Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | TEK tyrosine kinase, endothelial | Starlite/ChEMBL | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
CL (ADMET) | = 770 ml/hr.kg | Clearance in iv dosed rat | ChEMBL. | 17253678 |
IC50 (binding) | = 22 nM | Inhibition of Tie2 by HTRF assay | ChEMBL. | 17253678 |
IC50 (binding) | = 22 nM | Inhibition of Tie2 by HTRF assay | ChEMBL. | 17253678 |
IC50 (functional) | = 61 nM | Inhibition of angiopoietin1-stimulated Tie2 phosphorylation in EA.hy926 cells | ChEMBL. | 17253678 |
IC50 (functional) | = 61 nM | Inhibition of angiopoietin1-stimulated Tie2 phosphorylation in EA.hy926 cells | ChEMBL. | 17253678 |
IC50 (binding) | > 25000 nM | Inhibition of KDR by HTRF assay | ChEMBL. | 17253678 |
IC50 (binding) | > 25000 nM | Inhibition of KDR by HTRF assay | ChEMBL. | 17253678 |
MRT (ADMET) | = 0.47 hr | Mean residence time in rat | ChEMBL. | 17253678 |
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.