|
Inhibition of [3H]thymidine uptake into L1210 cells at a concentration of 1 uM
|
Mus musculus
|
89.0
%
|
|
|
Inhibition of [3H]thymidine uptake into L1210 cells at a concentration of 1 uM in the presence of 5 mg/mL of AGP (alpha1-acid glycoprotein)
|
Mus musculus
|
4.0
%
|
|
|
Inhibition of phosphodiesterase 5 (PDE5) from porcine platelets, range 0.244-1.35
|
Sus scrofa
|
574.0
nM
|
|
|
Inhibition of Phosphodiesterase 4 (PDE4) from guinea pig macrophages
|
Cavia porcellus
|
500.0
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
|
18.4
%
|
|
|
Displacement of 5-(SAENTA)-X8-fluorescein from K562 cell nucleoside transporter
|
Homo sapiens
|
8.79
nM
|
|
|
Inhibitory activity against cyclic GMP-phosphodiesterase (PDE V) isolated from porcine aorta.
|
Sus scrofa
|
520.0
nM
|
|
|
Inhibition of human phosphodiesterase 6
|
Homo sapiens
|
125.0
nM
|
|
|
Inhibition of human phosphodiesterase 7
|
Homo sapiens
|
600.0
nM
|
|
|
Inhibition of human phosphodiesterase 11
|
Homo sapiens
|
400.0
nM
|
|
|
Inhibition of [3H]thymidine uptake in L1210 cells
|
Mus musculus
|
340.0
nM
|
|
|
Inhibition of [3H]thymidine uptake in L1210 cells at 1 uM
|
Mus musculus
|
80.0
%
|
|
|
Inhibition of [3H]thymidine uptake in L1210 cells at 10 uM
|
Mus musculus
|
99.0
%
|
|
|
Inhibition of [3H]thymidine uptake in L1210 cells in the presence of 5 mg/mL human AGP at 1 uM
|
Mus musculus
|
4.0
%
|
|
|
Inhibition of [3H]-thymidine uptake in L1210 cells in the presence of 5 mg/mL human AGP at 10 uM
|
Mus musculus
|
13.0
%
|
|
|
Inhibition of ENT1 in human K562 cells at 10 uM by flow cytometric assay
|
Homo sapiens
|
86.7
%
|
|
|
Inhibition of ENT1 in human K562 cells by flow cytometric assay
|
Homo sapiens
|
144.8
nM
|
|
Inhibition of ENT1 in human K562 cells by flow cytometric assay
|
Homo sapiens
|
8.18
nM
|
|
|
Activity at androgen receptor ligand binding domain assessed as inhibition of SRC2-3 interaction at 50 uM after 2 hrs by fluorescence polarization assay
|
None
|
82.0
%
|
|
|
Inhibition of ENT-mediated [3H]thymidine incorporation in human COR-L23 cells by liquid scintillation counting
|
Homo sapiens
|
15.0
nM
|
|
|
Inhibition of ENT-mediated [3H]thymidine incorporation in human COR-L23 cells at 0.1 uM by liquid scintillation counting
|
Homo sapiens
|
78.0
%
|
|
|
Inhibition of ENT-mediated [3H]thymidine incorporation in human COR-L23 cells at 1 uM by liquid scintillation counting
|
Homo sapiens
|
96.0
%
|
|
|
DRUGMATRIX: Sodium/nucleoside co-transporter radioligand binding (ligand: nitrobenzylthioinosine)
|
Cavia porcellus
|
83.0
nM
|
|
DRUGMATRIX: Sodium/nucleoside co-transporter radioligand binding (ligand: nitrobenzylthioinosine)
|
Cavia porcellus
|
29.0
nM
|
|
|
DRUGMATRIX: GABAA, Flunitrazepam, Central radioligand binding (ligand: [3H] Flunitrazepam)
|
Rattus norvegicus
|
382.0
nM
|
|
DRUGMATRIX: GABAA, Flunitrazepam, Central radioligand binding (ligand: [3H] Flunitrazepam)
|
Rattus norvegicus
|
311.0
nM
|
|
|
Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB1 expressed in baculovirus infected insect Sf21 cells at 100 uM
|
Trypanosoma brucei
|
50.0
%
|
|
|
Inhibition of ABCC5 in human erythrocytes assessed as inhibition of ATP-mediated [3H]cGMP uptake in inside-out vesicles at 32 uM after 60 mins by liquid scintillation counting
|
Homo sapiens
|
95.0
%
|
|
|
Inhibition of norA-mediated ethidium bromide efflux in Staphylococcus aureus SA-1199B harboring grlA A116E mutant at 50 uM after 5 mins by fluorometric analysis
|
Staphylococcus aureus
|
42.3
%
|
|
|
Inhibition of human recombinant MDR1 expressed in mouse L5178Y cells assessed as inhibition of rhodamine-123 efflux at 10'-4 M preincubated for 10 mins measured after 20 mins by FACS analysis
