Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | smoothened, frizzled class receptor | No references |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Echinococcus granulosus | smoothened | Get druggable targets OG5_134998 | All targets in OG5_134998 |
Echinococcus multilocularis | smoothened | Get druggable targets OG5_134998 | All targets in OG5_134998 |
Loa Loa (eye worm) | hypothetical protein | Get druggable targets OG5_134998 | All targets in OG5_134998 |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Schistosoma mansoni | cpg binding protein | 0.0031 | 0.0159 | 0.0555 |
Echinococcus granulosus | DNA methyltransferase 2, putative | 0.0097 | 0.1873 | 0.1873 |
Toxoplasma gondii | hypothetical protein | 0.0079 | 0.1406 | 0.7508 |
Echinococcus multilocularis | disco interacting protein 2 | 0.0036 | 0.0281 | 0.0281 |
Schistosoma mansoni | cpg binding protein | 0.0031 | 0.0159 | 0.0555 |
Echinococcus multilocularis | DNA methyltransferase 2, putative | 0.0097 | 0.1873 | 0.1873 |
Trypanosoma cruzi | hypothetical protein, conserved | 0.0025 | 0 | 0.5 |
Trypanosoma cruzi | MIZ/SP-RING zinc finger, putative | 0.0025 | 0 | 0.5 |
Echinococcus multilocularis | cpg binding protein | 0.0031 | 0.0159 | 0.0159 |
Brugia malayi | Histone-lysine N-methyltransferase, H3 lysine-79 specific | 0.0136 | 0.2868 | 1 |
Brugia malayi | CXXC zinc finger family protein | 0.0031 | 0.0159 | 0.0555 |
Toxoplasma gondii | C-5 cytosine-specific DNA methylase superfamily protein | 0.0097 | 0.1873 | 1 |
Toxoplasma gondii | DNA methyltransferase 2, putative | 0.0097 | 0.1873 | 1 |
Loa Loa (eye worm) | CXXC zinc finger family protein | 0.0031 | 0.0159 | 0.0163 |
Plasmodium vivax | DNA (cytosine-5)-methyltransferase, putative | 0.0097 | 0.1873 | 0.5 |
Leishmania major | modification methylase-like protein | 0.0097 | 0.1873 | 1 |
Schistosoma mansoni | DNA (cytosine-5)-methyltransferase | 0.0097 | 0.1873 | 0.6531 |
Schistosoma mansoni | cpg binding protein | 0.0031 | 0.0159 | 0.0555 |
Trypanosoma brucei | cytosine-specific DNA methylase, putative | 0.0097 | 0.1873 | 1 |
Echinococcus granulosus | histone h3 methyltransferase | 0.0136 | 0.2868 | 0.2868 |
Loa Loa (eye worm) | hypothetical protein | 0.0136 | 0.2868 | 0.2932 |
Plasmodium falciparum | DNA (cytosine-5)-methyltransferase | 0.0097 | 0.1873 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0402 | 0.978 | 1 |
Echinococcus granulosus | cpg binding protein | 0.0031 | 0.0159 | 0.0159 |
Echinococcus multilocularis | smoothened | 0.041 | 1 | 1 |
Onchocerca volvulus | 0.0031 | 0.0159 | 0.5654 | |
Brugia malayi | Disco-interacting protein 2 homolog | 0.0036 | 0.0281 | 0.0982 |
Schistosoma mansoni | disco-interacting protein 2 (dip2) | 0.0036 | 0.0281 | 0.0982 |
Echinococcus multilocularis | histone h3 methyltransferase | 0.0136 | 0.2868 | 0.2868 |
Loa Loa (eye worm) | hypothetical protein | 0.0036 | 0.0281 | 0.0288 |
Trypanosoma cruzi | transcription elongation factor-like protein, putative | 0.0025 | 0 | 0.5 |
Schistosoma mansoni | histone J3 methyltransferase | 0.0136 | 0.2868 | 1 |
Trypanosoma cruzi | hypothetical protein, conserved | 0.0025 | 0 | 0.5 |
Echinococcus granulosus | disco interacting protein 2 | 0.0036 | 0.0281 | 0.0281 |
Trypanosoma cruzi | transcription elongation factor s-II, putative | 0.0025 | 0 | 0.5 |
Entamoeba histolytica | DNA (cytosine-5)-methyltransferase, putative | 0.0097 | 0.1873 | 1 |
Onchocerca volvulus | 0.0036 | 0.0281 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 100 nM | BindingDB_Patents: Radioligand Competition Binding Assay. For the binding competition assay, 100 µL of Assay Buffer was added to all the wells of a 96 well GF/B filter plate (Millipore MultiScreen-HTS-FB cat# MSFBN6B50) for 10 minutes to pre-wet the filter prior to evacuation of the buffer (8 inches Hg for 8 seconds). To the pre-wet wells is added: 20 µL of Assay Buffer, 10 µL diluted test agent, 20 µL of a tritiated Smo antagonist (15 nM stock solution), and 50 µL of membrane preparation (40 µg total protein per well). The plates are sealed and mixed at room temperature for 5 min, incubated at room temperature for 2 hours, then washed 5 times with 100 µL/each of wash buffer and vacuum dried for 8 seconds at 8 inches Hg. The plate is then dried for one hour in a 60° C. oven prior to the addition of 45 µL of Microscint 20 (Packard, #6013621) to each well and incubation at RT for 30 minutes to 1 hour. The plate is counted in a TopCount scintillation counter (Perkin Elmer). | ChEMBL. | No reference |
IC50 (binding) | = 100 nM | BindingDB_Patents: Radioligand Competition Binding Assay. For the binding competition assay, 100 µL of Assay Buffer was added to all the wells of a 96 well GF/B filter plate (Millipore MultiScreen-HTS-FB cat# MSFBN6B50) for 10 minutes to pre-wet the filter prior to evacuation of the buffer (8 inches Hg for 8 seconds). To the pre-wet wells is added: 20 µL of Assay Buffer, 10 µL diluted test agent, 20 µL of a tritiated Smo antagonist (15 nM stock solution), and 50 µL of membrane preparation (40 µg total protein per well). The plates are sealed and mixed at room temperature for 5 min, incubated at room temperature for 2 hours, then washed 5 times with 100 µL/each of wash buffer and vacuum dried for 8 seconds at 8 inches Hg. The plate is then dried for one hour in a 60° C. oven prior to the addition of 45 µL of Microscint 20 (Packard, #6013621) to each well and incubation at RT for 30 minutes to 1 hour. The plate is counted in a TopCount scintillation counter (Perkin Elmer). | ChEMBL. | 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.