Structure

InChI Key VKHAHZOOUSRJNA-GCNJZUOMSA-N
Smiles CC#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=CC(=O)CCC4=C3[C@@H](c3ccc(N(C)C)cc3)C[C@@]21C
InChI
InChI=1S/C29H35NO2/c1-5-15-29(32)16-14-26-24-12-8-20-17-22(31)11-13-23(20)27(24)25(18-28(26,29)2)19-6-9-21(10-7-19)30(3)4/h6-7,9-10,17,24-26,32H,8,11-14,16,18H2,1-4H3/t24-,25+,26-,28-,29-/m0/s1

Physicochemical Descriptors

Property Name Value
Molecular Formula C29H35NO2
Molecular Weight 429.6
AlogP 5.41
Hydrogen Bond Acceptor 3.0
Hydrogen Bond Donor 1.0
Number of Rotational Bond 2.0
Polar Surface Area 40.54
Molecular species NEUTRAL
Aromatic Rings 1.0
Heavy Atoms 32.0

Bioactivity

Mechanism of Action Action Reference
Glucocorticoid receptor antagonist ANTAGONIST PubMed DailyMed
Protein: Glucocorticoid receptor

Description: Glucocorticoid receptor

Organism : Homo sapiens

P04150 ENSG00000113580
Protein: Progesterone receptor

Description: Progesterone receptor

Organism : Homo sapiens

P06401 ENSG00000082175
Targets EC50(nM) IC50(nM) Kd(nM) Ki(nM) Inhibition(%)
Enzyme Cytochrome P450 Cytochrome P450 family 2 Cytochrome P450 family 2C Cytochrome P450 2C8
- 1500-1500 - - -
Enzyme Cytochrome P450 Cytochrome P450 family 2 Cytochrome P450 family 2C Cytochrome P450 2C9
- 4900 - - -
Enzyme Cytochrome P450 Cytochrome P450 family 3 Cytochrome P450 family 3A Cytochrome P450 3A4
- 9500-9500 - 4700-4700 -
Enzyme Transferase
- - - - 101
Other nuclear protein
1 - - - -
Transcription factor Nuclear receptor Nuclear hormone receptor subfamily 3 Nuclear hormone receptor subfamily 3 group A Nuclear hormone receptor subfamily 3 group A member 1
- 5000-5000 - - 44-50
Transcription factor Nuclear receptor Nuclear hormone receptor subfamily 3 Nuclear hormone receptor subfamily 3 group A Nuclear hormone receptor subfamily 3 group A member 2
- 2244 - 2876 92
Transcription factor Nuclear receptor Nuclear hormone receptor subfamily 3 Nuclear hormone receptor subfamily 3 group C Nuclear hormone receptor subfamily 3 group C member 1
1-872 0-18 15 0-169 97-100
Transcription factor Nuclear receptor Nuclear hormone receptor subfamily 3 Nuclear hormone receptor subfamily 3 group C Nuclear hormone receptor subfamily 3 group C member 2
- 590-6000 - 640-851 70-96
Transcription factor Nuclear receptor Nuclear hormone receptor subfamily 3 Nuclear hormone receptor subfamily 3 group C Nuclear hormone receptor subfamily 3 group C member 3
0 0-10 - 0-15 98-100
Transcription factor Nuclear receptor Nuclear hormone receptor subfamily 3 Nuclear hormone receptor subfamily 3 group C Nuclear hormone receptor subfamily 3 group C member 4
10-12 1-89 - 1-22 95
Transporter Electrochemical transporter SLC superfamily of solute carriers SLC21/SLCO family of organic anion transporting polypeptides
- - - - 71
Transporter Primary active transporter ATP-binding cassette ABCB subfamily
- 2020 20000 - -
Unclassified protein
- 20-33 - - -
Assay Description Organism Bioactivity Reference
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

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Resources Reference
ChEBI 50692
ChEMBL CHEMBL1276308
DrugBank DB00834
DrugCentral 1805
FDA SRS 320T6RNW1F
Human Metabolome Database HMDB0014972
Guide to Pharmacology 2805
KEGG C07652
PDB 486
PharmGKB PA450500
PubChem 55245
SureChEMBL SCHEMBL16087
ZINC ZINC000003831128