mouse thymocytes |
Function assay |
1 μM |
24 h |
Induction of apoptosis in mouse thymocytes assessed as internucleosomal DNA fragmentation at 1 uM after 24 hrs by agarose gel electrophoresis |
24794748 |
human monocytes |
Function assay |
5 μM |
20 h |
Antiinflammatory activity in human monocytes assessed as inhibition of LPS-induced COX2 expression at 5 uM after 20 hrs using rabbit polyclonal antibody IgG by SDS-PAGE analysis |
21843935 |
R1 |
Function assay |
10 uM |
24 hrs |
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, IC50 = 0.005 μM. |
18412397 |
NIH-3T3 |
Function assay |
0.01 mg/kg |
1 hr |
Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.01 mg/kg, po after 1 hr, Cp = 0.044 μM. |
20469868 |
NIH-3T3 |
Function assay |
0.1 mg/kg |
1 hr |
Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.1 mg/kg, po after 1 hr, Cp = 0.236 μM. |
20469868 |
NIH-3T3 |
Function assay |
1 mg/kg |
1 hr |
Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 1 mg/kg, po after 1 hr, Cp = 1.8 μM. |
20469868 |
NIH-3T3 |
Function assay |
10 mg/kg |
1 hr |
Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 10 mg/kg, po after 1 hr, Cp = 17.7 μM. |
20469868 |
NIH-3T3 |
Function assay |
0.01 mg/kg |
1 hr |
Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.01 mg/kg, po after 1 hr, Fu = 0.00203 μM. |
20469868 |
NIH-3T3 |
Function assay |
0.1 mg/kg |
1 hr |
Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.1 mg/kg, po after 1 hr, Fu = 0.0116 μM. |
20469868 |
NIH-3T3 |
Function assay |
1 mg/kg |
1 hr |
Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 1 mg/kg, po after 1 hr, Fu = 0.087 μM. |
20469868 |
NIH-3T3 |
Function assay |
10 mg/kg |
1 hr |
Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 10 mg/kg, po after 1 hr, Fu = 5.123 μM. |
20469868 |
RAW264.7 |
Antiinflammatory assay |
10 uM |
24 hrs |
Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as nitrite level at 10 uM after 24 hrs by Griess method, Activity = 1.54 μM. |
21353543 |
A549 |
Antiinflammatory assay |
1 uM |
30 mins |
Antiinflammatory activity in human A549 cells assessed as inhibition of IL-1beta-induced mPGES1 expression at 1 uM treated 30 mins prior to IL-1beta challenge measured after 48 hrs by Western blot analysis relative to control |
22795900 |
IOBA-NHC |
Function assay |
40 uM |
24 hrs |
Inhibition of NF-kappaB p65-mediated IL-6 release in HSV1 KOS infected human IOBA-NHC cells at 40 uM after 24 hrs by ELISA |
23219855 |
IOBA-NHC |
Function assay |
40 uM |
24 hrs |
Inhibition of NF-kappaB p65-mediated TNFalpha release in HSV1 KOS infected human IOBA-NHC cells at 40 uM after 24 hrs by ELISA |
23219855 |
IOBA-NHC |
Function assay |
40 uM |
24 hrs |
Inhibition of NF-kappaB p65-mediated IL-8 release in HSV1 KOS infected human IOBA-NHC cells at 40 uM after 24 hrs by ELISA |
23219855 |
HCLE |
Function assay |
40 uM |
24 hrs |
Inhibition of NF-kappaB p65-mediated IL-8 release in HSV1 KOS infected human HCLE cells at 40 uM after 24 hrs by ELISA |
23219855 |
HCT116 |
Function assay |
20 to 40 uM |
24 hrs |
Agonist activity at glucocorticoid receptor (unknown origin) expressed in human HCT116 cells co-expressing GRE at 20 to 40 uM after 24 hrs by luciferase reporter gene assay |
23276449 |
B16F10 |
Antitumor assay |
20 mg/kg |
24 days |
Antitumor activity against mouse B16F10 cells xenografted in C57BL/6 mouse assessed as inhibition tumor growth at 20 mg/kg, ip measured after 24 days of tumor inoculation |
24992071 |
B16F10 |
Antitumor assay |
20 mg/kg |
24 days |
Antitumor activity against mouse B16F10 cells xenografted in C57BL/6 mouse assessed as apoptotic regions at 20 mg/kg, ip measured after 24 days of tumor inoculation by TUNEL assay |
