| Leishmania donovani |
Inhibition |
= |
100.0 |
% |
Growth inhibition of Leishmania donovani promastigotes by the compound at 0.26 uM |
CHEMBL1126291 |
| Leishmania donovani |
Inhibition |
= |
88.0 |
% |
Growth inhibition of Leishmania donovani promastigotes by the compound at 0.26 uM |
CHEMBL1126291 |
| Protein-beta-aspartate methyltransferase |
Ki |
= |
47000.0 |
nM |
Kinetic constant was measured for Protein Methylase II of Leishmania donovani promastigotes using supernatant (S12) fraction |
CHEMBL1126291 |
| Protein-beta-aspartate methyltransferase |
Ki |
= |
126000.0 |
nM |
Kinetic constant was measured for Protein Methylase II of Leishmania donovani promastigotes using protein extracted from the 12000g pellet(P12). |
CHEMBL1126291 |
| Protein-arginine N-methyltransferase 1 |
IC50 |
< |
1000.0 |
nM |
Inhibition of GST-fused human recombinant PRMT1 after 90 mins by SDS-PAGE based scintillation counting |
CHEMBL1156943 |
| Histone-lysine N-methyltransferase SETD7 |
IC50 |
= |
2500.0 |
nM |
Inhibition of GST-fused human recombinant SET7 after 90 mins by SDS-PAGE based scintillation counting |
CHEMBL1156943 |
| Leishmania donovani |
IC50 |
= |
1000.0 |
nM |
Antimicrobial activity against Leishmania donovani |
CHEMBL1212812 |
| Histone-lysine N-methyltransferase SETD7 |
Inhibition |
|
|
% |
Inhibition of human SET7/9 |
CHEMBL2429843 |
| Unchecked |
IC50 |
= |
160000.0 |
nM |
Inhibition of Staphylococcus aureus TrmD using S-[methyl-3H] adenosyl-L-methionine as substrate assessed as leucine-tRNA methylation after 1 hr by scintillation proximity assay |
CHEMBL2429843 |
| Unchecked |
IC50 |
= |
1900.0 |
nM |
Inhibition of Haemophilus influenzae TrmD using S-[methyl-3H] adenosyl-L-methionine as substrate assessed as leucine-tRNA methylation after 1 hr by scintillation proximity assay |
CHEMBL2429843 |
| Unchecked |
IC50 |
= |
11000.0 |
nM |
Inhibition of Escherichia coli TrmD using S-[methyl-3H] adenosyl-L-methionine as substrate assessed as leucine-tRNA methylation after 1 hr by scintillation proximity assay |
CHEMBL2429843 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 |
IC50 |
= |
513000.0 |
nM |
Inhibition of methyltransferase activity of EHMT1 (unknown origin)-mediated dimethylation of a biotinylated histone H3 peptide at lysine-9 by FRET-based LANCE ultra G9a assay |
CHEMBL3259565 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 |
IC50 |
= |
509000.0 |
nM |
Inhibition of methyltransferase activity of EHMT2 (unknown origin)-mediated dimethylation of a biotinylated histone H3 peptide at lysine-9 by FRET-based LANCE ultra G9a assay |
CHEMBL3259565 |
| Thiopurine S-methyltransferase |
Kd |
= |
10000.0 |
nM |
Binding affinity to thiopurine methyltransferase (unknown origin) by NMR analysis |
CHEMBL3351755 |
| Unchecked |
Inhibition |
|
|
% |
Displacement of [3H]-SAM from biotinylated Dengue virus 3 methyltransferase expressed in Escherichia coli at 20 uM preincubated for 20 mins followed by [3H]-SAM addition measured after 15 mins by scintillation counting analysis |
CHEMBL3576816 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 |
Inhibition |
= |
100.0 |
% |
Inhibition of EHMT1 (unknown origin) at 200 uM preincubated for 5 mins followed by SAM and biotinylated H3K9 peptide addition measured after 120 mins by HTRF assay relative to control |
CHEMBL4043120 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 |
Inhibition |
= |
79.5 |
% |
