| tRNA (cytosine(38)-C(5))-methyltransferase |
Activity |
|
|
|
Binding affinity to full length human N-terminal his6-tagged DNMT2 expressed in Escherichia coli Rosetta2(DE3)pLysS at 100 uM incubated for 5 mins by microscale thermophoresis assay |
CHEMBL5131574 |
| tRNA (cytosine(38)-C(5))-methyltransferase |
Inhibition |
= |
62.8 |
% |
Inhibition of full length human N-terminal his6-tagged DNMT2 expressed in Escherichia coli Rosetta2(DE3)pLysS at 100 uM using tRNA asp as substrate and SAM as co-substrate incubated for 5 mins by tritium incorporation assay relative to control |
CHEMBL5131574 |
| tRNA (cytosine(38)-C(5))-methyltransferase |
Kd |
= |
10500.0 |
nM |
Binding affinity to full length human N-terminal his6-tagged DNMT2 expressed in Escherichia coli Rosetta2(DE3)pLysS assessed as dissociation constant at 100 uM by isothermal titration calorimetry assay |
CHEMBL5131574 |
| tRNA (cytosine(38)-C(5))-methyltransferase |
IC50 |
= |
32200.0 |
nM |
Inhibition of full length human N-terminal his6-tagged DNMT2 expressed in Escherichia coli Rosetta2(DE3)pLysS by isothermal titration calorimetry assay |
CHEMBL5131574 |
| Unchecked |
Selectivity ratio |
= |
3.0 |
|
Selectivity ratio of Kd for binding affinity to full length human N-terminal his6-tagged DNMT2 expressed in Escherichia coli Rosetta2(DE3)pLysS assessed as dissociation constant to IC50 for inhibition of full length human N-terminal his6-tagged DNMT2 expressed in Escherichia coli Rosetta2(DE3)pLysS |
CHEMBL5131574 |
| tRNA (cytosine(38)-C(5))-methyltransferase |
deltaG |
= |
-28.4 |
kJ/mol |
Binding affinity to full length human N-terminal his6-tagged DNMT2 expressed in Escherichia coli Rosetta2(DE3)pLysS assessed as gibbs free energy change at 100 uM by isothermal titration calorimetry assay |
CHEMBL5131574 |
| tRNA (cytosine(38)-C(5))-methyltransferase |
deltaH |
= |
-27.0 |
kJ/mol |
Binding affinity to full length human N-terminal his6-tagged DNMT2 expressed in Escherichia coli Rosetta2(DE3)pLysS assessed as change in enthalpy change at 100 uM by isothermal titration calorimetry assay |
CHEMBL5131574 |
| tRNA (cytosine(38)-C(5))-methyltransferase |
-TdeltaS |
= |
-1.4 |
kJ/mol |
Binding affinity to full length human N-terminal his6-tagged DNMT2 expressed in Escherichia coli Rosetta2(DE3)pLysS assessed as change in entropy at 100 uM by isothermal titration calorimetry assay |
CHEMBL5131574 |
| DNA (cytosine-5)-methyltransferase 3A |
Inhibition |
= |
95.3 |
% |
Inhibition of recombinant human DNMT3A-3L expressed in Escherichia coli Rosetta2(DE3)pLysS at 100 uM using Poly(dI-dC)-Poly(dI-dC) as substrate measured at 150 mins by liquid scintillation counting analysis |
CHEMBL5131574 |
| RNA cytosine C(5)-methyltransferase NSUN2 |
Inhibition |
|
|
% |
Inhibition of full length recombinant human NSUN2 expressed in Escherichia coli Rosetta2(DE3)pLysS at 100 uM measured at 20 mins by liquid scintillation counting analysis |
CHEMBL5131574 |
| tRNA (cytosine(72)-C(5))-methyltransferase NSUN6 |
Inhibition |
= |
22.7 |
% |
Inhibition of full length human NSUN6 expressed in Escherichia coli Rosetta2(DE3)pLysS at 100 uM measured at 20 mins by liquid scintillation counting analysis |
CHEMBL5131574 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 |
Inhibition |
= |
32.0 |
% |
Inhibition of recombinant human EHMT2 G9a expressed in Escherichia coli Rosetta2(DE3)pLysS at 100 uM using histone H3 as substrate measured at 120 mins by liquid scintillation counting analysis |
CHEMBL5131574 |
| tRNA (cytosine(38)-C(5))-methyltransferase |
Inhibition |
= |
62.8 |
% |
Inhibition of full length human N-terminal his6-tagged DNMT2 expressed in Escherichia coli Rosetta2(DE3)pLysS at 100 uM by liquid scintillation counting analysis |
CHEMBL5131574 |