24992071 |
B16F10 |
Apoptosis assay |
10 uM |
48 hrs |
Induction of apoptosis in mouse B16F10 cells assessed as increase in ratio of BAX/Bcl2 expression at 10 uM after 48 hrs by Western blot analysis relative to untreated control |
24992071 |
B16F10 |
Antitumor assay |
20 mg/kg |
24 days |
Antitumor activity against mouse B16F10 cells xenografted in C57BL/6 mouse assessed as apoptotic regions at 20 mg/kg, ip measured after 24 days of tumor inoculation by VE-cadherin |
24992071 |
RAW264.7 |
Antiinflammatory assay |
1 mM |
30 mins |
Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction of LPS-induced TNF mRNA expression cells at 1 mM treated 30 mins before LPS challenge measured after 3 hrs by qRT-PCR analysis |
25667960 |
J774 |
Antiinflammatory assay |
10 uM |
24 hrs |
Antiinflammatory activity against mouse J774 cells assessed as inhibition of LPS-induced iNOS expression at 10 uM after 24 hrs by Western blot analysis |
26915998 |
C57BL/6 |
Antiinflammatory assay |
10 mg/kg |
1 hr |
Antiinflammatory activity in C57BL/6 mouse assessed as inhibition of zymosan-induced mononuclear cells migration in articular cavity at 10 mg/kg, ip administered 1 hr prior to zymosan challenge measured at 6 to 24 hrs |
27227459 |
C57BL/6 |
Antiinflammatory assay |
10 mg/kg |
1 hr |
Antiinflammatory activity in C57BL/6 mouse assessed as inhibition of zymosan-induced infiltration of inflammatory cells into synovial tissue at 10 mg/kg, ip administered 1 hr prior to zymosan challenge measured at 6 to 24 hrs by hematoxylin and eosin stai |
27227459 |
J774A.1 |
Antiinflammatory assay |
1 uM |
1 hr |
Antiinflammatory activity in mouse J774A.1 cells assessed as inhibition of zymosan and IFNgamma-induced IL6 production in cell-free supernatant at 1 uM preincubated for 1 hr followed by zymosan and IFNgamma addition measured after 24 hrs by sandwich ELISA |
27227459 |
J774A.1 |
Antiinflammatory assay |
1 uM |
1 hr |
Antiinflammatory activity in mouse J774A.1 cells assessed as inhibition of zymosan and IFNgamma-induced COX2 expression at 1 uM preincubated for 1 hr followed by zymosan and IFNgamma addition measured after 24 hrs by Western blot analysis |
27227459 |
J774A.1 |
Antiinflammatory assay |
1 uM |
1 hr |
Antiinflammatory activity in mouse J774A.1 cells assessed as inhibition of zymosan and IFNgamma-induced nitric oxide production at 1 uM preincubated for 1 hr followed by zymosan and IFNgamma addition measured after 24 hrs by colorimetric Griess test |
27227459 |
Mino |
Antiproliferative assay |
100 uM |
48 hrs |
Antiproliferative activity against human Mino cells at 100 uM preincubated for 48 hrs followed by thymidine addition measure after 16 hrs by Thymidine incorporation assay |
28858511 |
RAW264.7 |
Function assay |
10 uM |
1 hr |
Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in COX2 mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR analysi |
29389121 |
RAW264.7 |
Function assay |
10 uM |
1 hr |
Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in iNOS mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR analysi |
29389121 |
RAW264.7 |
Function assay |
10 uM |
1 hr |
Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in TNFalpha mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR ana |
29389121 |
RAW264.7 |
Function assay |
10 uM |
1 hr |
Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-1beta mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR ana |
29389121 |
RAW264.7 |
Function assay |
10 uM |
1 hr |
Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-6 mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR analysi |
29389121 |
RAW264.7 |
Function assay |