Inhibition of EHMT2 (unknown origin) at 400 uM preincubated for 15 mins followed by SAM and biotinylated H3K9 peptide addition measured after 30 mins by TR-FRET assay relative to control |
CHEMBL4043120 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 |
IC50 |
= |
28400.0 |
nM |
Inhibition of EHMT1 (unknown origin) preincubated for 5 mins followed by SAM and biotinylated H3K9 peptide addition measured after 120 mins by HTRF assay |
CHEMBL4043120 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 |
IC50 |
= |
30100.0 |
nM |
Inhibition of EHMT2 (unknown origin) preincubated for 15 mins followed by SAM and biotinylated H3K9 peptide addition measured after 30 mins by TR-FRET assay |
CHEMBL4043120 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 |
Inhibition |
|
|
% |
Inhibition of EHMT1 (unknown origin) preincubated for 5 mins followed by SAM and biotinylated H3K9 peptide addition measured after 120 mins by HTRF assay |
CHEMBL4043120 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 |
Inhibition |
|
|
% |
Inhibition of EHMT2 (unknown origin) preincubated for 15 mins followed by SAM and biotinylated H3K9 peptide addition measured after 30 mins by TR-FRET assay |
CHEMBL4043120 |
| HL-60 |
Inhibition |
= |
41.0 |
% |
Antiproliferative activity against human HL60 cells at 200 uM after 72 hrs by CCK8 assay relative to control |
CHEMBL4043120 |
| MDA-MB-231 |
Inhibition |
= |
42.8 |
% |
Antiproliferative activity against human MDA-MB-231 cells at 200 uM after 72 hrs by sulforhodamine B assay relative to control |
CHEMBL4043120 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 |
IC50 |
= |
100.0 |
nM |
Inhibition of EHMT2 (unknown origin) |
CHEMBL4043120 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 |
IC50 |
= |
100.0 |
nM |
Inhibition of EHMT1 (unknown origin) |
CHEMBL4043120 |
| Histone-lysine N-methyltransferase, H3 lysine-79 specific |
IC50 |
= |
33710.0 |
nM |
Inhibition of recombinant human His6-SUMO tagged DOT1L (1 to 416 residues) expressed in Escherichia coli BL21(DE3) using oligonucleosome as substrate measured after 30 mins in presence of SAM by AlphaLISA assay |
CHEMBL4219142 |
| Zika virus |
IC50 |
> |
50000.0 |
nM |
Antiviral activity against Zika virus SMGC infected in BHK cells assessed as inhibition of virus induced cytopathic effect after 8 days by CellTiter-Glo luminescent cell viability assay |
CHEMBL4270631 |
| Unchecked |
CC50 |
|
|
|
Cytotoxicity against BHK cells after 8 days by CellTiter-Glo assay |
CHEMBL4270631 |
| SARS-CoV-2 |
Inhibition |
= |
2.28 |
% |
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging |
CHEMBL4303101 |
| Nicotinamide N-methyltransferase |
Inhibition |
>= |
50.0 |
% |
Inhibition of wild-type human full length NNMT expressed in Escherichia coli BL21(DE3) cells assessed as reduction in 1-methyl-nicotinamide formation at 250 uM pre-incubated for 10 mins followed by AdoMet and nicotinamide addition measured after 30 mins by UHP-HILIC/Q-TOF-MS analysis relative to control |
CHEMBL4304774 |
| Nicotinamide N-methyltransferase |
IC50 |
= |
12510.0 |
nM |
Inhibition of wild-type human full length NNMT expressed in Escherichia coli BL21(DE3) cells assessed as reduction in 1-methyl-nicotinamide formation pre-incubated for 10 mins followed by AdoMet and nicotinamide addition measured after 30 mins by UHP-HILIC/Q-TOF-MS analysis |
CHEMBL4304774 |
| Protein arginine N-methyltransferase 5 |
IC50 |
= |
8600.0 |
nM |
