
None
|
2.6
nM
|
|
|
Effective concentration for transcriptional activation of aromatase in Human cell native protein assay
|
Homo sapiens
|
45.0
nM
|
|
|
Effective concentration of compound for transcriptional activation of IL-6 in Human cell native protein assay
|
Homo sapiens
|
3.6
nM
|
|
|
Effective concentration of compound for transcriptional activation of PGE-2 in Human cell native protein assay
|
Homo sapiens
|
2.0
nM
|
|
|
Effective concentration of compound for transcriptional activation of TAT in Human cell native protein assay
|
Homo sapiens
|
48.0
nM
|
|
|
Effective concentration of compound for transcriptional activation of collagenase in Human cell native protein assay
|
Homo sapiens
|
0.4
nM
|
|
|
Effective concentration of compound for transcriptional activation of osteocalcin in Human cell native protein assay
|
Homo sapiens
|
32.0
nM
|
|
|
Repression activity of GR ligand with interleukin-6 receptor in native cell assay using Dexamethasone was determined as maximal potency
|
Homo sapiens
|
3.8
nM
|
|
|
Percent inhibition of anti-DNA antibody was evaluated by ELISA technique as a measure of auto-immune disease after injection of compound dose of 0.1 mg/kg in murine
|
Mus musculus
|
39.0
%
|
|
|
Percent inhibition of anti-DNA antibody was evaluated by ELISA technique as a measure of auto-immune disease after injection of compound dose of 1 mg/kg in murine
|
Mus musculus
|
39.0
%
|
|
|
Percent inhibition of anti-DNA antibody was evaluated by ELISA technique as a measure of auto-immune disease after injection of compound dose of 10 mg/kg in murine
|
Mus musculus
|
52.0
%
|
|
|
Percent inhibition of proteinuria by compound dose of 0.1 mg/kg given perorally to murine in chronic graft-versus-host-disease test
|
Mus musculus
|
53.0
%
|
|
|
Percent inhibition of proteinuria by compound dose of 1 mg/kg given perorally to murine in chronic graft-versus-host-disease test
|
Mus musculus
|
75.0
%
|
|
|
Percent inhibition of proteinuria by compound dose of 10 mg/kg given perorally to murine in chronic graft-versus-host-disease test
|
Mus musculus
|
100.0
%
|
|
|
Binding affinity towards aldosterone receptor (Mineralocorticoid receptor)
|
Homo sapiens
|
37.0
nM
|
|
|
Ability to induce mouse macrophage IL-6 assay in peritoneal exudate cells harvested by gavage from C57BI/6 mice.
|
Mus musculus
|
5.7
nM
|
|
|
Inhibition of concanavalin A stimulated T-cell proliferation in human PBMCs
|
Homo sapiens
|
25.0
nM
|
|
|
Adjuvant arthritic activity in rat injected leg on day 16 tested at 20 mg/kg perorally.
|
Rattus norvegicus
|
42.0
%
|
|
|
Adjuvant arthritic activity in rat injected leg on day 3 tested at 50 mg/kg perorally
|
Rattus norvegicus
|
28.0
%
|
|
|
Adjuvant arthritic activity in rat uninjected leg on day 16 tested at 20 mg/kg perorally.
|
Rattus norvegicus
|
54.0
%
|
|
|
Tested for inhibition of formation of granulation tissue around the cotton pellet treated with steroid
|
Rattus norvegicus
|
60.6
%
|
|
|
Tested for inhibition of formation of granulation tissue around the cotton pellet untreated with steroid
|
Rattus norvegicus
|
26.6
%
|
|
|
Tested for topical antiinflammatory activity in the croton oil ear edema assay
|
Rattus norvegicus
|
68.6
%
|
|
|
The antiinflammatory activity was evaluated as %inhibition of croton oil induced ear edema in the left ear of rat
|
Rattus norvegicus
|
49.6
%
|
|
|
The antiinflammatory activity was evaluated as %inhibition of croton oil induced ear edema in the right ear of rat
|
Rattus norvegicus
|
66.7
%
|
|
|
Transcriptional repression activity in HEP G2 cells expressing glucocorticoid receptor compared to Dexamethasone
|
Homo sapiens
|
2.1
nM
|
|
|
Inhibition of concanavalin A stimulated rat splenocyte proliferation
|
Rattus norvegicus
|
19.6
nM
|
|
|
Glucocorticoid induced transactivation of human tyrosine amino transferase in HepG2 cells
|
Homo sapiens
|
211.0
nM
|
|
|
The compound was tested for IL-1 generation on CMC-LPS air-pouch model at 10 mg/kg by oral administration
|
Rattus norvegicus
|
327.6
units ml-1
|
|
|
The compound was tested for IL-1 generation on CMC-LPS air-pouch model at 2.5 mg/kg by oral administration
|
Rattus norvegicus
|
596.1
units ml-1
|
|
|
% inhibition against arthritis on adjuvant-untreated paw in rats at 5 mg/kg by oral administration
|
Rattus norvegicus
|
44.4
%
|
|
|
Inhibitory activity against Granuloma on CMC-LPS air-pouch model at 10 mg/kg by oral administration
