| Adenosine deaminase |
Ki |
= |
1.13 |
nM |
Inhibitory activity against adenosine deaminase in calf intestinal mucosa. |
CHEMBL1129194 |
| Adenosine deaminase |
Ki |
= |
2.0 |
nM |
Binding affinity (Ki) at calf intestinal Adenosine deaminase |
CHEMBL1126223 |
| Adenosine deaminase |
Ki |
= |
2.0 |
nM |
Compound was evaluated for the inhibition of adenosine deaminase |
CHEMBL1121750 |
| No relevant target |
Kd |
= |
7.0 |
|
Dissociation constant was determined |
CHEMBL1130254 |
| Adenosine deaminase |
Ki |
= |
2.0 |
nM |
Compound was evaluated for inhibition of calf intestinal mucosa adenosine deaminase (ADA) |
CHEMBL1130858 |
| Adenosine deaminase |
Ki |
= |
1.13 |
nM |
Inhibition of Adenosine deaminase (ADA) of calf intestine |
CHEMBL1133542 |
| Adenosine deaminase |
Ki |
= |
0.82 |
nM |
Tested for binding affinity against calf intestinal Adenosine Deaminase (ADA) |
CHEMBL1127396 |
| Adenosine deaminase |
Ki |
= |
1.14 |
nM |
Inhibitory constant against bovine spleen Adenosine deaminase |
CHEMBL1141141 |
| Phosphodiesterase 1 |
IC50 |
> |
16000.0 |
nM |
Inhibitory activity against PDE1 by scintillation proximity assay |
CHEMBL1147762 |
| Phosphodiesterase 2A |
IC50 |
= |
635.0 |
nM |
Inhibitory activity against PDE2 by scintillation proximity assay |
CHEMBL1147762 |
| Phosphodiesterase 3 |
IC50 |
> |
16000.0 |
nM |
Inhibitory activity against PDE3 by scintillation proximity assay |
CHEMBL1147762 |
| Phosphodiesterase 4A |
IC50 |
> |
16000.0 |
nM |
Inhibitory activity against PDE4A by scintillation proximity assay |
CHEMBL1147762 |
| Phosphodiesterase 4B |
IC50 |
> |
16000.0 |
nM |
Inhibitory activity against PDE4B by scintillation proximity assay |
CHEMBL1147762 |
| Phosphodiesterase 4C |
IC50 |
> |
16000.0 |
nM |
Inhibitory activity against PDE4C by scintillation proximity assay |
CHEMBL1147762 |
| Phosphodiesterase 4D |
IC50 |
> |
16000.0 |
nM |
Inhibitory activity against PDE4D by scintillation proximity assay |
CHEMBL1147762 |
| Phosphodiesterase 5A |
IC50 |
> |
16000.0 |
nM |
Inhibitory activity against PDE5 by scintillation proximity assay |
CHEMBL1147762 |
| Phosphodiesterase 8A |
IC50 |
> |
16000.0 |
nM |
Inhibitory activity against PDE8A by scintillation proximity assay |
CHEMBL1147762 |
| Phosphodiesterase 8B |
IC50 |
> |
16000.0 |
nM |
Inhibitory activity against PDE8B by scintillation proximity assay |
CHEMBL1147762 |
| Phosphodiesterase 9A |
IC50 |
> |
16000.0 |
nM |
Inhibitory activity against PDE9 by scintillation proximity assay |
CHEMBL1147762 |
| Phosphodiesterase 10A |
IC50 |
> |
16000.0 |
nM |
Inhibitory activity against PDE10 by scintillation proximity assay |
CHEMBL1147762 |
| Phosphodiesterase 11A |
IC50 |
> |
16000.0 |
nM |
Inhibitory activity against PDE11 by scintillation proximity assay |
CHEMBL1147762 |
| Phosphodiesterase 2A |
Selectivity index |
> |
25.0 |
|
Selectivity for PDE2 |
CHEMBL1147762 |
| Liver microsomes |
T1/2 |
= |
0.5167 |
hr |
