Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | TTK protein kinase | Starlite/ChEMBL | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Drug metabolism (ADMET) | = 24 % | Drug metabolism in human liver microsomes at 10 uM after 30 mins by LC-MS/MS analysis | ChEMBL. | 24256217 |
IC50 (binding) | = 0.015 uM | Inhibition of N-terminal 6XHis-tagged/GST-tagged full length human MPS1 expressed in recombinant baculovirus infected sf9 insect cells using 5FAM-DHTGFLTEYVATRCONH2 as substrate after 60 to 90 mins by fluorescence assay | ChEMBL. | 24256217 |
IC50 (binding) | = 0.16 uM | Inhibition of Myc-tagged wild type MPS1 autophosphorylation in human HCT116 cells after 2 hrs in presence of proteosome inhibitor MG132 | ChEMBL. | 24256217 |
IC50 (binding) | > 100 uM | Inhibition of full length CDK2/Cyclin A (unknown origin) using 5FAMQSPKKG-CONH2 as substrate after 60 mins by fluorescence assay | ChEMBL. | 24256217 |
IC50 (binding) | > 100 uM | Inhibition of N-terminal His-tagged Aurora A (unknown origin) using 5FAM-LRRASLG-CONH2 as substrate after 60 mins by fluorescence assay | ChEMBL. | 24256217 |
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.