| Adenosylhomocysteinase |
Km |
= |
9700.0 |
nM |
Km for the compound was determined against the recombinant rat liver AdoHyc hydrolase (MV1304/pUCSAH) |
CHEMBL1135046 |
| Adenosylhomocysteinase |
Vmax |
= |
1.1 |
uM min-1mg-1 |
Vmax for the compound was determined against the recombinant rat liver AdoHyc hydrolase (MV1304/pUCSAH) |
CHEMBL1135046 |
| Catechol O-methyltransferase |
Inhibition |
= |
39.0 |
% |
Inhibition of Catechol O-methyltransferase at 0.1 mM |
CHEMBL1122976 |
| Catechol O-methyltransferase |
Inhibition |
= |
87.0 |
% |
Inhibition of Catechol O-methyltransferase at 1.0 mM |
CHEMBL1122976 |
| Phenylethanolamine N-methyltransferase |
Inhibition |
= |
49.0 |
% |
Inhibition of PNMT at 0.1 mM |
CHEMBL1122976 |
| Phenylethanolamine N-methyltransferase |
Inhibition |
= |
92.0 |
% |
Inhibition of PNMT at 1.0 mM |
CHEMBL1122976 |
| Histamine N-methyltransferase |
Inhibition |
= |
40.0 |
% |
Inhibition of Histamine N-methyl-transferase at 0.1 mM |
CHEMBL1122976 |
| Histamine N-methyltransferase |
Inhibition |
= |
89.0 |
% |
Inhibition of Histamine N-methyl-transferase at 1.0 mM |
CHEMBL1122976 |
| Phenylethanolamine N-methyltransferase |
Ki |
= |
29000.0 |
nM |
Inhibition constant was evaluated against PNMT |
CHEMBL1122976 |
| Histamine N-methyltransferase |
Ki |
= |
18100.0 |
nM |
Inhibition constant was evaluated against Histamine N-methyl-transferase |
CHEMBL1122976 |
| Indolethylamine N-methyltransferase |
Ki |
= |
2000.0 |
nM |
Inhibitory constant towards indole N-methyl-transferase |
CHEMBL1122373 |
| Catechol O-methyltransferase |
Inhibition |
= |
5.0 |
% |
Inhibition of Catechol O-methyltransferase at 0.1 mM |
CHEMBL1122976 |
| Catechol O-methyltransferase |
Inhibition |
= |
22.0 |
% |
Inhibition of Catechol O-methyltransferase at 1.0 mM |
CHEMBL1122976 |
| Phenylethanolamine N-methyltransferase |
Inhibition |
= |
14.0 |
% |
Inhibition of PNMT at 0.1 mM |
CHEMBL1122976 |
| Phenylethanolamine N-methyltransferase |
Inhibition |
= |
32.0 |
% |
Inhibition of PNMT at 1.0 mM |
CHEMBL1122976 |
| Histamine N-methyltransferase |
Inhibition |
= |
73.0 |
% |
Inhibition of Histamine N-methyl-transferase at 0.1 mM |
CHEMBL1122976 |
| Histamine N-methyltransferase |
Inhibition |
= |
99.0 |
% |
Inhibition of Histamine N-methyl-transferase at 1.0 mM |
CHEMBL1122976 |
| Phenylethanolamine N-methyltransferase |
Ki |
= |
62300.0 |
nM |
Inhibition constant was evaluated against PNMT |
CHEMBL1122976 |
| Histamine N-methyltransferase |
Ki |
= |
10500.0 |
nM |
Inhibition constant was evaluated against Histamine N-methyl-transferase |
CHEMBL1122976 |
| Fatty acid synthase |
Ki |
= |
150000.0 |
nM |
Inhibition constant against Escherichia coli cyclopropane fatty acid synthase |
CHEMBL1148231 |
| Leishmania donovani |
Ki |
= |
7200.0 |
nM |
Apparent kinetic activity measured for protein carboxyl methyltransferase in Leishmania donovani promastigotes |
CHEMBL1125204 |
| ADMET |
Ratio |
= |
0.13 |
|
It is the ratio of Ki value to that of Km. |
CHEMBL1125204 |
| rRNA adenine N-6-methyltransferase |
Ki |
= |
40000.0 |
nM |
Inhibitory activity against ErmAM methylase |
CHEMBL1132643 |
| rRNA adenine N-6-methyltransferase |
Ki |
= |
40000.0 |
nM |
Inhibition of ErmAM methylase |
CHEMBL1133152 |
| Unchecked |
Activity |
|
|
|
Inhibition of Escherichia coli DNA methyltransferase at 15 uM after 30 mins |
CHEMBL1142331 |
| Unchecked |
Activity |
|
|
|
Inhibition of M.HhaI DNA methyltransferase expressed in ER1727 cells at 15 uM after 30 mins |
CHEMBL1142331 |
| 5-methylthioadenosine/S-adenosylhomocysteine deaminase |
Km |
= |
210000.0 |
nM |
Activity of Thermotoga maritima S-adenosyl-homocysteine deaminase Tm0936 assessed as ammonia production |
CHEMBL1145524 |
| 5-methylthioadenosine/S-adenosylhomocysteine deaminase |
Kcat |
= |
12.2 |
/s |
Activity of Thermotoga maritima S-adenosyl-homocysteine deaminase Tm0936 assessed as ammonia production |
CHEMBL1145524 |
| 5-methylthioadenosine/S-adenosylhomocysteine deaminase |
Kcat/Km |
= |
5.8 |
10^4/M/s |
Ratio of Kcat to Km for Thermotoga maritima S-adenosyl-homocysteine deaminase Tm0936 assessed as ammonia production |
CHEMBL1145524 |
| Adenosylhomocysteinase |
Km |
= |
21000.0 |
nM |
Activity of Thermotoga maritima S-adenosyl-L-homocysteine hydrolase Tm0172 assessed as homocysteine hydrolysis |
CHEMBL1145524 |
| Adenosylhomocysteinase |
Kact |
= |
0.24 |
/min |
Activity of Thermotoga maritima S-adenosyl-L-homocysteine hydrolase Tm0172 assessed as homocysteine hydrolysis |
CHEMBL1145524 |
| Adenosylhomocysteinase |
Kcat/Km |
= |
1.1 |
10^2/M/s |
Ratio of Kcat to Km for Thermotoga maritima S-adenosyl-L-homocysteine hydrolase Tm0172 assessed as homocysteine hydrolysis |
CHEMBL1145524 |
| DNA (cytosine-5)-methyltransferase 1 |
IC50 |
= |
2000.0 |
nM |
Inhibition of human recombinant DNMT1 expressed in baculovirus infected high five insect cells |
CHEMBL1151871 |
| DNA (cytosine-5)-methyltransferase 3B |
IC50 |
= |
300.0 |
nM |
Inhibition of human recombinant DNMT3b2 expressed in baculovirus infected high five insect cells |
CHEMBL1151871 |
| DNA (cytosine-5)-methyltransferase 1 |
IC50 |
= |
800.0 |
nM |
Inhibition of human recombinant DNMT1 |
CHEMBL1151876 |
| DNA (cytosine-5)-methyltransferase 3B |
IC50 |
= |
200.0 |
nM |
Inhibition of human recombinant DNMT3b2 |
CHEMBL1151876 |
| DNA (cytosine-5)-methyltransferase 1 |
Inhibition |
= |
26.0 |
% |
Inhibition of human recombinant DNMT1 expressed in baculovirus-insect cell system at 100 uM by scintillation counting |
CHEMBL1157722 |
| DNA (cytosine-5)-methyltransferase 3B |
Inhibition |
= |
28.0 |
% |
Inhibition of human recombinant DNMT3B expressed in baculovirus-insect cell system at 100 uM by scintillation counting |
CHEMBL1157722 |
| DNA (cytosine-5)-methyltransferase 1 |
IC50 |
= |
4000.0 |
nM |
Inhibition of human recombinant DNMT1 expressed in baculovirus-insect cell system by scintillation counting |
CHEMBL1157722 |
| DNA (cytosine-5)-methyltransferase 3B |
IC50 |
= |
250.0 |
nM |
Inhibition of human recombinant DNMT3B expressed in baculovirus-insect cell system by scintillation counting |
CHEMBL1157722 |
| Nucleic Acid |
Activity |
|
|
|
Binding affinity to 2-amino purine labelled SAM2 riboswitch aptamer assessed as change in fluorescence at 5 mM to 10 mM at pH 8.3 by fluorescence binding assay |
CHEMBL1817644 |
| DNA (cytosine-5)-methyltransferase 1 |
Activity |
= |
0.5 |
% |
Inhibition of human recombinant DNMT1 expressed in Sf9 cells assessed as remaining activity at 2 mM after 3 hrs by scintillation counting in presence of [3H]S-adenosyl methionine |
CHEMBL1914404 |
| DNA (cytosine-5)-methyltransferase 1 |
IC50 |
= |
4000.0 |
nM |