|
Rattus norvegicus
|
88.0
%
|
|
|
Inhibitory activity against Granuloma on CMC-LPS air-pouch model at 2.5 mg/kg by oral administration
|
Rattus norvegicus
|
48.0
%
|
|
|
Inhibitory activity against IL-1 on CMC-LPS air-pouch model at 10 mg/kg by oral administration
|
Rattus norvegicus
|
64.0
%
|
|
|
Inhibitory activity against IL-1 on CMC-LPS air-pouch model at 2.5 mg/kg by oral administration
|
Rattus norvegicus
|
34.0
%
|
|
|
Inhibitory activity against PGE-2 on CMC-LPS air-pouch model at 10 mg/kg by oral administration
|
Rattus norvegicus
|
86.0
%
|
|
|
Inhibitory activity against PGE-2 on CMC-LPS air-pouch model at 2.5 mg/kg by oral administration
|
Rattus norvegicus
|
69.0
%
|
|
|
Binding affinity for mineralocorticoid receptor
|
Homo sapiens
|
37.0
nM
|
|
|
The compound was tested for PGE-2 generation on CMC-LPS air-pouch model at 10 mg/kg by oral administration
|
Rattus norvegicus
|
2.8
ng ml-1
|
|
|
The compound was tested for PGE-2 generation on CMC-LPS air-pouch model at 2.5 mg/kg by oral administration
|
Rattus norvegicus
|
6.2
ng ml-1
|
|
|
GR-mediated transrepression of IL-6 in human A549 lung carcinoma cells
|
Homo sapiens
|
4.5
nM
|
|
|
Inhibition of mouse glutamine synthetase by GR-mediated transactivation in C2C12 cells
|
Mus musculus
|
3.4
nM
|
|
|
Inhibition of GR-mediated tyrosine amino transferase activity in human HepG2 cells
|
Homo sapiens
|
24.0
nM
|
|
|
GR-mediated transrepression of IL-6 in peritoneal exudate cells harvested from C57BI/6 mice
|
Mus musculus
|
5.7
nM
|
|
|
Inhibition of human glucocorticoid receptor alpha by displacement of [3H]dexamethasone
|
Homo sapiens
|
13.8
nM
|
|
|
Percent absolute inhibition of LPS-induced tumor necrosis factor alpha release in mice at 3 mg/kg dose
|
Mus musculus
|
71.0
%
|
|
|
Percent inhibition of LPS-induced tumor necrosis factor alpha release in mice relative to prednisolone at 3 mg/kg dose
|
Mus musculus
|
100.0
%
|
|
|
Agonist activity at GR assessed as NF-kappaB-mediated transrepression of secreted placental alkaline phosphatase gene in human A549 cells
|
Homo sapiens
|
8.511
nM
|
|
|
Agonist activity at GR assessed as MMTV-mediated transactivation of renilla luciferase gene in human A549 cells relative to Dexamethasone
|
Homo sapiens
|
31.62
nM
|
|
|
Inhibition of tetramethylrhodamine labeled dexamethasone binding to GR by FP assay
|
None
|
15.0
nM
|
|
|
Inhibition of IL1-stimulated IL6 production in HFF cells
|
Homo sapiens
|
6.6
nM
|
|
|
Induction of aromatase activity in HFF cells assessed as production of beta estradiol by aromatase assay
|
Homo sapiens
|
19.0
nM
|
|
|
Activation of MMTV in HeLa cells measured by luciferase activity
|
Homo sapiens
|
16.0
nM
|
|
|
Inhibition of LPS-stimulated TNFalpha production in BALB/c mouse at 3 mg/kg, po
|
Mus musculus
|
84.0
%
|
|
|
Displacement of [3H]dexamethasone from human glucocorticoid receptor alpha
|
Homo sapiens
|
13.8
nM
|
|
|
Activity at human glucocorticoid receptor in human A549 cells assessed as repression of human IL6
|
Homo sapiens
|
4.5
nM
|
|
|
Activity at human glucocorticoid receptor in human HepG2 cells assessed as tyrosine amino transferase activity
|
Homo sapiens
|
24.0
nM
|
|
|
Activity at human glucocorticoid receptor in C57BI/6 mouse peritoneal exudate cells assessed as repression of mouse IL6
|
Homo sapiens
|
5.7
nM
|
|
|
Activity at human glucocorticoid receptor in C2C12 cells assessed as mouse glutamine synthetase activity
|
Homo sapiens
|
3.4
nM
|
|
|
Antiinflammatory activity in mouse assessed as inhibition of LPS-induced TNFalpha at 3 mg/kg relative to prednisolone
|
Mus musculus
|
100.0
%
|
|
|
Agonist activity at GR by GRE activation assay
|
None
|
5.3
nM
|
|
|
Activity at GR assessed as repression of TNFalpha and IL 1-beta induced E-selectin response
|
None
|
4.1
nM
|
|
|
Displacement of radiolabeled Dexamethasone from glucocorticoid receptor
|
None
|
5.3
nM
|
|
|
Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay
|
Homo sapiens
|
8.511
nM
|
|
|
Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay
|
Homo sapiens
|
31.62
nM
|
|
|
Inhibition of DNFB-induced ear edema in mouse chronic dermatitis model at 10 mg/kg, ip after 24 hrs relative to control
|
Mus musculus
|
54.6
%
|
|
|
Displacement of radiolabeled Dexamethasone from glucocorticoid receptor
|
None
|
5.3
nM
|
|
|
