| H9 |
Expression |
= |
79.0 |
% |
Percentage of gag protein expression using H9 cells at 0 uM on 7th day |
CHEMBL1124730 |
| H9 |
Expression |
= |
58.0 |
% |
Percentage of gag protein expression using H9 cells at 5 uM on 7th day |
CHEMBL1124730 |
| H9 |
Expression |
= |
61.0 |
% |
Percentage of gag protein expression using H9 cells at 20 uM on 7th day |
CHEMBL1124730 |
| H9 |
Expression |
= |
18.0 |
% |
Percentage of gag protein expression using H9 cells at 50 uM on 7th day |
CHEMBL1124730 |
| H9 |
Expression |
= |
10.0 |
% |
Percentage of gag protein expression using H9 cells at 100 uM on 7th day |
CHEMBL1124730 |
| H9 |
Expression |
= |
0.0 |
% |
Percentage of gag protein expression using H9 cells at 200 uM on 7th day |
CHEMBL1124730 |
| H9 |
Expression |
= |
71.0 |
% |
Percentage of gag protein expression using H9 cells at 0 uM on 10th day |
CHEMBL1124730 |
| H9 |
Expression |
= |
73.0 |
% |
Percentage of gag protein expression using H9 cells at 5 uM on 10th day |
CHEMBL1124730 |
| H9 |
Expression |
= |
37.0 |
% |
Percentage of gag protein expression using H9 cells at 20 uM on 10th day |
CHEMBL1124730 |
| H9 |
Expression |
= |
20.0 |
% |
Percentage of gag protein expression using H9 cells at 50 uM on 10th day |
CHEMBL1124730 |
| H9 |
Expression |
= |
34.0 |
% |
Percentage of gag protein expression using H9 cells at 100 uM on 10th day |
CHEMBL1124730 |
| H9 |
Expression |
= |
0.0 |
% |
Percentage of gag protein expression using H9 cells at 200 uM on 10th day |
CHEMBL1124730 |
| H9 |
Expression |
= |
79.0 |
% |
Percentage of gag protein expression using H9 cells at 0 uM on 12th day |
CHEMBL1124730 |
| H9 |
Expression |
= |
66.0 |
% |
Percentage of gag protein expression using H9 cells at 5 uM on 12th day |
CHEMBL1124730 |
| H9 |
Expression |
= |
53.0 |
% |
Percentage of gag protein expression using H9 cells at 20 uM on 12th day |
CHEMBL1124730 |
| H9 |
Expression |
= |
19.0 |
% |
Percentage of gag protein expression using H9 cells at 50 uM on 12th day |
CHEMBL1124730 |
| H9 |
Expression |
= |
50.0 |
% |
Percentage of gag protein expression using H9 cells at 100 uM on 12th day |
CHEMBL1124730 |
| H9 |
Expression |
= |
0.0 |
% |
Percentage of gag protein expression using H9 cells at 200 uM on 12th day |
CHEMBL1124730 |
| Human immunodeficiency virus 1 |
Activity |
|
|
|
Ability to protect CD4+ ATH8 cells from cytopathogenic effects of HIV-1; No effect |
CHEMBL1124730 |
| Human immunodeficiency virus type 1 reverse transcriptase |
Activity |
|
|
|
Inhibition of HIV-1 reverse transcriptase; + = active |
CHEMBL1127606 |
| Mus musculus |
AUC |
= |
3.0 |
|
Pharmacokinetic parameter AUC was measured at 20 mg/kg dose by intravenous administration in mice serum; AUC 0-r (mM.h) |
CHEMBL1129405 |
| Mus musculus |
AUC |
= |
3.9 |
|
Pharmacokinetic parameter AUC was measured at 20 mg/kg dose by intravenous administration in mice serum; AUC 0-r (mM.h). |
CHEMBL1129405 |
| Mus musculus |
AUC |
= |
0.8 |
|
Pharmacokinetic parameter AUC was measured at 20 mg/kg dose by oral administration in mice serum.; AUC 0-r (mM.h) |
CHEMBL1129405 |
| Mus musculus |
AUC |
= |
|
|
Pharmacokinetic parameter AUC was measured at 20 mg/kg dose by intravenous administration in mice brain; AUC 0-r (mM.h) |
CHEMBL1129405 |
| Mus musculus |
AUC |
= |
8.6 |
|
Pharmacokinetic parameter AUC was measured at 55 mg/kg dose by intravenous administration mice serum.; AUC 0-r (mM.h) |
CHEMBL1129405 |
| Mus musculus |
AUC |
= |
4.8 |
|
Pharmacokinetic parameter AUC was measured at 55 mg/kg dose by intravenous administration in mice brain; AUC 0-r (mM.h) |
