Antagonistic potency to the human progesterone receptor measured in the T-47D alkaline phosphatase assay
|
None
|
0.35
nM
|
|
Antagonistic activity against human androgen receptor (hAR) in co-transfected CV-1 cells.
|
None
|
5.0
nM
|
|
Displacement of [3H]mibolerone from human Androgen receptor
|
Homo sapiens
|
89.0
nM
|
|
Antagonist activity against the Androgen Receptor (AR)
|
None
|
5.0
nM
|
|
Inhibitory activity against human Androgen receptor
|
Homo sapiens
|
5.0
nM
|
|
Inhibition of antagonist activity towards Androgen receptor
|
Homo sapiens
|
8.3
nM
|
|
Binding affinity determined against human Androgen receptor
|
None
|
10.6
nM
|
|
Displacement of [3H]DHT from human Androgen receptor
|
Homo sapiens
|
4.6
nM
|
|
Binding affinity for human androgen receptor in transiently-transfected COS-1 cells.
|
None
|
22.0
nM
|
|
Inhibitory concentration against progesterone induced PRE-luciferase activity in CV-cells
|
Oryctolagus cuniculus
|
0.3
nM
|
|
Displacement of radioligand from human Estrogen receptor beta, percent inhibition at 10 uM
|
Homo sapiens
|
92.0
%
|
|
Displacement of radioligand from human Estrogen receptor alpha, percent inhibition at 10 uM
|
Homo sapiens
|
44.0
%
|
|
Inhibition of Dexamethasone stimulated transcriptional activity in CHO cells expressing glucocorticoid receptor
|
Homo sapiens
|
5.0
nM
|
|
Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR)
|
Homo sapiens
|
1.0
nM
|
|
Inhibition of Dexamethasone binding to Glucocorticoid receptor
|
Homo sapiens
|
1.1
nM
|
|
Antagonist activity against the Glucocorticoid Receptor (GR)
|
None
|
0.8
nM
|
|
Effect on human Glucocorticoid receptor (GR) in a whole cell assay to measure functional cellular GR-antagonism (GRAF)
|
None
|
5.0
nM
|
|
Inhibitory activity against human glucocorticoid receptor (hGR)
|
Homo sapiens
|
0.8
nM
|
|
Inhibition of antagonist activity towards glucocorticoid receptor
|
Homo sapiens
|
0.8
nM
|
|
Antagonist activity as displacement of 10 nM [3H]dexamethasone from human Glucocorticoid receptor, percent inhibition at 1 uM
|
Homo sapiens
|
100.0
%
|
|
Binding affinity was determined for human glucocorticoid receptor(hGR).
|
None
|
0.68
nM
|
|
Displacement of 10 nM [3H]dexamethasone from human Glucocorticoid receptor
|
Homo sapiens
|
0.24
nM
|
|
Antagonist activity against human mineralocorticoid receptor as displacement of radioligand, percent inhibition at 10 nM
|
Homo sapiens
|
69.7
%
|
|
In vitro antagonist potency in transactivation assay in neuroblastoma cells expressing human PR-A progesterone receptor
|
Homo sapiens
|
0.028
nM
|
|
In vitro antagonist potency in transactivation assay in CV-1 cells expressing androgen receptor
|
None
|
10.0
nM
|
|
In vitro antagonist potency in transactivation assay in NIH3T3 cells expressing glucocorticoid receptor
|
Mus musculus
|
2.2
nM
|
|
In vitro antagonist potency in transactivation assay in neuroblastoma cells expressing human PR-B progesterone receptor
|
Homo sapiens
|
0.025
nM
|
|
Antagonistic activity at human progesterone receptor in CV-1 cells.
|
None
|
0.3
nM
|
|
Antagonistic activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells.
|
None
|
0.18
nM
|
|
In vitro antagonist activity against human progesterone receptor isoform B(hPR-B) in mammalian(CV-1) cells
|
Homo sapiens
|
0.3
nM
|
|
Inhibitory concentration for antagonistic activity towards human progesterone receptor (hPR) using the cotransfection assay in CV-1 cells
|
None
|
0.3
nM
|
|
Inhibition of human progesterone receptor activation in T47D human breast cancer cell.
