| Nicotinamide N-methyltransferase |
Ki |
= |
0.5 |
nM |
Inhibition of N-terminal His6-tagged wild type human NNMT expressed in Escherichia coli NiCo21(DE3) assessed as reduction in 1-methylquinolinium level using quinoline as substrate in presence of SAM and measured every 27 seconds for 5.5 mins by fluorescence-based assay |
CHEMBL4414609 |
| Nicotinamide N-methyltransferase |
Ki |
= |
0.5012 |
nM |
Inhibition of N-terminal His6-tagged wild type human NNMT expressed in Escherichia coli NiCo21(DE3) assessed as reduction in 1-methylquinolinium level using quinoline as substrate in presence of SAM and measured every 27 seconds for 5.5 mins by fluorescence-based assay |
CHEMBL4414609 |
| Thiopurine S-methyltransferase |
Inhibition |
= |
76.0 |
% |
Inhibition of human TPMT expressed in Escherichia coli assessed as reduction in SAH level at 10 uM using 6-mercaptopurine as substrate in presence of SAM incubated for 30 mins by LC-MS/MS analysis relative to control |
CHEMBL4414609 |
| Indolethylamine N-methyltransferase |
Inhibition |
= |
53.0 |
% |
Inhibition of wild type human INMT expressed in Escherichia coli at 10 uM using tryptamine as substrate in presence of SAM incubated for 30 mins by MTase-Glo assay relative to control |
CHEMBL4414609 |
| Catechol O-methyltransferase |
Inhibition |
= |
43.0 |
% |
Inhibition of human COMT expressed in Escherichia coli at 10 uM assessed as reduction in SAH level using pyrocatechol as substrate in presence of SAM incubated for 15 mins by LC-MS/MS analysis relative to control |
CHEMBL4414609 |
| Phenylethanolamine N-methyltransferase |
Inhibition |
= |
26.0 |
% |
Inhibition of human PNMT expressed in Escherichia coli at 10 uM assessed as reduction in SAH level using DL-normetanephrine as substrate in presence of SAM incubated for 45 mins by LC-MS/MS analysis relative to control |
CHEMBL4414609 |
| Guanidinoacetate N-methyltransferase |
Inhibition |
= |
26.0 |
% |
Inhibition of human GAMT expressed in Escherichia coli at 10 uM assessed as reduction in SAH level using guanidineacetic acid as substrate in presence of SAM incubated for 30 mins by LC-MS/MS analysis relative to control |
CHEMBL4414609 |
| Glycine N-methyltransferase |
Inhibition |
= |
23.0 |
% |
Inhibition of human GNMT expressed in Escherichia coli at 10 uM assessed as reduction in SAH level using glycine as substrate in presence of SAM incubated for 30 mins by LC-MS/MS analysis relative to control |
CHEMBL4414609 |
| Histamine N-methyltransferase |
Inhibition |
= |
2.0 |
% |
Inhibition of human HNMT expressed in Escherichia coli at 10 uM assessed as reduction in SAH level using histamine as substrate in presence of SAM incubated for 15 mins by LC-MS/MS analysis relative to control |
CHEMBL4414609 |
| Thiopurine S-methyltransferase |
Inhibition |
= |
51.0 |
% |
Inhibition of human TPMT expressed in Escherichia coli assessed as reduction in SAH level at 1 uM using 6-mercaptopurine as substrate in presence of SAM incubated for 30 mins by LC-MS/MS analysis relative to control |
CHEMBL4414609 |
| Indolethylamine N-methyltransferase |
Inhibition |
= |
14.0 |
% |
Inhibition of wild type human INMT expressed in Escherichia coli at 1 uM using tryptamine as substrate in presence of SAM incubated for 30 mins by MTase-Glo assay relative to control |
CHEMBL4414609 |
| Catechol O-methyltransferase |
Inhibition |
= |
0.0 |
% |
Inhibition of human COMT expressed in Escherichia coli at 1 uM assessed as reduction in SAH level using pyrocatechol as substrate in presence of SAM incubated for 15 mins by LC-MS/MS analysis relative to control |
CHEMBL4414609 |
| Phenylethanolamine N-methyltransferase |
Inhibition |
= |
0.0 |
% |
Inhibition of human PNMT expressed in Escherichia coli at 1 uM assessed as reduction in SAH level using DL-normetanephrine as substrate in presence of SAM incubated for 45 mins by LC-MS/MS analysis relative to control |
CHEMBL4414609 |
| Guanidinoacetate N-methyltransferase |
Inhibition |
= |
0.0 |
% |
Inhibition of human GAMT expressed in Escherichia coli at 1 uM assessed as reduction in SAH level using guanidineacetic acid as substrate in presence of SAM incubated for 30 mins by LC-MS/MS analysis relative to control |
CHEMBL4414609 |
| Glycine N-methyltransferase |