Inhibition of full-length N-terminal FLAG-tagged PRMT5 (unknown origin) (1 to 637 residues) expressed in baculovirus infected Sf9 insect cells using histone H4 as peptide after 5 hrs in presence of [H3]AdoMet by scintillation proximity assay |
CHEMBL4325864 |
| NS5 |
IC50 |
= |
1180.0 |
nM |
Inhibition of Zika virus MTase (4 to 278 residues) expressed in Escherichia coli T7 using GpppAC4 as substrate in presence of [3H]SAM incubated for 30 mins by liquid scintillation counter method |
CHEMBL4354808 |
| NS5 |
IC50 |
= |
1620.0 |
nM |
Inhibition of Zika virus MTase (4 to 278 residues) expressed in Escherichia coli T7 using A27 RNA as substrate in presence of [3H]SAM incubated for 30 mins by liquid scintillation counter method |
CHEMBL4354808 |
| Unchecked |
IC50 |
= |
30.0 |
nM |
Inhibition of Dengue virus guanine N-7 methyltransferase using RNA substrate after 20 mins in presence of [methyl-3H]-AdoMet by microbeta counting analysis |
CHEMBL4431301 |
| Nonstructural protein 5 |
IC50 |
= |
41.0 |
nM |
Inhibition of Dengue virus ribose 2'-O methyltransferase using RNA substrate after 20 mins in presence of [methyl-3H]-AdoMet by microbeta counting analysis |
CHEMBL4431301 |
| Unchecked |
Kd |
= |
136.0 |
nM |
Binding affinity to His-tagged Dengue virus 3 methyltransferase expressed in Escherichia coli Rosetta 2(DE3) by VP-ITC isothermal titration calorimetry |
CHEMBL4431301 |
| Unchecked |
Ratio |
= |
6.0 |
|
Potency index, ratio of S-adenosyl-L-methionine Kd to sinefungin Kd for His-tagged Dengue virus 3 methyltransferase expressed in Escherichia coli Rosetta 2(DE3) |
CHEMBL4431301 |
| Replicase polyprotein 1ab |
Inhibition |
= |
4.11 |
% |
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate |
CHEMBL4495564 |
| Replicase polyprotein 1ab |
Inhibition |
= |
4.76 |
% |
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate |
CHEMBL4495564 |
| SARS-CoV-2 |
Inhibition |
= |
0.05 |
% |
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging |
CHEMBL4495565 |
| SARS-CoV-2 |
Inhibition |
= |
-0.06 |
% |
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging |
CHEMBL4495565 |
| SARS-CoV-2 |
Inhibition |
= |
-0.06 |
% |
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging |
CHEMBL4495565 |
| SARS-CoV-2 |
Inhibition |
= |
0.05 |
% |
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging |
CHEMBL4495565 |
| Unchecked |
IC50 |
= |
41.0 |
nM |
Inhibition of Dengue virus 2'-O methyltransferase incubated for 15 mins followed by [methyl-3-H]-AdoMet addition and measured after 30 mins by microbeta counter method |
CHEMBL4699605 |
| Unchecked |
IC50 |
= |
30.0 |
nM |
Inhibition of Dengue virus N-7 methyltransferase incubated for 15 mins followed by [methyl-3-H]-AdoMet addition and measured after 15 mins by microbeta counter method |
CHEMBL4699605 |
| Unchecked |
IC50 |
= |
1890.0 |
nM |
Inhibition of MHV-A59 guanine-N7 methyltransferase expressed in Saccharomyces cerevisiae YBS40 (MATa leu2 ade2 trp1 his3 ura3 can1 abd1::hisGp360-ABD1) |
CHEMBL4715856 |
| Unchecked |
IC50 |
= |
1670.0 |
nM |
Inhibition of Transmissible gastroenteritis coronavirus H16 guanine-N7 methyltransferase expressed in Saccharomyces cerevisiae YBS40 (MATa leu2 ade2 trp1 his3 ura3 can1 abd1::hisGp360-ABD1) |
CHEMBL4715856 |
| Unchecked |
IC50 |
= |
1900.0 |
nM |
Inhibition of Avian infectious bronchitis virus (strain-Beaudette CK) guanine-N7 methyltransferase expressed in Saccharomyces cerevisiae YBS40 (MATa leu2 ade2 trp1 his3 ura3 can1 abd1::hisGp360-ABD1) |
CHEMBL4715856 |
| mRNA cap guanine-N7 methyltransferase |
IC50 |