Half life in rat liver microsome |
CHEMBL1147762 |
| Caco-2 |
Papp |
= |
34.0 |
ucm/s |
Apical Caco-2 cell membrane permeability |
CHEMBL1147762 |
| Caco-2 |
Papp |
= |
18.0 |
ucm/s |
Basolateral Caco-2 cell membrane permeability |
CHEMBL1147762 |
| MDCK |
Papp |
|
|
|
Apical cell permeability in MDCK cells overexpressing human p-glycoprotein |
CHEMBL1147762 |
| MDCK |
Papp |
|
|
|
Basolateral cell permeability in MDCK with MDR transfectant overexpressing human p-glycoprotein |
CHEMBL1147762 |
| Homo sapiens |
Solubility |
> |
65.0 |
ug.mL-1 |
Turbidimetric solubility at pH 7 |
CHEMBL1147762 |
| Unchecked |
Ki |
= |
1.14 |
nM |
Inhibition of bovine spleen adenosine deaminase type 9 by spectrophotometry |
CHEMBL1152769 |
| Phosphodiesterase 4 |
IC50 |
= |
1700.0 |
nM |
Inhibition of PDE4 (unknown origin) |
CHEMBL3769307 |
| Unchecked |
IC50 |
= |
700.0 |
nM |
Inhibition of cGMP activated PDE2 (unknown origin) |
CHEMBL3769307 |
| Unchecked |
IC50 |
= |
2000.0 |
nM |
Inhibition of cGMP stimulated pig PDE2A |
CHEMBL3769307 |
| Phosphodiesterase 2A |
IC50 |
= |
800.0 |
nM |
Inhibition of cGMP stimulated human PDE2A |
CHEMBL3769307 |
| Adenosine deaminase |
Ki |
= |
2.2 |
nM |
Inhibition of bovine adenosine deaminase pre-incubated for 5 mins before adenosine addition |
CHEMBL4177582 |
| Rattus norvegicus |
AUC |
= |
97.08 |
ng.hr.mL-1 |
AUC (0 to t) in Wistar rat at 1 mg/kg, iv after 0.25 to 24 hrs by LC/MS/MS method |
CHEMBL4177582 |
| Rattus norvegicus |
Cp |
|
|
|
Plasma concentration in Wistar rat at 1 mg/kg, iv after 1 hr by LC/MS/MS method |
CHEMBL4177582 |
| Rattus norvegicus |
CL |
|
|
|
Clearance in Wistar rat at 1 mg/kg, iv after 1 hr by LC/MS/MS method |
CHEMBL4177582 |
| Phosphodiesterase 2A |
Inhibition |
= |
37.45 |
% |
Inhibition of recombinant human PDE2A catalytic domain (580 to 919 residues) expressed in Escherichia coli BL21 (Codonplus) at 1 uM using [3H]cGMP as substrate after 15 mins by liquid scintillation counting method relative to control |
CHEMBL4177707 |
| Unchecked |
IC50 |
= |
800.0 |
nM |
Inhibition of PDE2 (unknown origin) |
CHEMBL4177707 |
| Phosphodiesterase 2A |
IC50 |
= |
2460.0 |
nM |
Inhibition of recombinant human PDE2A catalytic domain (580 to 919 residues) expressed in Escherichia coli BL21 (Codonplus) using [3H]cGMP as substrate after 15 mins by liquid scintillation counting method |
CHEMBL4177707 |
| Phosphodiesterase 2A |
IC50 |
= |
800.0 |
nM |
Inhibition of human PDE2 using c[8-3H]cAMP or c[8-3H]cGMP as substrate measured after 10 mins by liquid scintillation counting method |
CHEMBL4371070 |
| Phosphodiesterase 2A |
IC50 |
= |
2620.0 |
nM |
Inhibition of human recombinant PDE2A using cGMP as substrate incubated for 20 mins measured by Kinase Glo reagent based microplate reader assay |
CHEMBL4732047 |
| Adenosine deaminase |
Ki |
= |
1.0 |
nM |
Binding affinity to ADA (unknown origin) assessed as inhibition constant |
CHEMBL5150007 |