|
None
|
3.3
nM
|
|
Antagonistic activity against Progesterone receptor (PR) in transcriptional activation assay in human T47D breast carcinoma cell line
|
Homo sapiens
|
0.2
nM
|
|
Progesterone receptor antagonist activity based on its ability to block progesterone induced alkaline phosphatase in the human breast cancer cell line T47D
|
None
|
0.1
nM
|
|
Antagonist activity against human Progesterone receptor as displacement of radioligand, percent inhibition at 1 uM
|
Homo sapiens
|
100.0
%
|
|
Binding affinity against Baculovirus-Expressed hPR-A
|
Homo sapiens
|
1.1
nM
|
|
Binding affinity towards progesterone receptor was measured
|
None
|
1.1
nM
|
|
Displacement of radioligand from human Progesterone receptor
|
Homo sapiens
|
15.0
nM
|
|
Binding affinity to human progesterone receptor
|
None
|
1.1
nM
|
|
Binding affinity at human progesterone receptor.
|
None
|
1.1
nM
|
|
Antagonist activity against the Progesterone Receptor (PR)
|
None
|
0.3
nM
|
|
Inhibition of [3H]R5020 binding to cytosolic progesterone receptor (PRc) of rat uterus
|
Rattus norvegicus
|
3.5
nM
|
|
Displacement of [3H]progesterone at progesterone receptor of T47D cells
|
Homo sapiens
|
0.7
nM
|
|
Binding affinity against human progesterone receptor-A (hPR-A)
|
None
|
1.1
nM
|
|
Binding affinity determined for human Progesterone receptor A isoform
|
None
|
0.58
nM
|
|
Antagonist activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells
|
None
|
0.3
nM
|
|
Concentration required to give half-maximal inhibition against human Progesterone receptor B isoform in co-transfected CV-1 cell lines.
|
None
|
0.18
nM
|
|
Displacement of [3H]progesterone from human Progesterone receptor
|
Homo sapiens
|
3.0
nM
|
|
Ability to block progesterone induced stimulation of rat uterine luminal cells at 3 mg/kg peroral dose in rat decidualisation assay
|
Rattus norvegicus
|
100.0
%
|
|
Inhibitory concentration against progesterone stimulated alkaline phosphatase activity in T47D human breast carcinoma cell line
|
None
|
0.2
nM
|
|
Inhibition of prednisilone-induced tyrosine aminotransferase (TAT) activity in rat hepatocytes
|
Rattus norvegicus
|
410.0
nM
|
|
Antagonist activity against progesterone receptor (PR) in an alkaline phosphatase assay in the T47D human breast carcinoma cell line
|
None
|
0.13
nM
|
|
Antagonist activity against progesterone receptor (PR) using PRE-luciferase plasmid co-transfected CV-1 cells
|
None
|
0.3
nM
|
|
Inhibition of human androgen receptor
|
Homo sapiens
|
0.65
nM
|
|
Inhibition of human progesterone receptor
|
Homo sapiens
|
0.64
nM
|
|
Inhibition of human Estrogen receptor beta
|
Homo sapiens
|
750.0
nM
|
|
Inhibition of human Estrogen receptor alpha
|
Homo sapiens
|
200.0
nM
|
|
Inhibition of human glucocorticoid receptor
|
Homo sapiens
|
0.1
nM
|
|
Inhibition of human Mineralocorticoid receptor
|
Homo sapiens
|
640.0
nM
|
|
Inhibition of glucocorticoid receptor mediated tyrosine amino transferase activity
|
Homo sapiens
|
120.0
nM
|
|
Displacement of fluorescent ligand from binding domain of progesterone receptor
|
Homo sapiens
|
10.0
nM
|
|
Antagonistic activity against VP-16 transcriptional activation domain protein
|
Herpes simplex virus (type 1 / strain 17)
|
0.7
nM
|
|
Inhibition of human progesterone receptor
|
Homo sapiens
|
2.9
nM
|
|
Inhibition of [3H]dexamethasone binding to human glucocorticoid receptor
|
Homo sapiens
|
1.1
nM
|
|
Inhibition of CHO-K1 cells expressing glucocorticoid receptor
|
None
|
0.008
nM
|
|
Inhibition of human androgen receptor
|
Homo sapiens
|
8.8
nM
|
|
Inhibition of [3H]dexamethasone binding to rat glucocorticoid receptor
