Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | B-Raf proto-oncogene, serine/threonine kinase | Starlite/ChEMBL | No references |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
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 |
Brugia malayi | Raf kinase | 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 |
---|---|---|---|---|
Schistosoma mansoni | hypothetical protein | 0.0723 | 0.9979 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0723 | 0.9979 | 0.9979 |
Echinococcus granulosus | raf serine:threonine protein kinase | 0.0262 | 0.2501 | 0.2506 |
Schistosoma mansoni | subfamily S1A unassigned peptidase (S01 family) | 0.0197 | 0.1461 | 0.1465 |
Loa Loa (eye worm) | TKL/RAF/RAF protein kinase | 0.0148 | 0.0666 | 0.0666 |
Brugia malayi | Raf kinase | 0.0253 | 0.2353 | 0.2353 |
Schistosoma mansoni | serine/threonine protein kinase | 0.0262 | 0.2501 | 0.2506 |
Echinococcus granulosus | tissue type plasminogen activator | 0.0723 | 0.9979 | 1 |
Schistosoma mansoni | subfamily S1A unassigned peptidase (S01 family) | 0.0197 | 0.1461 | 0.1465 |
Echinococcus multilocularis | raf serine:threonine protein kinase | 0.0262 | 0.2501 | 0.2506 |
Loa Loa (eye worm) | hypothetical protein | 0.0197 | 0.1461 | 0.1461 |
Trypanosoma cruzi | hypothetical protein, conserved | 0.0723 | 0.9979 | 0.5 |
Loa Loa (eye worm) | raf kinase | 0.026 | 0.248 | 0.248 |
Plasmodium vivax | cysteine repeat modular protein 1, putative | 0.0723 | 0.9979 | 0.5 |
Onchocerca volvulus | 0.0197 | 0.1461 | 0.1465 | |
Toxoplasma gondii | kringle domain-containing protein | 0.0723 | 0.9979 | 0.5 |
Leishmania major | hypothetical protein, conserved | 0.0723 | 0.9979 | 0.5 |
Onchocerca volvulus | 0.0723 | 0.9979 | 1 | |
Brugia malayi | Kringle domain containing protein | 0.0723 | 0.9979 | 0.9979 |
Brugia malayi | Trypsin family protein | 0.0197 | 0.1461 | 0.1461 |
Echinococcus multilocularis | tissue type plasminogen activator | 0.0723 | 0.9979 | 1 |
Loa Loa (eye worm) | TK/ROR protein kinase | 0.0725 | 1 | 1 |
Mycobacterium ulcerans | hypothetical protein | 0.0107 | 0 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0197 | 0.1461 | 0.1461 |
Plasmodium falciparum | cysteine repeat modular protein 1 | 0.0723 | 0.9979 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 4 nM | BindingDB_Patents: kinase Assay. The final concentration of DMSO is 5%. 10 µL of the B-Raf (V600E)-kinase solution are pipetted in (containing 0.5 ng B-Raf (V600E)-kinase in 20 mM Tris-HCl pH 7.5, 0.1 mM EDTA, 0.1 mM EGTA, 0.286 mM sodium orthovanadate, 10% glycerol, 1 mg/mL bovine serum albumin, 1 mM dithiothreitol) and the mixture is incubated for 24 h at RT under with shaking. The kinase reaction is started by the addition of 20 µL ATP solution [final concentration: 250 µM ATP, 30 mM Tris-HCl pH 7.5, 0.02% Brij, 0.2 mM sodium orthovanadate, 10 mM magnesium acetate, 0.1 mM EGTA, phosphatase cocktail (Sigma, # P2850, dilution recommended by the manufacturer), 0.1 mM EGTA] and 10 µL MEK1 solution [containing 50 ng biotinylated MEK1 (prepared from purified MEK1 according to standard procedure, e.g. with EZ-Link Sulpho-NHS-LC-Biotin reagent, Pierce, #21335) and carried out for 60 min at RT with constant shaking. | ChEMBL. | No reference |
IC50 (binding) | = 4 nM | kinase Assay | BINDINGDB. | No reference |
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.