10 uM |
1 hr |
Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in NO production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs by Grie |
29389121 |
RAW264.7 |
Function assay |
10 uM |
1 hr |
Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-1beta production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs b |
29389121 |
RAW264.7 |
Function assay |
10 uM |
1 hr |
Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-6 production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs by EL |
29389121 |
RAW264.7 |
Function assay |
10 uM |
1 hr |
Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in TNFalpha production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 3 hrs by |
29389121 |
RAW264.7 |
Function assay |
10 uM |
1 hr |
Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in iNOS protein level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs by |
29389121 |
HeLa |
Function assay |
0.4 uM |
24 hrs |
Transrepression of GCR in human HeLa cells assessed as suppression of DEX-induced GILZ mRNA expression at 0.4 uM after 24 hrs by Taqman-based real-time PCR analysis |
29670697 |
RAW264.7 |
Antiinflammatory assay |
20 uM |
6 hrs |
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA |
30215255 |
RAW264.7 |
Antiinflammatory assay |
20 uM |
6 hrs |
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-1beta production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA |
30215255 |
RAW264.7 |
Antiinflammatory assay |
20 uM |
6 hrs |
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrite production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA |
30215255 |
RAW264.7 |
Antiinflammatory assay |
20 uM |
6 hrs |
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA |
30215255 |
A549 |
Function assay |
10 uM |
|
Antagonist activity for Glucocorticoid receptor in MMTV transactivation assay in human A549 lung epithelial cells at 10 uM, IC50 = 10 μM. |
15999989 |
COS7 |
Function assay |
1 uM |
|
Agonist activity at glucocorticoid receptor Q570A mutant in COS7 cells at 1 uM by NF-kappaB-luciferase reporter gene assay |
18038970 |
RAW264.7 |
Function assay |
10 uM |
|
Inhibition of LPS-stimulated COX2 expression in mouse RAW264.7 cells at 10 uM by Western blot |
18790649 |
RAW264.7 |
Function assay |
|
2 hrs |
Inhibition of mPGES1 expression in LPS-stimulated mouse RAW264.7 cells after 2 hrs by Western blot analysis |
17407277 |
RAW264.7 |
Function assay |
|
2 hrs |
Inhibition of COX2 expression in LPS-stimulated mouse RAW264.7 cells after 2 hrs by Western blot analysis |
17407277 |
RAW 264.7 |
Function assay |
|
24 hrs |
Inhibition of interferon gamma-stimulated NO production in RAW 264.7 cells after 24 hrs, IC50 = 0.02 μM. |
17367124 |
RAW264.7 |
Antiinflammatory assay |
|
24 hrs |
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, IC50 = 0.7 μM. |
11908984 |
rat polymorphonuclear leukocytes |
Function assay |
|
20 mins |
Antiinflammatory activity in rat polymorphonuclear leukocytes assessed as inhibition of LPS-stimulated nitric oxide production after 20 mins by Griess method, IC50=2.3 nM |
22506620 |
RPMI8226 |
Antiproliferative assay |
|
4 days |
Antiproliferative activity against human RPMI8226 cells after 4 days, IC50 = 0.0065 μM. |
17705362 |
TH2 |
Function assay |
|
48 hrs |
Inhibition of pro-inflammatory cytokine IL5 production in ovalbumin-stimulated BALB/c mouse TH2 cells after 48 hrs by sandwich-ELISA, IC50 = 0.005 μM. |
19323483 |
TH2 |
Function assay |
|
48 hrs |
Inhibition of pro-inflammatory cytokine IL13 production in ovalbumin-stimulated BALB/c mouse TH2 cells after 48 hrs by sandwich-ELISA, IC50 = 0.005 μM. |
19323483 |
A549 |
Function assay |
