Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (binding) | Stabilization of recombinant human topoisomerase 1-pBR322 DNA cleavage complex assessed as linear DNA formation at 0.5 uM after 60 mins by agarose gel electrophoresis | ChEMBL. | 25626146 | |
GI50 (functional) | = 0.5 uM | Antiproliferative activity against human HL60 cells after 72 hrs by SRB assay | ChEMBL. | 22417638 |
GI50 (functional) | = 0.9 uM | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay | ChEMBL. | 22417638 |
IC50 (functional) | = 19 nM | Antiproliferative activity against mouse L1210 cells after 48 hrs by Coulter counter method | ChEMBL. | 25626146 |
IC50 (functional) | = 185 nM | Antiproliferative activity against human CEM cells after 96 hrs by Coulter counter method | ChEMBL. | 25626146 |
Inhibition (binding) | Inhibition of recombinant human topoisomerase 1-mediated relaxation of supercoiled pBR322 DNA at 10 uM after 60 mins by agarose gel electrophoresis | ChEMBL. | 25626146 | |
Inhibition (binding) | = 12 % | Inhibition of SIRT1 (unknown origin) using KI177 as substrate preincubated at 200 uM for 5 mins before substrate addition measured after 1 hr by Fluor de Lys fluorescence assay | ChEMBL. | 25626146 |
Inhibition (binding) | = 12 % | Inhibition of recombinant human SIRT1 expressed in Escherichia coli at 200 uM by Fluor de Lys assay relative to control | LITERATURE. | 27153347 |
Inhibition (binding) | = 65 % | Inhibition of SIRT2 (unknown origin) using KI179 as substrate preincubated at 200 uM for 5 mins before substrate addition measured after 1 hr by Fluor de Lys fluorescence assay | ChEMBL. | 25626146 |
Inhibition (binding) | = 65 % | Inhibition of recombinant human SIRT2 expressed in Escherichia coli at 200 uM by Fluor de Lys assay relative to control | LITERATURE. | 27153347 |
Species name | Source | Reference | Is orphan |
---|---|---|---|
Homo sapiens | ChEMBL23 | 25626146 | |
Mus musculus | ChEMBL23 | 25626146 |
Many chemical entities in TDR Targets come from high-throughput screenings with whole cells or tissue samples, and not all assayed compounds have been tested against a single a single target protein, probably because they get ruled out during screening process. Even if these compounds may have not been of interest in the original screening, they may come as interesting leads for other screening assays. Furthermore, we may be able to propose drug-target associations using chemical similarities and network patterns.
2 literature references were collected for this gene.