Agonist activity at glucocorticoid receptor assessed as glucose response element transcriptional transactivation by luciferase assay
|
None
|
5.3
nM
|
|
|
Antagonist activity at glucocorticoid receptor assessed as inhibition of dexamethasone-induced glucose response element transcriptional transactivation by luciferase assay
|
None
|
1.0
nM
|
|
|
Activity at glucocorticoid receptor assessed as repression of TNFalpha and IL1 beta-induced E-selectin expression
|
None
|
4.1
nM
|
|
|
Displacement of FITC-dexamethasone from human recombinant glucocorticoid receptor alpha by fluorescence polarization assay
|
Homo sapiens
|
1.5
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
|
15.8
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
|
13.6
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
|
82.7
nM
|
|
|
Inhibition of lipopolysaccharide IL1-beta production in human PMNC at 0.3 ug/mL by ELISA
|
Homo sapiens
|
24.8
%
|
|
|
Inhibition of lipopolysaccharide IL2 production in human PMNC at 0.3 ug/mL by ELISA
|
Homo sapiens
|
30.6
%
|
|
|
Inhibition of lipopolysaccharide IL4 production in human PMNC at 0.3 ug/mL by ELISA
|
Homo sapiens
|
40.7
%
|
|
|
Inhibition of lipopolysaccharide TNFalpha production in human PMNC at 0.3 ug/mL by ELISA
|
Homo sapiens
|
47.9
%
|
|
|
Immunosuppressive activity in human PBMC assessed as inhibition of LPS-stimulated TNFalpha production at 0.3 ug/mL after 18 to 24 hrs by ELISA
|
Homo sapiens
|
52.0
%
|
|
|
Immunosuppressive activity in human PBMC assessed as inhibition of LPS-stimulated IL1-beta production at 0.3 ug/mL after 18 to 24 hrs by ELISA
|
Homo sapiens
|
68.0
%
|
|
|
Immunosuppressive activity in human PBMC assessed as inhibition of LPS-stimulated IL8 production at 0.3 ug/mL after 18 to 24 hrs by ELISA
|
Homo sapiens
|
15.0
%
|
|
|
Immunosuppressive activity in human PBMC assessed as inhibition of LPS-stimulated IL2 production at 0.3 ug/mL after 18 to 24 hrs by ELISA
|
Homo sapiens
|
65.0
%
|
|
|
Immunosuppressive activity in human PBMC assessed as inhibition of LPS-stimulated IL4 production at 0.3 ug/mL after 18 to 24 hrs by ELISA
|
Homo sapiens
|
76.0
%
|
|
|
Immunosuppressive activity in human PBMC assessed as inhibition of LPS-stimulated IFN-gamma production at 0.3 ug/mL after 18 to 24 hrs by ELISA
|
Homo sapiens
|
75.0
%
|
|
|
Inhibition of granuloma formation in cotton pellet implanted Lewis rat at 1.0 mg/kg, po bid
|
Rattus norvegicus
|
37.6
%
|
|
|
Inhibition of granuloma formation in cotton pellet implanted Lewis rat at 6.0 mg/kg, po bid
|
Rattus norvegicus
|
56.2
%
|
|
|
Inhibition of granuloma formation in cotton pellet implanted Lewis rat at 2.5 mg/kg, po bid
|
Rattus norvegicus
|
49.3
%
|
|
|
Immunosuppressive activity against human PBMC assessed as inhibition of LPS-induced TNFalpha production at 0.3 ug/ml after 24 hrs by ELISA
|
Homo sapiens
|
88.5
%
|
|
|
Immunosuppressive activity against human PBMC assessed as inhibition of LPS-induced IL8 production at 0.3 ug/ml after 24 hrs by ELISA
|
Homo sapiens
|
90.3
%
|
|
|
Immunosuppressive activity against human PBMC assessed as inhibition of LPS-induced IL1-beta production at 0.3 ug/ml after 24 hrs by ELISA
|
Homo sapiens
|
88.5
%
|
|
|
Immunosuppressive activity against human PBMC assessed as inhibition of LPS-induced IL4 production at 0.3 ug/ml after 24 hrs by ELISA
|
Homo sapiens
|
96.1
%
|
|
|
Immunosuppressive activity against human PBMC assessed as inhibition of LPS-induced IL2 production at 0.3 ug/ml after 24 hrs by ELISA
|
Homo sapiens
|
93.9
%
|
|
|
Immunosuppressive activity against human PBMC assessed as inhibition of LPS-induced IFN-gamma production at 0.3 ug/ml after 24 hrs by ELISA
|
Homo sapiens
|
95.4
%
|
|
|
Inhibition of LPS-induced IL10 production in human PBMC at 0.3 mg/mL after 48 hrs by ELISA
|
Homo sapiens
|
0.14
%
|
|
|
Inhibition of LPS-induced IL12 production in human PBMC at 0.3 mg/mL after 48 hrs by ELISA
|
Homo sapiens
|
0.24
%
|
|
|
Inhibition of LPS-induced TNFalpha production in human PBMC at 0.3 mg/mL after 48 hrs by ELISA
|
Homo sapiens
|
0.44
%
|
|
|
Immunosuppressive activity against human peripheral mononuclear cells assessed as inhibition of LPS-stimulated IL4 production at 0.3 ug/mL
|
Homo sapiens
|
55.3
%
|
|
|
Immunosuppressive activity against human peripheral mononuclear cells assessed as inhibition of LPS-stimulated IL2 production at 0.3 ug/mL
|
Homo sapiens
|
65.6
%
|
|
|
