| Unchecked |
Inhibition |
= |
95.7 |
% |
Inhibition of HCV J4 genotype 1b recombinant His-tagged NS5B truncated at 21 C-terminal expressed in Escherichia coli C41 (DE3) assessed as synthesis of double stranded DNA at 20 uM |
CHEMBL3792370 |
| Unchecked |
IC50 |
= |
600.0 |
nM |
Inhibition of HCV J4 genotype 1b recombinant His-tagged NS5B truncated at 21 C-terminal expressed in Escherichia coli C41 (DE3) assessed as synthesis of double stranded DNA |
CHEMBL3792370 |
| Hepatitis C virus |
EC50 |
= |
9100.0 |
nM |
Antiviral activity against HCV genotype 2a/2a J6/JFH1 model infected in Huh7.5 cells after 72 hrs by luciferase reporter gene assay |
CHEMBL3792370 |
| SARS-CoV-2 |
Inhibition index |
= |
0.184 |
|
Inhibition of cell viability relative to arbidol control (inhibition index > 1 indicates higher activity) measured by fluorescence (OD590nm) in Vero E6 cells infected with SARS-CoV-2 (strain BavPat1) at MOI 0.002 after 72hrs |
CHEMBL4303097 |
| SARS-CoV-2 |
Inhibition |
= |
-10.02 |
% |
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 |
CHEMBL4303101 |
| SARS-CoV-2 |
Hit score |
= |
0.3029 |
|
Antiviral activity against SARS-CoV-2 (USA-WA1/2020 strain) measured by imaging in HRCE cells at MOI 0.4 after 96 hrs (reported as hit score from 0-1 for on-disease vs off-disease activity: scores >0.6 considered hits) |
CHEMBL4303122 |
| Hepatitis C virus NS5B RNA-dependent RNA polymerase |
EC50 |
= |
1.8 |
nM |
Inhibition of HCV genotype 1b NS5B RNA dependent RNA polymerase |
CHEMBL4373658 |
| Replicase polyprotein 1ab |
Inhibition |
= |
17.1 |
% |
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate |
CHEMBL4495564 |
| SARS-CoV-2 |
Inhibition |
= |
0.55 |
% |
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 |
CHEMBL4495565 |
| Hepatitis C virus serine protease, NS3/NS4A |
Inhibition |
> |
99.5 |
% |
Inhibition of HCV NS3/4a protease |
CHEMBL4609973 |
| ADMET |
T1/2 |
= |
5.5 |
hr |
Half life in human |
CHEMBL4609973 |
| ADMET |
F |
= |
70.0 |
% |
Absolute bioavailability in human |
CHEMBL4609973 |
| ADMET |
Drugexcretion |
= |
26.2 |
% |
Drug excretion in human feces assessed as dasabuvir level |
CHEMBL4609973 |
| ADMET |
Drugexcretion |
= |
94.4 |
% |
Drug excretion in human feces |
CHEMBL4609973 |
| ADMET |
Drugexcretion |
= |
2.0 |
% |
Drug excretion in human urine |
CHEMBL4609973 |
| SARS-CoV-2 |
Inhibition |
= |
0.55 |
% |
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 |
CHEMBL4495565 |
| Protein cereblon |
Ki |
= |
4710.0 |
nM |
Binding affinity to human CRBN-thalidomide binding domain expressed in Escherichia coli by measuring baseline corrected normalized fluorescence by MST based assay |
CHEMBL4673389 |
| Protein cereblon |
IC50 |
= |
15600.0 |
nM |
Binding affinity to human CRBN-thalidomide binding domain expressed in Escherichia coli by measuring baseline corrected normalized fluorescence by MST based assay |
CHEMBL4673389 |