|
Homo sapiens
|
4.7
%
|
|
|
Inhibition of p-glycoprotein-mediated calcein-AM efflux
|
None
|
90.0
%
|
|
|
Inhibition of human prune assessed as reduction of cAMP-phosphodiesterase activity
|
Homo sapiens
|
780.0
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
|
91.9
%
|
|
|
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
|
91.8
%
|
|
|
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
|
83.1
%
|
|
|
Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation at 20 uM after 45 mins by spectrophotometric analysis relative to control
|
Mus musculus
|
55.0
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
312.58
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
89.24
%
|
|
|
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
|
-23.93
%
|
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
7.34
%
|
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
2.81
%
|
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
9.85
%
|
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
12.25
%
|
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
2.59
%
|
|
|
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
|
5.59
%
|
|
|
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
|
10.45
%
|
|
|
Inhibition of recombinant N-terminal GST tagged and C-terminal His-tagged human PDE7B (109-ens aa) expressed in Sf9 cells using FAM-cAMP as substrate at 0.1xIC50 incubated for 60 mins by fluorescence plate reader analysis
|
Homo sapiens
|
3.0
%
|
|
|
Inhibition of recombinant N-terminal GST-tagged full length human PDE8A1 expressed in Sf9 cells using FAM-cAMP as substrate at 0.1xIC50 incubated for 60 mins by fluorescence plate reader analysis
|
Homo sapiens
|
13.0
%
|
|
|
Inhibition of recombinant N-terminal GST-tagged full length human PDE11A4 expressed in Sf9 cells using FAM-cAMP as substrate at 0.1xIC50 incubated for 60 mins by fluorescence plate reader analysis
|
Homo sapiens
|
16.0
%
|
|
|
Inhibition of recombinant N-terminal GST tagged and C-terminal His-tagged human PDE7B (109-ens aa) expressed in Sf9 cells using FAM-cAMP as substrate at 1xIC50 incubated for 60 mins by fluorescence plate reader analysis
|
Homo sapiens
|
48.0
%
|
|
|
Inhibition of recombinant N-terminal GST-tagged full length human PDE8A1 expressed in Sf9 cells using FAM-cAMP as substrate at 1xIC50 incubated for 60 mins by fluorescence plate reader analysis
|
Homo sapiens
|
55.0
%
|
|
|
Inhibition of recombinant N-terminal GST-tagged full length human PDE11A4 expressed in Sf9 cells using FAM-cAMP as substrate at 1xIC50 incubated for 60 mins by fluorescence plate reader analysis
|
Homo sapiens
|
57.0
%
|
|
|
Inhibition of recombinant N-terminal GST tagged and C-terminal His-tagged human PDE7B (109-ens aa) expressed in Sf9 cells using FAM-cAMP as substrate at 10xIC50 incubated for 60 mins by fluorescence plate reader analysis
|
Homo sapiens
|
92.0
%
|
|
|
Inhibition of recombinant N-terminal GST-tagged full length human PDE8A1 expressed in Sf9 cells using FAM-cAMP as substrate at 10xIC50 incubated for 60 mins by fluorescence plate reader analysis
|
Homo sapiens
|
88.0
%
|
|
|
Inhibition of recombinant N-terminal GST-tagged full length human PDE11A4 expressed in Sf9 cells using FAM-cAMP as substrate at 10xIC50 incubated for 60 mins by fluorescence plate reader analysis
|
Homo sapiens
|
92.0
%
|
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
-1.034
%
|
|
|
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
|
0.24
%
|
|
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
|
0.24
%
|
|
