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=0.005μM |
18412397 |
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=0.00203μM |
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=0.0116μM |
20469868 |
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=0.044μM |
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=0.087μM |
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=0.236μM |
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=1.8μM |
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=5.123μM |
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=17.7μM |
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=1.54μM |
21353543 |
A549 |
Antiinflammatory assay |
1 uM |
48 hrs |
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 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-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 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 |
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 |
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 |
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 |
inflammatory cells |
Antiinflammatory assay |
10 mg/kg |
6 to 24 hrs |
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 |
mononuclear cells |
Antiinflammatory assay |
10 mg/kg |
6 to 24 hrs |
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 |
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 iNOS protein level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 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 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 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 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 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 |
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 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 |
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 |
Sf9 |
Function assay |
10 uM |
4 hrs |
Displacement of [3H] dexamethasone from human recombinant GR expressed in Sf9 insect cells at 10 uM incubated for 4 hrs by scintillation counting method |
30929949 |
RAW264.7 |
Antiinflammatory assay |
10 uM |
1 hrs |
Antiinflammatory activity against mouse RAW264.7 cells assessed as downregulation of LPS-stimulated iNOS protein expression at 10 uM pretreated for 1 hrs followed by LPS addition and measured after 24 hrs by Western blot analysis |
31301566 |
RAW264.7 |
Antiinflammatory assay |
10 uM |
1 hrs |
Antiinflammatory activity against mouse RAW264.7 cells assessed as downregulation of LPS-stimulated COX2 protein expression at 10 uM pretreated for 1 hrs followed by LPS addition and measured after 24 hrs by Western blot analysis |
31301566 |
RAW264.7 |
Antiinflammatory assay |
254.8 uM |
24 hrs |
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition LPS-induced NO production at 254.8 uM measured after 24 hrs by griess reagent based assay |
31465218 |
LO2 |
Function assay |
0.25 uM |
24 hrs |
Agonist activity at FXR in guggulsterone-treated human LO2 cells assessed as increase in BSEP mRNA expression at 0.25 uM treated with FXR antagonist, guggulsterone for 24 hrs followed by incubation with compound for 24 hrs by RT-qPCR analysis |
31494470 |
LO2 |
Function assay |
0.25 uM |
24 hrs |
Agonist activity at FXR in guggulsterone-treated human LO2 cells assessed as increase in UGT2A4 mRNA expression at 0.25 uM treated with FXR antagonist, guggulsterone for 24 hrs followed by incubation with compound for 24 hrs by RT-qPCR analysis |
31494470 |
LO2 |
Function assay |
0.25 uM |
24 hrs |
Upregulation of FXR protein expression in human LO2 cells at 0.25 uM after 24 hrs by Western blot analysis |
31494470 |
LO2 |
Function assay |
0.25 uM |
24 hrs |
Agonist activity at FXR in human LO2 cells assessed as increase in SHP1 protein expression at 0.25 uM after 24 hrs by Western blot analysis |
31494470 |
LO2 |
Function assay |
0.25 uM |
24 hrs |
Agonist activity at FXR in human LO2 cells assessed as increase in BSEP protein expression at 0.25 uM after 24 hrs by Western blot analysis |
31494470 |
LO2 |
Function assay |
0.25 uM |
24 hrs |
Agonist activity at FXR in human LO2 cells assessed as increase in MRP2 protein expression at 0.25 uM after 24 hrs by Western blot analysis |
31494470 |
LO2 |
Function assay |
0.25 uM |
24 hrs |
Agonist activity at FXR in human LO2 cells assessed as increase in SULT2A protein expression at 0.25 uM after 24 hrs by Western blot analysis |
31494470 |
LO2 |
Function assay |
0.25 uM |
24 hrs |
Agonist activity at FXR in human LO2 cells assessed as decrease in CYP7A1 protein expression at 0.25 uM after 24 hrs by Western blot analysis |
31494470 |
LO2 |
Function assay |
0.25 uM |
24 hrs |
Agonist activity at FXR in human LO2 cells assessed as decrease in CYP8B1 protein expression at 0.25 uM after 24 hrs by Western blot analysis |
31494470 |
LO2 |
Function assay |
0.25 uM |
24 hrs |
Agonist activity at FXR in human LO2 cells assessed as decrease in NTCP protein expression at 0.25 uM after 24 hrs by Western blot analysis |
