Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | arachidonate 5-lipoxygenase-activating protein | Starlite/ChEMBL | No references |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Schistosoma mansoni | hypothetical protein | 0.008 | 0.2289 | 0.2214 |
Loa Loa (eye worm) | RNA recognition domain-containing protein domain-containing protein | 0.0094 | 0.2843 | 0.6943 |
Toxoplasma gondii | MAPEG family protein | 0.0135 | 0.4538 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0037 | 0.054 | 0.112 |
Echinococcus multilocularis | Basic leucine zipper (bZIP) transcription | 0.008 | 0.2289 | 0.1699 |
Schistosoma mansoni | membrane associated proteins in eicosanoid and glutathione metabolism family member | 0.0135 | 0.4538 | 0.4485 |
Schistosoma mansoni | tar DNA-binding protein | 0.0094 | 0.2843 | 0.2773 |
Echinococcus granulosus | microsomal glutathione S transferase 3 | 0.0135 | 0.4538 | 0.4121 |
Echinococcus multilocularis | Lysosomal Pro X carboxypeptidase | 0.0269 | 1 | 1 |
Schistosoma mansoni | subfamily S9B unassigned peptidase (S09 family) | 0.0123 | 0.4052 | 0.3994 |
Leishmania major | dipeptidyl-peptidase 8-like serine peptidase, putative,serine peptidase, Clan SC, Family S9B | 0.0041 | 0.071 | 1 |
Brugia malayi | Corticotropin releasing factor receptor 2 precursor, putative | 0.0039 | 0.0596 | 0.1472 |
Toxoplasma gondii | dipeptidyl peptidase iv (dpp iv) n-terminal region domain-containing protein | 0.0041 | 0.071 | 0.0426 |
Echinococcus multilocularis | dipeptidyl aminopeptidaseprotein | 0.0123 | 0.4052 | 0.3597 |
Brugia malayi | latrophilin 2 splice variant baaae | 0.0026 | 0.0097 | 0.0239 |
Trypanosoma brucei | Dipeptidyl-peptidase 8-like, putative | 0.0041 | 0.071 | 1 |
Schistosoma mansoni | tar DNA-binding protein | 0.0094 | 0.2843 | 0.2773 |
Schistosoma mansoni | tar DNA-binding protein | 0.0094 | 0.2843 | 0.2773 |
Brugia malayi | hypothetical protein | 0.008 | 0.2289 | 0.5649 |
Schistosoma mansoni | transcription factor LCR-F1 | 0.008 | 0.2289 | 0.2214 |
Echinococcus granulosus | dipeptidyl aminopeptidaseprotein | 0.0123 | 0.4052 | 0.3597 |
Schistosoma mansoni | dipeptidyl-peptidase 9 (S09 family) | 0.0041 | 0.071 | 0.0619 |
Schistosoma mansoni | tar DNA-binding protein | 0.0094 | 0.2843 | 0.2773 |
Entamoeba histolytica | hypothetical protein | 0.008 | 0.2289 | 0.5 |
Brugia malayi | prolyl oligopeptidase family protein | 0.0123 | 0.4052 | 1 |
Brugia malayi | hypothetical protein | 0.0032 | 0.0311 | 0.0767 |
Loa Loa (eye worm) | hypothetical protein | 0.0039 | 0.0596 | 0.1263 |
Brugia malayi | prolyl oligopeptidase family protein | 0.0041 | 0.071 | 0.1752 |
Loa Loa (eye worm) | prolyl oligopeptidase | 0.0123 | 0.4052 | 1 |
Brugia malayi | TAR-binding protein | 0.0094 | 0.2843 | 0.7016 |
Plasmodium falciparum | ataxin-2 like protein, putative | 0.0037 | 0.054 | 0.5 |
Onchocerca volvulus | Dipeptidyl peptidase family member 1 homolog | 0.0123 | 0.4052 | 0.5 |
Entamoeba histolytica | hypothetical protein | 0.008 | 0.2289 | 0.5 |
Brugia malayi | RNA binding protein | 0.0094 | 0.2843 | 0.7016 |
Brugia malayi | MH2 domain containing protein | 0.0093 | 0.2799 | 0.6907 |
Plasmodium vivax | ataxin-2 like protein, putative | 0.0037 | 0.054 | 0.5 |
Trypanosoma brucei | serine peptidase, Clan SC, Family S9B | 0.0041 | 0.071 | 1 |
Loa Loa (eye worm) | TAR-binding protein | 0.0094 | 0.2843 | 0.6943 |
Echinococcus multilocularis | microsomal glutathione S transferase 3 | 0.0135 | 0.4538 | 0.4121 |
Loa Loa (eye worm) | pigment dispersing factor receptor c | 0.0039 | 0.0596 | 0.1263 |
Echinococcus multilocularis | tar DNA binding protein | 0.0094 | 0.2843 | 0.2296 |
Trypanosoma cruzi | serine peptidase, Clan SC, Family S9B | 0.0041 | 0.071 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0032 | 0.0311 | 0.0542 |
Loa Loa (eye worm) | MH2 domain-containing protein | 0.0093 | 0.2799 | 0.6832 |
Plasmodium falciparum | ataxin-2 like protein, putative | 0.0037 | 0.054 | 0.5 |
Brugia malayi | RNA recognition motif domain containing protein | 0.0094 | 0.2843 | 0.7016 |
Entamoeba histolytica | hypothetical protein | 0.008 | 0.2289 | 0.5 |
Loa Loa (eye worm) | RNA binding protein | 0.0094 | 0.2843 | 0.6943 |
Echinococcus granulosus | tar DNA binding protein | 0.0094 | 0.2843 | 0.2296 |
Schistosoma mansoni | family S28 unassigned peptidase (S28 family) | 0.0269 | 1 | 1 |
Loa Loa (eye worm) | transcription factor SMAD2 | 0.0093 | 0.2799 | 0.6832 |