|
6 hrs |
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, EC50 = 0.0011 μM. |
20047280 |
A549 |
Function assay |
|
6 hrs |
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, EC50 = 0.0025 μM. |
20047280 |
U2OS |
Function assay |
|
18 hrs |
Agonist activity at glucocorticoid receptor-LBD in human U2OS cells transfected with Gal4-DBD assessed as increase of transactivation activity after 18 hrs by luciferase reporter gene assay, EC50 = 15.8489 μM. |
20812681 |
U2OS |
Function assay |
|
18 hrs |
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, IC50 = 0.0005082 μM. |
20812681 |
HepG2 |
Function assay |
|
24 hrs |
Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis, EC50 = 2.6 μM. |
20966043 |
13D3/Huh7 |
Function assay |
|
24 hrs |
Transactivation activity at glucocorticoid receptor in human 13D3/Huh7 cells assessed as induction of tyrosine aminotransferase activity after 24 hrs, EC50 = 0.005 μM. |
21073190 |
RAW264.7 |
Antiinflammatory assay |
|
18 hrs |
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, IC50 = 0.86 μM. |
21288727 |
HMC1 |
Function assay |
|
1 hr |
Immunomodulatory activity in human HMC1 cells assessed as inhibition of phorbol 12-myristate 13-acetate/A23187-stimulated IL1-beta secretion treated 1 hr prior to 30 mins phorbol 12-myristate 13-acetate/A23187 challenge by Western blotting analysis |
21302967 |
RAW264.7 |
Antiinflammatory assay |
|
18 hrs |
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha secretion after 18 hrs, IC50 = 0.01 μM. |
21353543 |
RAW264.7 |
Antiinflammatory assay |
|
24 hrs |
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess method, IC50 = 0.8 μM. |
21353543 |
RAW264.7 |
Antiinflammatory assay |
|
24 hrs |
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFN-gamma induced NO production after 24 hrs by Griess reaction, IC50 = 0.02 μM. |
21361338 |
RAW264.7 |
Function assay |
|
20 mins |
Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells pre-incubated for 20 mins before LPS challenge measured 18 hrs post LPS challenge by Griess method |
21775152 |
RAW264.7 |
Function assay |
|
30 mins |
Inhibition of LPS-induced TNFalpha production in mouse RAW264.7 cells pre-incubated for 30 mins before LPS challenge measured 6 hrs post LPS challenge by ELISA |
21775152 |
RAW264.7 |
Antiinflammatory assay |
|
2 hrs |
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, IC50 = 0.47 μM. |
22372956 |
RAW264.7 |
Antiinflammatory assay |
|
2 hrs |
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, IC50 = 0.98 μM. |
22537362 |
H13 |
Function assay |
|
3 hrs |
Inhibition of glucocorticoid receptor in human H13 cells assessed as inhibition of glucocorticoid-induced cell proliferation after 3 hrs by [3H]-thymidine incorporation assay, EC50 = 0.0097 μM. |
23199485 |
293 MSR |
Function assay |
|
60 mins |
Displacement of [3H]-dexamethasone human glucocorticoid receptor alpha expressed in 293 MSR cells after 60 mins by scintillation counting, EC50 = 0.0125 μM. |
23199485 |
RAW264.7 |
Antiinflammatory assay |
|
2 hrs |
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 2 hrs prior to LPS-challenge measured after 24 hrs by Griess method, IC50 = 1.43 μM. |
23373965 |
HeLaS3 |
Function assay |
|
2 hrs |
Displacement of [3H]Dexamethasone from glucocorticoid receptor in human HeLaS3 cells after 2 hrs, IC50 = 0.0041 μM. |
23403082 |
HeLaS3 |
Function assay |
|
2 hrs |
Displacement of [3H]Dexamethasone from glucocorticoid receptor in human HeLaS3 cells after 2 hrs, Ki = 0.0022 μM. |
23403082 |
CUTLL1 |
Growth inhibition assay |
|
48 hrs |
Growth inhibition of human CUTLL1 cells with high GR expression levels after 48 hrs by alamar blue assay |
