Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | solute carrier family 6 (neurotransmitter transporter, glycine), member 9 | Starlite/ChEMBL | No references |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Echinococcus multilocularis | serotonin transporter | solute carrier family 6 (neurotransmitter transporter, glycine), member 9 | 633 aa | 616 aa | 38.6 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Brugia malayi | Eukaryotic-type carbonic anhydrase family protein | 0.0136 | 0.079 | 1 |
Chlamydia trachomatis | sulfate transporter | 0.0036 | 0.004 | 0.5 |
Echinococcus granulosus | sodium and chloride dependent glycine | 0.0096 | 0.0488 | 0.6176 |
Plasmodium falciparum | inorganic anion exchanger, inorganic anion antiporter | 0.0036 | 0.004 | 1 |
Brugia malayi | Sodium:neurotransmitter symporter family protein | 0.0096 | 0.0488 | 0.6176 |
Mycobacterium tuberculosis | Beta-carbonic anhydrase CanB | 0.0288 | 0.1939 | 0.031 |
Trypanosoma cruzi | carbonic anhydrase-like protein, putative | 0.0136 | 0.079 | 1 |
Loa Loa (eye worm) | eukaryotic-type carbonic anhydrase | 0.0136 | 0.079 | 1 |
Schistosoma mansoni | sodium/chloride dependent transporter | 0.0096 | 0.0488 | 0.1217 |
Mycobacterium ulcerans | carbonic anhydrase | 0.0562 | 0.4007 | 0.3983 |
Loa Loa (eye worm) | hypothetical protein | 0.0096 | 0.0488 | 0.6176 |
Echinococcus multilocularis | sodium and chloride dependent glycine | 0.0096 | 0.0488 | 0.6176 |
Schistosoma mansoni | carbonic anhydrase II (carbonate dehydratase II) | 0.0136 | 0.079 | 0.1971 |
Schistosoma mansoni | sodium/chloride dependent transporter | 0.0096 | 0.0488 | 0.1217 |
Onchocerca volvulus | Putative sulfate transporter | 0.0227 | 0.1481 | 1 |
Echinococcus multilocularis | Basic leucine zipper (bZIP) transcription factor | 0.0043 | 0.0088 | 0.1114 |
Trichomonas vaginalis | conserved hypothetical protein | 0.1356 | 1 | 0.5 |
Leishmania major | carbonic anhydrase family protein, putative | 0.0562 | 0.4007 | 1 |
Mycobacterium leprae | CARBONIC ANHYDRASE (CARBONATE DEHYDRATASE) (CARBONIC DEHYDRATASE) | 0.0562 | 0.4007 | 1 |
Entamoeba histolytica | carbonic anhydrase, putative | 0.0562 | 0.4007 | 0.5 |
Loa Loa (eye worm) | carbonic anhydrase 3 | 0.0136 | 0.079 | 1 |
Mycobacterium tuberculosis | Probable transmembrane carbonic anhydrase (carbonate dehydratase) (carbonic dehydratase) | 0.0536 | 0.3815 | 0.3344 |
Echinococcus multilocularis | carbonic anhydrase II | 0.0136 | 0.079 | 1 |
Echinococcus granulosus | carbonic anhydrase II | 0.0136 | 0.079 | 1 |
Plasmodium vivax | sulfate transporter, putative | 0.0036 | 0.004 | 0.5 |
Echinococcus multilocularis | sodium and chloride dependent glycine | 0.0096 | 0.0488 | 0.6176 |
Schistosoma mansoni | carbonic anhydrase | 0.0562 | 0.4007 | 1 |
Brugia malayi | bZIP transcription factor family protein | 0.0043 | 0.0088 | 0.1114 |
Schistosoma mansoni | hypothetical protein | 0.0035 | 0.0028 | 0.0069 |
Onchocerca volvulus | 0.0227 | 0.1481 | 1 | |
Schistosoma mansoni | carbonic anhydrase II (carbonate dehydratase II) | 0.0136 | 0.079 | 0.1971 |
Echinococcus granulosus | Basic leucine zipper bZIP transcription factor | 0.0043 | 0.0088 | 0.1114 |
Trypanosoma cruzi | carbonic anhydrase-like protein, putative | 0.0136 | 0.079 | 1 |
Brugia malayi | hypothetical protein | 0.0033 | 0.0019 | 0.024 |
Trichomonas vaginalis | conserved hypothetical protein | 0.1356 | 1 | 0.5 |
Echinococcus granulosus | jun protein | 0.0043 | 0.0088 | 0.1114 |
