Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | Raf-1 proto-oncogene, serine/threonine kinase | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Brugia malayi | Raf kinase | Get druggable targets OG5_130459 | All targets in OG5_130459 |
Echinococcus granulosus | raf serine:threonine protein kinase | Get druggable targets OG5_130459 | All targets in OG5_130459 |
Schistosoma japonicum | ko:K04365 B-Raf proto-oncogene serine/threonine-protein kinase, putative | Get druggable targets OG5_130459 | All targets in OG5_130459 |
Echinococcus multilocularis | raf serine:threonine protein kinase | Get druggable targets OG5_130459 | All targets in OG5_130459 |
Loa Loa (eye worm) | raf kinase | Get druggable targets OG5_130459 | All targets in OG5_130459 |
Schistosoma mansoni | serine/threonine protein kinase | Get druggable targets OG5_130459 | All targets in OG5_130459 |
Loa Loa (eye worm) | TKL/RAF/RAF protein kinase | Get druggable targets OG5_130459 | All targets in OG5_130459 |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Onchocerca volvulus | 0.0092 | 0.2752 | 0.5 | |
Onchocerca volvulus | 0.0092 | 0.2752 | 0.5 | |
Loa Loa (eye worm) | raf kinase | 0.026 | 0.9945 | 1 |
Schistosoma mansoni | hypothetical protein | 0.0092 | 0.2752 | 0.2752 |
Brugia malayi | SEA domain containing protein | 0.0092 | 0.2752 | 0.2669 |
Loa Loa (eye worm) | DOMON domain-containing protein | 0.0092 | 0.2752 | 0.2576 |
Loa Loa (eye worm) | hypothetical protein | 0.0092 | 0.2752 | 0.2576 |
Onchocerca volvulus | 0.0092 | 0.2752 | 0.5 | |
Schistosoma mansoni | subfamily S1A unassigned peptidase (S01 family) | 0.0045 | 0.072 | 0.072 |
Schistosoma mansoni | serine/threonine protein kinase | 0.0262 | 1 | 1 |
Onchocerca volvulus | 0.0092 | 0.2752 | 0.5 | |
Loa Loa (eye worm) | TKL/RAF/RAF protein kinase | 0.0148 | 0.515 | 0.5051 |
Brugia malayi | Raf kinase | 0.0253 | 0.9609 | 1 |
Brugia malayi | Muscle positioning protein 4 | 0.0092 | 0.2752 | 0.2669 |
Onchocerca volvulus | 0.0092 | 0.2752 | 0.5 | |
Echinococcus multilocularis | raf serine:threonine protein kinase | 0.0262 | 1 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0092 | 0.2752 | 0.2576 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
AUC (ADMET) | = 29 uM.hr | AUC (0 to t) in BALB-nu/u mouse at 200 mg/kg, po after 24 hrs by LC/MS/MS analysis | ChEMBL. | 24157370 |
IC50 (binding) | = 120 nM | Inhibition of C-RAF (unknown origin)-mediated inactive MEK1 K97R mutant phosphorylation after 45 mins by TR-FRET assay | ChEMBL. | 24157370 |
IC50 (functional) | = 370 nM | Growth inhibition of human HT-29 cells after 96 hrs by CCK-8 assay | ChEMBL. | 24157370 |
TGI (functional) | = 38 % | Antitumor activity against human HCT116 cells xenografted in BALB-nu/u mouse assessed as tumor growth inhibition at 200 mg/kg, po qd for 11 days relative to control | ChEMBL. | 24157370 |
Species name | Source | Reference | Is orphan |
---|---|---|---|
Homo sapiens | ChEMBL23 | 24157370 |
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.