Inhibition of human recombinant DNMT1 expressed in Sf9 cells assessed as incorporation of [3H]S-adenosyl methionine into hemimethylated oligonucleotide substrate after 3 hrs by scintillation counting |
CHEMBL1914404 |
| Unchecked |
IC50 |
= |
11900.0 |
nM |
Inhibition of Yersinia pestis Dam using oligonucleotide 1 as substrate after 2000 to 3000 sec by micro plate reader based real-time break-light assay |
CHEMBL2016468 |
| DNA (cytosine-5)-methyltransferase 1 |
IC50 |
= |
941.0 |
nM |
Inhibition of human Dnmt1 using oligonucleotide 2 as substrate after 5000 sec by micro plate reader based real-time break-light assay |
CHEMBL2016468 |
| Unchecked |
Ratio IC50 |
= |
0.1 |
|
Selectivity ratio of IC50 for human Dnmt1 to IC50 for Yersinia pestis Dam |
CHEMBL2016468 |
| DNA (cytosine-5)-methyltransferase 1 |
Inhibition |
|
|
% |
Inhibition of full length N-terminal His6-tagged human DNMT1 at 30 uM after 1 hr by fluorescence analysis |
CHEMBL2046381 |
| DNA (cytosine-5)-methyltransferase 1 |
IC50 |
= |
900.0 |
nM |
Inhibition of full length N-terminal His6-tagged human DNMT1 after 1 hr by fluorescence analysis |
CHEMBL2046381 |
| Histone-lysine N-methyltransferase, H3 lysine-79 specific |
Kd |
= |
150.0 |
nM |
Binding affinity at human recombinant DOT1L catalytic domain amino acid (1 to 472)-nucleosome complex by isothermal titration calorimetric assay |
CHEMBL2169812 |
| Histone-lysine N-methyltransferase, H3 lysine-79 specific |
Kd |
= |
360.0 |
nM |
Binding affinity at human recombinant DOT1L catalytic domain amino acid (1 to 472) by isothermal titration calorimetric assay |
CHEMBL2169812 |
| Histone-lysine N-methyltransferase SUV39H1 |
Ki |
= |
4900.0 |
nM |
Inhibition of SUV39H1 |
CHEMBL2169812 |
| Histone-arginine methyltransferase CARM1 |
Ki |
= |
860.0 |
nM |
Inhibition of CARM1 |
CHEMBL2169812 |
| Protein-arginine N-methyltransferase 1 |
Ki |
= |
400.0 |
nM |
Inhibition of PRMT1 |
CHEMBL2169812 |
| Histone-lysine N-methyltransferase, H3 lysine-79 specific |
Ki |
= |
160.0 |
nM |
Inhibition of human recombinant DOT1L catalytic domain amino acid (1 to 472) using [3H]-SAM after 30 mins by scintillation counter |
CHEMBL2169812 |
| Histone-lysine N-methyltransferase, H3 lysine-79 specific |
IC50 |
= |
600.0 |
nM |
Competitive inhibition of human recombinant DOT1L (1 to 420 amino acid residues) overexpressed in Escherichia coli BL21 (DE3) using [3H]-SAM as substrate assessed as inhibition of nucleosome methylation incubated for 30 mins prior to substrate addition measured after 1 hr by scintillation counting analysis |
CHEMBL2346640 |
| Histone-lysine N-methyltransferase, H3 lysine-79 specific |
IC50 |
= |
600.0 |
nM |
Competitive inhibition of human recombinant DOT1L (1 to 472 amino acid residues) expressed in Escherichia coli BL21 (DE3) using [3H]-SAM assessed as inhibition of nucleosome methylation incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis |
CHEMBL2346640 |
| Histone-arginine methyltransferase CARM1 |
Ki |
= |
400.0 |
nM |
Inhibition of CARM1 (unknown origin) |
CHEMBL3085656 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 |
Ki |
= |
570.0 |
nM |
Inhibition of G9a (unknown origin) |
CHEMBL3085656 |
| Histone-lysine N-methyltransferase, H3 lysine-79 specific |
Ki |
= |
160.0 |
nM |
Competitive inhibition of recombinant human DOT1L using adenosine/deazaadenosine as substrate and SAM cofactor |
CHEMBL3085656 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 |
Inhibition |
|
|
% |
Inhibition of N-terminal GST-tagged recombinant human Histone-lysine N-methyltransferase G9a using S-(5'-adenosyl)-L-methionine chloride as substrate assessed as nonspecific denaturation of enzyme at 0.05 to 25 uM preincubated for 30 mins in presence of urea and DTT |
CHEMBL3124916 |
| Catechol O-methyltransferase |
Inhibition |
= |
39.0 |
% |
Inhibition of Sprague-Dawley rat liver COMT at 0.2 mM by radiochemical technique |
CHEMBL3244179 |
| Phenylethanolamine N-methyltransferase |
Inhibition |
= |
49.0 |
% |
Inhibition of bovine adrenal medulla PNMT at 0.2 mM by radiochemical technique |
CHEMBL3244179 |
| Histamine N-methyltransferase |
Inhibition |
= |
40.0 |
% |
Inhibition of guinea pig HMT at 0.2 mM by radiochemical technique |
CHEMBL3244179 |
| Acetylserotonin O-methyltransferase |
Inhibition |
= |
71.0 |
% |
Inhibition of bovine pineal gland HIOMT at 0.2 mM by radiochemical technique |
CHEMBL3244179 |
| Catechol O-methyltransferase |
Inhibition |
= |
87.0 |
% |
Inhibition of Sprague-Dawley rat liver COMT at 2 mM by radiochemical technique |
CHEMBL3244179 |
| Phenylethanolamine N-methyltransferase |
Inhibition |
= |
92.0 |
% |
Inhibition of bovine adrenal medulla PNMT at 2 mM by radiochemical technique |
CHEMBL3244179 |
| Histamine N-methyltransferase |
Inhibition |
= |
89.0 |
% |
Inhibition of guinea pig HMT at 2 mM by radiochemical technique |
CHEMBL3244179 |
| Acetylserotonin O-methyltransferase |
Inhibition |
= |
94.0 |
% |
Inhibition of bovine pineal gland HIOMT at 2 mM by radiochemical technique |
CHEMBL3244179 |
| No relevant target |
Rf |
= |
0.73 |
|
Retardation factor, Rf of the compound on silica gel GF containing 5% Na2HPO4 by chromatography |
CHEMBL3244179 |
| No relevant target |
Rf |
= |
0.73 |
|
Retardation factor, Rf of the compound on silica gel GF containing EtOH-HOAc-H2O (20:2:2)/0.1 M phosphate buffer at 7.4 by chromatography |
CHEMBL3244179 |
| Catechol O-methyltransferase |
Inhibition |
= |
5.0 |
% |
Inhibition of Sprague-Dawley rat liver COMT at 0.2 mM by radiochemical technique |
CHEMBL3244179 |
| Phenylethanolamine N-methyltransferase |
Inhibition |
= |
14.0 |
% |
Inhibition of bovine adrenal medulla PNMT at 0.2 mM by radiochemical technique |
CHEMBL3244179 |
| Histamine N-methyltransferase |
Inhibition |
= |
73.0 |
% |
Inhibition of guinea pig HMT at 0.2 mM by radiochemical technique |
CHEMBL3244179 |
| Acetylserotonin O-methyltransferase |
Inhibition |
= |
1.0 |
% |
Inhibition of bovine pineal gland HIOMT at 0.2 mM by radiochemical technique |
CHEMBL3244179 |
| Catechol O-methyltransferase |
Inhibition |
= |
22.0 |
% |
Inhibition of Sprague-Dawley rat liver COMT at 2 mM by radiochemical technique |
CHEMBL3244179 |
| Phenylethanolamine N-methyltransferase |
Inhibition |
= |
32.0 |
% |
Inhibition of bovine adrenal medulla PNMT at 2 mM by radiochemical technique |
CHEMBL3244179 |
| Histamine N-methyltransferase |
Inhibition |
= |
99.0 |
% |
Inhibition of guinea pig HMT at 2 mM by radiochemical technique |
CHEMBL3244179 |
| Acetylserotonin O-methyltransferase |
Inhibition |
= |
6.0 |
% |
Inhibition of bovine pineal gland HIOMT at 2 mM by radiochemical technique |
CHEMBL3244179 |
| No relevant target |
Rf |
= |
0.73 |
|