31494470 |
THP1 |
Antiinflammatory assay |
200 uM |
4 hrs |
Antiinflammatory activity against human THP1 cells assessed as inhibition of LPS-induced TNFalpha production at 200 uM preincubated for 4 hrs followed by LPS challenge and measured after 24 hrs incubation by ELISA |
31804830 |
A549 |
Function assay |
1 uM |
48 hrs |
Downregulation of DNA replication in human A549 cells at 1 uM after 48 hrs by UV-visible spectrophotometric analysis |
ChEMBL |
U2OS |
Function assay |
0.1 uM |
24 hrs |
Activation of glulcocorticoid receptor (unknown origin) expressed in human U2OS cells at 0.1 uM incubated for 24 hrs by luciferase reporter gene assay |
ChEMBL |
A549 |
Function assay |
10 uM |
|
Antagonist activity for Glucocorticoid receptor in MMTV transactivation assay in human A549 lung epithelial cells at 10 uM, IC50<10μM |
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 |
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=0.7μM |
11908984 |
RAW 264.7 |
Function assay |
|
24 hrs |
Inhibition of interferon gamma-stimulated NO production in RAW 264.7 cells after 24 hrs, IC50=0.02μM |
17367124 |
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 |
RPMI8226 |
Antiproliferative assay |
|
4 days |
Antiproliferative activity against human RPMI8226 cells after 4 days, IC50=0.0065μM |
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=0.005μM |
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=0.005μM |
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=0.0011μM |
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=0.0025μM |
20047280 |
inflammatory cells |
Antiinflammatory assay |
|
2 mg/kg |
Antiinflammatory activity in human CKLF1-electroporated transfected mouse assessed as decrease in infiltration of inflammatory cells at 2 mg/kg, po |
20099827 |
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=0.0005082μM |
20812681 |
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<15.8489μM |
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=2.6μM |
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=0.005μM |
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=0.86μM |
21288727 |
HMC1 |
Immunomodulatory assay |
|
30 mins |
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=0.01μM |
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=0.8μM |
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=0.02μM |
21361338 |
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 |
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 |
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=0.47μM |
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=0.98μM |
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=0.0097μM |
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=0.0125μM |
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=1.43μM |
23373965 |
HeLaS3 |
Function assay |
|
2 hrs |
Displacement of [3H]Dexamethasone from glucocorticoid receptor in human HeLaS3 cells after 2 hrs, Ki=0.0022μM |
23403082 |
HeLaS3 |
Function assay |
|
2 hrs |
Displacement of [3H]Dexamethasone from glucocorticoid receptor in human HeLaS3 cells after 2 hrs, IC50=0.0041μM |
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=0.8μM |
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=0.0018μM |
25706100 |
RAW264.7 |
Function assay |
|
6 hrs |
Inhibition of TNFalpha production in mouse RAW264.7 cells incubated for 6 hrs by sandwich immunoassay, IC50=0.04μM |
25824662 |
J774A.1 |
Function assay |
|
6 hrs |
Inhibition of TNFalpha production in mouse J774A.1 cells incubated for 6 hrs by sandwich immunoassay, IC50=0.4μM |
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=4.7μM |
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=22μM |
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=0.63μM |
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=0.025μM |
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=0.8μM |
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=0.63μM |
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=7μM |
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=2.5μM |
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=10.7μM |
29518326 |
RAW264.7 |
Antiinflammatory assay |
|
30 mins |
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production pretreated for 30 mins followed by LPS stimulation for 24 hrs by ELISA, IC50=8.7μM |
30528697 |
RAW264.7 |
Antiinflammatory assay |
|
48 hrs |
Anti-inflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced TNF-alpha production after 48 hrs by ELISA, IC50=1.2μM |
30579802 |
RAW264.7 |
Antiinflammatory assay |
|
48 hrs |
Anti-inflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced IL-6 production after 48 hrs by ELISA, IC50=9.4μM |
30579802 |
RAW264.7 |
Antiinflammatory assay |
|
1 hr |
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, IC50=0.13μM |
30808589 |
RAW264.7 |
Antiinflammatory assay |
|
3 hrs |
Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production preincubated for 3 hrs followed by LPS-stimulation and measured after 24 hrs by Griess assay, IC50=7.9μM |
