| Hepatitis C virus NS5B RNA-dependent RNA polymerase |
IC50 |
> |
50000.0 |
nM |
Inhibition HCV NS5B-mediated RNA synthesis |
CHEMBL1149159 |
| Hepatitis C virus NS5B RNA-dependent RNA polymerase |
EC50 |
> |
50000.0 |
nM |
Inhibition HCV RNA replication |
CHEMBL1149159 |
| Adenosine A1 receptor |
Ki |
= |
49500.0 |
nM |
Inhibitory activity at Adenosine A1 receptor by inhibition of [3H]CHA binding to bovine brain cortical membranes. |
CHEMBL1131221 |
| Adenosine A2a receptor |
Inhibition |
= |
12.0 |
% |
Inhibitory activity against Adenosine A2A receptor by inhibition of [3H]-CGS- 21680 binding to bovine striatal membranes |
CHEMBL1131221 |
| Adenosine A3 receptor |
Inhibition |
= |
8.0 |
% |
Inhibitory activity against Adenosine A3 receptor by inhibition of [3H](R)-PIA binding to rat testis membranes |
CHEMBL1131221 |
| Unchecked |
Selectivity |
> |
202.0 |
|
Inhibitory selectivity at Adenosine 2A receptor compared to Adenosine 1 receptor. |
CHEMBL1131221 |
| Unchecked |
Selectivity |
> |
202.0 |
|
Inhibitory selectivity at Adenosine A3 receptor compared to Adenosine 1 receptor. |
CHEMBL1131221 |
| Adenosine A1 receptor |
Ki |
= |
51000.0 |
nM |
Inhibition of [3H]CHA (N6-cyclohexyl adenosine) to rat brain membrane Adenosine A1 receptor |
CHEMBL1135881 |
| Adenosine A2a receptor |
Displacement |
= |
12.0 |
% |
Ability to displace [3H]-CGS- 21680 from Adenosine A2A receptor of rat brain striatum at 10e-5 M |
CHEMBL1135881 |
| Adenosine receptors; A1 & A2a |
Selectivity |
> |
202.0 |
|
Selectivity for Adenosine A2A over Adenosine A1 receptor |
CHEMBL1135881 |
| Adenosine receptors; A1 & A3 |
Selectivity |
> |
202.0 |
|
Selectivity for Adenosine A3 over Adenosine A1 receptor |
CHEMBL1135881 |
| Adenosine A1 receptor |
Ki |
= |
51000.0 |
nM |
Binding affinity to adenosine A1 receptor in rat brain membranes by measuring displacement of specific [3H]PIA as radioligand. |
CHEMBL1128285 |
| Adenosine A2a receptor |
Displacement |
= |
13.0 |
% |
Binding affinity determined on Adenosine A2A receptor in rat striatal membranes by measuring displacement of specific [3H]-CGS- 21680 as radioligand. |
CHEMBL1128285 |
| Adenosine A3 receptor |
Displacement |
= |
9.0 |
% |
Binding affinity determined by displacement of specific binding of [125I]N-(4-amino-3-iodophenethyl)-adenosine in membranes of CHO cells stably transfected with the rat Adenosine A3 receptor |
CHEMBL1128285 |
| K562 |
IC50 |
= |
18200.0 |
nM |
In vitro inhibitory activity against human myelogenous leukemia K562 cell line |
CHEMBL1140342 |
| K562 |
IC50 |
= |
38300.0 |
nM |
In vitro inhibitory activity against human leukemia K562IU cell line |
CHEMBL1140342 |
| HT-29 |
IC50 |
= |
23200.0 |
nM |
In vitro inhibitory activity against human colon carcinoma HT-29 cell line |
CHEMBL1140342 |
| MCF7 |
IC50 |
= |
17500.0 |
nM |
In vitro inhibitory activity against human breast carcinoma MCF-7 cell line |
CHEMBL1140342 |
| Adenosine A1 receptor |
Displacement |
= |
13.0 |
% |
Percent displacement of [3H]DPCPX binding to adenosine A1 receptors of bovine cortical membranes at 0.00005 M |
CHEMBL1144357 |
| Adenosine A2a receptor |
Displacement |
= |
4.0 |
% |
Percent displacement of [3H]CGS-21680 binding to adenosine A2A receptors of bovine striatal membranes at 0.00005 M |
CHEMBL1144357 |
| Adenosine A3 receptor |
Displacement |
= |
0.0 |
% |
Percent displacement of [125I]AB-MECA binding to adenosine A3 receptors of bovine cortical membranes at 0.00005 M |
CHEMBL1144357 |
| K562 |
GI50 |
= |
9400.0 |
nM |
Antitumor activity against human K562 cells after 48 hrs by MTS assay |
CHEMBL1155110 |
| Caco-2 |
GI50 |
= |
23200.0 |
nM |
Antitumor activity against human CaCo2 cells after 48 hrs by MTS assay |
CHEMBL1155110 |
| HT-29 |
GI50 |
= |
26100.0 |
nM |
Antitumor activity against human HT29 cells after 48 hrs by MTS assay |
CHEMBL1155110 |
| MCF7 |
GI50 |
= |
22400.0 |
nM |
Antitumor activity against human MCF7 cells after 48 hrs by MTS assay |
CHEMBL1155110 |
| K562 |
GI50 |
= |
9400.0 |
nM |
Antiproliferative activity against human K562 cells after 72 hrs by MTS assay |