25050160 |
RAW264.7 |
Function assay |
|
24 hrs |
Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay relative to vehicle-treated control, IC50 = 0.8 μM. |
25499882 |
SW1353 |
Function assay |
|
24 hrs |
Transrepression activity at glucocorticoid receptor in human SW1353 cells assessed as repression of IL-1-induced MMP-13 production after 24 hrs by ELISA, IC50 = 0.0018 μM. |
25706100 |
RAW264.7 |
Function assay |
|
6 hrs |
Inhibition of TNFalpha production in mouse RAW264.7 cells incubated for 6 hrs by sandwich immunoassay, IC50 = 0.04 μM. |
25824662 |
J774A.1 |
Function assay |
|
6 hrs |
Inhibition of TNFalpha production in mouse J774A.1 cells incubated for 6 hrs by sandwich immunoassay, IC50 = 0.4 μM. |
25824662 |
RAW264.7 |
Function assay |
|
12 hrs |
Inhibition of IL-1beta production in mouse RAW264.7 cells incubated for 12 hrs by sandwich immunoassay, IC50 = 4.7 μM. |
25824662 |
J774A.1 |
Function assay |
|
12 hrs |
Inhibition of IL-1beta production in mouse J774A.1 cells incubated for 12 hrs by sandwich immunoassay, IC50 = 22 μM. |
25824662 |
RAW264.7 |
Antiinflammatory assay |
|
24 hrs |
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50 = 0.63 μM. |
26087384 |
BV2 |
Antiinflammatory assay |
|
24 hrs |
Antiinflammatory activity in C57BL6/J mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50 = 0.025 μM. |
26110443 |
RAW264.7 |
Function assay |
|
24 hrs |
Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay, IC50 = 0.8 μM. |
26305406 |
RAW264.7 |
Antiinflammatory assay |
|
24 hrs |
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, IC50 = 0.63 μM. |
27825545 |
RAW264.7 |
Antiinflammatory assay |
|
30 mins |
Antiinflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced NO production pretreated for 30 mins followed by LPS stimulation for 24 hrs by Griess assay, IC50 = 7 μM. |
28499733 |
RAW264.7 |
Function assay |
|
24 hrs |
Inhibition of LPS-induced NO production in mouse RAW264.7 cells after 24 hrs by Griess assay, IC50 = 2.5 μM. |
28598633 |
RAW264.7 |
Function assay |
|
24 hrs |
Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay, IC50 = 10.7 μM. |
29518326 |
HFF |
Antiinflammatory assay |
|
|
Antiinflammatory activity assessed as upregulation of aromatase in HFF cells by transactivation assay, EC50 = 0.002 μM. |
17692519 |
HFF |
Antiinflammatory assay |
|
|
Antiinflammatory activity assessed as inhibition of IL1 stimulated IL6 production in HFF cells by transrepression assay, EC50 = 0.0005 μM. |
17692519 |
A549 |
Function assay |
|
|
Antagonist activity at glucocorticoid receptor in human A549 cells transfected with MMTV luciferase reporter gene assessed as inhibition of dexamethasone-induced activation, IC50 = 1 μM. |
17616395 |
A549 |
Function assay |
|
|
Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001 μM. |
17616395 |
A549 |
Function assay |
|
|
Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay, EC50 = 0.00537 μM. |
17616395 |
HFF |
Function assay |
|
|
Inhibition of IL1-stimulated IL6 production in HFF cells, IC50 = 0.00051 μM. |
17181172 |
HeLa |
Function assay |
|
|
Activation of MMTV in HeLa cells measured by luciferase activity, EC50 = 0.017 μM. |
17181172 |
HFF |
Function assay |
|
|
Induction of aromatase activity in HFF cells assessed as production of beta estradiol by aromatase assay, EC50 = 0.0019 μM. |
17181172 |
A549 |
Function assay |
|
|
Agonist activity at GR assessed as NF-kappaB-mediated transrepression of secreted placental alkaline phosphatase gene in human A549 cells, IC50 = 0.001175 μM. |
16821781 |
A549 |
Function assay |
|
|
Agonist activity at GR assessed as MMTV-mediated transactivation of renilla luciferase gene in human A549 cells relative to Dexamethasone, EC50 = 0.005012 μM. |