Retardation factor, Rf of the compound on silica gel GF containing 5% Na2HPO4 by chromatography |
CHEMBL3244179 |
| No relevant target |
Rf |
= |
0.73 |
|
Retardation factor, Rf of the compound on silica gel GF containing EtOH-HOAc-H2O (20:2:2)/0.1 M phosphate buffer at 7.4 by chromatography |
CHEMBL3244179 |
| Catechol O-methyltransferase |
Inhibition |
= |
24.0 |
% |
Inhibition of catechol O-methyltransferase (unknown origin) using 1 mM SAM as substrate at 0.1 mM |
CHEMBL3272009 |
| Catechol O-methyltransferase |
Inhibition |
= |
33.0 |
% |
Inhibition of catechol O-methyltransferase (unknown origin) using 1 mM SAM as substrate at 0.2 mM |
CHEMBL3272009 |
| Catechol O-methyltransferase |
Inhibition |
= |
64.0 |
% |
Inhibition of catechol O-methyltransferase (unknown origin) using 1 mM SAM as substrate at 0.6 mM |
CHEMBL3272009 |
| Unchecked |
Inhibition |
= |
77.0 |
% |
Inhibition of tRNA-methyltransferase (unknown origin) using 0.1 mM SAM and 40 ug tRNA as substrate at 0.1 mM |
CHEMBL3272009 |
| Unchecked |
Inhibition |
= |
83.0 |
% |
Inhibition of tRNA-methyltransferase (unknown origin) using 0.1 mM SAM and 40 ug tRNA as substrate at 0.2 mM |
CHEMBL3272009 |
| Unchecked |
Ki |
= |
25000.0 |
nM |
Inhibition of tRNA-methyltransferase (unknown origin) using 0.1 mM SAM and 40 ug tRNA as substrate by Dixon plot analysis |
CHEMBL3272009 |
| Catechol O-methyltransferase |
Kis |
= |
36.3 |
uM |
Inhibition of Sprague-Dawley rat liver catechol O-methyltransferase using 24 to 210 uM S-adenosylmethionine substrate |
CHEMBL3272184 |
| Phenylethanolamine N-methyltransferase |
Kis |
= |
29.0 |
uM |
Inhibition of bovine adrenal medulla phenylethanolamine N-methyltransferase using 24 to 210 uM S-adenosylmethionine substrate |
CHEMBL3272184 |
| Histamine N-methyltransferase |
Kis |
= |
18.1 |
uM |
Inhibition of guinea pig brain histamine N-methyltransferase using 24 to 210 uM S-adenosylmethionine substrate |
CHEMBL3272184 |
| Acetylserotonin O-methyltransferase |
Kis |
= |
18.5 |
uM |
Inhibition of bovine pineal gland hydroxyindole O-methyltransferase using 24 to 210 uM S-adenosylmethionine substrate |
CHEMBL3272184 |
| DNA (cytosine-5)-methyltransferase 1 |
Inhibition |
|
|
% |
Inhibition of N-terminal His6-tagged mouse DNMT1 (731 to 1602 residues) at 200 uM expressed in Escherichia coli BL21 (DE3) incubated for 2 hrs using S-adenosylmethionine by ELISA |
CHEMBL3351464 |
| N-lysine methyltransferase SMYD2 |
IC50 |
= |
180.0 |
nM |
Inhibition of SMYD2 (unknown origin) by HMT assay |
CHEMBL3396964 |
| Histone-lysine N-methyltransferase SUV420H2 |
IC50 |
= |
10000.0 |
nM |
Inhibition of SUV420H2 (unknown origin) by HMT assay |
CHEMBL3396964 |
| Histone-lysine N-methyltransferase SUV39H2 |
IC50 |
= |
32000.0 |
nM |
Inhibition of SUV39H2 (unknown origin) by HMT assay |
CHEMBL3396964 |
| Histone-lysine N-methyltransferase SUV39H1 |
IC50 |
= |
1200.0 |
nM |
Inhibition of SUV39H1 (unknown origin) by HMT assay |
CHEMBL3396964 |
| Histone-lysine N-methyltransferase SETDB1 |
IC50 |
= |
2200.0 |
nM |
Inhibition of SETDB1 (unknown origin) by HMT assay |
CHEMBL3396964 |
| Histone-lysine N-methyltransferase SETD7 |
IC50 |
= |
30000.0 |
nM |
Inhibition of SETD7 (unknown origin) by HMT assay |
CHEMBL3396964 |
| Histone-lysine N-methyltransferase MLL |
IC50 |
= |
2300.0 |
nM |
Inhibition of MLL (unknown origin) by HMT assay |
CHEMBL3396964 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 |
IC50 |
= |
230.0 |
nM |
Inhibition of EHMT1 (unknown origin) by HMT assay |
CHEMBL3396964 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 |
IC50 |
= |
2000.0 |
nM |
Inhibition of G9a (unknown origin) by HMT assay |
CHEMBL3396964 |
| Histone-lysine N-methyltransferase EZH1 |
IC50 |
= |
6400.0 |
nM |
Inhibition of EZH1 (unknown origin) by HMT assay |
CHEMBL3396964 |
| Histone-lysine N-methyltransferase EZH2 |
Inhibition |
|
|
% |
Inhibition of EZH2 (unknown origin) at 100 uM by cell-based assay |
CHEMBL3396964 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
11000.0 |
nM |
Inhibition of N-terminally FLAG-tagged wild type EZH2 in EZH2/SUZ12/EED/RbAp48 complex (unknown origin) expressed in baculovirus infected in SF9 cells assessed as inhibition of methylation of nucleosomes at H3K27 by scintillation counting in presence of [3H]SAM |
CHEMBL3396964 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
1900.0 |
nM |
Inhibition of N-terminally FLAG-tagged EZH2 Y641N mutant in EZH2/SUZ12/EED/RbAp48 complex (unknown origin) expressed in baculovirus infected in SF9 cells assessed as inhibition of methylation of nucleosomes at H3K27 by scintillation counting in presence of [3H]SAM |
CHEMBL3396964 |
| Protein-arginine N-methyltransferase 1 |
IC50 |
= |
420.0 |
nM |
Displacement of [3H]-SAM from recombinant His6-tagged PRMT1 (unknown origin) expressed in Escherichia coli BL21(DE3) incubated for 5 mins prior to H4(1 to 20)-BTN peptide addition measured after 8 mins by scintillation proximity assay |
CHEMBL3407369 |
| Protein arginine N-methyltransferase 5 |
IC50 |
> |
50000.0 |
nM |
Inhibition of human full length PRMT5 expressed in Sf9 cells |
CHEMBL3576805 |
| Protein arginine N-methyltransferase 7 |
IC50 |
> |
50000.0 |
nM |
Inhibition of human full length PRMT7 expressed in Sf9 cells |
CHEMBL3576805 |
| DNA (cytosine-5)-methyltransferase 3A |
IC50 |
> |
50000.0 |
nM |
Inhibition of human full length DNMT3A expressed in Sf9 cells |
CHEMBL3576805 |
| DNA (cytosine-5)-methyltransferase 3B |
IC50 |
> |
50000.0 |
nM |
Inhibition of human full length DNMT3B expressed in Sf9 cells |
CHEMBL3576805 |
| Protein-arginine N-methyltransferase 1 |
IC50 |
= |
500.0 |
nM |
Inhibition of PRMT1 (unknown origin) using biotinylated histone H4-derived peptide as substrate after 60 mins by AlphaLISA assay |
CHEMBL3632463 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
467.0 |
nM |
Inhibition Assay: Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibition standard) was 100 μM final concentration of SAH and negative control (0% inhibition standard) contained 1 μL of DMSO. Compound 75 was then incubated for 30 minutes with 40 μL per well of EZH2 wild-type and mutants at 8 nM in pH 7.6 assay buffer (20 mM BICINE, 100 mM KCl, 1 mM DTT, 0.002% Tween 20, 0.005% BSG). A substrate mix at 10 μL per well was added which contained 5-adenosylmethionine-Cl (SAM) at 150 nM and tritiated SAM at 100 nM, and biotinylated oligonucleosome at 150 nM in pH 7.6 assay buffer. Quenched enzyme reaction was transferred to a streptavidin-coated Flashplate (Perkin Elmer, catalog number SMP410), allowed to bind for one hour, and detected on a TopCount NXT HTS (Perkin Elmer). |
CHEMBL3638524 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