Immunosuppressive activity against human peripheral mononuclear cells assessed as inhibition of LPS-stimulated IFN-gamma production at 0.3 ug/mL
|
Homo sapiens
|
60.2
%
|
|
|
Inhibition of IL4 and LPS-induced IgE production in BALB/c mouse spleen B cell after 6 days by ELISA
|
Mus musculus
|
5.9
nM
|
|
|
Immunosuppressive activity in rat lymphocytes assessed as inhibition of mixed-lymphocyte reaction
|
Rattus norvegicus
|
78.0
nM
|
|
|
Inhibition of PHA-induced BALB/c mouse T cell proliferation at 10 uM
|
Mus musculus
|
84.0
%
|
|
|
Displacement of fluorescent labelled Dexamethasone from glucocorticoid receptor
|
None
|
12.59
nM
|
|
|
Inhibition of TNF-induced NF-kappaB activation in human A549 cells after 15 hrs
|
Homo sapiens
|
10.0
nM
|
|
|
Agonist activity at human glucocorticoid receptor in human A549 cells assessed as transcriptional activity by MMTV luciferase reporter gene assay
|
Homo sapiens
|
50.12
nM
|
|
|
Antiinflammatory activity in BALB/c mouse model assessed as inhibition of ovalbumin-induced ear swelling at 10 mg/kg, po administered 60 mins before ovalbumin challenge measured 1 hr after elicitation by immediate type reaction assay
|
Mus musculus
|
22.0
%
|
|
|
Antiinflammatory activity in BALB/c mouse model assessed as inhibition of ovalbumin-induced ear swelling at 10 mg/kg, po administered 60 mins before ovalbumin challenge measured 24 hrs after elicitation by late type reaction assay
|
Mus musculus
|
81.0
%
|
|
|
Antiinflammatory activity in albino rat assessed as inhibition of increase in plasma PGE2 level at 25 mg/kg, po by EIA
|
Rattus norvegicus
|
77.0
%
|
|
|
Antiinflammatory activity in albino rat assessed as inhibition of increase in plasma PGE2 level at 50 mg/kg, po by EIA
|
Rattus norvegicus
|
91.0
%
|
|
|
Displacement of [3H]DEX from human glucocorticoid receptor
|
Homo sapiens
|
2.4
nM
|
|
|
Binding affinity to human glucocorticoid receptor by fluorescence polarization competitive binding assay
|
Homo sapiens
|
7.0
nM
|
|
|
Agonist activity at glucocorticoid receptor in human fibroblast assessed as inhibition of IL-1-beta-induced IL6 production treated 1 hr before IL1-beta challenge measured after 24 hrs by transrepression assay
|
Homo sapiens
|
3.0
nM
|
|
|
Agonist activity at glucocorticoid receptor in human MDA-kb2 cells transfected with MMTV-LUC assessed as induction of MMTV-LTR/promoter linked LUC gene by luciferase transactivation assay
|
Homo sapiens
|
55.0
nM
|
|
|
Binding affinity to glucocorticoid receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled Dexamethasone by fluorescence polarization microplate assay
|
None
|
15.0
nM
|
|
|
Binding affinity to mineralocorticoid receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled Dexamethasone by fluorescence polarization microplate assay
|
None
|
44.0
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
|
6.6
nM
|
|
|
Antiinflammatory effect in collagen and Freund's complete adjuvant-induced B10.RIII mouse arthritis model assessed as inhibition of disease progression at 30 mg/kg, po qd for 5 weeks
|
Mus musculus
|
77.0
%
|
|
|
Displacement of radiolabeled Dexamethasone from glucocorticoid receptor expressed in baculovirus
|
None
|
5.3
nM
|
|
|
Agonist activity at glucocorticoid receptor in human HepG2 cells co-transfected with GRE assessed as transactivation activity by luciferase reporter gene assay
|
Homo sapiens
|
5.3
nM
|
|
|
Transrepression activity at glucocorticoid receptor in TNFalpha/IL1beta-stimulated human HepG2 cells assessed as inhibition of NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay
|
Homo sapiens
|
4.1
nM
|
|
|
Transrepression activity at glucocorticoid receptor in IL-1beta-stimulated human HepG2 cells assessed as inhibition of AP1 response element-induced IL-6 production by ELISA
|
Homo sapiens
|
23.0
nM
|
|
|
Displacement of radiolabeled Dexamethasone from GR
|
None
|
5.3
nM
|
|
|
Agonist activity at GR expressed in african green monkey CV1 cells transfected with luciferase gene linked to MMTV promoter assessed as induction of luciferase transactivation activity
|
None
|
5.3
nM
|
|
|
Agonist activity at GR expressed in rat H4IIEC3 cells assessed as induction of PEPCK transactivation by luciferase reporter gene assay
|
None
|
26.0
nM
|
|
|
Transrepression activity at GR expressed in IL-1beta- and TNFalpha-stimulated HepG2 cells assessed as inhibition of NFKB- or AP-1 mediated E-selectin transcription by luciferase reporter gene assay