16821781 |
A549 |
Function assay |
|
|
Activity at glucocorticoid receptor in human A549 cells assessed as effect on GRE promoter response by luciferase reporter assay, EC50 = 0.001 μM. |
16643060 |
RAW 264.7 |
Function assay |
|
|
Inhibitory activity against TNF-alpha release in RAW 264.7 cells in the supernatant, IC50 = 0.42 μM. |
12361395 |
N9 |
Function assay |
|
|
Inhibitory activity against TNF-alpha release in N9 cells in the supernatant, IC50 = 0.074 μM. |
12361395 |
PBMC |
Function assay |
|
|
Inhibitory concentration against growth of LPS stimulated human peripheral blood mononuclear cells, IC50 = 0.04 μM. |
11229767 |
PBMC |
Function assay |
|
|
Inhibitory concentration against TNF-alpha production from human peripheral blood mononuclear cells stimulated by LPS, IC50 = 0.01 μM. |
11229767 |
T-cell |
Function assay |
|
|
Inhibitory concentration against T cell proliferation using concanavalin A stimulated mice spleen cells, IC50 = 0.005 μM. |
11229767 |
CV1 |
Function assay |
|
|
Agonist activity at human GR expressed in CV1 cells by GRE activation assay, EC50 = 0.0002 μM. |
17705362 |
NHDFneo |
Function assay |
|
|
Activity at human GR expressed in NHDFneo cells assessed as inhibition of IL-6 production, IC50 = 0.0014 μM. |
17705362 |
J774A.1 |
Function assay |
|
|
Inhibition of LPS-induced TNFalpha production in mouse J774A.1 cells, IC50 = 0.048 μM. |
17892941 |
CV1 |
Function assay |
|
|
Activity at human glucocorticoid receptor expressed in CV1 cells assessed as repression of TNF and IL-1-beta-induced E-selectin gene expression by luciferase reporter gene assay, ED50 = 0.0001 μM. |
18032610 |
A549 |
Function assay |
|
|
Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay, EC50 = 0.005012 μM. |
18038970 |
A549 |
Function assay |
|
|
Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001175 μM. |
18038970 |
HeLa |
Cytotoxicity assay |
|
|
Cytotoxicity against human HeLa cells assessed as inhibition of DNA replication by imaging analysis |
18066055 |
HeLa |
Function assay |
|
|
Inhibition of mitosis in human HeLa cells by imaging analysis |
18066055 |
THP1 |
Antiinflammatory assay |
|
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL6 by ELISA, IC50 = 0.007 μM. |
18625560 |
THP1 |
Antiinflammatory assay |
|
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha by ELISA, IC50 = 0.05 μM. |
18625560 |
RAW264.7 |
Function assay |
|
|
Inhibition of LPS-stimulated microsomal prostaglandin E synthase 1 expression at 10 uM in mouse RAW264.7 cells by Western blot |
18790649 |
A549 |
Function assay |
|
|
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, EC50 = 0.0011 μM. |
19321341 |
A549 |
Function assay |
|
|
Transrepression activity at GR in PMA-stimulated human A549 cells assessed as inhibition of AP1 response element-induced luciferase reporter gene activity, EC50 = 0.0025 μM. |
19321341 |
NP1 |
Function assay |
|
|
Agonist activity at GR ligand binding domain expressed in human NP1 cells assessed as glucocorticoid response element transactivation by GAL4 luciferase reporter gene assay, EC50 = 0.0042 μM. |
19321341 |
MDA-kb2 |
Function assay |
|
|
Agonist activity at androgen receptor in human MDA-kb2 cells assessed as stimulation of luciferase activity by luciferase reporter gene assay, EC150 = 0.194 μM. |
19592245 |
MDA-kb2 |
Function assay |
|
|
Agonist activity at glucocorticoid receptor in human MDA-kb2 cells assessed as stimulation of luciferase activity by luciferase reporter gene assay, EC150 = 0.194 μM. |
19592245 |
A549 |
Function assay |
|
|
Agonist activity at GR in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001 μM. |