263.0 |
nM |
Inhibition Assay: Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibition standard) was 100 μM final concentration of SAH and negative control (0% inhibition standard) contained 1 μL of DMSO. Compound 75 was then incubated for 30 minutes with 40 μL per well of EZH2 wild-type and mutants at 8 nM in pH 7.6 assay buffer (20 mM BICINE, 100 mM KCl, 1 mM DTT, 0.002% Tween 20, 0.005% BSG). A substrate mix at 10 μL per well was added which contained 5-adenosylmethionine-Cl (SAM) at 150 nM and tritiated SAM at 100 nM, and biotinylated oligonucleosome at 150 nM in pH 7.6 assay buffer. Quenched enzyme reaction was transferred to a streptavidin-coated Flashplate (Perkin Elmer, catalog number SMP410), allowed to bind for one hour, and detected on a TopCount NXT HTS (Perkin Elmer). |
CHEMBL3638524 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
283.0 |
nM |
Inhibition Assay: Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibition standard) was 100 μM final concentration of SAH and negative control (0% inhibition standard) contained 1 μL of DMSO. Compound 75 was then incubated for 30 minutes with 40 μL per well of EZH2 wild-type and mutants at 8 nM in pH 7.6 assay buffer (20 mM BICINE, 100 mM KCl, 1 mM DTT, 0.002% Tween 20, 0.005% BSG). A substrate mix at 10 μL per well was added which contained 5-adenosylmethionine-Cl (SAM) at 150 nM and tritiated SAM at 100 nM, and biotinylated oligonucleosome at 150 nM in pH 7.6 assay buffer. Quenched enzyme reaction was transferred to a streptavidin-coated Flashplate (Perkin Elmer, catalog number SMP410), allowed to bind for one hour, and detected on a TopCount NXT HTS (Perkin Elmer). |
CHEMBL3638524 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
380.0 |
nM |
Inhibition Assay: Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibition standard) was 100 μM final concentration of SAH and negative control (0% inhibition standard) contained 1 μL of DMSO. Compound 75 was then incubated for 30 minutes with 40 μL per well of EZH2 wild-type and mutants at 8 nM in pH 7.6 assay buffer (20 mM BICINE, 100 mM KCl, 1 mM DTT, 0.002% Tween 20, 0.005% BSG). A substrate mix at 10 μL per well was added which contained 5-adenosylmethionine-Cl (SAM) at 150 nM and tritiated SAM at 100 nM, and biotinylated oligonucleosome at 150 nM in pH 7.6 assay buffer. Quenched enzyme reaction was transferred to a streptavidin-coated Flashplate (Perkin Elmer, catalog number SMP410), allowed to bind for one hour, and detected on a TopCount NXT HTS (Perkin Elmer). |
CHEMBL3638524 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
4800.0 |
nM |
Inhibition Assay: Compound 75 was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibition standard) was 100 μM final concentration of SAH and negative control (0% inhibition standard) contained 1 μL of DMSO. Compound 75 was then incubated for 30 minutes with 40 μL per well of EZH2 wild-type and mutants at 8 nM in pH 7.6 assay buffer (20 mM BICINE, 100 mM KCl, 1 mM DTT, 0.002% Tween 20, 0.005% BSG). A substrate mix at 10 μL per well was added which contained 5-adenosylmethionine-Cl (SAM) at 150 nM and tritiated SAM at 100 nM, and biotinylated oligonucleosome at 150 nM in pH 7.6 assay buffer. Quenched enzyme reaction was transferred to a streptavidin-coated Flashplate (Perkin Elmer, catalog number SMP410), allowed to bind for one hour, and detected on a TopCount NXT HTS (Perkin Elmer). |
CHEMBL3638524 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
467.0 |
nM |
Inhibition Assay: S-Adenosyl-L-homocysteine (SAH) was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibition standard) was 100 μM final concentration of SAH and negative control (0% inhibition standard) contained 1 μL of DMSO. SAH was then incubated for 30 minutes with 40 μL per well of EZH2 wild-type and mutants at 8 nM in pH 7.6 assay buffer (20 mM BICINE, 100 mM KCl, 1 mM DTT, 0.002% TWEEN® 20 (generic: polvsorbate 20), 0.005% BSG). A substrate mix at 10 μL per well was added which contained S-adenosylmethionine-Cl (SAM) at 150 nM and tritiated SAM at 100 nM, and biotinylated oligonucleosome at 150 nM in pH 7.6 assay buffer. Quenched enzyme reaction was transferred to a streptavidin-coated FLASHPLATE™ (Perkin Elmer, catalog number SMP410), allowed to bind for one hour, and detected on a TOPCOUNT NXT HTS (Perkin Elmer). |
CHEMBL3886332 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
263.0 |
nM |
Inhibition Assay: S-Adenosyl-L-homocysteine (SAH) was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibition standard) was 100 μM final concentration of SAH and negative control (0% inhibition standard) contained 1 μL of DMSO. SAH was then incubated for 30 minutes with 40 μL per well of EZH2 wild-type and mutants at 8 nM in pH 7.6 assay buffer (20 mM BICINE, 100 mM KCl, 1 mM DTT, 0.002% TWEEN® 20 (generic: polvsorbate 20), 0.005% BSG). A substrate mix at 10 μL per well was added which contained S-adenosylmethionine-Cl (SAM) at 150 nM and tritiated SAM at 100 nM, and biotinylated oligonucleosome at 150 nM in pH 7.6 assay buffer. Quenched enzyme reaction was transferred to a streptavidin-coated FLASHPLATE™ (Perkin Elmer, catalog number SMP410), allowed to bind for one hour, and detected on a TOPCOUNT NXT HTS (Perkin Elmer). |
CHEMBL3886332 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
283.0 |
nM |
Inhibition Assay: S-Adenosyl-L-homocysteine (SAH) was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibition standard) was 100 μM final concentration of SAH and negative control (0% inhibition standard) contained 1 μL of DMSO. SAH was then incubated for 30 minutes with 40 μL per well of EZH2 wild-type and mutants at 8 nM in pH 7.6 assay buffer (20 mM BICINE, 100 mM KCl, 1 mM DTT, 0.002% TWEEN® 20 (generic: polvsorbate 20), 0.005% BSG). A substrate mix at 10 μL per well was added which contained S-adenosylmethionine-Cl (SAM) at 150 nM and tritiated SAM at 100 nM, and biotinylated oligonucleosome at 150 nM in pH 7.6 assay buffer. Quenched enzyme reaction was transferred to a streptavidin-coated FLASHPLATE™ (Perkin Elmer, catalog number SMP410), allowed to bind for one hour, and detected on a TOPCOUNT NXT HTS (Perkin Elmer). |
CHEMBL3886332 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
380.0 |
nM |
