Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (binding) | Activation of ERK1/2 in human HL60 cells at 0.1 to 1 uM after 48 hrs by Western blot analysis | ChEMBL. | 27089210 | |
Activity (binding) | Activation of endonuclease G in human HL60 cells at 0.1 to 1 uM after 48 hrs by Western blot analysis | ChEMBL. | 27089210 | |
GI (functional) | = 90.9 % | Anti-trypanosomal activity against Trypanosoma brucei gambiense Feo bloodstream forms assessed as inhibition of parasite growth rate at 50 ug/mL after 72 hrs by resazurin assay | ChEMBL. | 25089808 |
IC50 (functional) | = 0.7 uM | Antiproliferative activity against mouse L1210 cells after 72 hrs by MTT assay | ChEMBL. | 27089210 |
IC50 (functional) | = 1.1 uM | Anti-trypanosomal activity against Trypanosoma brucei gambiense Feo bloodstream forms assessed as inhibition of parasite growth rate after 72 hrs by resazurin assay | ChEMBL. | 25089808 |
IC50 (functional) | = 1.1 uM | Antiproliferative activity against human Jurkat cells after 72 hrs by MTT assay | ChEMBL. | 27089210 |
Inhibition (binding) | Inhibition of retinoblastoma protein phosphorylation in human HL60 cells at 0.1 to 1 uM after 48 hrs by Western blot analysis | ChEMBL. | 27089210 |
Species name | Source | Reference | Is orphan |
---|---|---|---|
Trypanosoma brucei gambiense | ChEMBL23 | 25089808 | |
Homo sapiens | ChEMBL23 | 27089210 | |
Mus musculus | ChEMBL23 | 27089210 |
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.
1 literature reference was collected for this gene.