|
Rattus norvegicus
|
1.4
nM
|
|
Inhibition of human progesterone receptor
|
Homo sapiens
|
2.9
nM
|
|
Inhibition of AR-dimerization in CHO-K1 cells expressing human androgen receptor
|
Homo sapiens
|
7.8
nM
|
|
Inhibition of [3H]dexamethasone binding to human glucocorticoid receptor
|
Homo sapiens
|
1.1
nM
|
|
Inhibition of human androgen receptor expressed in Escherichia coli
|
Homo sapiens
|
2.2
nM
|
|
Inhibition of dexamethasone-induced glucocorticoid receptor mediated tyrosine aminotransferase in rat hepatocytes
|
Rattus norvegicus
|
270.0
nM
|
|
Inhibition of dexamethasone-induced GR-mediated tyrosine amino transferase activity in rat hepatocytes
|
Rattus norvegicus
|
270.0
nM
|
|
Inhibition of glucocorticoid receptor mediated glycogen deposition
|
Rattus norvegicus
|
77.0
%
|
|
Inhibition of glucocorticoid receptor mediated tyrosine aminotransferase activity
|
None
|
101.0
%
|
|
Inhibition of glucocorticoid receptor dependent alkaline phosphatase activity
|
Homo sapiens
|
0.44
nM
|
|
Inhibition of 4 nM progesterone-stimulated transactivation of MMTV-Luc reporter in CV-1 cells expressing PR-B
|
None
|
0.2512
nM
|
|
Antagonistic activity against 5 nM Dexamethasone induced glucocorticoid receptor mediated alkaline phosphatase activity
|
Homo sapiens
|
4.8
nM
|
|
Inhibition of human lymph node carcinoma of prostate (LNCaP) cell proliferation
|
Homo sapiens
|
23.0
nM
|
|
Inhibition of glucocorticoid receptor Dexamethasone response in reporter gene assay
|
Homo sapiens
|
4.8
nM
|
|
Inhibition of dexamethasone-induced glucocorticoid receptor mediated alkaline phosphatase activity
|
Homo sapiens
|
4.8
nM
|
|
Inhibitory activity against human lymphocytes
|
Homo sapiens
|
104.0
%
|
|
Effective concentration against inhibition of Dexamethasone induced glucocorticoid receptor transactivation of mouse mammary tumor virus luciferase gene in HeLa cells
|
Homo sapiens
|
2.0
nM
|
|
Percentage inhibition of dexamethasone-induced glucocorticoid receptor transactivation of the mouse mammary tumor virus(MMTV) luciferase gene in HeLa cells at a concentration of 100 nM
|
Homo sapiens
|
100.0
%
|
|
Binding affinity at PR by fluorescence binding assay
|
Homo sapiens
|
10.0
nM
|
|
Antagonist activity against PR beta-mediated transactivation of MMTV luciferase reporter gene in BacMam transduced progesterone-stimulated CV1 cells
|
None
|
0.2512
nM
|
|
Inhibition of fluorescent-labeled Dexamethasone binding to GR
|
Homo sapiens
|
5.754
nM
|
|
Activity at GR assessed as ability to antagonize dexamethasone-induced MMTV luciferase reporter gene transactivation in human A549 cells
|
Homo sapiens
|
4.677
nM
|
|
Binding affinity to human GR
|
Homo sapiens
|
1.1
nM
|
|
Activity at GR expressed in CHO cells assessed as decrease in dexamethasone-stimulated alkaline phosphatase production by GRAF assay
|
None
|
5.0
nM
|
|
Inhibition of prednisilone-stimulated TAT production in Sprague-Dawley rat at 100 mg/kg, po
|
Rattus norvegicus
|
101.0
%
|
|
Inhibition of prednisilone-induced glycogen deposition in Sprague-Dawley rat at 100 mg/kg, po
|
Rattus norvegicus
|
77.0
%
|
|
Inhibition of prednisilone-induced lymphopenia in Sprague-Dawley rat at 100 mg/kg, po
|
Rattus norvegicus
|
104.0
%
|
|
Displacement of radiolabeled Dexamethasone from human GR
|
Homo sapiens
|
1.1
nM
|
|
Inhibition of human GR expressed in hGRAF cells
|
Homo sapiens
|
5.0
nM
|
|
Inhibition of human GR transcriptional activation by HepTAT cells
|
Homo sapiens
|
169.0
nM
|
|
Inhibition of prednisilone-induced TAT level in Sprague-Dawley rats at 100 mg/kg, po
|
Rattus norvegicus
|
101.0
%
|
|