Inhibition Assay: S-Adenosyl-L-homocysteine (SAH) was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibition standard) was 100 μM final concentration of SAH and negative control (0% inhibition standard) contained 1 μL of DMSO. SAH was then incubated for 30 minutes with 40 μL per well of EZH2 wild-type and mutants at 8 nM in pH 7.6 assay buffer (20 mM BICINE, 100 mM KCl, 1 mM DTT, 0.002% TWEEN® 20 (generic: polvsorbate 20), 0.005% BSG). A substrate mix at 10 μL per well was added which contained S-adenosylmethionine-Cl (SAM) at 150 nM and tritiated SAM at 100 nM, and biotinylated oligonucleosome at 150 nM in pH 7.6 assay buffer. Quenched enzyme reaction was transferred to a streptavidin-coated FLASHPLATE™ (Perkin Elmer, catalog number SMP410), allowed to bind for one hour, and detected on a TOPCOUNT NXT HTS (Perkin Elmer). |
CHEMBL3886332 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
4800.0 |
nM |
Inhibition Assay: S-Adenosyl-L-homocysteine (SAH) was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibition standard) was 100 μM final concentration of SAH and negative control (0% inhibition standard) contained 1 μL of DMSO. SAH was then incubated for 30 minutes with 40 μL per well of EZH2 wild-type and mutants at 8 nM in pH 7.6 assay buffer (20 mM BICINE, 100 mM KCl, 1 mM DTT, 0.002% TWEEN® 20 (generic: polvsorbate 20), 0.005% BSG). A substrate mix at 10 μL per well was added which contained S-adenosylmethionine-Cl (SAM) at 150 nM and tritiated SAM at 100 nM, and biotinylated oligonucleosome at 150 nM in pH 7.6 assay buffer. Quenched enzyme reaction was transferred to a streptavidin-coated FLASHPLATE™ (Perkin Elmer, catalog number SMP410), allowed to bind for one hour, and detected on a TOPCOUNT NXT HTS (Perkin Elmer). |
CHEMBL3886332 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
6908.2 |
nM |
Inhibition Assay: Test compounds were serially diluted 3-fold in DMSO in a 10 point-curve and 1 uL was spotted into a 384-well microplate in duplicate using a Platemate Plus equipped with 384-channel head (Thermo Scientific). The final top concentration of test compounds in the assay was 10 uM. Positive control (100% inhibition standard) was 1 mM final concentration of SAH and negative control (0% inhibition standard) contained 1 uL of DMSO. Test compounds were then incubated for 30 minutes with 40 uL per well of wild-type EZH2 (final concentration was 4 nM), Y641F EZH2 (final concentration was 0.1 nM) and A677G and A687V EZH2 (for each, final concentration was 2nM) and peptide in 1x assay buffer (20 mM BICINE pH =7.6, 1 mM DTT, 0.002% TWEEN 20 (generic: polysorbate 20), 0.005% BSG). For the wild-type EZH2 and A677G EZH2 assays, biotinylated peptide H3:21-44 with unmethylated K27 was present at a final concentration of 200 nM, while in the A687V EZH2 assay, biotinylated peptide H3. |
CHEMBL3886332 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
16619.3 |
nM |
Inhibition Assay: Test compounds were serially diluted 3-fold in DMSO in a 10 point-curve and 1 uL was spotted into a 384-well microplate in duplicate using a Platemate Plus equipped with 384-channel head (Thermo Scientific). The final top concentration of test compounds in the assay was 10 uM. Positive control (100% inhibition standard) was 1 mM final concentration of SAH and negative control (0% inhibition standard) contained 1 uL of DMSO. Test compounds were then incubated for 30 minutes with 40 uL per well of wild-type EZH2 (final concentration was 4 nM), Y641F EZH2 (final concentration was 0.1 nM) and A677G and A687V EZH2 (for each, final concentration was 2nM) and peptide in 1x assay buffer (20 mM BICINE pH =7.6, 1 mM DTT, 0.002% TWEEN 20 (generic: polysorbate 20), 0.005% BSG). For the wild-type EZH2 and A677G EZH2 assays, biotinylated peptide H3:21-44 with unmethylated K27 was present at a final concentration of 200 nM, while in the A687V EZH2 assay, biotinylated peptide H3. |
CHEMBL3886332 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
6237.9 |
nM |
Inhibition Assay: Test compounds were serially diluted 3-fold in DMSO in a 10 point-curve and 1 uL was spotted into a 384-well microplate in duplicate using a Platemate Plus equipped with 384-channel head (Thermo Scientific). The final top concentration of test compounds in the assay was 10 uM. Positive control (100% inhibition standard) was 1 mM final concentration of SAH and negative control (0% inhibition standard) contained 1 uL of DMSO. Test compounds were then incubated for 30 minutes with 40 uL per well of wild-type EZH2 (final concentration was 4 nM), Y641F EZH2 (final concentration was 0.1 nM) and A677G and A687V EZH2 (for each, final concentration was 2nM) and peptide in 1x assay buffer (20 mM BICINE pH =7.6, 1 mM DTT, 0.002% TWEEN 20 (generic: polysorbate 20), 0.005% BSG). For the wild-type EZH2 and A677G EZH2 assays, biotinylated peptide H3:21-44 with unmethylated K27 was present at a final concentration of 200 nM, while in the A687V EZH2 assay, biotinylated peptide H3. |
CHEMBL3886332 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
5903.4 |
nM |
Inhibition Assay: Test compounds were serially diluted 3-fold in DMSO in a 10 point-curve and 1 uL was spotted into a 384-well microplate in duplicate using a Platemate Plus equipped with 384-channel head (Thermo Scientific). The final top concentration of test compounds in the assay was 10 uM. Positive control (100% inhibition standard) was 1 mM final concentration of SAH and negative control (0% inhibition standard) contained 1 uL of DMSO. Test compounds were then incubated for 30 minutes with 40 uL per well of wild-type EZH2 (final concentration was 4 nM), Y641F EZH2 (final concentration was 0.1 nM) and A677G and A687V EZH2 (for each, final concentration was 2nM) and peptide in 1x assay buffer (20 mM BICINE pH =7.6, 1 mM DTT, 0.002% TWEEN 20 (generic: polysorbate 20), 0.005% BSG). For the wild-type EZH2 and A677G EZH2 assays, biotinylated peptide H3:21-44 with unmethylated K27 was present at a final concentration of 200 nM, while in the A687V EZH2 assay, biotinylated peptide H3. |
CHEMBL3886332 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
467.0 |
nM |
Inhibition Assay: S-Adenosyl-L-homocysteine (SAH) was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibition standard) was 100 μM final concentration of SAH and negative control (0% inhibition standard) contained 1 μL of DMSO. SAH was then incubated for 30 minutes with 40 μL per well of EZH2 wild-type and mutants at 8 nM in pH 7.6 assay buffer (20 mM BICINE, 100 mM KCl, 1 mM DTT, 0.002% Tween 20, 0.005% BSG). A substrate mix at 10 μL per well was added which contained S-adenosylmethionine-Cl (SAM) at 150 nM and tritiated SAM at 100 nM, and biotinylated oligonucleosome at 150 nM in pH 7.6 assay buffer. Quenched enzyme reaction was transferred to a streptavidin-coated Flashplate (Perkin Elmer, catalog number SMP410), allowed to bind for one hour, and detected on a TopCount NXT HTS (Perkin Elmer). |
CHEMBL3886691 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