|
None
|
4.1
nM
|
|
|
Transrepression activity at GR expressed in NHDF cells assessed as IL-1beta-mediated IL-6 transcription by ELISA
|
None
|
23.0
nM
|
|
|
Displacement of radiolabeled Dexamethasone from GR
|
None
|
5.3
nM
|
|
|
Agonist activity at GR expressed in african green monkey CV1 cells transfected with luciferase gene linked to MMTV promoter assessed as induction of luciferase transactivation activity relative to Dexamethasone
|
None
|
5.3
nM
|
|
|
Agonist activity at GR expressed in IL-1beta- and TNFalpha-stimulated HepG2 cells assessed as inhibition of NFKB- or AP-1 mediated E-selectin transcription by luciferase reporter gene assay relative to Dexamethasone
|
None
|
4.1
nM
|
|
|
Agonist activity at human GR expressed in NHDF cells assessed as inhibition of IL-6 production by ELISA relative to Dexamethasone
|
Homo sapiens
|
23.0
nM
|
|
|
Displacement of radiolabeled Dexamethasone from glucocorticoid receptor expressed in baculovirus
|
None
|
5.3
nM
|
|
|
Transrepression activity at glucocorticoid receptor in human HepG2 cells assessed as inhibition of TNFalpha/IL1beta-stimulated NFkappaB-dependent E-selectin repression by luciferase reporter gene assay
|
Homo sapiens
|
4.1
nM
|
|
|
Transrepression activity at glucocorticoid receptor in human NHDF cells assessed as inhibition of IL-1beta-stimulated AP1 dependent IL-6 repression by ELISA
|
Homo sapiens
|
23.0
nM
|
|
|
Agonist activity at glucocorticoid receptor in human HepG2 cells co-transfected with GRE assessed as GRE activation by luciferase reporter gene assay
|
Homo sapiens
|
5.3
nM
|
|
|
Agonist activity at glucocorticoid receptor in human HepG2 cells co-transfected with PEPCK assessed as GRE activation by luciferase reporter gene assay
|
Homo sapiens
|
26.0
nM
|
|
|
Displacement of GS-red from GRapha by fluorescence polarization assay
|
None
|
1.5
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
|
15.8
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
|
82.7
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
|
13.6
nM
|
|
|
Transactivation activity at glucocorticoid receptor in human 13D3/Huh7 cells assessed as induction of tyrosine aminotransferase activity after 24 hrs
|
Homo sapiens
|
57.4
nM
|
|
|
Agonist activity at mineralocorticoid receptor in human A549 cells
|
Homo sapiens
|
2.0
nM
|
|
|
Antiinflammatory activity against carrageenan-induced paw edema Sprague-Dawley rat model assessed as inhibition of hind paw swelling at 30 mg/kg, po measured after 5 hrs post carrageenan challenge
|
Rattus norvegicus
|
57.0
%
|
|
Antiinflammatory activity against carrageenan-induced paw edema Sprague-Dawley rat model assessed as inhibition of hind paw swelling at 30 mg/kg, po measured after 5 hrs post carrageenan challenge
|
Rattus norvegicus
|
42.0
%
|
|
|
DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
|
None
|
16.0
nM
|
|
DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
|
None
|
7.397
nM
|
|
|
Displacement of tetramethylrhodamine-labeled Dexamethasone from human recombinant glucocorticoid receptor expressed in baculovirus infected insect cells by fluorescence polarization assay
|
Homo sapiens
|
15.0
nM
|
|
|
Displacement of tetramethylrhodamine-labeled Dexamethasone from human recombinant mineralocorticoid receptor expressed in baculovirus infected insect cells by fluorescence polarization assay
|
Homo sapiens
|
44.0
nM
|
|
|
Agonist activity at glucocorticoid receptor in HFF assessed as inhibition of IL1-induced IL-6 production after 18 to 24 hrs
|
Homo sapiens
|
7.0
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
|
19.0
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
|
16.0
nM
|
|
|
Antiinflammatory activity in mouse plasma assessed as inhibition of LPS-induced TNFalpha production at 10 mg/kg, po administered 1 hr before LPS challenge measured after 1 hr
|
Mus musculus
|
84.0
%
|
|
|
Antiarthritic activity in B10.R3 mouse collagen-induced arthritis model assessed as AUC of disease progression inhibition at 30 mg/kg, po qd for 5 weeks
|
Mus musculus
|
80.0
%
|
|
|
Antiarthritic activity in B10.R3 mouse collagen-induced arthritis model assessed as AUC of disease progression inhibition at 3 mg/kg, po qd for 5 weeks
|
Mus musculus
|
42.0
%
|
|
|
Antiarthritic activity in B10.R3 mouse collagen-induced arthritis model assessed as AUC of disease progression inhibition at 10 mg/kg, po qd for 5 weeks