19592247 |
COS7 |
Function assay |
|
|
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, EC50 = 0.0072 μM. |
19863083 |
HeLa |
Function assay |
|
|
Transactivation of GAL-4 tagged glucocorticoid receptor ligand binding domain expressed in human HeLa cells assessed as NP1 activation by luciferase reporter gene assay, EC50 = 0.0045 μM. |
20047280 |
HeLa |
Function assay |
|
|
Transactivation activity at glucocorticoid receptor in human HeLa cells assessed as induction of MMTV promoter activity by luciferase reporter gene assay, EC50 = 0.007943 μM. |
20727743 |
HeLa |
Function assay |
|
|
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, IC50 = 0.001585 μM. |
20727743 |
THP1 |
Function assay |
|
|
Transrepression activity at glucocorticoid receptor-mediated antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL-8 production, IC50 = 0.002512 μM. |
20727743 |
Sf9 |
Function assay |
|
|
Binding affinity to human recombinant glucocorticoid receptor expressed in baculovirus infected Sf9 cells, IC50 = 0.01259 μM. |
20727743 |
insect cells |
Function assay |
|
|
Binding affinity to glucocorticoid receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled Dexamethasone by fluorescence polarization microplate assay, IC50 = 0.0034 μM. |
20735001 |
insect cells |
Function assay |
|
|
Binding affinity to mineralocorticoid receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled Dexamethasone by fluorescence polarization microplate assay, IC50 = 0.033 μM. |
20735001 |
A549 |
Function assay |
|
|
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, EC50 = 0.0011 μM. |
21073190 |
A549 |
Function assay |
|
|
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, EC50 = 0.0025 μM. |
21073190 |
NP-1 Hela |
Function assay |
|
|
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, EC50 = 0.0042 μM. |
21073190 |
A549 |
Function assay |
|
|
Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001 μM. |
21257309 |
A549 |
Function assay |
|
|
Agonist activity at GR in human A549 cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity, IC50 = 0.003981 μM. |
21257309 |
HeLa |
Function assay |
|
|
Agonist activity at glucocorticoid receptor in human HeLa cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity, EC50 = 0.017 μM. |
21963986 |
insect cells |
Function assay |
|
|
Displacement of tetramethylrhodamine-labeled Dexamethasone from human recombinant glucocorticoid receptor expressed in baculovirus infected insect cells by fluorescence polarization assay, IC50 = 0.003 μM. |
21963986 |
insect cells |
Function assay |
|
|
Displacement of tetramethylrhodamine-labeled Dexamethasone from human recombinant mineralocorticoid receptor expressed in baculovirus infected insect cells by fluorescence polarization assay, IC50 = 0.033 μM. |
21963986 |
A549 |
Function assay |
|
|
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, EC50 = 0.0011 μM. |
23916594 |
A549 |
Function assay |
|
|
Transrepression activity at glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-stimulated AP1 response element by luciferase reporter gene assay, EC50 = 0.0025 μM. |
23916594 |
Hela |
Function assay |
|
|
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, EC50 = 0.0045 μM. |
23916594 |
A549 |
Function assay |
|
|
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, EC50 = 0.0011 μM. |
23953070 |
A549 |
Function assay |
|
|
Agonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-induced AP-1 activation by luciferase reporter gene assay, EC50 = 0.0025 μM. |
23953070 |
HeLa |
Function assay |
|
|
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, EC50 = 0.0045 μM. |