263.0 |
nM |
Inhibition Assay: S-Adenosyl-L-homocysteine (SAH) was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibition standard) was 100 μM final concentration of SAH and negative control (0% inhibition standard) contained 1 μL of DMSO. SAH was then incubated for 30 minutes with 40 μL per well of EZH2 wild-type and mutants at 8 nM in pH 7.6 assay buffer (20 mM BICINE, 100 mM KCl, 1 mM DTT, 0.002% Tween 20, 0.005% BSG). A substrate mix at 10 μL per well was added which contained S-adenosylmethionine-Cl (SAM) at 150 nM and tritiated SAM at 100 nM, and biotinylated oligonucleosome at 150 nM in pH 7.6 assay buffer. Quenched enzyme reaction was transferred to a streptavidin-coated Flashplate (Perkin Elmer, catalog number SMP410), allowed to bind for one hour, and detected on a TopCount NXT HTS (Perkin Elmer). |
CHEMBL3886691 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
283.0 |
nM |
Inhibition Assay: S-Adenosyl-L-homocysteine (SAH) was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibition standard) was 100 μM final concentration of SAH and negative control (0% inhibition standard) contained 1 μL of DMSO. SAH was then incubated for 30 minutes with 40 μL per well of EZH2 wild-type and mutants at 8 nM in pH 7.6 assay buffer (20 mM BICINE, 100 mM KCl, 1 mM DTT, 0.002% Tween 20, 0.005% BSG). A substrate mix at 10 μL per well was added which contained S-adenosylmethionine-Cl (SAM) at 150 nM and tritiated SAM at 100 nM, and biotinylated oligonucleosome at 150 nM in pH 7.6 assay buffer. Quenched enzyme reaction was transferred to a streptavidin-coated Flashplate (Perkin Elmer, catalog number SMP410), allowed to bind for one hour, and detected on a TopCount NXT HTS (Perkin Elmer). |
CHEMBL3886691 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
380.0 |
nM |
Inhibition Assay: S-Adenosyl-L-homocysteine (SAH) was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibition standard) was 100 μM final concentration of SAH and negative control (0% inhibition standard) contained 1 μL of DMSO. SAH was then incubated for 30 minutes with 40 μL per well of EZH2 wild-type and mutants at 8 nM in pH 7.6 assay buffer (20 mM BICINE, 100 mM KCl, 1 mM DTT, 0.002% Tween 20, 0.005% BSG). A substrate mix at 10 μL per well was added which contained S-adenosylmethionine-Cl (SAM) at 150 nM and tritiated SAM at 100 nM, and biotinylated oligonucleosome at 150 nM in pH 7.6 assay buffer. Quenched enzyme reaction was transferred to a streptavidin-coated Flashplate (Perkin Elmer, catalog number SMP410), allowed to bind for one hour, and detected on a TopCount NXT HTS (Perkin Elmer). |
CHEMBL3886691 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
4800.0 |
nM |
Inhibition Assay: S-Adenosyl-L-homocysteine (SAH) was serially diluted 3 fold in DMSO for 10 points and 1 μL was plated in a 384 well microtiter plate. Positive control (100% inhibition standard) was 100 μM final concentration of SAH and negative control (0% inhibition standard) contained 1 μL of DMSO. SAH was then incubated for 30 minutes with 40 μL per well of EZH2 wild-type and mutants at 8 nM in pH 7.6 assay buffer (20 mM BICINE, 100 mM KCl, 1 mM DTT, 0.002% Tween 20, 0.005% BSG). A substrate mix at 10 μL per well was added which contained S-adenosylmethionine-Cl (SAM) at 150 nM and tritiated SAM at 100 nM, and biotinylated oligonucleosome at 150 nM in pH 7.6 assay buffer. Quenched enzyme reaction was transferred to a streptavidin-coated Flashplate (Perkin Elmer, catalog number SMP410), allowed to bind for one hour, and detected on a TopCount NXT HTS (Perkin Elmer). |
CHEMBL3886691 |
| Protein-arginine N-methyltransferase 1 |
Inhibition |
= |
90.0 |
% |
Inhibition of recombinant human N-terminal GST-tagged PRMT1 (2 to end residues) expressed in baculovirus infected Sf9 insect cells at 9 uM using biotinylated histone H4 peptide as substrate preincubated for 15 mins followed by substrate/[3H]-SAM addition measured after 60 mins by microbeta liquid scintillation counting analysis |
CHEMBL4043236 |
| Protein-arginine N-methyltransferase 1 |
IC50 |
= |
550.0 |
nM |
Inhibition of recombinant human N-terminal GST-tagged PRMT1 (2 to end residues) expressed in baculovirus infected Sf9 insect cells using biotinylated histone H4 peptide as substrate preincubated for 15 mins followed by substrate/[3H]-SAM addition measured after 60 mins by microbeta liquid scintillation counting analysis |
CHEMBL4043236 |
| PRMT5/MEP50 complex |
IC50 |
= |
600.0 |
nM |
Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (2 to end residues) /human N-terminal His-tagged MEP50 (2 to end residues) expressed in HEK293F cells using substrate pretreated for 15 mins followed by substrate and [3H]-SAM addition measured after 60 mins by scintillation proximity assay |
CHEMBL4118120 |
| 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 |
= |
35300.0 |
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 |
| Histone-lysine N-methyltransferase, H3 lysine-79 specific |
Ki |
= |
270.0 |
nM |
Inhibition of DOT1-like Histone H3 Methyltransferase (unknown origin) |
CHEMBL4321790 |
| PRMT5/MEP50 complex |
IC50 |
= |
560.0 |
nM |
Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (2 to end residues) /human N-terminal His-tagged MEP50 (2 to end residues) expressed in HEK293F cells pretreated for 15 mins followed by substrate and [3H]-SAM addition measured after 60 mins by scintillation proximity assay |
CHEMBL4325864 |
| tRNA (guanine-N(1)-)-methyltransferase |
Kd |
= |
5900.0 |
nM |
Binding affinity to Pseudomonas aeruginosa tRNA (guanine(37)-N1)-methyltransferase (Leu5 to Asp25 residues) expressed in Escherichia coli BL21 (DE3) Rosetta T1R cells by surface plasmon resonance assay |
CHEMBL4373727 |
| tRNA (guanine-N(1)-)-methyltransferase |
Kd |
= |
10100.0 |
nM |
Binding affinity to full length Mycobacterium tuberculosis tRNA (guanine(37)-N1)-methyltransferase expressed in Escherichia coli BL21 (DE3) by surface plasmon resonance assay |
CHEMBL4373727 |
| tRNA (guanine-N(1)-)-methyltransferase |
Kd |
= |
3300.0 |
nM |
Binding affinity to full length Staphylococcus aureus tRNA (guanine(37)-N1)-methyltransferase expressed in Escherichia coli BL21 (DE3) by surface plasmon resonance assay |
CHEMBL4373727 |
| tRNA (guanine-N(1)-)-methyltransferase |
Ka |
= |
55500.0 |
/M/s |
Binding affinity to Pseudomonas aeruginosa tRNA (guanine(37)-N1)-methyltransferase (Leu5 to Asp25 residues) expressed in Escherichia coli BL21 (DE3) Rosetta T1R cells assessed as association rate constant by surface plasmon resonance assay |
CHEMBL4373727 |
| tRNA (guanine-N(1)-)-methyltransferase |
Ka |
= |
7700.0 |
/M/s |
