|
Agonistic activity measures the ability to induce alkaline phosphatase in T47D human breast cancer cell line
|
None
|
0.5
nM
|
|
|
Agonistic activity against Human androgen receptor(hAR) expressed in CV-1 cells
|
Homo sapiens
|
6.1
nM
|
|
|
Effective concentration against Androgen receptor
|
Mus musculus
|
6.1
nM
|
|
Effective concentration against Androgen receptor
|
Mus musculus
|
159.0
%
|
|
|
Inhibition of human androgen receptor at 10e-12 to 10e-5 M
|
Homo sapiens
|
6.1
nM
|
|
|
Displacement of DHT from human androgen receptor
|
Homo sapiens
|
2.9
nM
|
|
|
Inhibition of DHT binding to human androgen receptor expressed in baculovirus SF-12 cells
|
Homo sapiens
|
2.9
nM
|
|
|
Binding affinity against human androgen receptor
|
None
|
2.9
nM
|
|
|
Binding affinity against baculovirus expressed human androgen receptor (hAR)
|
None
|
2.9
nM
|
|
|
Binding affinity was determined on Human androgen receptor (hAR) using progesterone as radioligand.
|
None
|
2.9
nM
|
|
|
Effective concentration against Androgen receptor in mouse fibroblast L929 cells
|
Mus musculus
|
6.1
nM
|
|
|
Effective concentration (EC50) against human progesterone receptor expressed in CV-1 cell
|
Homo sapiens
|
0.15
nM
|
|
|
Inhibitory activity (IC50) against human androgen receptor expressed in CV-1 cells
|
Homo sapiens
|
6.1
nM
|
|
|
IC50 determined against human estrogen receptor in CV-1 cells
|
None
|
924.0
nM
|
|
|
Inhibitory activity (IC50) against human glucocorticoid receptor expressed in CV-1 cells
|
Homo sapiens
|
10.0
nM
|
|
|
Agonistic activity against Human estrogen receptor(hER) expressed in CV-1 cells
|
Homo sapiens
|
924.0
nM
|
|
|
Inhibition of binding to human estrogen receptor
|
Homo sapiens
|
924.0
nM
|
|
|
Agonist activity against Human glucocorticoid receptor(hGR) expressed in CV-1 cells
|
Homo sapiens
|
10.0
nM
|
|
|
Effective concentration against glucocorticoid receptor in human lung A549 cells
|
Homo sapiens
|
10.0
nM
|
|
|
Inhibition of human glucocorticoid receptor at 10e-12 to 10e-5 M
|
Homo sapiens
|
10.0
nM
|
|
|
Displacement of Dexamethasone from human glucocorticoid receptor
|
Homo sapiens
|
13.2
nM
|
|
|
Inhibition of Dexamethasone binding to human glucocorticoid receptor expressed in baculovirus SF-12 cells
|
Homo sapiens
|
13.2
nM
|
|
|
Binding affinity against human glucocorticoid receptor expressed in SF-12 cells
|
Homo sapiens
|
13.2
nM
|
|
|
Binding affinity against baculovirus expressed human glucocorticoid receptor (hGR)
|
None
|
13.2
nM
|
|
|
Binding affinity was determined on Human glucocorticoid receptor (hAR) using progesterone as radioligand.
|
None
|
13.2
nM
|
|
|
Effective concentration against GR (glucocorticoid receptor)
|
Homo sapiens
|
10.0
nM
|
|
Effective concentration against GR (glucocorticoid receptor)
|
Homo sapiens
|
157.0
%
|
|
|
Agonistic activity against human progesterone receptor expressed in CV-1 cells
|
Homo sapiens
|
0.15
nM
|
|
|
Agonistic activity against human progesterone receptor in T47D breast cancer cells
|
None
|
0.33
nM
|
|
|
Agonist activity was determined against hPR (human progesterone receptor) compared to that of progesterone (100%)
|
None
|
0.15
nM
|
|
|
Agonistic activity to the human progesterone receptor (hPR)assayed in CV-1 cells in cotransfection assay.
|
None
|
0.15
nM
|
|
|
Agonistic activity was measured for modulation of hPR-B (human progesterone receptor) in co-transfected CV-1 cells.
|
Homo sapiens
|
0.15
nM
|
|
|
Compound was tested for agonistic activity by cotransfection assay against human Progesterone receptor in CV-1 cells
|
None
|
0.15
nM
|
|
|
Agonistic activity by cotransfection assay against human Progesterone receptor in T47D cells
|
None
|
0.33
nM
|
|
|
Effective concentration against PR (progesterone receptor)
|
Homo sapiens
|
0.12
nM
|
|
|
Agonistic activity against progesterone receptor in alkaline phosphatase assay using human T47D breast carcinoma cell line
|
None
|
0.12
nM
|
|
|
Inhibition of [3H]P4 to progesterone receptor (PR) of human T47D breast carcinoma cells
|
Homo sapiens
|
10.8
nM
|
|
|
Inhibition of 3 nM [3H]R5020 binding to progesterone receptor in human T47D cells
|
Homo sapiens
|
10.8
nM
|
|
|
Binding affinity for Progesterone receptor (PR) in human T47D breast carcinoma cells
|
Homo sapiens
|
10.8
nM
|
|
|
Binding affinity was determined against hPR-A (human progesterone receptor) using progesterone radioligand in competitive binding assay
|
None
|
0.34
nM
|
|
|
Binding affinity against human progesterone receptor
|
None
|
0.34
nM
|
|
|
Compound was evaluated for its binding affinity against baculovirus expressed Progesterone receptor
|
None
|
0.34
nM
|
|
|
The binding affinity on Human progesterone receptor (hPR-A) using progesterone as radioligand.
