| Unchecked |
Inhibition |
|
|
% |
Inhibition of HCV C-terminal His-tagged NS5Bdelta21 enzyme assessed as reduction in NS5B-mediated RNA polymerization using [32P]-GpG primer, RNA template and rNTP nucleotide mix incubated for 120 mins by PAGE method |
CHEMBL3421565 |
| Unchecked |
IC50 |
= |
5600.0 |
nM |
Inhibition of HCV C-terminal His-tagged NS5Bdelta21 enzyme assessed as reduction in NS5B-mediated RNA polymerization using [32P]-GpG primer, RNA template and rNTP nucleotide mix incubated for 120 mins by PAGE method |
CHEMBL3421565 |
| Unchecked |
Inhibition |
|
|
% |
Inhibition of HCV C-terminal His-tagged NS5Bdelta21 enzyme assessed as induction of pausing at sites of GMP incorporation during NS5B-mediated RNA polymerization using [32P]-GpG primer, RNA template and rNTP nucleotide mix incubated for 120 mins by PAGE method |
CHEMBL3421565 |
| Hepatocyte |
Drug metabolism |
|
|
|
Drug level in human primary hepatocytes treated with 50 uM Ethyl 3-(2-(((R)-(((2R,3R,4R,5R)-5-(2,6-Diamino-9H-purin-9-yl)-3,4-dihydroxy-4-methyltetrahydrofuran-2-yl)methoxy)(((S)-1-ethoxy-1-oxopropan-2-yl)amino)phosphoryl)oxy)phenyl)-propanoate assessed as compound formation incubated for 4 hrs at 37 degC by LC-MS/MS method |
CHEMBL3421565 |
| ADMET |
Drug metabolism |
|
|
|
Drug level in human HuH7 cells treated with 50 uM Ethyl 3-(2-(((R)-(((2R,3R,4R,5R)-5-(2,6-Diamino-9H-purin-9-yl)-3,4-dihydroxy-4-methyltetrahydrofuran-2-yl)methoxy)(((S)-1-ethoxy-1-oxopropan-2-yl)amino)phosphoryl)oxy)phenyl)-propanoate assessed as compound formation incubated for 4 hrs at 37 degC by LC-MS/MS method |
CHEMBL3421565 |
| Hepatocyte |
Drug metabolism |
|
|
|
Drug level in human primary hepatocytes treated with 50 uM beta-D-2,6-diaminopurine nucleoside assessed as compound formation incubated for 4 hrs at 37 degC by LC-MS/MS method |
CHEMBL3421565 |
| ADMET |
Drug metabolism |
|
|
|
Drug level in human HuH7 cells treated with 50 uM beta-D-2,6-diaminopurine nucleoside assessed as compound formation incubated for 4 hrs at 37 degC by LC-MS/MS method |
CHEMBL3421565 |
| ADMET |
Drug metabolism |
|
|
|
Drug level in human HuH7 cells treated with 50 uM Isopropyl 3-(2-(((S)-(((2R,3S,4R,5R)-5-(2,6-Diamino-9H-purin-9-yl)-3,4-dihydroxy-4-methyltetrahydrofuran-2-yl)methoxy)-(((S)-1-isopropoxy-1-oxopropan-2-yl)amino)phosphoryl)oxy)-phenyl)propanoate 15c(Sp) and Isopropyl 3-(2-(((R)-(((2R,3S,4R,5R)-5-(2,6-Diamino-9H-purin-9-yl)-3,4-dihydroxy-4-methyltetrahydrofuran-2-yl)methoxy)(((S)-1-isopropoxy-1-oxopropan-2-yl)amino)phosphoryl)oxy)phenyl)propanoate assessed as compound formation incubated for 4 hrs at 37 degC by LC-MS/MS method |
CHEMBL3421565 |
| Hepatocyte |
Drug metabolism |
|
|
|
Drug level in human primary hepatocytes treated with 50 uM Isopropyl 3-(2-(((S)-(((2R,3S,4R,5R)-5-(2,6-Diamino-9H-purin-9-yl)-3,4-dihydroxy-4-methyltetrahydrofuran-2-yl)methoxy)-(((S)-1-isopropoxy-1-oxopropan-2-yl)amino)phosphoryl)oxy)-phenyl)propanoate 15c(Sp) and Isopropyl 3-(2-(((R)-(((2R,3S,4R,5R)-5-(2,6-Diamino-9H-purin-9-yl)-3,4-dihydroxy-4-methyltetrahydrofuran-2-yl)methoxy)(((S)-1-isopropoxy-1-oxopropan-2-yl)amino)phosphoryl)oxy)phenyl)propanoate assessed as compound formation incubated for 4 hrs at 37 degC by LC-MS/MS method |
CHEMBL3421565 |
| ADMET |
Drug metabolism |
|
|
|
Drug level in human HuH7 cells treated with 2-Amino-6-[N-(t-butyloxycarbonyl)aminoxy]-9H-(2'-C-methyl-beta-D-ribofuranosyl)-purine at 50 uM after 4 hrs by LC-MS/MS analysis |
CHEMBL3792308 |
| ADMET |
Drug metabolism |
|
|
|
Drug level in human HuH7 cells treated with Ethyl((((2R,3S,4R,5R)-5-(2-amino-6-(((tert-butoxycarbonyl)amino)oxy)-9H-purin-9-yl)-3,4-dihydroxy-4-methyltetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)-Lalaninate at 50 uM after 4 hrs by LC-MS/MS analysis |
CHEMBL3792308 |
| Hepatitis C virus NS5B RNA-dependent RNA polymerase |
IC50 |
= |
420.0 |
nM |
Inhibition of HCV NS5B RNA-dependent RNA polymerase activity assessed as reduction in radiolabeled ribonucleotide monophosphates incorporation into RNA using cIRES template measured after 2 hrs by microscintillation counting method |
CHEMBL4622986 |
| DNA polymerase alpha subunit |
Inhibition |
= |
3.6 |
% |
Inhibition of human DNA polymerase alpha at 100 uM using calf DNA as substrate by microbeta scintillation counting method relative to control |
CHEMBL4622986 |
| DNA polymerase beta |
Inhibition |
= |
15.3 |
% |
Inhibition of human DNA polymerase beta at 100 uM using calf DNA as substrate by microbeta scintillation counting method relative to control |
CHEMBL4622986 |
| Unchecked |
Inhibition |
= |
7.1 |
% |
Inhibition of human DNA polymerase gamma at 100 uM using calf DNA as substrate by microbeta scintillation counting method relative to control |
CHEMBL4622986 |
| Unchecked |
IC50 |
> |
100000.0 |
nM |
Inhibition of RNA polymerase 2 in human HeLa cell nuclear extract assessed as reduction in RNA transcription by polyacrylamide gel electrophoresis method |
CHEMBL4622986 |
| Unchecked |
Activity |
|
|
|
Substrate activity at human mitochondrial RNA polymerase assessed as nucleotide incorporation into RNA at 100 uM using [33P]-labeled 5'-UUUUGCCGCGCC-3' and 3'-CGGCGCGGCACGTAAGGG-5' RNA/DNA primer/template by polyacrylamide gel electrophoresis method |
CHEMBL4622986 |