Binding affinity to full length Mycobacterium tuberculosis tRNA (guanine(37)-N1)-methyltransferase expressed in Escherichia coli BL21 (DE3) assessed as association rate constant by surface plasmon resonance assay |
CHEMBL4373727 |
| tRNA (guanine-N(1)-)-methyltransferase |
Ka |
= |
279000.0 |
/M/s |
Binding affinity to full length Staphylococcus aureus tRNA (guanine(37)-N1)-methyltransferase expressed in Escherichia coli BL21 (DE3) assessed as association rate constant by surface plasmon resonance assay |
CHEMBL4373727 |
| tRNA (guanine-N(1)-)-methyltransferase |
Kdiss |
= |
0.326 |
/s |
Binding affinity to Pseudomonas aeruginosa tRNA (guanine(37)-N1)-methyltransferase (Leu5 to Asp25 residues) expressed in Escherichia coli BL21 (DE3) Rosetta T1R cells assessed as dissociation rate constant by surface plasmon resonance assay |
CHEMBL4373727 |
| tRNA (guanine-N(1)-)-methyltransferase |
Kdiss |
= |
0.0775 |
/s |
Binding affinity to full length Mycobacterium tuberculosis tRNA (guanine(37)-N1)-methyltransferase expressed in Escherichia coli BL21 (DE3) assessed as dissociation rate constant by surface plasmon resonance assay |
CHEMBL4373727 |
| tRNA (guanine-N(1)-)-methyltransferase |
Kdiss |
= |
0.92 |
/s |
Binding affinity to full length Staphylococcus aureus tRNA (guanine(37)-N1)-methyltransferase expressed in Escherichia coli BL21 (DE3) assessed as dissociation rate constant by surface plasmon resonance assay |
CHEMBL4373727 |
| tRNA (guanine-N(1)-)-methyltransferase |
Delta Tm |
= |
4.0 |
degrees C |
Binding affinity to Pseudomonas aeruginosa tRNA (guanine(37)-N1)-methyltransferase (Leu5 to Asp25 residues) expressed in Escherichia coli BL21 (DE3) Rosetta T1R cells assessed as thermal stabilization of protein by measuring change in melting temperature at 2 mM by SYPRO orange based thermal shift assay |
CHEMBL4373727 |
| tRNA (guanine-N(1)-)-methyltransferase |
Tm |
= |
62.0 |
degrees C |
Binding affinity to Pseudomonas aeruginosa tRNA (guanine(37)-N1)-methyltransferase (Leu5 to Asp25 residues) expressed in Escherichia coli BL21 (DE3) Rosetta T1R cells assessed as thermal stabilization of protein by measuring melting temperature at 2 mM by SYPRO orange based thermal shift assay (Rvb = 50 degreeC) |
CHEMBL4373727 |
| tRNA (guanine-N(1)-)-methyltransferase |
Tm |
= |
57.0 |
degrees C |
Binding affinity to full length Mycobacterium tuberculosis tRNA (guanine(37)-N1)-methyltransferase expressed in Escherichia coli BL21 (DE3) assessed as thermal stabilization of protein by measuring melting temperature at 2 mM by SYPRO orange based thermal shift assay (Rvb = 54 degreeC) |
CHEMBL4373727 |
| DNA (cytosine-5)-methyltransferase 1 |
IC50 |
= |
600.0 |
nM |
Inhibition of DNMT1 (unknown origin) using biotinylated substrate using [3H]-SAM after 1 hr by scintillation proximity assay |
CHEMBL4422660 |
| DNMT3A2/3L complex |
Activity |
= |
20.0 |
% |
Binding affinity to DNMT3A/3L (unknown origin) assessed as active protein binding by SPR assay |
CHEMBL4422660 |
| Unchecked |
IC50 |
= |
1770.0 |
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 |
= |
490.0 |
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 |
| Histone-lysine N-methyltransferase, H3 lysine-79 specific |
IC50 |
= |
220.0 |
nM |
Inhibition of human recombinant DOT1L (1 to 420 amino acids) expressed in Escherichia coli |
CHEMBL4477246 |
| DNA (cytosine-5)-methyltransferase 1 |
IC50 |
= |
200.0 |
nM |
Inhibition of DNMT1 (unknown origin) |
CHEMBL4477246 |
| Protein arginine N-methyltransferase 3 |
IC50 |
= |
2000.0 |
nM |
Inhibition of PRMT3 (unknown origin) |
CHEMBL4477246 |
| Protein arginine N-methyltransferase 5 |
IC50 |
= |
200.0 |
nM |
Inhibition of PRMT5 (unknown origin) |
CHEMBL4477246 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 |
IC50 |
= |
4100.0 |
nM |
Inhibition of G9a (unknown origin) |
CHEMBL4477246 |
| Histone-lysine N-methyltransferase SETD7 |
IC50 |
= |
47000.0 |
nM |
Inhibition of SETD7 (unknown origin) |
CHEMBL4477246 |
| Histone-lysine N-methyltransferase SUV39H2 |
IC50 |
= |
22000.0 |
nM |
Inhibition of SUV39H2 (unknown origin) |
CHEMBL4477246 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
65000.0 |
nM |
Inhibition of EZH2 (unknown origin) |
CHEMBL4477246 |
| Replicase polyprotein 1ab |
Inhibition |
= |
20.82 |
% |
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate |
CHEMBL4495564 |
| SARS-CoV-2 |
Inhibition |
= |
-0.22 |
% |
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 |
| MLL1-ASH2L/RbBP5/WDR5/DPY30 |
IC50 |
= |
724.0 |
nM |
Inhibition of recombinant human MLL1 complex (MLL1/Ash2L/RbBP5/WDR5/DPY-30) expressed in Escherichia coli Rosetta 2 (DE3) cells using H3 (1 to 21) peptide as substrate incubated for 1 hr in presence of 3[H] SAM by AlphaLISA assay |
CHEMBL4616718 |
| SARS-CoV-2 |
Inhibition |
= |
-0.22 |
% |
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 |
| DNA (cytosine-5)-methyltransferase 1 |
IC50 |
= |
71.0 |
nM |
Inhibition of recombinant human DNMT1 using poly(dl-dC) as substrate by hotspot assay |
CHEMBL4680176 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
22600.0 |
nM |
Inhibition of recombinant human EZH2 using core histone as substrate by hotspot assay |
CHEMBL4680176 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 |
IC50 |
= |
1820.0 |
nM |
Inhibition of recombinant human G9a using histone H3 (1 to 21) as substrate by hotspot assay |
CHEMBL4680176 |
| Histone-lysine N-methyltransferase SETD7 |
IC50 |
|
|
|
Inhibition of recombinant human SET7/9 using core histone as substrate by hotspot assay |
CHEMBL4680176 |
| Protein arginine N-methyltransferase 3 |
IC50 |
= |
760.0 |
nM |
Inhibition of recombinant human PRMT3 using histone H4 as substrate by hotspot assay |
CHEMBL4680176 |
| Protein arginine N-methyltransferase 5 |
IC50 |
|
|
|
Inhibition of recombinant human PRMT5 using histone H2A as substrate by hotspot assay |
CHEMBL4680176 |
| Protein arginine N-methyltransferase 7 |
IC50 |
= |
110.0 |
nM |
Inhibition of recombinant human PRMT7 using GST-GAR as substrate by hotspot assay |
CHEMBL4680176 |
| Protein arginine N-methyltransferase 3 |
IC50 |
= |
110.0 |
nM |
Inhibition of recombinant human PRMT8 using histone H4 as substrate by hotspot assay |
CHEMBL4680176 |
| Phenylethanolamine N-methyltransferase |
Ki |
= |
14000.0 |
nM |
Competitive inhibition of C-terminal hexahistidine tag in human recombinant PNMT expressed in Escherichia coli assessed as inhibition constant using PEA as substrate in presence of 100 uM AdoMet as co-substrate by Sigma-plot analysis |
CHEMBL4699623 |
| Phenylethanolamine N-methyltransferase |
Kis |
|
|
|
