Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | receptor (TNFRSF)-interacting serine-threonine kinase 1 | Starlite/ChEMBL | References |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | eukaryotic-type carbonic anhydrase | 0.0245 | 0.2325 | 0.0749 |
Trypanosoma brucei | carbonic anhydrase-like protein | 0.0558 | 1 | 1 |
Toxoplasma gondii | hypothetical protein | 0.0245 | 0.2325 | 1 |
Schistosoma mansoni | carbonic anhydrase-related | 0.0245 | 0.2325 | 0.0749 |
Loa Loa (eye worm) | hypothetical protein | 0.0245 | 0.2325 | 0.0749 |
Mycobacterium tuberculosis | Beta-carbonic anhydrase CanB | 0.015 | 0 | 0.5 |
Onchocerca volvulus | 0.0219 | 0.1703 | 0.5 | |
Entamoeba histolytica | carbonic anhydrase, putative | 0.0264 | 0.2802 | 0.5 |
Schistosoma mansoni | carbonic anhydrase | 0.0264 | 0.2802 | 0.1325 |
Brugia malayi | Eukaryotic-type carbonic anhydrase family protein | 0.0245 | 0.2325 | 0.0749 |
Schistosoma mansoni | carbonic anhydrase-related | 0.0245 | 0.2325 | 0.0749 |
Loa Loa (eye worm) | hypothetical protein | 0.0245 | 0.2325 | 0.0749 |
Brugia malayi | Eukaryotic-type carbonic anhydrase family protein | 0.0245 | 0.2325 | 0.0749 |
Trypanosoma cruzi | carbonic anhydrase-like protein, putative | 0.0558 | 1 | 1 |
Leishmania major | carbonic anhydrase family protein, putative | 0.0264 | 0.2802 | 0.1325 |
Schistosoma mansoni | hypothetical protein | 0.0245 | 0.2325 | 0.0749 |
Mycobacterium leprae | CARBONIC ANHYDRASE (CARBONATE DEHYDRATASE) (CARBONIC DEHYDRATASE) | 0.0264 | 0.2802 | 0.5 |
Schistosoma mansoni | carbonic anhydrase II (carbonate dehydratase II) | 0.0558 | 1 | 1 |
Mycobacterium ulcerans | carbonic anhydrase | 0.0264 | 0.2802 | 0.5 |
Leishmania major | carbonic anhydrase-like protein | 0.0558 | 1 | 1 |
Schistosoma mansoni | carbonic anhydrase II (carbonate dehydratase II) | 0.0558 | 1 | 1 |
Trypanosoma cruzi | carbonic anhydrase-like protein, putative | 0.0558 | 1 | 1 |
Echinococcus granulosus | carbonic anhydrase II | 0.0558 | 1 | 1 |
Loa Loa (eye worm) | eukaryotic-type carbonic anhydrase | 0.0558 | 1 | 1 |
Brugia malayi | Carbonic anhydrase like protein 2 precursor | 0.0245 | 0.2325 | 0.0749 |
Schistosoma mansoni | carbonic anhydrase | 0.0245 | 0.2325 | 0.0749 |
Brugia malayi | Eukaryotic-type carbonic anhydrase family protein | 0.0245 | 0.2325 | 0.0749 |
Schistosoma mansoni | carbonic anhydrase-related | 0.0245 | 0.2325 | 0.0749 |
Plasmodium falciparum | carbonic anhydrase | 0.0245 | 0.2325 | 0.5 |
Loa Loa (eye worm) | carbonic anhydrase 3 | 0.0558 | 1 | 1 |
Brugia malayi | Carbonic anhydrase like protein 2 precursor | 0.0245 | 0.2325 | 0.0749 |
Brugia malayi | Putative carbonic anhydrase 5 precursor | 0.0558 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0245 | 0.2325 | 0.0749 |
Echinococcus multilocularis | carbonic anhydrase II | 0.0558 | 1 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 0.016 uM | Inhibition of human N-terminal His-GST-TEV-fused RIP1 kinase domain (1 to 375) autophosphorylation expressed in baculovirus infected insect Sf9 cells after 4 hrs by ADP-Glo luminescence assay | ChEMBL. | 24900635 |
IC50 (binding) | = 0.016 uM | Displacement of (14-(2-{[3-({2-{[4-(cyanomethyl)phenyl]amino}-6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-4-pyrimidinyl}amino)propyl]amino}-2-oxoethyl)-16,16,18,18-tetramethyl-6,7,7a,8a,9,10,16,18-octahydrobenzo[2'',3'']indolizino[8'',7'':5',6']pyrano[3',2':3,4]pyrido[1,2-a]indol-5-ium-2-sulfonate from human N-terminal His-GST-TEV-fused RIP1 kinase domain (1 to 375) expressed in baculovirus infected insect Sf9 cells preincubated for 10 mins followed by fluorescent ligand addition measured after 15 mins by fluorescence polarization assay | ChEMBL. | 24900635 |
IC50 (binding) | = 0.32 uM | Inhibition of RIP1 in human U937 cells assessed as prevention of TNFalpha/zVAD.fmk-induced necrotic cell death preincubated for 30 to 60 mins followed by TNF-alpha induction measured after overnight incubation by Cell Titer-Glo luminescence assay | ChEMBL. | 24900635 |
Ratio IC50 (binding) | = 10 | Ratio of IC50 for RIP1 in TNFalpha/zVAD.fmk-stimulated human U937 cells by Cell Titer-Glo luminescence assay to IC50 for human N-terminal His-GST-TEV-fused RIP1 kinase domain (1 to 375) expressed in baculovirus infected insect Sf9 cells by fluorescence polarization assay | ChEMBL. | 24900635 |
Ratio IC50 (binding) | = 10 | Ratio of IC50 for RIP1 in TNFalpha/zVAD.fmk-stimulated human U937 cells by Cell Titer-Glo luminescence assay to IC50 for human N-terminal His-GST-TEV-fused RIP1 kinase domain (1 to 375) expressed in baculovirus infected insect Sf9 cells by ADP-Glo luminescence assay | ChEMBL. | 24900635 |
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.