|
In vitro antagonist activity against rat prostatic androgen receptor (AR)
|
None
|
3.2
nM
|
|
|
Binding affinity against rat prostate cytosolic Androgen receptor using [3H]mibolerone as radioligand
|
None
|
4.9
nM
|
|
|
Inhibitory constant against rat prostate cytosol androgen receptor using [3H]mibolerone
|
Rattus norvegicus
|
1.4
nM
|
|
|
Binding affinity to human CBG receptor (corticosteroid-binding globulins)
|
None
|
190.55
nM
|
|
|
Inhibition of human placental aromatase Cytochrome P450 19A1
|
Homo sapiens
|
600.0
nM
|
|
|
Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM
|
Cavia porcellus
|
21.7
%
|
|
|
Inhibition of rat prostate cytosolic androgen receptor
|
Rattus norvegicus
|
4.9
nM
|
|
|
Inhibition of [3H]mibolerone binding to cytosolic androgen receptor of rat ventral prostate
|
Rattus norvegicus
|
1.413
nM
|
|
|
Inhibition of human androgen receptor expressed in Escherichia coli
|
Homo sapiens
|
3.9
nM
|
|
|
Inhibitory activity against AR
|
Homo sapiens
|
2.7
nM
|
|
|
Displacement of [3H]DHT from human SHBG
|
Homo sapiens
|
14.0
nM
|
|
|
Binding affinity to androgen receptor
|
None
|
2.7
nM
|
|
|
Binding affinity at AR
|
None
|
2.7
nM
|
|
|
Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin
|
Homo sapiens
|
0.631
nM
|
|
|
Activity of human recombinant CYP3A4 assessed as conversion of testosterone to 6-beta-hydroxytestesterone at 25 uM after 60 mins in presence of 1 uM Miconazole
|
Homo sapiens
|
41.1
%
|
|
|
Activity of human recombinant CYP3A4 assessed as conversion of testosterone to 6-beta-hydroxytestesterone at 25 uM after 60 mins in presence of 10 uM Miconazole
|
Homo sapiens
|
10.5
%
|
|
|
Activity of human recombinant CYP3A4 assessed as conversion of testosterone to 6-beta-hydroxytestesterone at 25 uM after 60 mins in presence of 25 uM Miconazole
|
Homo sapiens
|
4.38
%
|
|
|
Activity of human recombinant CYP3A4 assessed as conversion of testosterone to 6-beta-hydroxytestesterone at 25 uM after 60 mins in presence of 1 uM deoxypodophyllotoxin
|
Homo sapiens
|
61.0
%
|
|
|
Activity of human recombinant CYP3A4 assessed as conversion of testosterone to 6-beta-hydroxytestesterone at 25 uM after 60 mins in presence of 10 uM deoxypodophyllotoxin
|
Homo sapiens
|
10.4
%
|
|
|
Activity of human recombinant CYP3A4 assessed as conversion of testosterone to 6-beta-hydroxytestesterone at 25 uM after 60 mins in presence of 25 uM deoxypodophyllotoxin
|
Homo sapiens
|
4.85
%
|
|
|
Activity of human recombinant CYP3A4 assessed as conversion of testosterone to 6-beta-hydroxytestesterone at 25 uM after 60 mins in presence of 1 uM epipodophyllotoxin
|
Homo sapiens
|
69.4
%
|
|
|
Activity of human recombinant CYP3A4 assessed as conversion of testosterone to 6-beta-hydroxytestesterone at 25 uM after 60 mins in presence of 10 uM epipodophyllotoxin
|
Homo sapiens
|
7.96
%
|
|
|
Activity of human recombinant CYP3A4 assessed as conversion of testosterone to 6-beta-hydroxytestesterone at 25 uM after 60 mins in presence of 25 uM epipodophyllotoxin
|
Homo sapiens
|
11.46
%
|
|
|
Activity of human recombinant CYP3A4 assessed as conversion of testosterone to 6-beta-hydroxytestesterone at 25 uM after 60 mins in presence of 1 uM podophyllotoxin
|
Homo sapiens
|
44.1
%
|
|
|
Activity of human recombinant CYP3A4 assessed as conversion of testosterone to 6-beta-hydroxytestesterone at 25 uM after 60 mins in presence of 10 uM podophyllotoxin
|
Homo sapiens
|
7.82
%
|
|
|
Activity of human recombinant CYP3A4 assessed as conversion of testosterone to 6-beta-hydroxytestesterone at 25 uM after 60 mins in presence of 25 uM podophyllotoxin
|
Homo sapiens
|
7.04
%
|
|
|
Activity of human recombinant CYP3A4 assessed as conversion of testosterone to 6-beta-hydroxytestesterone at 25 uM after 60 mins in presence of 1 uM demethylene-deoxy-podophyllotoxin
|
Homo sapiens
|
103.0
%
|
|
|
Activity of human recombinant CYP3A4 assessed as conversion of testosterone to 6-beta-hydroxytestesterone at 25 uM after 60 mins in presence of 10 uM demethylene-deoxy-podophyllotoxin
|
Homo sapiens
|
69.6
%
|
|
|
Activity of human recombinant CYP3A4 assessed as conversion of testosterone to 6-beta-hydroxytestesterone at 25 uM after 60 mins in presence of 25 uM demethylene-deoxy-podophyllotoxin
|
Homo sapiens
|
69.7
%
|
|
|