30817151 |
RAW264.7 |
Antiinflammatory assay |
|
30 mins |
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, IC50=0.01μM |
30931559 |
RAW264.7 |
Antiinflammatory assay |
|
12 hrs |
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production preincubated for 12 hrs followed by LPS-stimulation and measured after 24 hrs by Griess assay, IC50=18.4μM |
31181925 |
RAW264.7 |
Antiinflammatory assay |
|
1 hr |
Antiinflammatory activity against LPS-induced mouse RAW264.7 cells assessed as inhibition of NO overproduction preincubated for 1 hr prior to Escherichia coli LPS stimulation followed by further incubation for 24 hrs by Griess reagent based spectrophotome, IC50=5.02μM |
31260892 |
RAW264.7 |
Antiinflammatory assay |
|
1 hr |
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, IC50=0.01μM |
31301930 |
RAW264.7 |
Antiinflammatory assay |
|
24 hrs |
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 24 hrs by Griess reagent-based assay, IC50=6μM |
31577434 |
RAW264.7 |
Antiinflammatory assay |
|
24 hrs |
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha secretion after 24 hrs by ELISA, IC50=6.1μM |
31577434 |
RAW264.7 |
Antiinflammatory assay |
|
24 hrs |
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 secretion after 24 hrs by ELISA, IC50=8.4μM |
31577434 |
RPMI18226 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human RPMI18226 cells after 72 hrs by XTT assay, IC50=0.0078μM |
ChEMBL |
RAW264.7 |
Antiinflammatory assay |
|
2 hrs |
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production pretreated for 2 hrs followed by LPS stimulation measured after 24 hrs by Griess assay, IC50=2.66μM |
ChEMBL |
RAW 264.7 |
Function assay |
|
|
Inhibitory activity against TNF-alpha release in RAW 264.7 cells in the supernatant, IC50=0.42μM |
12361395 |
N9 |
Function assay |
|
|
Inhibitory activity against TNF-alpha release in N9 cells in the supernatant, IC50=0.074μM |
12361395 |
PBMC |
Function assay |
|
|
Inhibitory concentration against growth of LPS stimulated human peripheral blood mononuclear cells, IC50=0.04μM |
11229767 |
PBMC |
Function assay |
|
|
Inhibitory concentration against TNF-alpha production from human peripheral blood mononuclear cells stimulated by LPS, IC50=0.01μM |
11229767 |
mice spleen cells |
Function assay |
|
|
Inhibitory concentration against T cell proliferation using concanavalin A stimulated mice spleen cells, IC50=0.005μM |
11229767 |
A549 |
Function assay |
|
|
Activity at glucocorticoid receptor in human A549 cells assessed as effect on GRE promoter response by luciferase reporter assay, EC50=0.001μM |
16643060 |
A549 |
Function assay |
|
|
Agonist activity at GR assessed as NF-kappaB-mediated transrepression of secreted placental alkaline phosphatase gene in human A549 cells, IC50=0.001175μM |
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=0.005012μM |
16821781 |
HFF |
Function assay |
|
|
Inhibition of IL1-stimulated IL6 production in HFF cells, IC50=0.00051μM |
17181172 |
HFF |
Function assay |
|
|
Induction of aromatase activity in HFF cells assessed as production of beta estradiol by aromatase assay, EC50=0.0019μM |
17181172 |
HeLa |
Function assay |
|
|
Activation of MMTV in HeLa cells measured by luciferase activity, EC50=0.017μM |
17181172 |
A549 |
Function assay |
|
|
Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay, IC50=0.001μM |
17616395 |
A549 |
Function assay |
|
|
Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay, EC50=0.00537μM |
17616395 |
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<1μM |
17616395 |
HFF |
Antiinflammatory assay |
|
|
Antiinflammatory activity assessed as inhibition of IL1 stimulated IL6 production in HFF cells by transrepression assay, EC50=0.0005μM |
17692519 |
HFF |
Antiinflammatory assay |
|
|
Antiinflammatory activity assessed as upregulation of aromatase in HFF cells by transactivation assay, EC50=0.002μM |
17692519 |
CV1 |
Function assay |
|
|
Agonist activity at human GR expressed in CV1 cells by GRE activation assay, EC50=0.0002μM |
17705362 |
NHDFneo |
Function assay |
|
|
Activity at human GR expressed in NHDFneo cells assessed as inhibition of IL-6 production, IC50=0.0014μM |
17705362 |
J774A.1 |
Function assay |
|
|
Inhibition of LPS-induced TNFalpha production in mouse J774A.1 cells, IC50=0.048μM |
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=0.0001μM |
18032610 |
A549 |
Function assay |
|
|
Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay, IC50=0.001175μM |
18038970 |
A549 |
Function assay |
|
|
Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay, EC50=0.005012μM |
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=0.007μM |
18625560 |
THP1 |
Antiinflammatory assay |
|
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha by ELISA, IC50=0.05μM |
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=0.0011μM |
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=0.0025μM |
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=0.0042μM |
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=0.194μM |