Non-competitive inhibition of C-terminal hexahistidine tag in human recombinant PNMT expressed in Escherichia coli assessed as slope inhibition constant in presence of 5 uM PEA as substrate and AdoMet as co-substrate by Sigma-plot analysis |
CHEMBL4699623 |
| Alpha-2a adrenergic receptor |
Ki |
|
|
|
Displacement of [3H]-clonidine from Sprague-Dawley rat alpha2 adrenergic receptor by radioligand binding assay |
CHEMBL4699623 |
| Unchecked |
Ratio Ki |
|
|
|
Selectivity index, ratio of Ki for alpha2 adrenergic receptor in Sprague-dawley rat to Ki for competitive inhibition of C-terminal hexahistidine tag in human recombinant PNMT expressed in Escherichia coli in presence of PEA as substrate and AdoMet as co-substrate by Sigma-plot analysis |
CHEMBL4699623 |
| Phenylethanolamine N-methyltransferase |
Kii |
|
|
|
Non-competitive inhibition of C-terminal hexahistidine tag in human recombinant PNMT expressed in Escherichia coli assessed as intercept inhibition constant in presence of 5 uM PEA as substrate and AdoMet as co-substrate by Sigma-plot analysis |
CHEMBL4699623 |
| Unchecked |
Delta Tm |
= |
6.5 |
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 |
| Histone-lysine N-methyltransferase NSD2 |
IC50 |
= |
39100.0 |
nM |
Inhibition of recombinant human N-terminal GST-tagged NSD2 CD (941 to 1240 residues) expressed in Escherichia coli using SAM as substrate in presence of nucleosomes by AlphaLISA method |
CHEMBL4825702 |
| Histone-lysine N-methyltransferase NSD2 |
Inhibition |
= |
54.0 |
% |
Inhibition of NSD2 (953 to 1240 residues) (unknown origin) at 30 uM using SAM as substrate in presence of nucleosome by AlphaScreen assay relative to control |
CHEMBL4825702 |
| N6-adenosine-methyltransferase catalytic subunit |
IC50 |
= |
590.0 |
nM |
Inhibition of recombinant METLL3 (unknown origin) expressed in baculovirus infected Sf9 cells assessed as decrease in N6-methyladenosine level in oligonucleotide substrate by TR-FRET assay |
CHEMBL5053501 |
| METTL3/METTL14 |
Delta Tm |
= |
3.7 |
degrees C |
Binding affinity to human METTL3/METLL14 assessed as change in melting temperature at 1000 uM by thermal shift assay |
CHEMBL5053501 |
| Unchecked |
Delta Tm |
= |
0.8 |
degrees C |
Binding affinity to human METTL16 assessed as change in melting temperature at 1000 uM by thermal shift assay |
CHEMBL5053501 |
| Unchecked |
Delta Tm |
= |
6.3 |
degrees C |
Binding affinity to human METTL1 assessed as change in melting temperature at 1000 uM by thermal shift assay |
CHEMBL5053501 |
| Histone-lysine N-methyltransferase, H3 lysine-79 specific |
Inhibition |
= |
100.0 |
% |
Inhibition of DOTL1 (unknown origin) using [3H]SAM and HeLa oligo nucleosomes as substrates at 100 uM incubated for 1 hr relative to control |
CHEMBL5120862 |
| Histone-lysine N-methyltransferase, H3 lysine-79 specific |
IC50 |
= |
140.0 |
nM |
Inhibition of DOTL1 (unknown origin) using [3H]SAM and HeLa oligo nucleosomes as substrates incubated for 1 hr |
CHEMBL5120862 |
| N-lysine methyltransferase SETD8 |
Inhibition |
|
|
% |
Inhibition of SETD8 (unknown origin) using [3H]SAM and HeLa nucleosomes as substrates at 100 uM incubated for 1 hr relative to control |
CHEMBL5120862 |
| N-lysine methyltransferase SETD8 |
IC50 |
|
|
|
Inhibition of SETD8 (unknown origin) using [3H]SAM and HeLa nucleosomes as substrates incubated for 1 hr |
CHEMBL5120862 |
| Histone-lysine N-methyltransferase EZH2 |
Inhibition |
= |
84.2 |
% |
Inhibition of EZH2 (unknown origin) using [3H]SAM and chicken core histone as substrates at 100 uM incubated for 1 hr relative to control |
CHEMBL5120862 |
| Histone-lysine N-methyltransferase EZH2 |
IC50 |
= |
23700.0 |
nM |
Inhibition of EZH2 (unknown origin) using [3H]SAM and chicken core histone as substrates incubated for 1 hr |
CHEMBL5120862 |
| Protein-arginine N-methyltransferase 1 |
Inhibition |
= |
100.0 |
% |
Inhibition of PRMT1 (unknown origin) using [3H]SAM and chicken histone 4 as substrates at 100 uM incubated for 1 hr relative to control |
CHEMBL5120862 |
| Protein-arginine N-methyltransferase 1 |
IC50 |
= |
250.0 |
nM |
Inhibition of PRMT1 (unknown origin) using [3H]SAM and chicken histone 4 as substrates incubated for 1 hr |
CHEMBL5120862 |
| Monoamine oxidase A |
Inhibition |
|
|
% |
Inhibition of human MAO-A using p-tyramine as substrate at 100 uM by fluorimetric analysis relative to control |
CHEMBL5120862 |
| Monoamine oxidase A |
IC50 |
|
|
|
Inhibition of human MAO-A using p-tyramine as substrate by fluorimetric analysis |
CHEMBL5120862 |
| Monoamine oxidase B |
Inhibition |
|
|
% |
Inhibition of human MAO-B using p-tyramine as substrate at 100 uM by fluorimetric analysis relative to control |
CHEMBL5120862 |
| Monoamine oxidase B |
IC50 |
|
|
|
Inhibition of human MAO-B using p-tyramine as substrate by fluorimetric analysis |
CHEMBL5120862 |
| 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 |
= |
85.7 |
% |
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 |
= |
13600.0 |
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 |
= |
15800.0 |
nM |
Inhibition of full length human N-terminal his6-tagged DNMT2 expressed in Escherichia coli Rosetta2(DE3)pLysS by isothermal titration calorimetry assay |
CHEMBL5131574 |
| tRNA (cytosine(38)-C(5))-methyltransferase |
deltaG |
= |
-27.8 |
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 |
= |
-55.3 |
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 |
= |
27.5 |
kJ/mol |
Binding affinity to full length human N-terminal his6-tagged DNMT2 expressed in Escherichia coli Rosetta2(DE3)pLysS assessed as change in entropy at 100 uM by isothermal titration calorimetry assay |
CHEMBL5131574 |
| DNA (cytosine-5)-methyltransferase 3A |
Inhibition |
= |
96.7 |
% |
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 |
= |
97.3 |
% |
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 |
= |
99.6 |
% |
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 |
= |
94.3 |
% |
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 |
= |
85.7 |
% |
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 |
| DNA (cytosine-5)-methyltransferase 1 |
IC50 |
= |
700.0 |
nM |
Inhibition of human recombinant full-length DNMT1 expressed in Sf9 cells assessed as inhibition of methylated dI-dC formation using poly dI-dC and [Me-3H]SAM as substrate incubated for 2 hrs by liquid scintillation counting analysis |
CHEMBL5137006 |
| DNA (cytosine-5)-methyltransferase 3B |
IC50 |
= |
700.0 |
nM |
Inhibition of human C-terminal domain DNMT3b catalytic domain (568 to 853 residues) expressed in Escherichia coli BL21 (DE3) pLysS cells assessed as inhibition of methylated dI-dC formation using poly dI-dC and [Me-3H]SAM as substrate incubated for 45 mins in presence of DNMT3L by liquid scintillation counting analysis |
CHEMBL5137006 |