|
Mus musculus
|
62.0
%
|
|
|
Displacement of GS-red from glucocorticoid receptor by fluorescence polarization assay
|
None
|
1.5
nM
|
|
|
Agonist activity at human mineralocorticoid receptor expressed in human A549 cells by fluorescence polarization assay
|
Homo sapiens
|
0.002
nM
|
|
|
Transrepression activity at glucocorticoid receptor alpha in phorbol myristate acetate-stimulated human A549 cells assessed as inhibition of AP1 response element by luciferase reporter gene assay
|
Homo sapiens
|
16.1
nM
|
|
|
Transrepression activity at glucocorticoid receptor alpha in IL-1beta-stimulated human A549 cells assessed as inhibition of NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay
|
Homo sapiens
|
14.4
nM
|
|
|
Transactivation activity at GR-alpha in human NP1 Hela cells assessed as induction of GAL4-DBD after 20 hrs by luciferase reporter gene assay
|
Homo sapiens
|
73.9
nM
|
|
|
Transactivation activity at glucocorticoid receptor alpha human 13D3/Huh7 cells assessed as induction of TAT activity after 4 hrs by spectrophotometry
|
Homo sapiens
|
64.0
nM
|
|
|
Transactivation activity at GR-alpha in human NP1 Hela cells assessed as inhibition of GAL4-DBD after 20 hrs by luciferase reporter gene assay
|
Homo sapiens
|
21.0
nM
|
|
|
Induction of glutamine synthase expression in human MG63 cells after overnight incubation by spectrophotometry
|
Homo sapiens
|
19.0
nM
|
|
|
Antiinflammatory activity in human whole blood assessed as inhibition of LPS-induced TNFalpha production after overnight incubation by ELISA
|
Homo sapiens
|
89.0
nM
|
|
|
Antiinflammatory activity in human whole blood assessed as inhibition of TNF-alpha-induced IL-8 production after overnight incubation by ELISA
|
Homo sapiens
|
124.0
nM
|
|
|
Antiinflammatory activity in human whole blood assessed as inhibition of IL-1beta-induced IL-8 production after overnight incubation by ELISA
|
Homo sapiens
|
104.0
nM
|
|
|
Antiinflammatory activity in Sprague-Dawley rat assessed as inhibition of carrageenan-induced paw edema at 30 mg/kg, po administered as a single dose 2 hrs before carrageenan challenge measured 4 hrs post carrageenan challenge by plethysmometry relative to control
|
Rattus norvegicus
|
49.0
%
|
|
|
Transrepression activity at glucocorticoid receptor in human H292 cells assessed as inhibition of TNF-stimulated IL-8 production
|
Homo sapiens
|
7.7
nM
|
|
|
Transactivation of glucocorticoid receptor in rat H42E cells assessed as induction of TAT measuring degradation of tyrosine to p-hydroxy phenyl pyruvate
|
Rattus norvegicus
|
65.4
nM
|
|
|
Transactivation of glucocorticoid receptor in human HepG2 cells assessed as induction of TAT measuring degradation of tyrosine to p-hydroxy phenyl pyruvate
|
Homo sapiens
|
340.0
nM
|
|
|
Antiinflammatory activity in ovalbumin-induced allergic Brown Norway rat lung inflammation model assessed as inhibition of forced vital capacity at 3 mg/kg, po qd administered 3 days before ovalbumin-challenge measured 24 hrs of post ovalbumin challenge
|
Rattus norvegicus
|
43.0
%
|
|
|
Antiinflammatory activity in ovalbumin-induced allergic Brown Norway rat lung inflammation model assessed as inhibition of forced vital capacity at 10 mg/kg, po qd administered 3 days before ovalbumin-challenge measured 24 hrs of post ovalbumin challenge
|
Rattus norvegicus
|
81.0
%
|
|
|
Antiinflammatory activity in ovalbumin-induced allergic Brown Norway rat lung inflammation model assessed as inhibition of forced vital capacity at 30 mg/kg, po qd administered 3 days before ovalbumin-challenge measured 24 hrs of post ovalbumin challenge
|
Rattus norvegicus
|
111.0
%
|
|
|
Antiinflammatory activity in LPS-stimulated acute inflammation BALB/c mouse model assessed as inhibition of plasma PAI-1 level at 10 mg/kg, po administered 2 hrs before LPS challenge
|
Mus musculus
|
43.0
%
|
|
|
Antiinflammatory activity in LPS-stimulated acute inflammation BALB/c mouse model assessed as inhibition of plasma IL-6 level at 10 mg/kg, po administered 2 hrs before LPS challenge
|
Mus musculus
|
59.0
%
|
|
|
Antiinflammatory activity in LPS-stimulated acute inflammation BALB/c mouse model assessed as inhibition of plasma MCP-1 level at 10 mg/kg, po administered 2 hrs before LPS challenge
|
Mus musculus
|
49.0
%
|
|
|
Antiinflammatory activity in LPS-stimulated acute inflammation BALB/c mouse model assessed as inhibition of plasma TNF-alpha level at 10 mg/kg, po administered 2 hrs before LPS challenge