Inhibition of prednisilone-induced glycogen depostion in Sprague-Dawley rats at 100 mg/kg, po
|
Rattus norvegicus
|
77.0
%
|
|
Inhibition of prednisilone-induced lymphopenia in Sprague-Dawley rats at 100 mg/kg, po
|
Rattus norvegicus
|
104.0
%
|
|
Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity
|
Homo sapiens
|
1.4
nM
|
|
Antagonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of corticoid-induced GRE-linked luciferase reporter gene activity
|
Homo sapiens
|
1.6
nM
|
|
Antagonist activity at human progesterone receptor assessed as inhibition of alkaline phosphatase activity in human T47D cells
|
Homo sapiens
|
1.4
nM
|
|
Antagonist activity at human glucocorticoid receptor assessed as inhibition of corticoid-induced transcription in human A549 cells by GRE-linked luciferase reporter gene assay
|
Homo sapiens
|
1.6
nM
|
|
Antagonist activity at human GR expressed in CV1 cells by GRE activation assay
|
Homo sapiens
|
0.6
nM
|
|
Binding affinity to glucocorticoid receptor
|
None
|
6.918
nM
|
|
Antagonist activity at glucocorticoid receptor in human A549 cells transfected with MMTV luciferase reporter gene assessed as inhibition of dexamethasone-induced activation
|
Homo sapiens
|
11.48
nM
|
|
Antagonist activity at glucocorticoid receptor in human A549 cells transfected with MMTV luciferase reporter gene assessed as inhibition of dexamethasone-induced activation
|
Homo sapiens
|
100.0
%
|
|
Displacement of fluorescent labeled Dexamethasone from glucocorticoid receptor
|
None
|
5.754
nM
|
|
Antagonist activity at glucocorticoid receptor in human A549 cells transfected with MMTV luciferase reporter gene assessed as inhibition of dexamethasone-induced activation
|
Homo sapiens
|
4.677
nM
|
|
Antagonist activity at glucocorticoid receptor expressed in human A549 cells assessed as inhibition of corticoid-induced transcription by glucocorticoid response element-linked luciferase reporter gene assay
|
None
|
1.0
nM
|
|
Antagonist activity at progesterone receptor expressed in human T47 cells assessed as blockade of progesterone-induced alkaline phosphatase activity
|
None
|
2.6
nM
|
|
Binding affinity to rat glucocorticoid receptor
|
Rattus norvegicus
|
2.512
nM
|
|
Binding affinity to progesterone receptor
|
None
|
15.85
nM
|
|
Displacement of [3H]dexamethasone from human glucocorticoid receptor expressed in recombinant baculovirus
|
Homo sapiens
|
0.4
nM
|
|
Antagonist activity at human glucocorticoid receptor in SW1353 cells assessed as inhibition of dexamethasone-induced luciferase expression by MMTV5 reporter gene assay
|
Homo sapiens
|
1.2
nM
|
|
Binding affinity to glucocorticoid receptor in SW1353 cells by whole-cell binding assay
|
Homo sapiens
|
0.82
nM
|
|
Antagonist activity at progesterone receptor expressed in human T47D cells assessed as inhibition of promegestone-induced alkaline phosphatase activity
|
None
|
0.054
nM
|
|
Antagonist activity at glucocorticoid receptor expressed in A549 cells assessed as inhibition of corticoid-induced gene transcription by luciferase reporter gene assay
|
Homo sapiens
|
6.0
nM
|
|
Displacement of [3H]dexamethasone from human recombinant GR
|
Homo sapiens
|
0.4
nM
|
|
Antagonist activity at GR in SW1353/MMTV5 cells assessed as inhibition of dexamethasone-induced luciferase expression
|
None
|
1.2
nM
|
|
Antagonist activity at human PR expressed in human T47D cells assessed as inhibition of progesterone induced alkaline phosphatase
|
Homo sapiens
|
0.2
nM
|
|
Displacement of [3H]R5020 from human PR in human T47D cells by whole cell assay
|
Homo sapiens
|
0.6
nM
|
|
