| Human immunodeficiency virus type 1 reverse transcriptase |
Activity |
|
|
|
Inhibition of HIV-1 reverse transcriptase; + = active |
CHEMBL1127606 |
| Moloney murine leukemia virus |
ED50 |
= |
3.7 |
uM |
In vitro inhibitory activity against Moloney murine leukemia virus (M-MULV) replication, a mammalian T-lymphotropic retrovirus |
CHEMBL1123685 |
| HepG2 |
ED50 |
= |
10.0 |
nM |
Concentration required to inhibit 50% of extracellular circular replication of HBV DNA using 2215 cell line |
CHEMBL1129064 |
| HepG2 |
ED50 |
= |
8.0 |
nM |
Concentration required to inhibit 50% of intracellular circular replication of HBV DNA using 2215 cell line |
CHEMBL1129064 |
| MT2 |
ED50 |
= |
1.0 |
uM |
Concentration required to inhibit 50% of HIV activity in MT-2 cells |
CHEMBL1129064 |
| CCRF-CEM |
ED50 |
= |
20.0 |
uM |
In vitro concentration required to inhibit 50% of CEM cell growth |
CHEMBL1129064 |
| CCRF-CEM |
ED50 |
> |
20.0 |
uM |
In vitro concentration required to decrease 50% of mitochondrial DNA content in CEM cells |
CHEMBL1129064 |
| ATH-8 cell line |
ED50 |
= |
0.3 |
uM |
Protection of ATH8 cells against the cytopathic effect of HIV. |
CHEMBL1123791 |
| ATH-8 cell line |
ID50 |
= |
30.0 |
uM |
Required dose to reduce viability of normal uninfected ATH8 cells. |
CHEMBL1123791 |
| MT4 |
Toxicity |
> |
90.0 |
% |
Toxicity was determined by evaluation of cluster morphology and reclustering properties in mock infected MT-4 cells at 125 uM concentration |
CHEMBL1123791 |
| MT4 |
Toxicity |
< |
10.0 |
% |
Toxicity was determined by evaluation of cluster morphology and reclustering properties in mock infected MT-4 cells at 5 uM concentration |
CHEMBL1123791 |
| MT4 |
Protection |
> |
90.0 |
% |
Protection was determined by evaluation of cluster morphology and reclustering properties in mock infected MT-4 cells at 5 uM concentration. |
CHEMBL1123791 |
| MT4 |
Toxicity |
< |
10.0 |
% |
Toxicity was determined by evaluation of cluster morphology and reclustering properties in mock infected MT-4 cells at 0.2 uM concentration |
CHEMBL1123791 |
| MT4 |
Protection |
= |
40.0 |
% |
Protection was determined by evaluation of cluster morphology and reclustering properties in mock infected MT-4 cells at 0.2 uM concentration; Range is 40-60 |
CHEMBL1123791 |
| MT4 |
Protection |
< |
10.0 |
% |
Protection was determined by evaluation of cluster morphology and reclustering properties in mock infected MT-4 cells at 0.008 uM concentration. |
CHEMBL1123791 |
| ADMET |
Ratio |
= |
100.0 |
|
Therapeutic index (Ratio = ID50/ED50). |
CHEMBL1123791 |
| No relevant target |
LogP |
= |
-1.57 |
|
Partition coefficient (logP) |
CHEMBL1126075 |
| No relevant target |
P |
= |
0.2 |
|
Partition coefficient (P) in 1-octanol and 0.1 M Na3PO4 at pH 7 |
CHEMBL1124944 |
| Deoxycytidine kinase |
Ki |
= |
1100000.0 |
nM |
Inhibitory affect against rabbit deoxycytidine kinase |
CHEMBL1124944 |
| Deoxycytidine kinase |
Ki |
= |
4600000.0 |
nM |
Inhibitory affect against rabbit deoxycytidine kinase and represented as molt/4F kinase. |
CHEMBL1124944 |
| Human immunodeficiency virus 1 |
ED50 |
= |
0.13 |
uM |
Effective dose achieving 50% protection of MT-4 cells against the cytopathic effect of HIV |
CHEMBL1124810 |
| MT4 |
CD50 |
= |
7.9 |
uM |
Cytotoxic dose required to reduce the viability of normal uninfected MT-4 cells by 50% |
CHEMBL1124810 |
| MT4 |
Selectivity index |
= |
61.0 |
|
Selectivity index of CD50 to ED50 of MT-4 cells |
CHEMBL1124810 |
| Human immunodeficiency virus 1 |
EC50 |
= |
5.0 |
nM |
Effective concentration against HIV-1 in human peripheral blood mononuclear cells (PBMC) |
CHEMBL1148339 |
| ADMET |
IC50 |
= |
65000.0 |
nM |
Cytotoxicity against human peripheral blood mononuclear cells (PBMC) |
CHEMBL1148339 |
| ADMET |
T1/2 |
= |
1.0 |
hr |
t1/2 (half life) period was determined |
CHEMBL1148339 |