|
Mus musculus
|
94.0
%
|
|
|
Antiinflammatory activity in Brown Norway rat lung inflammation model assessed as total cell inhibition at 10 mg/kg, po for 3 days
|
Rattus norvegicus
|
56.0
%
|
|
|
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
|
2.3
%
|
|
|
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
|
9.6
%
|
|
|
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
|
27.6
%
|
|
|
In vivo inhibition of PGE2 in albino rat plasma at 50 mg/kg, po administered 1 hr prior to carrageenan challenge measured after 4 hrs by EIA relative to control
|
Rattus norvegicus
|
92.1
%
|
|
|
In vivo inhibition of PGE2 in albino rat plasma at 25 mg/kg, po administered 1 hr prior to carrageenan challenge measured after 4 hrs by EIA relative to control
|
Rattus norvegicus
|
78.1
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
79.83
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
110.37
%
|
|
|
Antiinflammatory activity in PMA-differentiated human U937 cells assessed as inhibition of LPS-induced TNFalpha production incubated for 60 mins prior to LPS challenge measured after 24 hrs
|
Homo sapiens
|
8.2
nM
|
|
|
Antiinflammatory activity in human CCD-39SK cells assessed as inhibition of IL-1beta-induced IL-6 production incubated for 60 mins prior to IL-1beta induction measured after 24 hrs
|
Homo sapiens
|
7.26
nM
|
|
|
Displacement of [3H]-dexamethasone from human glucocorticoid receptor expressed in HEK293 cells
|
Homo sapiens
|
1.14
nM
|
|
|
Displacement of [3H]-aldosterone from human mineralocorticoid receptor expressed in HEK293 cells
|
Homo sapiens
|
0.29
nM
|
|
|
Displacement of TAMRA-labeled dexamethasone from glucocorticoid receptor (unknown origin) by fluorescence polarization assay
|
Homo sapiens
|
15.0
nM
|
|
|
Displacement of TAMRA-labeled dexamethasone from mineralocorticoid receptor (unknown origin) by fluorescence polarization assay
|
Homo sapiens
|
44.0
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
|
6.0
nM
|
|
|
Antiinflammatory activity in mouse assessed as inhibition of LPS-induced TNFalpha production at 3 mg/kg, po
|
Mus musculus
|
87.0
%
|
|
|
Antiinflammatory activity in Lewis rat assessed as inhibition of LPS-induced TNF-alpha production at 30 mg/kg, po administered 90 mins prior to LPS challenge measured after 90 mins relative to vehicle-treated control
|
Rattus norvegicus
|
75.0
%
|
|
|
Fluorescence Polarization Ligand Binding Assay: The glucocorticoid receptor fluorescence polarization ligand binding (GRFP) assay is used to evaluate direct binding of testing compounds to full-length glucocorticoid (GR) protein. Reagents for this assay are purchased from Invitrogen in a test kit. A fluorescent labeled GR ligand is used as a fluorescent tracer and test compounds compete with the fluorescent tracer for GR binding. The change in polarization value in the presence of test compounds is due to binding of test compounds to GR and is used to determine IC50 and relative binding affinity of test compounds for GR.
|
None
|
4.2
nM
|
|
|
Fluorescence Polarization Ligand Binding Assay: The glucocorticoid receptor fluorescence polarization ligand binding (GRFP) assay is used to evaluate direct binding of testing compounds to full-length glucocorticoid (GR) protein. Reagents for this assay are purchased from Invitrogen in a test kit. A fluorescent labeled GR ligand is used as a fluorescent tracer and test compounds compete with the fluorescent tracer for GR binding. The change in polarization value in the presence of test compounds is due to binding of test compounds to GR and is used to determine IC50 and relative binding affinity of test compounds for GR.
|
None
|
14.9
nM
|
|
|
Fluorescence Polarization Ligand Binding Assay: The glucocorticoid receptor fluorescence polarization ligand binding (GRFP) assay is used to evaluate direct binding of testing compounds to full-length glucocorticoid (GR) protein. Reagents for this assay are purchased from Invitrogen in a test kit. A fluorescent labeled GR ligand is used as a fluorescent tracer and test compounds compete with the fluorescent tracer for GR binding. The change in polarization value in the presence of test compounds is due to binding of test compounds to GR and is used to determine IC50 and relative binding affinity of test compounds for GR.