CHEMBL1772936 |
| HeLa |
GI50 |
= |
23300.0 |
nM |
Antiproliferative activity against human HeLa cells after 72 hrs by MTS assay |
CHEMBL1772936 |
| Caco-2 |
GI50 |
= |
24300.0 |
nM |
Antiproliferative activity against human Caco2 cells after 72 hrs by MTS assay |
CHEMBL1772936 |
| HT-29 |
GI50 |
= |
26100.0 |
nM |
Antiproliferative activity against human HT-29 cells after 72 hrs by MTS assay |
CHEMBL1772936 |
| MCF7 |
GI50 |
= |
22400.0 |
nM |
Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay |
CHEMBL1772936 |
| NON-PROTEIN TARGET |
Activity |
|
|
|
Cytotoxicity against human HL60 cells at 20 to 100 uM after 24 to 48 hrs in presence of 2 mM VPA by trypan blue dye exclusion method |
CHEMBL3351354 |
| NON-PROTEIN TARGET |
Activity |
|
|
|
Cytotoxicity against human HL60 cells at 20 to 100 uM after 24 to 48 hrs in presence of 1 mM VPA by trypan blue dye exclusion method |
CHEMBL3351354 |
| HL-60 |
Activity |
= |
90.0 |
% |
Induction of apoptosis in human HL60 cells at 20 uM in presence of 2 mM VPA after 24 to 48 hrs by acridine orange and ethidium bromide staining based fluorescence microscopy |
CHEMBL3351354 |
| HL-60 |
Activity |
|
|
|
Induction of apoptosis in human HL60 cells at 20 uM in presence of 1 mM VPA after 24 to 48 hrs by acridine orange and ethidium bromide staining based fluorescence microscopy |
CHEMBL3351354 |
| NON-PROTEIN TARGET |
IC50 |
= |
15600.0 |
nM |
Growth inhibition of human HL60 cells after 48 hrs by MTT assay |
CHEMBL3351354 |
| K562 |
IC50 |
= |
9400.0 |
nM |
Growth inhibition of human K562 cells after 48 hrs by MTT assay |
CHEMBL3351354 |
| HuT78 |
IC50 |
= |
17300.0 |
nM |
Growth inhibition of human HUT78 cells after 48 hrs by MTT assay |
CHEMBL3351354 |
| HT-29 |
IC50 |
= |
26100.0 |
nM |
Growth inhibition of human HT-29 cells after 48 hrs by MTT assay |
CHEMBL3351354 |
| MCF7 |
IC50 |
= |
22400.0 |
nM |
Growth inhibition of human MCF7 cells after 48 hrs by MTT assay |
CHEMBL3351354 |
| HeLa |
IC50 |
= |
23300.0 |
nM |
Growth inhibition of human HeLa cells after 48 hrs by MTT assay |
CHEMBL3351354 |
| NON-PROTEIN TARGET |
IC50 |
= |
24300.0 |
nM |
Growth inhibition of human Caco2 cells after 48 hrs by MTT assay |
CHEMBL3351354 |
| NON-PROTEIN TARGET |
IC50 |
= |
15000.0 |
nM |
Cytotoxicity against human HL60 cells after 24 to 48 hrs by trypan blue dye exclusion method |
CHEMBL3351354 |
| HL-60 |
AC50 |
= |
75000.0 |
nM |
Induction of apoptosis in human HL60 cells after 24 to 48 hrs by acridine orange and ethidium bromide staining based fluorescence microscopy |
CHEMBL3351354 |
| Serum |
T1/2 |
= |
43.5 |
hr |
Half life in RPMI-1640 medium containing 10% fetal calf serum assessed as compound disappearance by HPLC-DAD-ESI-MS method |
CHEMBL3351354 |
| HL-60 |
Activity |
= |
31.0 |
% |
Induction of cell cycle arrest in human HL60 cells assessed as accumulation at G1 phase at 20 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 32%) |
CHEMBL3351354 |
| HL-60 |
Activity |
= |
60.0 |
% |
Induction of cell cycle arrest in human HL60 cells assessed as accumulation at S phase at 20 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 54%) |
CHEMBL3351354 |
| HL-60 |
Activity |
= |
9.0 |
% |
Induction of cell cycle arrest in human HL60 cells assessed as accumulation at G2M phase at 20 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 12%) |
CHEMBL3351354 |
| HL-60 |
Activity |
= |
28.0 |
% |
Induction of cell cycle arrest in human HL60 cells assessed as accumulation at G1 phase at 20 uM in presence of 2 mM VPA after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 32%) |
CHEMBL3351354 |
| HL-60 |
Activity |
= |
61.0 |
% |
Induction of cell cycle arrest in human HL60 cells assessed as accumulation at S phase at 20 uM in presence of 2 mM VPA after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 54%) |
CHEMBL3351354 |
| HL-60 |
Activity |
= |
11.0 |
% |
Induction of cell cycle arrest in human HL60 cells assessed as accumulation at G2M phase at 20 uM in presence of 2 mM VPA after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 12%) |
CHEMBL3351354 |