Activity of human recombinant CYP3A4 assessed as conversion of testosterone to 6-beta-hydroxytestesterone at 25 uM after 60 mins in presence of 1 uM demethylenepodophyllotoxin
|
Homo sapiens
|
95.0
%
|
|
|
Activity of human recombinant CYP3A4 assessed as conversion of testosterone to 6-beta-hydroxytestesterone at 25 uM after 60 mins in presence of 10 uM demethylenepodophyllotoxin
|
Homo sapiens
|
98.7
%
|
|
|
Activity of human recombinant CYP3A4 assessed as conversion of testosterone to 6-beta-hydroxytestesterone at 25 uM after 60 mins in presence of 25 uM demethylenepodophyllotoxin
|
Homo sapiens
|
97.1
%
|
|
|
Agonist activity at androgen receptor in mouse NIH3T3 cells transiently transfected with beta-galactosidase reporter gene assessed as cellular transformation by R-SAT assay
|
Mus musculus
|
1.995
nM
|
|
|
Agonist activity at androgen receptor in human MDA-KB2 cells transfected with MMTV linked luciferase assessed as transcriptional activation by luciferase reporter gene assay
|
Homo sapiens
|
3.162
nM
|
|
|
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
|
7.5
%
|
|
|
Binding affinity to androgen receptor by fluorescence binding assay
|
None
|
30.0
nM
|
|
|
Displacement of fluorescent-tagged R1881 from androgen receptor after 4 hrs by fluorometric assay
|
None
|
29.0
nM
|
|
|
DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
|
Bos taurus
|
252.0
nM
|
|
|
DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
|
Escherichia coli
|
6.169
nM
|
|
DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
|
Escherichia coli
|
4.112
nM
|
|
|
Displacement of [3H]R1881 from wild type human androgen receptor expressed in COS-1 cells co-transfected with pSG5 after 15 mins by scintillation assay relative to untreated control
|
Homo sapiens
|
0.1
%
|
|
|
Displacement of [3H]R1881 from wild type human androgen receptor expressed in COS-1 cells co-transfected with pSG5 after 15 mins by scintillation assay
|
Homo sapiens
|
4.571
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
|
33.2
%
|
|
|
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
|
37.4
%
|
|
|
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
|
-175.1
%
|
|
|
Displacement of [3H]Mibolerone from rat recombinant androgen receptor expressed in Escherichia coli after 4 hrs
|
Rattus norvegicus
|
4.3
nM
|
|
Displacement of [3H]Mibolerone from rat recombinant androgen receptor expressed in Escherichia coli after 4 hrs
|
Rattus norvegicus
|
6.5
nM
|
|
|
Displacement of [3H]Mibolerone from rat recombinant androgen receptor expressed in Escherichia coli at 10 uM after 4 hrs relative to control
|
Rattus norvegicus
|
2.0
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
79.99
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
92.19
%
|
|
|
Antagonist activity against pSG5-tagged human androgen receptor expressed in COS1 cells assessed as reduction in receptor-mediated transcriptional activity by AR-regulated rat probasin promoter fragment driven firefly luciferase reporter assay
|
Homo sapiens
|
4.17
nM
|
|
|
Displacement of [3H]R1881 from pSG5-tagged human androgen receptor expressed in COS1 cells assessed as relative binding inhibition
|
Homo sapiens
|
4.27
nM
|
|
|
Antagonist activity against pSG5-tagged human androgen receptor expressed in COS1 cells assessed as receptor-mediated testosterone-induced transcriptional activity at 10 uM by AR-regulated rat probasin promoter fragment driven firefly luciferase reporter assay (Rvb = 100 +/- 5.7%)
|
Homo sapiens
|
100.0
%
|
|
|
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
|
Homo sapiens
|
34.0
nM
|
|
|
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
|
Homo sapiens
|
38.4
nM
|
|
|
Androgenic activity at human androgen receptor expressed in African green monkey CV-1 cells assessed as increase in interaction between VP16-fused AR-NTD and GAL4-fused AR-LBD after 17 hrs by luciferase reporter gene assay
|
Homo sapiens
|
1.1
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
|
-3.69
%
|
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
-8.96
%
|
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
3.5
%
|
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
-7.2
%
|
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
8.83
%
|
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
3.12
%
|
|
|
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
|
1.59
%
|
|