|
None
|
0.526
nM
|
|
|
Inhibition of LPS-induced TNF-alpha production in mouse RAW264.7 cells pretreated with compound at 10 uM for 1 hr followed by addition of 1 ug/ml LPS for 6 hrs by ELISA
|
Mus musculus
|
42.8
%
|
|
|
Agonist activity at TGR5 in human whole blood assessed as inhibition of LPS-induced TNF-alpha release
|
Homo sapiens
|
251.0
nM
|
|
|
Binding affinity to GR (unknown origin) by FP assay
|
Homo sapiens
|
6.1
nM
|
|
|
Antiinflammatory activity in human primary PBMC assessed as inhibition of LPS-induced TNFalpha release preincubated for 45 mins followed by LPS addition after 18 hrs by ELISA
|
Homo sapiens
|
45.0
nM
|
|
|
Antiinflammatory activity in human whole blood assessed as inhibition of LPS-induced TNFalpha release preincubated for 45 mins followed by LPS addition after 18 hrs by ELISA
|
Homo sapiens
|
160.0
nM
|
|
|
Displacement of 3H-aldosterone from MR (unknown origin) ligand binding domain by SPA assay
|
Homo sapiens
|
18.0
nM
|
|
|
Antiinflammatory activity in Wistar rat PBMC assessed as inhibition of LPS-induced TNFalpha release preincubated for 45 mins followed by LPS addition after 18 hrs by ELISA
|
Rattus norvegicus
|
13.0
nM
|
|
|
Antiinflammatory activity in rat whole blood assessed as inhibition of LPS-induced TNFalpha release preincubated for 45 mins followed by LPS addition after 18 hrs by ELISA
|
Rattus norvegicus
|
50.0
nM
|
|
|
Antiarthritic activity in rat model of collagen-induced arthritis assessed as inhibition of paw swelling at 3 mg/kg, bid for 8 days relative to control
|
Rattus norvegicus
|
86.0
%
|
|
|
Displacement of fluormone RED from human full length glucocorticoid receptor after 4 hrs by fluorescence polarization assay
|
Homo sapiens
|
7.0
nM
|
|
|
Transactivation activity at glucocorticoid receptor (unknown origin) expressed in human ChaGoK1 cells incubated for 24 hrs by beta-galactosidase reporter gene assay
|
Homo sapiens
|
110.0
nM
|
|
|
Transrepression activity at glucocorticoid receptor (unknown origin) expressed in human ChaGoK1 cells assessed as inhibition of PMA-stimulated gene expression incubated for 24 hrs by beta-galactosidase reporter gene assay
|
Homo sapiens
|
40.0
nM
|
|
|
Transrepression of GR in human whole blood assessed as inhibition of LPS-induced TNF-alpha release preincubated for 45 mins followed by LPS addition after 18 hrs by AlphaLISA method
|
Homo sapiens
|
300.0
nM
|
|
|
Displacement of [3H]-aldosterone from human mineralocorticoid receptor LBD (729 to 984 residues) after 1 hr by scintillation proximity assay
|
Homo sapiens
|
11.0
nM
|
|
|
Modulation of glucocorticoid receptor in rat whole blood
|
Rattus norvegicus
|
52.0
nM
|
|
|
Modulation of glucocorticoid receptor in rat plasma
|
Rattus norvegicus
|
52.0
nM
|
|
|
Antibacterial activity against Staphylococcus aureus MRSA ATCC 43300 (CO-ADD:GP_020); MIC in CAMBH media, using NBS plates, by OD(600)
|
Staphylococcus aureus subsp. aureus
|
7.56
%
|
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
7.41
%
|
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
15.03
%
|
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
12.94
%
|
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
15.17
%
|
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
1.1
%
|
|
|
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
|
-7.92
%
|
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging
|
Homo sapiens
|
4.68
%
|
|
|
Antiinflammatory activity in Sprague-Dawley rat whole blood assessed as inhibition of LPS-induced TNFalpha production measured after 18 hrs by AlphaLisa assay
|
Rattus norvegicus
|
4.6
nM
|
|
|
Displacement of [3H]dexamethasone from GR in human IM9 cells after 6 hrs by scintillation counting method
|
Homo sapiens
|
13.0
nM
|
|
|
Antiinflammatory activity in human A549 cells assessed as inhibition of IL1beta-induced IL6 production preincubated for 30 mins followed by IL1beta-stimulation and measured after 20 hrs by AlphaLisa assay
|
Homo sapiens
|
5.8
nM
|
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
25.57
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
14.7
%
|
|
|
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
|
0.0
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
0.07
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
0.0
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
0.07
%
|
|
|
Antiinflammatory activity in human U937 cells assessed as inhibition of PMA/LPS-stimulated TNFalpha production at 1 uM after 24 hrs by ELISA relative to control
|
Homo sapiens
|
98.0
%
|
|
|
Antiinflammatory activity in human U937 cells assessed as inhibition of PMA/LPS-stimulated TNFalpha production after 24 hrs by ELISA
|
Homo sapiens
|
33.0
nM
|
|
|
Inhibition of LPS-induced TNF-alpha expression in human U-937 cells preincubated for 1 hr followed by LPS addition and measured after 24 hrs by ELISA
|
Homo sapiens
|
640.0
nM
|
|
|
Inhibition of LPS-induced IL-1beta expression in human U-937 cells preincubated for 1 hr followed by LPS addition and measured after 24 hrs by ELISA
|
Homo sapiens
|
440.0
nM
|
|