Echinococcus granulosus | sodium and chloride dependent glycine | 0.0096 | 0.0488 | 0.6176 |
Loa Loa (eye worm) | Sodium:neurotransmitter symporter family protein | 0.0096 | 0.0488 | 0.6176 |
Echinococcus multilocularis | jun protein | 0.0043 | 0.0088 | 0.1114 |
Loa Loa (eye worm) | hypothetical protein | 0.0041 | 0.0079 | 0.1002 |
Mycobacterium tuberculosis | Beta-carbonic anhydrase | 0.1082 | 0.7932 | 1 |
Brugia malayi | Putative carbonic anhydrase 5 precursor | 0.0136 | 0.079 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0096 | 0.0488 | 0.6176 |
Trypanosoma brucei | carbonic anhydrase-like protein | 0.0136 | 0.079 | 1 |
Toxoplasma gondii | inorganic anion transporter, sulfate permease (SulP) family protein | 0.0036 | 0.004 | 1 |
Schistosoma mansoni | jun-related protein | 0.0035 | 0.0028 | 0.0069 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | < 1000000 nM | BindingDB_Patents: Glycine Uptake Assay. [3H]-Glycine uptake into recombinant CHO cells expressing human GlyT1: Human GlyT1c expressing recombinant hGlyT1c5_CHO cells were plated at 20,000 cells per well in 96 well Cytostar-T scintillation microplates (Amersham Biosciences) and cultured to sub-confluency for 24 h. For glycine uptake assays the culture medium was aspirated and the cells were washed once with 100 ul HBSS (Gibco BRL, #14025-050) with 5 mM L-Alanine (Merck #1007). 80 ul HBSS buffer were added, followed by 10 ul inhibitor or vehicle (10% DMSO) and 10 ul [3H]-glycine (TRK71, Amersham Biosciences) to a final concentration of 200 nM for initiation of glycine uptake. The plates were placed in a Wallac Microbeta (PerkinElmer) and continuously counted by solid phase scintillation spectrometry during up to 3 hours. Nonspecific uptake was determined in the presence of 10 uM Org24598. IC50 calculations were made by four-parametric logistic nonlinear regression analysis (GraphPad Prism). | ChEMBL. | No reference |
IC50 (binding) | < 1000000 nM | BindingDB_Patents: Glycine Uptake Assay. [3H]-Glycine uptake into recombinant CHO cells expressing human GlyT1: Human GlyT1c expressing recombinant hGlyT1c5_CHO cells were plated at 20,000 cells per well in 96 well Cytostar-T scintillation microplates (Amersham Biosciences) and cultured to sub-confluency for 24 h. For glycine uptake assays the culture medium was aspirated and the cells were washed once with 100 ul HBSS (Gibco BRL, #14025-050) with 5 mM L-Alanine (Merck #1007). 80 ul HBSS buffer were added, followed by 10 ul inhibitor or vehicle (10% DMSO) and 10 ul [3H]-glycine (TRK71, Amersham Biosciences) to a final concentration of 200 nM for initiation of glycine uptake. The plates were placed in a Wallac Microbeta (PerkinElmer) and continuously counted by solid phase scintillation spectrometry during up to 3 hours. Nonspecific uptake was determined in the presence of 10 uM Org24598. IC50 calculations were made by four-parametric logistic nonlinear regression analysis (GraphPad Prism). | ChEMBL. | No reference |
Ki (binding) | < 10000 nM | BindingDB_Patents: Radioligand Binding Assay. Radioligand binding to human GlyT1c transporter-expressing membranes was carried out as described in Mezler et al., Molecular Pharmacology 74:1705-1715, 2008. | ChEMBL. | No reference |
Ki (binding) | < 10000 nM | BindingDB_Patents: Radioligand Binding Assay. Radioligand binding to human GlyT1c transporter-expressing membranes was carried out as described in Mezler et al., Molecular Pharmacology 74:1705-1715, 2008. | 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.