|
Inhibition of 1.0 nM [3H]mibolerone binding to human androgen receptor of PC3/AR cell lysate
|
Homo sapiens
|
154.0
nM
|
|
|
Inhibition of beta-lactamase at 100 uM
|
None
|
5.0
%
|
|
|
Inhibition of chymotrypsin at 250 uM
|
unidentified
|
5.0
%
|
|
|
Compound was tested for the inhibition of malate dehydrogenase (MDH) at 100 uM
|
None
|
5.0
%
|
|
|
Inhibition of [3H]mibolerone binding to human Androgen receptor of PC3/AR Cell Lysate
|
Homo sapiens
|
154.0
nM
|
|
|
Inhibition of prostate weight in intact Sprague-Dawley rat at 30 mg/kg relative to control
|
Rattus norvegicus
|
51.0
%
|
|
|
Antagonist activity at human androgen receptor expressed in mouse NIH3T3 cells assessed as inhibition of DHT-induced transcriptional activation after 24 hrs by androgen response element-mediated luciferase reporter gene assay
|
Homo sapiens
|
580.0
nM
|
|
|
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy
|
Homo sapiens
|
34.1
%
|
|
|
Binding affinity to androgen receptor in hamster DDT cells by scintillation counting
|
Cricetinae
|
630.96
nM
|
|
|
Binding affinity to androgen receptor LBD T877A mutant in hamster DDT cells by scintillation counting
|
Cricetinae
|
398.11
nM
|
|
|
Inhibition of human 17beta-HSD7 expressed in HEK293 cells assessed as inhibition of reduction of [14C]estrone into [14C]estradiol at 0.3 uM after 7 hrs
|
Homo sapiens
|
18.6
%
|
|
|
Inhibition of human 17beta-HSD7 expressed in HEK293 cells assessed as inhibition of reduction of [14C]estrone into [14C]estradiol at 3 uM after 7 hrs
|
Homo sapiens
|
10.8
%
|
|
|
Antagonist activity at human androgen receptor expressed in mouse NIH3T3 cells assessed as inhibition of dihydrotestosterone -induced luciferase transactivation activity at 0.1 nM by ARE-luciferase reporter gene assay
|
Homo sapiens
|
20.0
%
|
|
|
Displacement of [3H]dihydrotestosterone from GST-tagged human androgen receptor expressed in Escherichia coli HB101 at 10 uM by liquid scintillation counting relative to dihydrotestosterone
|
Homo sapiens
|
12.0
%
|
|
|
Growth inhibition of mouse SC3 cells after 3 days by WST-8 assay
|
Mus musculus
|
720.0
nM
|
|
|
Anticancer activity against human LNCAP cells assessed as change in PSA gene expression at 10 umol after 48 hrs by RT-PCR analysis
|
Homo sapiens
|
99.0
%
|
|
|
Anticancer activity against human LNCAP cells after 24 hrs by MTT assay in presence of testosterone
|
Homo sapiens
|
900.0
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
|
6.8
%
|
|
|
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
|
9.0
%
|
|
|
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
|
65.8
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
130.85
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
133.56
%
|
|
|
Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate assessed as formation of prostanoid products at 500 uM preincubated for 10 mins prior to substrate addition measured after 2 mins by Ellman's method relative to control
|
Homo sapiens
|
100.0
%
|
|
|
Inhibition of COX-1 (unknown origin) using arachidonic acid as substrate assessed as formation of prostanoid products at 500 uM preincubated for 10 mins prior to substrate addition measured after 2 mins by Ellman's method relative to control
|
Homo sapiens
|
100.0
%
|
|
|
Inhibition of AADAC in human kidney microsome
|
Homo sapiens
|
600.0
nM
|
|
|
Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2B6 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2C9 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2C19 in human liver microsomes at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2D6 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP3A4 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2C8 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Induction of mitochondrial dysfunction in Sprague-Dawley rat liver mitochondria assessed as inhibition of mitochondrial respiration per mg mitochondrial protein measured for 20 mins by A65N-1 oxygen probe based fluorescence assay
|
Rattus norvegicus
|
57.6
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
|
10.52
%
|
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
4.1
%
|
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
13.37
%
|
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
6.76
%
|
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
31.86
%
|
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
3.45
%
|
|
|
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
|
1.08
%
|
|
|
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
|
44.86
%
|
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
15.67
%
|
|
|
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
|
-0.08
%
|
|
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
|
-0.08
%
|
|
|
Antiproliferative activity against androgen-sensitive human LNCAP cells assessed as inhibition of cell growth at 50 uM incubated for 48 hrs by sulforhodamine B assay relative to control
|
Homo sapiens
|
-3.4
%
|
|
|
Antiproliferative activity against androgen-sensitive human LNCAP cells assessed as inhibition of testosterone-induced cell growth at 50 uM incubated for 48 hrs by sulforhodamine B assay relative to control
|
Homo sapiens
|
29.6
%
|
|
|
Antiproliferative activity against androgen-sensitive human LNCAP cells assessed as inhibition of DHT-induced cell growth at 50 uM incubated for 48 hrs by sulforhodamine B assay relative to control
|
Homo sapiens
|
25.11
%
|
|