Inhibition |
= |
4.0 |
% |
Inhibition of human GNMT expressed in Escherichia coli at 1 uM assessed as reduction in SAH level using glycine as substrate in presence of SAM incubated for 30 mins by LC-MS/MS analysis relative to control |
CHEMBL4414609 |
| Histamine N-methyltransferase |
Inhibition |
= |
6.0 |
% |
Inhibition of human HNMT expressed in Escherichia coli at 1 uM assessed as reduction in SAH level using histamine as substrate in presence of SAM incubated for 15 mins by LC-MS/MS analysis relative to control |
CHEMBL4414609 |
| DNA (cytosine-5)-methyltransferase 3A |
IC50 |
= |
7600.0 |
nM |
Inhibition of human DNMT3a expressed in insect sf9 cells assessed as reduction in methylated poly(dI-dC)-Poly(dI-dC) level using poly(dI-dC)-poly(dI-dC) as substrate in presence of [3H] SAM incubated for 10 mins by scintillation counting |
CHEMBL4414609 |
| Protein-arginine N-methyltransferase 1 |
IC50 |
> |
10000.0 |
nM |
Inhibition of human PRMT1 expressed in Escherichia coli assessed as reduction in methylated histone H4 full length level using histone H4 full length as substrate in presence of [3H] SAM incubated for 20 mins by scintillation counting |
CHEMBL4414609 |
| Histone-lysine N-methyltransferase ASH1L |
IC50 |
> |
10000.0 |
nM |
Inhibition of human ASH1L expressed in Escherichia coli assessed as reduction in methylated polynucleosome level using polynucleosome as substrate in presence of [3H] SAM incubated for 15 mins by scintillation counting |
CHEMBL4414609 |
| Histone-lysine N-methyltransferase, H3 lysine-79 specific |
IC50 |
> |
10000.0 |
nM |
Inhibition of human DOT1L expressed in Escherichia coli assessed as reduction in methylated polynucleosome level using polynucleosome as substrate in presence of [3H] SAM incubated for 15 mins by scintillation counting |
CHEMBL4414609 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 |
IC50 |
> |
10000.0 |
nM |
Inhibition of human EHMT1 expressed in Escherichia coli assessed as reduction in methylated histone H3 full length using histone H3 full length as substrate in presence of [3H] SAM incubated for 120 mins by scintillation counting |
CHEMBL4414609 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 |
IC50 |
> |
10000.0 |
nM |
Inhibition of human G9a expressed in Escherichia coli assessed as reduction in methylated histone H3 full length using histone H3 full length level as substrate in presence of [3H] SAM incubated for 120 mins by scintillation counting |
CHEMBL4414609 |
| Histone-lysine N-methyltransferase SETDB1 |
IC50 |
> |
10000.0 |
nM |
Inhibition of human SETDB1 expressed in sf9 insect cells assessed as reduction in methylated histone H3 full length level using histone H3 full length as substrate in presence of [3H] SAM incubated for 30 mins by scintillation counting |
CHEMBL4414609 |
| Thiopurine S-methyltransferase |
IC50 |
= |
1000.0 |
nM |
Inhibition of human TPMT expressed in Escherichia coli assessed as reduction in SAH level using 6-mercaptopurine as substrate in presence of SAM incubated for 30 mins by LC-MS/MS analysis |
CHEMBL4414609 |
| Indolethylamine N-methyltransferase |
IC50 |
= |
3400.0 |
nM |
Inhibition of wild type human INMT expressed in Escherichia coli using tryptamine as substrate in presence of SAM incubated for 30 mins by MTase-Glo assay |
CHEMBL4414609 |
| Nicotinamide N-methyltransferase |
Delta Tm |
= |
8.0 |
degrees C |
Binding affinity to NNMT in human K562 cell lysates assessed as change in melting temperature at 100 uM incubated for 30 mins by CETSA-based Western blot analysis |
CHEMBL4414609 |
| Nicotinamide N-methyltransferase |
Activity |
|
|
|
Binding affinity to NNMT in human K562 cell lysates incubated for 30 mins by CETSA-based Western blot analysis |
CHEMBL4414609 |
| U2OS |
Activity |
|
|
|
Cytotoxicity against human U2OS cells at 100 uM after 48 hrs by CellTiter-Glo luminescent cell viability |
CHEMBL4414609 |
| Nicotinamide N-methyltransferase |
Inhibition |
|
|
% |
Inhibition of NNMT in human U2OS cells assessed as reduction in MNAM level incubated for 24 hrs by LC-MS/MS analysis |
CHEMBL4414609 |
| ADMET |
permeability |
|
|
|
Permeability across apical to basolateral side in human Caco2 cells after 60 mins by HPLC-MS/MS analysis |
CHEMBL4414609 |