Entamoeba histolytica | hypothetical protein | 0.008 | 0.2289 | 0.5 |
Brugia malayi | Calcitonin receptor-like protein seb-1 | 0.0039 | 0.0596 | 0.1472 |
Brugia malayi | hypothetical protein | 0.0037 | 0.054 | 0.1332 |
Echinococcus granulosus | Basic leucine zipper bZIP transcription | 0.008 | 0.2289 | 0.1699 |
Schistosoma mansoni | tar DNA-binding protein | 0.0094 | 0.2843 | 0.2773 |
Trypanosoma cruzi | dipeptidyl-peptidase 8-like serine peptidase | 0.0041 | 0.071 | 1 |
Schistosoma mansoni | microsomal glutathione s-transferase | 0.0135 | 0.4538 | 0.4485 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Ki (binding) | = 45 nM | BindingDB_Patents: Homogeneous Time Resolved Fluorescence Assay. FLAP-containing membranes were prepared as was a FITC-labeled FLAP modulator (3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl)-2,2-dimethylpropanoic acid). The FLAP binding assay is performed in HTRF format (homogeneous time resolved fluorescence). FLAP-containing membranes (1 µg/well final for human) are incubated in the presence of the HTRF ligand, [5-[({[2-(2-{3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropanoyl}hydrazino)-2-oxoethyl]sulfanyl}acetyl)amino]-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid] (25 nM final), a terbium labeled anti-His tag antibody (0.5 ng/well final, from Cisbio) and compounds. The reaction is allowed to proceed for two hours after which the plate is read on an Envision plate reader in HTRF mode. | ChEMBL. | No reference |
Ki (binding) | = 45 nM | BindingDB_Patents: Binding Assay. The assay below is used to test the modulatory activity of compounds against FLAP. Human and mouse FLAP-encoding DNA was amplified by polymerase chain reaction and cloned into pFastBac1 (Invitrogen) with a NH2-terminal 6-His tag for expression in Spodoptera frugiperda (Sf-9) cells. FLAP-containing membranes were prepared as was a FITC-labeled FLAP modulator (3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl)-2,2-dimethylpropanoic acid). The FLAP binding assay is performed in HTRF format (homogeneous time resolved fluorescence). FLAP-containing membranes (1 µg/well final for human) are incubated in the presence of the HTRF ligand, [5-[({[2-(2-{3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropanoyl}hydrazino)-2-oxoethyl]sulfanyl}acetyl)amino]-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid] (25 nM final), a terbium labeled anti-His tag antibody (0.5 ng/well final, from Cisbio) and compounds. | ChEMBL. | No reference |
Ki (binding) | = 45 nM | BindingDB_Patents: Binding Assay. The assay below is used to test the modulatory activity of compounds against FLAP. Human and mouse FLAP-encoding DNA was amplified by polymerase chain reaction and cloned into pFastBac1 (Invitrogen) with a NH2-terminal 6-His tag for expression in Spodoptera frugiperda (Sf-9) cells. FLAP-containing membranes were prepared as was a FITC-labeled FLAP modulator (3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl)-2,2-dimethylpropanoic acid). The FLAP binding assay is performed in HTRF format (homogeneous time resolved fluorescence). FLAP-containing membranes (1 µg/well final for human) are incubated in the presence of the HTRF ligand, [5-[({[2-(2-{3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropanoyl}hydrazino)-2-oxoethyl]sulfanyl}acetyl)amino]-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid] (25 nM final), a terbium labeled anti-His tag antibody (0.5 ng/well final, from Cisbio) and compounds. | ChEMBL. | No reference |
Ki (binding) | = 45 nM | BindingDB_Patents: Homogeneous Time Resolved Fluorescence Assay. FLAP-containing membranes were prepared as was a FITC-labeled FLAP modulator (3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl)-2,2-dimethylpropanoic acid). The FLAP binding assay is performed in HTRF format (homogeneous time resolved fluorescence). FLAP-containing membranes (1 µg/well final for human) are incubated in the presence of the HTRF ligand, [5-[({[2-(2-{3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropanoyl}hydrazino)-2-oxoethyl]sulfanyl}acetyl)amino]-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid] (25 nM final), a terbium labeled anti-His tag antibody (0.5 ng/well final, from Cisbio) and compounds. The reaction is allowed to proceed for two hours after which the plate is read on an Envision plate reader in HTRF mode. | 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.