CHEMBL1129405 |
| Mus musculus |
AUC |
= |
1.0 |
|
Pharmacokinetic parameters was measured at 55 mg/kg dose by oral administration in mice serum.; AUC 0-r (mM.h) |
CHEMBL1129405 |
| Mus musculus |
AUC |
= |
|
|
Pharmacokinetic parameter AUC was measured at 55 mg/kg dose by oral administration in mice brain.; AUC 0-r (mM.h) |
CHEMBL1129405 |
| Mus musculus |
T1/2 |
= |
2.92 |
|
t1/2 was measured at 55 mg/kg dose by intravenous administration in mice serum; t1/2 (h) |
CHEMBL1129405 |
| Mus musculus |
Ratio |
= |
0.04 |
|
The ratio of AUC / dose (mM.h/uMol)/kg at 112 mg/kg dose after intravenous administration in mice serum; AUC/Dose (uM) |
CHEMBL1129405 |
| Mus musculus |
T1/2 |
= |
0.91 |
|
t1/2 was measured AT 55 mg/Kg dose by intravenous administration in mice brain; t1/2 (h) |
CHEMBL1129405 |
| Mus musculus |
Ratio |
= |
0.02 |
|
The ratio of AUC / dose (mM.h/uMol)/kg at 112 mg/kg dose after intravenous administration in mice brain; AUC/Dose (uM) |
CHEMBL1129405 |
| Mus musculus |
T1/2 |
= |
1.74 |
|
t1/2 was measured at 55 mg/kg dose by oral administration in mice serum; t1/2 (h) |
CHEMBL1129405 |
| Mus musculus |
Ratio |
= |
0.005 |
|
The ratio of AUC / dose (mM.h/uMol)/kg at 112 mg/kg dose after oral administration in mice serum; AUC/Dose (uM) |
CHEMBL1129405 |
| Mus musculus |
T1/2 |
= |
|
|
t1/2 was measured at 55 mg/kg dose by oral administration in mice brain; t1/2 (h) |
CHEMBL1129405 |
| Mus musculus |
Ratio |
= |
|
|
The ratio of AUC / dose (mM.h/uMol)/kg at 112 mg/kg dose after oral administration in mice brain; AUC/Dose (uM) |
CHEMBL1129405 |
| ADMET |
EC50 |
= |
100000.0 |
nM |
In vitro anti-HIV activity was evaluated in human peripheral blood mononuclear (PBM) cells |
CHEMBL1151095 |
| Homo sapiens |
EC50 |
> |
10000.0 |
nM |
In vitro anti-HBV activity in 2.2.15 cells |
CHEMBL1151095 |
| ADMET |
IC50 |
> |
100000.0 |
nM |
Cytotoxicity in human peripheral blood mononuclear (PBM) cells |
CHEMBL1151095 |
| CCRF-CEM |
IC50 |
> |
100000.0 |
nM |
Cytotoxicity in CEM cells |
CHEMBL1151095 |
| Vero |
IC50 |
> |
100000.0 |
nM |
Cytotoxicity in Vero cells |
CHEMBL1151095 |
| Homo sapiens |
IC50 |
> |
200000.0 |
nM |
Cytotoxicity in 2.2.15 cells |
CHEMBL1151095 |
| MT4 |
CD50 |
> |
625.0 |
uM |
Cytotoxicity was determined as the dose required to reduce the viability of uninfected MT-4 cells by 50% |
CHEMBL1123895 |
| MT4 |
ED50 |
= |
35.0 |
uM |
Anti-HIV activity was determined as dose required to protect 50% of the HIV-infected MT-4 cells against destruction |
CHEMBL1123895 |
| Unchecked |
Ratio |
> |
18.0 |
|
Selectivity ratio CD50 to ED50 |
CHEMBL1123895 |
| No relevant target |
LogP |
= |
-0.18 |
|
Partition coefficient (logP) |
CHEMBL1125695 |
| ADMET |
Km |
= |
0.00033 |
|
Kinetic parameter KM at pH 7.4 and 37 degree Centigrade |
CHEMBL1125695 |
| ADMET |
Vmax |
= |
0.23 |
|
Kinetic parameter Vmax at pH 7.4 and 37 degree Centigrade |
CHEMBL1125695 |
| ADMET |
Relative rate |
= |
6.0 |
|
Kinetic parameter relative rate measured at 50 uM at pH 7.4 and 37 degree Centigrade |
CHEMBL1125695 |
| ADMET |
Protection |
= |
0.0 |
% |
Anti-HIV activity (% protection) in ATH-8 cells at 5 uM in absence of 2'-deoxycoformycin at 0 uM |
CHEMBL1125695 |
| ADMET |
Toxicity |
= |
0.0 |
% |
Anti-HIV activity (% toxicity) in ATH-8 cells at 5 uM in absence of 2'-deoxycoformycin at 0 uM |
CHEMBL1125695 |
| ADMET |
Protection |
= |
70.0 |
% |
Anti-HIV activity (% protection) in ATH-8 cells at 5 uM in absence of 2'-deoxycoformycin at 20 uM |
CHEMBL1125695 |
| ADMET |
Toxicity |
= |
0.0 |
% |