Antagonist activity at human AR ligand binding domain expressed in african green monkey COS7 cells in presence of 5-alpha-dihydrotestosterone by Gal4 hybrid assay
|
Homo sapiens
|
6.9
nM
|
|
Antagonist activity at human GR ligand binding domain expressed in african green monkey COS7 cells in presence of Dexamethasone by Gal4 hybrid assay
|
Homo sapiens
|
0.6
nM
|
|
Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity after 48 hrs
|
Homo sapiens
|
0.045
nM
|
|
Antagonist activity at progesterone receptor in human T47D-C124 cells transfected with luciferase gene linked to MMTV promoter assessed as inhibition of progesterone-induced luciferase transactivation activity after 24 hrs
|
Homo sapiens
|
0.021
nM
|
|
Antagonist activity at progesterone receptor assessed as progesterone-induced alkaline phosphatase activity in human T47D cells
|
Homo sapiens
|
0.2
nM
|
|
Antagonist activity at androgen receptor by Gal4-DNA binding domain-hormone receptor LBD one-hybrid assay
|
None
|
6.9
nM
|
|
Antagonist activity at glucocorticoid receptor by Gal4-DNA binding domain-hormone receptor LBD one-hybrid assay
|
None
|
0.6
nM
|
|
Antagonist activity at mineralocorticoid receptor by Gal4-DNA binding domain-hormone receptor LBD one-hybrid assay
|
None
|
590.0
nM
|
|
Inhibition of progesterone receptor mediated progesterone-induced alkaline phosphatase activity in human T47D cells
|
Homo sapiens
|
0.2
nM
|
|
Antagonist activity at cloned estrogen receptor-ligand binding domain expressed in african green monkey COS7 cells by GAL4 luciferase reporter assay
|
None
|
50.0
%
|
|
Antagonist activity at cloned androgen receptor-ligand binding domain expressed in african green monkey COS7 cells by two hybrid luciferase assay
|
None
|
6.9
nM
|
|
Antagonist activity at cloned androgen receptor-ligand binding domain expressed in african green monkey COS7 cells by two hybrid luciferase assay
|
None
|
95.0
%
|
|
Antagonist activity at cloned glucocorticoid receptor-ligand binding domain expressed in african green monkey COS7 cells by GAL4 luciferase reporter assay
|
None
|
0.6
nM
|
|
Antagonist activity at cloned glucocorticoid receptor-ligand binding domain expressed in african green monkey COS7 cells by GAL4 luciferase reporter assay
|
None
|
97.0
%
|
|
Antagonist activity at cloned mineralocorticoid receptor-ligand binding domain expressed in african green monkey COS7 cells by GAL4 luciferase reporter assay
|
None
|
590.0
nM
|
|
Antagonist activity at cloned mineralocorticoid receptor-ligand binding domain expressed in african green monkey COS7 cells by GAL4 luciferase reporter assay
|
None
|
96.0
%
|
|
Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity
|
Homo sapiens
|
1.4
nM
|
|
Antagonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of corticoid-induced transcription after 16 hrs by glucocorticoid response element-driven luciferase reporter gene assay
|
Homo sapiens
|
1.6
nM
|
|
Blockade of progesterone-dependent inhibition of ethinyl estradiol-induced complement C3 expression in po dosed ovariectomized Sprague-Dawley rat uterus
|
Rattus norvegicus
|
4.6
mg kg-1
|
|
Antiprogestagenic activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity
|
Homo sapiens
|
0.05
nM
|
|
Antagonist activity at glucocorticoid receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay
|
None
|
3.2
nM
|
|
Displacement of [3H]DEX from human glucocorticoid receptor
|
Homo sapiens
|
0.24
nM
|
|
Displacement of fluorescent-labeled Dexamethasone from GR by fluorescent polarization assay
|
None
|
6.31
nM
|
|
Binding affinity to AR
|
None
|
63.1
nM
|
|
Binding affinity to PR
|
None
|
7.943
nM
|
|