= |
0.55 |
nM |
Inhibition of human guanine-N7 methyltransferase expressed in Saccharomyces cerevisiae YBS40 (MATa leu2 ade2 trp1 his3 ura3 can1 abd1::hisGp360-ABD1) |
CHEMBL4715856 |
| Unchecked |
IC50 |
= |
1680.0 |
nM |
Inhibition of SARS coronavirus WHU guanine-N7 methyltransferase expressed in Saccharomyces cerevisiae YBS40 (MATa leu2 ade2 trp1 his3 ura3 can1 abd1::hisGp360-ABD1) |
CHEMBL4715856 |
| Unchecked |
Ratio IC50 |
= |
0.32 |
|
Selectivity index, ratio of IC50 for human guanine-N7 methyltransferase expressed in Saccharomyces cerevisiae YBS40 (MATa leu2 ade2 trp1 his3 ura3 can1 abd1::hisGp360-ABD1) to IC50 for SARS coronavirus WHU guanine-N7 methyltransferase expressed in Saccharomyces cerevisiae YBS40 (MATa leu2 ade2 trp1 his3 ura3 can1 abd1::hisGp360-ABD1) |
CHEMBL4715856 |
| mRNA cap guanine-N7 methyltransferase |
IC50 |
< |
50.0 |
nM |
Inhibition of N-terminus hexa-histidine tagged-human guanine-N7 methyltransferase expressed in Escherichia coli using GpppAC4 RNA as substrate incubated for 30 mins by liquid scintillation counting method |
CHEMBL4715856 |
| Unchecked |
Ratio IC50 |
< |
2.63 |
|
Selectivity ratio of IC50 for N-terminus hexa-histidine tagged-human guanine-N7 methyltransferase expressed in Escherichia coli to IC50 for N-terminus hexa-histidine tagged-SARS-coV guanine-N7 methyltransferase expressed in Escherichia coli |
CHEMBL4715856 |
| Unchecked |
Inhibition |
= |
98.3 |
% |
Inhibition of N7-MTase activity of N-terminal His6-tagged SARS-CoV nsp14 expressed in Escherichia coli using GpppAC4 and [3H]SAM as substrate at 50 uM preincubated with enzyme followed by substrate addition and measured after 30 mins by filter binding assay |
CHEMBL4765355 |
| Unchecked |
Inhibition |
= |
99.8 |
% |
Inhibition of N7-MTase activity of Vaccinia virus mRNA capping enzyme D1/D12 complex using GpppAC4 and [3H]SAM as substrate at 50 uM preincubated with enzyme followed by substrate addition and measured after 30 mins by filter binding assay |
CHEMBL4765355 |
| mRNA cap guanine-N7 methyltransferase |
Inhibition |
= |
99.8 |
% |
Inhibition of N-terminal His6-tagged human RNA-N7 MTase expressed in Escherichia coli using GpppAC4 and [3H]SAM as substrate at 50 uM preincubated with enzyme followed by substrate addition and measured after 30 mins by filter binding assay |
CHEMBL4765355 |
| Unchecked |
IC50 |
= |
360.0 |
nM |
Inhibition of N7-MTase activity of N-terminal His6-tagged SARS-CoV nsp14 expressed in Escherichia coli using GpppAC4 and [3H]SAM as substrate preincubated with enzyme followed by substrate addition and measured after 30 mins by filter binding assay |
CHEMBL4765355 |
| mRNA cap guanine-N7 methyltransferase |
IC50 |
< |
50.0 |
nM |
Inhibition of N-terminal His6-tagged human RNA-N7 MTase expressed in Escherichia coli using GpppAC4 and [3H]SAM as substrate preincubated with enzyme followed by substrate addition and measured after 30 mins by filter binding assay |
CHEMBL4765355 |
| Unchecked |
Delta Tm |
= |
4.4 |
degrees C |
Binding affinity to SARS-CoV nsp14 assessed as increase in melting temperature at 1 mM at pH 7.5 by differential scanning fluorimetry |
CHEMBL4765355 |
| Unchecked |
IC50 |
= |
450.0 |
nM |
Inhibition of MTase activity of N-terminal 6XHis-tagged SARS-CoV-2 NSP14 expressed in Escherichia coli BL21(DE3) using GpppG and SAM as substrate incubated for 20 mins by HTRF assay |
CHEMBL4834465 |
| Unchecked |
IC50 |
= |
860.0 |
nM |