|
None
|
0.34
nM
|
|
|
The binding affinity measured using baculovirus-expressed hPR-A in sf21 cells.
|
Homo sapiens
|
0.34
nM
|
|
|
Binding affinity towards human progesterone receptor A isoform using progesterone as radioligand
|
None
|
0.34
nM
|
|
|
Inhibitory progestational activity on oral administration in uterine C3 model
|
Rattus norvegicus
|
0.026
mg kg-1
|
|
|
Effective concentration on alkaline phosphatase activity in human T47D breast carcinoma cell line.
|
Homo sapiens
|
0.1
nM
|
|
|
Effective concentration of progesterone receptor agonist induction of alkaline phosphatase activity in human T47D breast carcinoma cells
|
Homo sapiens
|
0.5
nM
|
|
|
Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881)
|
Rattus norvegicus
|
794.33
nM
|
|
Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881)
|
Rattus norvegicus
|
35.48
nM
|
|
|
Displacement of [3H]progesterone from Progesterone receptor
|
Homo sapiens
|
0.3388
nM
|
|
|
Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin
|
Homo sapiens
|
630.96
nM
|
|
|
Agonist activity at human progesterone receptor
|
Homo sapiens
|
0.5
nM
|
|
|
Agonist activity at human progesterone receptor in human T47D cells assessed as alkaline phosphatase activity
|
Homo sapiens
|
0.4
nM
|
|
|
Binding affinity at human progesterone receptor
|
Homo sapiens
|
1.4
nM
|
|
|
DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
|
Bos taurus
|
2.247
nM
|
|
DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
|
Bos taurus
|
0.293
nM
|
|
|
DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
|
Escherichia coli
|
7.259
nM
|
|
DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
|
Escherichia coli
|
4.839
nM
|
|
|
DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
|
None
|
19.0
nM
|
|
DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
|
None
|
8.637
nM
|
|
|
Inhibition of recombinant AKR1C3 (unknown origin) assessed as decrease in oxidation of 1-acenaphthenol substrate by spectrophotometric analysis
|
Homo sapiens
|
300.0
nM
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
105.87
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
104.39
%
|
|
|
Discontinuous Radiometric Assay: Compounds may be evaluated as selective reversible inhibitors of AKR1C3 by screening them against homogeneous recombinant AKR1C1-AKR1C4 expressed in E. coli. In each case, a discontinuous radiometric assay may be used to monitor the inhibition of progesterone reduction (20-ketosteroid reduction) catalyzed by AKR1C1, the inhibition of Δ4-AD reduction (17-ketosteroid reduction) catalyzed by AKR1C3, and the inhibition of 5α-DHT reduction (3-ketosteroid reduction) catalyzed by AKR1C2 and AKR1C4 (by measuring the formation of 20α-hydroxyprogesterone, testosterone or 3α-androstanediol by radiochromatography). Secondary screens of the compounds of interest include: (a) a full-screen against all nine human recombinant AKR enzymes to ensure there are no-intended off-target effects (in this context AKR1B10 (retinal reductase; SEQ ID NO:5) has been shown to be potently inhibited by N-phenylanthranilates) (Endo et al., 2010, Biol. Pharm. Bull. 33:886-90); (b) a screen against COX-1 and COX-2 to reaffirm that compounds do not act as NSAIDs; and (c) an expanded screen against other nuclear receptors (especially other steroid hormone receptors).
|
Homo sapiens
|
280.0
nM
|
|
|
Discontinuous Radiometric Assay: Compounds may be evaluated as selective reversible inhibitors of AKR1C3 by screening them against homogeneous recombinant AKR1C1-AKR1C4 expressed in E. coli. In each case, a discontinuous radiometric assay may be used to monitor the inhibition of progesterone reduction (20-ketosteroid reduction) catalyzed by AKR1C1, the inhibition of Δ4-AD reduction (17-ketosteroid reduction) catalyzed by AKR1C3, and the inhibition of 5α-DHT reduction (3-ketosteroid reduction) catalyzed by AKR1C2 and AKR1C4 (by measuring the formation of 20α-hydroxyprogesterone, testosterone or 3α-androstanediol by radiochromatography). Secondary screens of the compounds of interest include: (a) a full-screen against all nine human recombinant AKR enzymes to ensure there are no-intended off-target effects (in this context AKR1B10 (retinal reductase; SEQ ID NO:5) has been shown to be potently inhibited by N-phenylanthranilates) (Endo et al., 2010, Biol. Pharm. Bull. 33:886-90); (b) a screen against COX-1 and COX-2 to reaffirm that compounds do not act as NSAIDs; and (c) an expanded screen against other nuclear receptors (especially other steroid hormone receptors).
|
Homo sapiens
|
700.0
nM
|
|
|
Antibacterial activity against Staphylococcus aureus MRSA ATCC 43300 (CO-ADD:GP_020); MIC in CAMBH media, using NBS plates, by OD(600)
|
Staphylococcus aureus subsp. aureus
|
10.39
%
|
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
2.0
%
|
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
17.28
%
|
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
8.66
%
|
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
28.19
%
|
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
4.88
%
|
|
|
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
|
-5.46
%
|
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
-3.44
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
10.47
%
|
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
-0.07
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
0.93
%
|
|
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
|
0.93
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
-0.07
%
|
|