Antagonist activity at GR in human A549 cells transfected with luciferase gene linked to MMTV promoter assessed as inhibition of dexamethasone-induced luciferase transactivation activity after 24 hrs
|
Homo sapiens
|
6.31
nM
|
|
Displacement of [3H]DHT from human androgen receptor after 16 hrs by scintillation counting
|
Homo sapiens
|
8.4
nM
|
|
Antagonist activity at human progesterone receptor B expressed in african green monkey CV1 cells co-transfected with MMTV-Luc assessed as effect on progesterone-induced activity by luciferase reporter gene assay
|
Homo sapiens
|
0.6
nM
|
|
Displacement of [3H]dexamethasone from human glucocorticoid receptor after 16 hrs by scintillation counting
|
Homo sapiens
|
0.84
nM
|
|
Agonist activity at human androgen receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc after 24 hrs by luciferase reporter gene assay
|
Homo sapiens
|
10.0
nM
|
|
Agonist activity at human glucocorticoid receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc after 24 hrs by luciferase reporter gene assay
|
Homo sapiens
|
872.0
nM
|
|
Antagonist activity at human ERbeta expressed in african green monkey CV1 cells co-transfected with ERE-MMTV-Luc by luciferase reporter gene assay
|
Homo sapiens
|
812.0
nM
|
|
Antagonist activity at human androgen receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc by luciferase reporter gene assay
|
Homo sapiens
|
1.0
nM
|
|
Antagonist activity at human glucocorticoid receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc by luciferase reporter gene assay
|
Homo sapiens
|
0.95
nM
|
|
Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity
|
Homo sapiens
|
0.2
nM
|
|
Antagonist activity at androgen receptor ligand binding domain by two hybrid assay
|
None
|
6.9
nM
|
|
Antagonist activity at glucocorticoid receptor ligand binding domain by two hybrid assay
|
None
|
0.6
nM
|
|
Antagonist activity at mineralocorticoid receptor ligand binding domain by two hybrid assay
|
None
|
590.0
nM
|
|
DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid)
|
Oryctolagus cuniculus
|
555.0
nM
|
|
DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine)
|
None
|
997.0
nM
|
|
DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
|
Bos taurus
|
3.245
nM
|
|
DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
|
Bos taurus
|
0.423
nM
|
|
DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
|
Escherichia coli
|
8.345
nM
|
|
DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
|
Escherichia coli
|
5.563
nM
|
|
DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
|
None
|
2.232
nM
|
|
DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
|
None
|
1.014
nM
|
|
Antagonist activity at progesterone receptor
|
None
|
10.0
nM
|
|
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
|
81.2
%
|
|
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
|
80.3
%
|
|
Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting
|
Homo sapiens
|
70.7
%
|
|
Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay
|
Homo sapiens
|
900.0
nM
|
|
Displacement of [3H]-dexamethasone from cytosolic fraction of human recombinant glucocorticoid receptor by scintillation counting analysis
|
Homo sapiens
|
6.0
nM
|
|
Displacement of [3H]-progesterone from cytosolic fraction of human recombinant progesterone-B receptor by scintillation counting analysis
|
Homo sapiens
|
15.0
nM
|
|
Displacement of [3H]-dexamethasone from human glucocorticoid receptor expressed in HEK293 cells by scintillation counting based radioligand competition binding assay
|
Homo sapiens
|
0.299
nM
|
|
