Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | perforin 1 (pore forming protein) | Starlite/ChEMBL | References |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Schistosoma mansoni | glutaminyl cyclase (M28 family) | 0.057 | 1 | 1 |
Toxoplasma gondii | peptidase, M28 family protein | 0.0091 | 0 | 0.5 |
Mycobacterium tuberculosis | Conserved protein | 0.0091 | 0 | 0.5 |
Trichomonas vaginalis | conserved hypothetical protein | 0.0091 | 0 | 0.5 |
Trichomonas vaginalis | Clan MH, family M28, aminopeptidase S-like metallopeptidase | 0.0091 | 0 | 0.5 |
Trypanosoma cruzi | glutaminyl cyclase, putative | 0.0091 | 0 | 0.5 |
Trichomonas vaginalis | conserved hypothetical protein | 0.0091 | 0 | 0.5 |
Onchocerca volvulus | Glutaminyl cyclase homolog | 0.057 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.057 | 1 | 1 |
Echinococcus multilocularis | glutaminyl peptide cyclotransferase | 0.057 | 1 | 1 |
Mycobacterium tuberculosis | Probable lipoprotein aminopeptidase LpqL | 0.0091 | 0 | 0.5 |
Mycobacterium ulcerans | lipoprotein aminopeptidase LpqL | 0.0091 | 0 | 0.5 |
Trypanosoma cruzi | glutaminyl cyclase, putative | 0.0091 | 0 | 0.5 |
Echinococcus granulosus | glutaminyl peptide cyclotransferase | 0.057 | 1 | 1 |
Mycobacterium ulcerans | hypothetical protein | 0.0091 | 0 | 0.5 |
Leishmania major | glutaminyl cyclase, putative | 0.0091 | 0 | 0.5 |
Trichomonas vaginalis | conserved hypothetical protein | 0.0091 | 0 | 0.5 |
Trypanosoma brucei | glutaminyl cyclase, putative | 0.0091 | 0 | 0.5 |
Toxoplasma gondii | hypothetical protein | 0.0091 | 0 | 0.5 |
Leishmania major | hypothetical protein, conserved | 0.0091 | 0 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 1.14 uM | Inhibition of recombinant perforin (unknown origin)-mediated lysis of human [51Cr]-labelled Jurkat cells assessed as release of [51Cr] preincubated for 30 mins followed by addition of cells measured after 4 hrs by gamma counting analysis | ChEMBL. | 24195776 |
Inhibition (binding) | = 34 % | Inhibition of perforin-mediated lysis of human [51Cr]-labeled K562 cells assessed as release of [51Cr] at 5 uM preincubated for 20 mins with human KHYG-1 cells followed by addition of human [51Cr]-labeled K562 cells measured after 4 hrs by gamma counting analysis in presence of 10% mouse serum | ChEMBL. | 24195776 |
Inhibition (functional) | = 40 % | Inhibition of perforin pore formation in human HeLa cells at 20 uM preincubated for 10 mins with Fluo-4AM labelled human NK cells followed by HeLa cells addition by propidium iodide staining-based real-time microscopy | ChEMBL. | 24195776 |
Inhibition (binding) | = 51 % | Inhibition of perforin-mediated lysis of human [51Cr]-labeled K562 cells assessed as release of [51Cr] at 5 uM preincubated for 20 mins with human KHYG-1 cells followed by addition of human [51Cr]-labeled K562 cells measured after 4 hrs by gamma counting analysis in absence of mouse serum | ChEMBL. | 24195776 |
Inhibition (binding) | = 81 % | Inhibition of perforin-mediated lysis of human [51Cr]-labeled K562 cells assessed as release of [51Cr] at 20 uM preincubated for 20 mins with human KHYG-1 cells followed by addition of human [51Cr]-labeled K562 cells measured after 4 hrs by gamma counting analysis in presence of 10% mouse serum | ChEMBL. | 24195776 |
Inhibition (binding) | = 83 % | Inhibition of perforin-mediated lysis of human [51Cr]-labeled K562 cells assessed as release of [51Cr] at 20 uM preincubated for 20 mins with human KHYG-1 cells followed by addition of human [51Cr]-labeled K562 cells measured after 4 hrs by gamma counting analysis in absence of mouse serum | ChEMBL. | 24195776 |
MTD (ADMET) | = 40 mg kg-1 | Toxicity in ip dosed C57BL/6 mouse administered as bid for 3 days measured after 4 days of post dose | ChEMBL. | 24195776 |
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.