Inhibition of MTase activity of N-terminal 6XHis-tagged SARS-CoV-2 Wuhan-Hu-1 NSP16/10 expressed in Escherichia coli using m7GpppA-RNA and SAM as substrate incubated for 2 hrs by HTRF assay |
CHEMBL4834465 |
| Glycine N-methyltransferase |
IC50 |
= |
316000.0 |
nM |
Inhibition of N-terminal His-tagged human recombinant Glycine-N-methyltransferase (1 to 295 residues) expressed in Escherichia coli using glycine and SAM as substrate incubated for 30 mins by HTRF assay |
CHEMBL4834465 |
| Unchecked |
CC50 |
= |
99210.0 |
nM |
Cytotoxicity against mouse BALB/c3T3 clone A31 cells assessed as reduction in cell viability measured after 48 hrs by neutral red uptake assay |
CHEMBL4834465 |
| HepG2 |
CC50 |
> |
100000.0 |
nM |
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 48 hrs by neutral red uptake assay |
CHEMBL4834465 |
| A549 |
CC50 |
= |
72930.0 |
nM |
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 48 hrs by neutral red uptake assay |
CHEMBL4834465 |
| ADMET |
permeability |
|
|
|
Permeability of the compound in human A549 cells at 20 uM incubated for 24 hrs with 1*10^4 cells/ml media by LC/MS analysis |
CHEMBL4834465 |
| ADMET |
permeability |
|
|
|
Permeability of the compound in human A549 cells at 20 uM incubated for 24 hrs with 2*10^4 cells/ml media by LC/MS analysis |
CHEMBL4834465 |
| Unchecked |
IC50 |
= |
496.0 |
nM |
Inhibition of MTase activity of N-terminal 6XHis-tagged SARS-CoV-1 NSP14 (5903 to 6429 residues) expressed in Escherichia coli C41(DE3) using GpppAC5 and [3H]AdoMet as substrate incubated for 4 hrs by filter binding assay |
CHEMBL4834465 |
| Unchecked |
IC50 |
= |
736.0 |
nM |
Inhibition of MTase activity of N-terminal 6XHis-tagged SARS-CoV-1 NSP16 (6776 to 7073 residues) expressed in Escherichia coli C41(DE3) using 7MeGpppAC5 and [3H]AdoMet as substrate incubated for 4 hrs by filter binding assay |
CHEMBL4834465 |
| Unchecked |
IC50 |
= |
383.0 |
nM |
Inhibition of MTase activity of SARS-CoV-1 WHU NSP14 expressed in Escherichia coli BL21(DE3) using GpppA and S-adenosyl-[methyl-3H]methionine as substrate preincubated with enzyme for 20 mins followed by S-adenosyl-[methyl-3H]methionine addition and measured after 1.5 hrs by scintillation counting analysis |
CHEMBL4834465 |
| Unchecked |
IC50 |
= |
112.0 |
nM |
Inhibition of MTase activity of N-terminal 6XHis-tagged SARS-CoV-1 NSP14 expressed in Escherichia coli using GpppAC4 and [3H]SAM as substrate incubated for 30 mins by filter binding assay |
CHEMBL4834465 |
| Unchecked |
IC50 |
= |
630.0 |
nM |
Inhibition of DENV NS5-MTase domain using GpppA2'OMe-RNA74 as a substrate incubated for 30 mins by filter binding assay |
CHEMBL4842338 |
| Unchecked |
IC50 |
= |
1180.0 |
nM |
Inhibition of full length ZIKV NS5-MTase domain using 7MeGpppAC4 as a substrate incubated for 30 mins by filter binding assay |
CHEMBL4842338 |
| 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 |
= |
83.5 |
% |
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 |
= |
7500.0 |
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 |
= |
13200.0 |
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 |
= |
2.0 |
|
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 |
= |
-29.3 |
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 |
= |
-24.5 |
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 |
= |
-4.8 |
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 |
= |
98.0 |
% |
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 |
= |
77.1 |
% |
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 |