Displacement of [3H]-aldosterone from human mineralocorticoid receptor expressed in HEK293 cells by scintillation counting based radioligand competition binding assay
|
Homo sapiens
|
851.0
nM
|
|
Displacement of [3H]-methyltrienolone from human androgen receptor expressed in HEK293 cells by scintillation counting based radioligand competition binding assay
|
Homo sapiens
|
5.95
nM
|
|
Displacement of [3H]-progesterone from human progesterone receptor expressed in HEK293 cells by scintillation counting based radioligand competition binding assay
|
Homo sapiens
|
0.998
nM
|
|
Antagonist activity against glucocorticoid receptor (unknown origin) expressed in HEK293 cells by GRE-dependent luciferase reporter gene assay
|
Homo sapiens
|
0.298
nM
|
|
Antagonist activity against glucocorticoid receptor in rat H4-IIE cells assessed as inhibition of dexamethasone-induced receptor transactivation pre-incubated for 1 hr before dexamethasone addition and measured 24 hrs post dexamethasone stimulation by tyrosine aminotransferase enzyme assay
|
Rattus norvegicus
|
1.94
nM
|
|
Reduction in LDL level in high fat and high cholesterol diet fed Syrian golden hamster at 30 mg/kg, po qd for 14 days
|
Mesocricetus auratus
|
43.0
%
|
|
Displacement of fluormone GS Red from human glucocorticoid receptor after 4 hrs by fluorescence polarization assay
|
Homo sapiens
|
0.09
nM
|
|
Antagonist activity at glucocorticoid receptor in human HepG2 cells assessed as inhibition of dexamethasone-induced tyrosine amino transferase activity preincubated for 30 mins followed by dexamethasone addition measured after 20 hrs
|
Homo sapiens
|
3.0
nM
|
|
Antagonist activity at PR in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity measured after 24 hrs
|
Homo sapiens
|
0.073
nM
|
|
Displacement of [1,2,6,7-3H]progesterone from recombinant human GST-tagged PGR LBD (678 to 933 residues) expressed in baculovirus-infected insect cells measured after 24 hrs by liquid scintillation counting method
|
Homo sapiens
|
5.2
nM
|
|
Antagonist activity at human AR assessed as reduction in DHT-induced transactivation
|
Homo sapiens
|
5.0
nM
|
|
Antagonist activity at human PRB expressed in African green monkey CV1 cells
|
Homo sapiens
|
0.3
nM
|
|
Antagonist activity at human GR assessed as reduction in dexamethasone-induced transactivation
|
Homo sapiens
|
0.8
nM
|
|
Antagonist activity at human GR expressed in CHO-K1 cells assessed as reduction in dexamethasone-induced response incubated for 20 hrs by luciferase reporter gene assay
|
Homo sapiens
|
3.3
nM
|
|
Agonist activity at AR (unknown origin) expressed in human LNCaP cells incubated for 20 hrs by luciferase reporter gene assay
|
Homo sapiens
|
11.9
nM
|
|
Antagonist activity at human PR expressed in CHO-K1 cells assessed as reduction in progesterone-induced response incubated for 20 hrs by luciferase reporter gene assay
|
Homo sapiens
|
0.4
nM
|
|
Antagonist activity at GR in human PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 6 hrs by RT-qPCR method
|
Homo sapiens
|
17.8
nM
|
|
Antagonist activity at GR in human PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 6 hrs by RT-qPCR method
|
Homo sapiens
|
14.8
nM
|
|
Antagonist activity at GR in dog PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 6 hrs by RT-qPCR method
|
Canis lupus familiaris
|
32.6
nM
|
|
Antagonist activity at GR in dog PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 6 hrs by RT-qPCR method
|
Canis lupus familiaris
|
20.2
nM
|
|
Antagonist activity at GR in monkey PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 6 hrs by RT-qPCR method
|
Macaca mulatta
|
13.9
nM
|
|