Anti-HIV activity (% toxicity) in ATH-8 cells at 5 uM in absence of 2'-deoxycoformycin at 20 uM |
CHEMBL1125695 |
| ADMET |
Protection |
= |
84.0 |
% |
Anti-HIV activity (% protection) in ATH-8 cells at 5 uM in absence of 2'-deoxycoformycin at 50 uM |
CHEMBL1125695 |
| ADMET |
Toxicity |
= |
0.0 |
% |
Anti-HIV activity (% toxicity) in ATH-8 cells at 5 uM in absence of 2'-deoxycoformycin at 50 uM |
CHEMBL1125695 |
| ADMET |
Protection |
= |
0.0 |
% |
Anti-HIV activity (% protection) in ATH-8 cells at 5 uM in presence of 2'-deoxycoformycin at 0 uM |
CHEMBL1125695 |
| ADMET |
Toxicity |
= |
11.0 |
% |
Anti-HIV activity (% toxicity) in ATH-8 cells at 5 uM in presence of 2'-deoxycoformycin at 0 uM |
CHEMBL1125695 |
| ADMET |
Protection |
= |
68.0 |
% |
Anti-HIV activity (% protection) in ATH-8 cells at 5 uM in presence of 2'-deoxycoformycin at 20 uM |
CHEMBL1125695 |
| ADMET |
Toxicity |
= |
17.0 |
% |
Anti-HIV activity (% toxicity) in ATH-8 cells at 5 uM in presence of 2'-deoxycoformycin at 20 uM |
CHEMBL1125695 |
| ADMET |
Protection |
= |
48.0 |
% |
Anti-HIV activity (% protection) in ATH-8 cells at 5 uM in presence of 2'-deoxycoformycin at 50 uM |
CHEMBL1125695 |
| ADMET |
Toxicity |
= |
54.0 |
% |
Anti-HIV activity (% toxicity) in ATH-8 cells at 5 uM in presence of 2'-deoxycoformycin at 50 uM |
CHEMBL1125695 |
| ADMET |
T1/2 |
|
|
hr |
Hydrolysis half life in phosphate buffer; Not available |
CHEMBL1132719 |
| No relevant target |
LogP |
= |
-0.61 |
|
Partition coefficient (logP) |
CHEMBL1132719 |
| CCRF-CEM |
EC50 |
= |
36700.0 |
nM |
Antiviral activity evaluated as the ability to inhibit the replication of HIV-1 in human T-lymphocytic cells (CEM) |
CHEMBL1132719 |
| CCRF-CEM |
EC50 |
= |
40000.0 |
nM |
Antiviral activity evaluated as the ability to inhibit the replication of HIV-2 in human T-lymphocytic cells (CEM) |
CHEMBL1132719 |
| C3H/3T3 |
EC50 |
> |
50000.0 |
nM |
Effect of compound against Moloney murine sarcoma virus (MSV)-induced transformation of C3H/3T3 embryo murine fibroblasts |
CHEMBL1132719 |
| CCRF-CEM |
CC50 |
> |
250000.0 |
nM |
Cytotoxic concentration in Wild Type CEM cells |
CHEMBL1132719 |
| C3H/3T3 |
MCC |
> |
50000.0 |
nM |
Minimal cytotoxic concentration required to cause morphological alteration of C3H/3T3 fibroblast culture cells |
CHEMBL1132719 |
| Unchecked |
SI |
> |
6.8 |
|
Selectivity index by CC50 of CEM cells/EC50 of CEM cells against HIV-1 |
CHEMBL1132719 |
| ADMET |
IC50 |
= |
3300.0 |
nM |
Anti-HIV activity by using phytohemagglutininin-stimulated peripheral blood mononuclear cell(PHA/PBM) test system |
CHEMBL1129582 |
| No relevant target |
LogP |
= |
-0.183 |
|
Partition coefficient (logP) |
CHEMBL1129582 |
| Human immunodeficiency virus 1 |
EC50 |
= |
1160.0 |
nM |
Antiviral activity against HIV1 3B in human H9 cells assessed as inhibition of virus-induced cytopathic effect by formazan-based conventional colorimetric technique |
CHEMBL1137804 |
| Human immunodeficiency virus 1 |
EC50 |
= |
1160.0 |
nM |
Antiviral activity against HIV1 RF in human H9 cells assessed as inhibition of virus-induced cytopathic effect by formazan-based conventional colorimetric technique |
CHEMBL1137804 |
| ADMET |
TI |
> |
17.0 |
|
Therapeutic index, ratio of cytotoxicity against human H9 cells to EC50 for HIV1 3B |
CHEMBL1137804 |
| ADMET |
TI |
> |
17.0 |
|
Therapeutic index, ratio of cytotoxicity against human H9 cells to EC50 for HIV1 RF |
CHEMBL1137804 |
| Human immunodeficiency virus 1 |
EC50 |
= |
4400.0 |
nM |
Antiviral activity against HIV1 infected in human PBM cells assessed as inhibition of viral replication |
CHEMBL3632481 |