= |
70.2 |
% |
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 |
= |
43.0 |
% |
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 |
= |
83.5 |
% |
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 |
| HEK293 |
CC50 |
> |
500000.0 |
nM |
Cytotoxicity against human HEK293 cells assessed as cell viability at 100 uM measured after 24 hrs by MTT assay |
CHEMBL5131574 |
| tRNA (cytosine(38)-C(5))-methyltransferase |
Inhibition |
|
|
% |
Inhibition of DNMT2-mediated tRNA methylation in human HEK293 cells assessed as reduction in m5C at C38 of tRNA at 100 uM incubated for 24 hrs by LC-MS/MS analysis |
CHEMBL5131574 |
| tRNA (cytosine(38)-C(5))-methyltransferase |
Inhibition |
= |
94.0 |
% |
Inhibition of DNMT2-mediated tRNA methylation in human HEK293 cells assessed as reduction in m5C at C38 of tRNA by measuring m5C level at 100 uM incubated for 24 hrs by bisulfite sequencing analysis |
CHEMBL5131574 |
| Indolethylamine N-methyltransferase |
IC50 |
= |
4000.0 |
nM |
Inhibition of N-terminal 6His-tagged full length human recombinant INMT (1 to 263 residues) expressed in Escherichia coli BL21 (DE3) cells using S-(5'-Adenosyl)-L-methionine chloride dihydrochloride and 9H-pyrido[3,4-b]indole as substrate incubated for 2.5 hrs by MTase-Glo assay |
CHEMBL5137077 |
| Nicotinamide N-methyltransferase |
IC50 |
> |
100000.0 |
nM |
Inhibition of NNMT in HEK293 cells measured after 20 to 24 hrs by RapidFire Mass Spectrometry |
CHEMBL5137077 |
| Nicotinamide N-methyltransferase |
IC50 |
= |
5200.0 |
nM |
Inhibition of N-terminal 6His-tagged full length human recombinant NNMT (1 to 264 residues) expressed in Escherichia coli BL21 (DE3) cells using S-adenosyl-L-methionine and NAM as substrate incubated for 2 hrs by by RapidFire Mass Spectrometry |
CHEMBL5137077 |
| Replicase polyprotein 1ab |
IC50 |
= |
260.0 |
nM |
Inhibition of MTase activity of SARS-CoV-2 NSP14 expressed in Escherichia coli BL21(DE3) using GpppA and SAM as substrate preincubated for 15 mins followed by SAM addition incubated for 15 mins by LC-MS/MS analysis |
CHEMBL5143750 |
| SARS-CoV-2 |
Inhibition |
< |
15.0 |
% |
Antiviral activity against SARS-CoV-2 infected in human A549 cells overexpressing ACE2 and TMPRSS2 assessed as inhibition of viral growth at 50 uM incubated for 48 hrs by DAPI staining based immunofluorescence assay |
CHEMBL5143750 |
| A549 |
Activity |
> |
95.0 |
% |
Cytotoxicity against human A549 cells overexpressing ACE2 and TMPRSS2 assessed as cell viability at 50 uM incubated for 48 hrs by MTS assay |
CHEMBL5143750 |
| Replicase polyprotein 1ab |
IC50 |
= |
278.0 |
nM |
Inhibition of N7-MTase activity of SARS-CoV-2 N-terminus hexahistidine tag nsp14 expressed in Escherichia coli C2566 using [3H]SAM as substrate incubated for 30 mins in presence of mGpppAC4 synthetic RNA by radioactive filter binding assay |
CHEMBL5154878 |
| Replicase polyprotein 1ab |
IC50 |
= |
360.0 |
nM |
Inhibition of SARS-CoV-2 nsp14 N7-MTase activity using [3H]SAM as substrate incubated for 30 mins in presence of GpppAC4 synthetic RNA and 7mGpppAC4 by DEAE radioactive filter binding assay |
CHEMBL5154878 |
| Replicase polyprotein 1ab |
Inhibition |
= |
100.0 |
% |
Inhibition of N7-MTase activity of SARS-CoV-2 N-terminus hexahistidine tag nsp14 expressed in Escherichia coli C2566 at 5 uM using [3H]SAM as substrate incubated for 30 mins in presence of mGpppAC4 synthetic RNA by filter binding assay relative to control |
CHEMBL5154878 |