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=0.194μM |
19592245 |
A549 |
Function assay |
|
|
Agonist activity at GR in human A549 cells by NF-kappaB transrepression assay, IC50=0.001μM |
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=0.0072μM |
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=0.0045μM |
20047280 |
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=0.001585μM |
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=0.002512μM |
20727743 |
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=0.007943μM |
20727743 |
Sf9 |
Function assay |
|
|
Binding affinity to human recombinant glucocorticoid receptor expressed in baculovirus infected Sf9 cells, IC50=0.01259μM |
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=0.0034μM |
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=0.033μM |
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=0.0011μM |
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=0.0025μM |
21073190 |
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=0.0042μM |
21073190 |
A549 |
Function assay |
|
|
Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay, IC50=0.001μM |
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=0.003981μM |
21257309 |
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=0.003μM |
21963986 |
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=0.017μM |
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=0.033μM |
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=0.0011μM |
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=0.0025μM |
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=0.0045μM |
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=0.0011μM |
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=0.0025μM |
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=0.0045μM |
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=0.0025μM |
24011644 |
HeLa |
Function assay |
|
|
Transactivation of GR-LBD expressed in human HeLa cells co-expressing GAL4-DBD by luciferase reporter gene assay, EC50=0.0042μM |
24011644 |
HEK293 |
Function assay |
|
|
Displacement of [3H]-aldosterone from human mineralocorticoid receptor expressed in HEK293 cells, Ki=0.00036μM |
24446728 |
HEK293 |
Function assay |
|
|
Displacement of [3H]-dexamethasone from human glucocorticoid receptor expressed in HEK293 cells, Ki=0.00069μM |
24446728 |
HEK293 |
Function assay |
|
|
Displacement of [3H]-methyltrienolone from human progesterone receptor expressed in HEK293 cells, Ki=0.561μM |
24446728 |
HEK293 |
Function assay |
|
|
Displacement of [3H]-methyltrienolone from human androgen receptor expressed in HEK293 cells, Ki=1.41μM |
24446728 |
HeLa |
Function assay |
|
|
Transactivation of glucocorticoid receptor in human HeLa cells harboring MMTV promoter by luciferase reporter gene assay, EC50=0.017μM |
24656565 |
A549 |
Function assay |
|
|
Agonist activity at glucocorticoid receptor in human A549 cells assessed as E-selectin transrepression by luciferase reporter gene assay, EC50=0.0011μM |
24980053 |
A549 |
Function assay |
|
|
Agonist activity at glucocorticoid receptor in human A549 cells assessed as AP-1 transrepression by luciferase reporter gene assay, EC50=0.0025μM |
24980053 |
HeLa |
Function assay |
|
|
Agonist activity at glucocorticoid receptor in human HeLa cells assessed as NP-1 transactivation by luciferase reporter gene assay, EC50=0.0045μM |
24980053 |
HEK293 |
Function assay |
|
|
Agonist activity at human GCR expressed in HEK293 cells by luciferase reporter gene assay, EC50=0.0013μM |
25305688 |
HFF |
Function assay |
|
|
Agonist activity at GR in HFF cells assessed as suppression of IL-1-induced IL-6 production, IC50=0.001μM |
25516791 |
IM9 |
Function assay |
|
|
Displacement of [3H]dexamethasone from glucocorticoid receptor in human IM9 cells, IC50=0.0038μM |
26988801 |
IM9 |
Function assay |
|
|
Displacement of [3H]dexamethasone from GR receptor in human IM9 cells, IC50=0.0038μM |
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=0.001585μM |
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=0.002512μM |
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=0.007943μM |
28043796 |
Sf9 |
Function assay |
|
|
Binding affinity to recombinant human glucocorticoid receptor expressed in baculovirus infected sf9 cells, IC50=0.01259μM |
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=0.8μM |
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=9.5μM |
29482940 |
RAW264.7 |
Antiinflammatory assay |
|
|
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production, IC50=8.3μM |
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=0.00235μM |
30144697 |
CV1 |
Function assay |
|
|
Agonist activity at recombinant human glucocorticoid receptor expressed in African green monkey CV1 cells by MMTV luciferase reporter gene assay, EC50=0.0001μM |
30359818 |
RAW264.7 |
Antiinflammatory assay |
|
|
Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of lipopolysaccharide-induced nitric oxide production, IC50=5.5μM |
31873014 |