23953070 |
A549 |
Function assay |
|
|
Transrepression of glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-induced AP-1 activity by luciferase reporter gene assay, EC50 = 0.0025 μM. |
24011644 |
HeLa |
Function assay |
|
|
Transactivation of GR-LBD expressed in human HeLa cells co-expressing GAL4-DBD by luciferase reporter gene assay, EC50 = 0.0042 μM. |
24011644 |
HEK293 |
Function assay |
|
|
Displacement of [3H]-aldosterone from human mineralocorticoid receptor expressed in HEK293 cells, Ki = 0.00036 μM. |
24446728 |
HEK293 |
Function assay |
|
|
Displacement of [3H]-dexamethasone from human glucocorticoid receptor expressed in HEK293 cells, Ki = 0.00069 μM. |
24446728 |
HEK293 |
Function assay |
|
|
Displacement of [3H]-methyltrienolone from human progesterone receptor expressed in HEK293 cells, Ki = 0.561 μM. |
24446728 |
HEK293 |
Function assay |
|
|
Displacement of [3H]-methyltrienolone from human androgen receptor expressed in HEK293 cells, Ki = 1.41 μM. |
24446728 |
HeLa |
Function assay |
|
|
Transactivation of glucocorticoid receptor in human HeLa cells harboring MMTV promoter by luciferase reporter gene assay, EC50 = 0.017 μM. |
24656565 |
A549 |
Function assay |
|
|
Agonist activity at glucocorticoid receptor in human A549 cells assessed as E-selectin transrepression by luciferase reporter gene assay, EC50 = 0.0011 μM. |
24980053 |
A549 |
Function assay |
|
|
Agonist activity at glucocorticoid receptor in human A549 cells assessed as AP-1 transrepression by luciferase reporter gene assay, EC50 = 0.0025 μM. |
24980053 |
HeLa |
Function assay |
|
|
Agonist activity at glucocorticoid receptor in human HeLa cells assessed as NP-1 transactivation by luciferase reporter gene assay, EC50 = 0.0045 μM. |
24980053 |
HEK293 |
Function assay |
|
|
Agonist activity at human GCR expressed in HEK293 cells by luciferase reporter gene assay, EC50 = 0.0013 μM. |
25305688 |
HFF |
Function assay |
|
|
Agonist activity at GR in HFF cells assessed as suppression of IL-1-induced IL-6 production, IC50 = 0.001 μM. |
25516791 |
IM9 |
Function assay |
|
|
Displacement of [3H]dexamethasone from glucocorticoid receptor in human IM9 cells, IC50 = 0.0038 μM. |
26988801 |
IM9 |
Function assay |
|
|
Displacement of [3H]dexamethasone from GR receptor in human IM9 cells, IC50 = 0.0038 μM. |
27876250 |
HeLa |
Function assay |
|
|
Transrepression activity at glucocorticoid receptorin human HeLa cells assessed as inhibition of TPA-induced collagenase promoter activity by luciferase reporter gene assay, IC50 = 0.001585 μM. |
28043796 |
THP1 |
Function assay |
|
|
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, IC50 = 0.002512 μM. |
28043796 |
HeLa |
Function assay |
|
|
Transactivation activity at glucocorticoid receptor in human HeLa cells assessed as induction of MMTV promoter activity by luciferase reporter gene assay, IC50 = 0.007943 μM. |
28043796 |
Sf9 |
Function assay |
|
|
Binding affinity to recombinant human glucocorticoid receptor expressed in baculovirus infected sf9 cells, IC50 = 0.01259 μM. |
28043796 |
RAW264.7 |
Antiinflammatory assay |
|
|
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production by griess assay, IC50 = 0.8 μM. |
29272126 |
SK-N-MC |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells |
29435139 |
BV2 |
Antiinflammatory assay |
|
|
Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production, IC50 = 9.5 μM. |
29482940 |
RAW264.7 |
Antiinflammatory assay |
|
|
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production, IC50 = 8.3 μM. |
29741372 |
HEK 293T |
Function assay |
|
|
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, IC50 = 0.00235 μM. |
30144697 |