Antagonist activity at GR in monkey PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 6 hrs by RT-qPCR method
|
Macaca mulatta
|
21.9
nM
|
|
Antagonist activity at GR in mini pig PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 24 hrs by RT-qPCR method
|
Sus scrofa
|
10.9
nM
|
|
Antagonist activity at GR in mini pig PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 24 hrs by RT-qPCR method
|
Sus scrofa
|
19.7
nM
|
|
Antagonist activity at GR in human OVCAR5 assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 24 hrs by RT-qPCR method
|
Homo sapiens
|
13.0
nM
|
|
Displacement of fluormone RED from human full length glucocorticoid receptor after 4 hrs by fluorescence polarization assay
|
Homo sapiens
|
8.7
nM
|
|
Antagonist activity at glucocorticoid receptor (unknown origin) expressed in human ChaGoK1 cells assessed as inhibition of dexamethasone induced transactivation incubated for 24 hrs by beta-galactosidase reporter gene assay
|
Homo sapiens
|
15.0
nM
|
|
Antagonist activity at PR-b (unknown origin) expressed in Ishikawa cells assessed as inhibition of progesterone-induced PRE activity after 24 hrs by luciferase reporter gene based luminescence assay
|
Homo sapiens
|
98.0
%
|
|
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
|
11.2
%
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
-7.81
%
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
3.7
%
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
4.18
%
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
17.82
%
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
3.98
%
|
|
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
|
-10.45
%
|
|
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
|
-4.55
%
|
|
Binding affinity to GR (unknown origin)
|
Homo sapiens
|
15.0
nM
|
|
Antagonist activity at human progesterone receptor expressed in CHO-K1 cells harboring firefly luciferase gene after 20 hrs by One-Glo luciferase reporter gene assay
|
Homo sapiens
|
0.4
nM
|
|
Agonist activity at human androgen receptor in human LNCAP cells harboring firefly luciferase gene after 20 hrs by One-Glo luciferase reporter gene assay
|
Homo sapiens
|
11.9
nM
|
|
Antagonist activity at human glucocorticoid receptor expressed in CHO-K1 cells harboring firefly luciferase gene after 20 hrs by One-Glo luciferase reporter gene assay
|
Homo sapiens
|
3.26
nM
|
|
Displacement of fluormone tracer from full length human recombinant glucocorticoid receptor expressed in baculovirus expression system incubated for 2 hrs by competitive fluorescence polarization binding assay
|
Homo sapiens
|
2.3
nM
|
|
Antagonist activity at human glucocorticoid receptor expressed in CHO-K1 cells assessed as inhibition of glucocorticoid receptor-dexamethasone coactivator protein-protein interaction incubated for 24 hrs by bioluminescence assay
|
Homo sapiens
|
3.5
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
|
5.7
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
12.92
%
|
|
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
|
0.05
%
|
|
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
|
-0.13
%
|
|
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
|
0.05
%
|
|
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
|
-0.13
%
|
|
Inhibition of P4 induced antiproliferative activity against CD-1 mouse uterine epithelial cell at 10 mg/kg, ip for 7 days by immunohistochemistry method
|
Mus musculus
|
23.0
%
|
|
Antagonist activity at glucocorticoid receptor in human HeLa cells assessed as reduction in dexamethasone-induced luciferase activity by dual-Glo luciferase assay
|
Homo sapiens
|
0.64
nM
|
|