Compound ID |
Cluster
|
Compound Type
|
Target/Cell | Structure | Activity | Assay Description | Source | ||||
---|---|---|---|---|---|---|---|---|---|---|---|
Type
|
Relation
|
Value
|
Unit
|
||||||||
NAs.000068 | 2 | all-match | Trypanosoma brucei brucei | ![]() |
IC50 | > | 100000.0 | nM | Antitrypanosomal activity against bloodstream form of Trypanosoma brucei brucei LAB 110 EATRO after 48 hrs by Z1 zoulter counter | CHEMBL1151452 | |
NAs.000068 | 2 | all-match | Trypanosoma brucei brucei | ![]() |
IC50 | = | 72500.0 | nM | Antitrypanosomal activity against pentamidine and melarsoprol-resistant bloodstream form of Trypanosoma brucei brucei isolate KETRI 243 after 48 hrs by Z1 zoulter counter | CHEMBL1151452 | |
NAs.000068 | 2 | all-match | Trypanosoma brucei brucei | ![]() |
IC50 | > | 100000.0 | nM | Antitrypanosomal activity against pentamidine-resistant bloodstream form of Trypanosoma brucei brucei isolate KETRI 269 after 48 hrs by Z1 zoulter counter | CHEMBL1151452 | |
NAs.000068 | 2 | all-match | Trypanosoma brucei brucei | ![]() |
IC50 | = | 15750.0 | nM | Antitrypanosomal activity against diamidine and melarsoprol-resistant bloodstream form of Trypanosoma brucei brucei isolate KETRI 243-As10-3 after 48 hrs by Z1 zoulter counter | CHEMBL1151452 | |
NAs.000068 | 2 | all-match | Unchecked | ![]() |
Other | = | 46.0 | % | Activity at bloodstream Trypanosoma brucei brucei 5'-deoxy-5'-(methylthio)-adenosine phosphorylase by spectrophotometry in presence of 50 mM PO4- relative to control | CHEMBL1151452 | |
NAs.000068 | 2 | all-match | Unchecked | ![]() |
Other | = | 60.0 | % | Activity at bloodstream Trypanosoma brucei brucei 5'-deoxy-5'-(methylthio)-adenosine phosphorylase by spectrophotometry relative to control | CHEMBL1151452 | |
NAs.000068 | 2 | all-match | DNA (cytosine-5)-methyltransferase 1 | ![]() |
IC50 | > | 45000.0 | nM | Inhibition of human recombinant DNMT1 | CHEMBL1151876 | |
NAs.000068 | 2 | all-match | DNA (cytosine-5)-methyltransferase 3B | ![]() |
IC50 | = | 17000.0 | nM | Inhibition of human recombinant DNMT3b2 | CHEMBL1151876 | |
NAs.000068 | 2 | all-match | Histone-lysine N-methyltransferase, H3 lysine-79 specific | ![]() |
Ki | = | 100000.0 | nM | Inhibition of human recombinant DOT1L catalytic domain amino acid (1 to 472) using [3H]-SAM after 30 mins by scintillation counter | CHEMBL2169812 | |
NAs.000068 | 2 | all-match | Histone-lysine N-methyltransferase, H3 lysine-79 specific | ![]() |
Ki | = | 100000.0 | nM | Competitive inhibition of recombinant human DOT1L using adenosine/deazaadenosine as substrate and SAM cofactor | CHEMBL3085656 | |
NAs.000068 | 2 | all-match | Histone-lysine N-methyltransferase EZH2 | ![]() |
Other | None | None | % | 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 at 20 uM by scintillation counting in presence of [3H]SAM | CHEMBL3396964 | |
NAs.000068 | 2 | all-match | tRNA (cytosine(38)-C(5))-methyltransferase | ![]() |
Other | None | None | None | 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 | |
NAs.000068 | 2 | all-match | tRNA (cytosine(38)-C(5))-methyltransferase | ![]() |
Other | None | None | % | 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 |