Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Rattus norvegicus | P2X purinoceptor 4 | Starlite/ChEMBL | References |
Homo sapiens | purinergic receptor P2X, ligand-gated ion channel, 2 | Starlite/ChEMBL | References |
Homo sapiens | purinergic receptor P2X, ligand-gated ion channel, 7 | Starlite/ChEMBL | References |
Homo sapiens | purinergic receptor P2X, ligand-gated ion channel, 1 | Starlite/ChEMBL | References |
Mus musculus | purinergic receptor P2X, ligand-gated ion channel 4 | Starlite/ChEMBL | References |
Homo sapiens | purinergic receptor P2X, ligand-gated ion channel, 4 | Starlite/ChEMBL | References |
Homo sapiens | purinergic receptor P2X, ligand-gated ion channel, 3 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Schistosoma japonicum | ko:K00599 protein arginine N-methyltransferase 5 [EC:2.1.1.-], putative | P2X purinoceptor 4 | 388 aa | 445 aa | 25.6 % |
Echinococcus granulosus | p2X purinoceptor 4 | purinergic receptor P2X, ligand-gated ion channel, 2 | 370 aa | 409 aa | 29.1 % |
Schistosoma japonicum | ko:K05218 purinergic receptor P2X, ligand-gated ion channel 4, putative | P2X purinoceptor 4 | 388 aa | 359 aa | 46.0 % |
Echinococcus granulosus | p2X purinoceptor 4 | purinergic receptor P2X, ligand-gated ion channel, 3 | 397 aa | 383 aa | 37.1 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | hypothetical protein | 0.1579 | 1 | 0.5 |
Echinococcus granulosus | acetylcholinesterase | 0.1579 | 1 | 1 |
Echinococcus granulosus | carboxylesterase 5A | 0.1579 | 1 | 1 |
Echinococcus granulosus | acetylcholinesterase | 0.1579 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.1579 | 1 | 0.5 |
Loa Loa (eye worm) | acetylcholinesterase 1 | 0.1579 | 1 | 0.5 |
Echinococcus multilocularis | acetylcholinesterase | 0.1579 | 1 | 1 |
Loa Loa (eye worm) | carboxylesterase | 0.1579 | 1 | 0.5 |
Echinococcus multilocularis | carboxylesterase 5A | 0.1579 | 1 | 1 |
Schistosoma mansoni | family S9 non-peptidase homologue (S09 family) | 0.1579 | 1 | 1 |
Brugia malayi | Carboxylesterase family protein | 0.1579 | 1 | 0.5 |
Echinococcus multilocularis | acetylcholinesterase | 0.1579 | 1 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (functional) | = 9 % | Antagonist activity at human P2X7 receptor at 10 uM by cell-based calcium influx assay | ChEMBL. | 23075067 |
Activity (functional) | = 13 % | Antagonist activity at human P2X2 receptor at 10 uM by cell-based calcium influx assay | ChEMBL. | 23075067 |
Activity (functional) | = 49 % | Antagonist activity at human P2X3 receptor at 10 uM by cell-based calcium influx assay | ChEMBL. | 23075067 |
IC50 (functional) | = 0.189 uM | Antagonist activity at human P2X4 receptor expressed in 1321N1 cells assessed as inhibition of ATP-induced cytosolic calcium influx compound preincubated for 30 mins before ATP treatment by Fluo-4 AM fluorescence method | ChEMBL. | 23075067 |
IC50 (binding) | = 0.189 uM | Antagonist activity at human P2X4 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced cytosolic calcium influx preincubated for 30 mins followed by ATP addition by Fluo-4 AM dye-based fluorescence assay | ChEMBL. | 24411477 |
IC50 (functional) | = 1.77 uM | Antagonist activity at mouse P2X4 receptor by cell-based calcium influx assay | ChEMBL. | 23075067 |
IC50 (functional) | = 2.1 uM | Antagonist activity at rat P2X4 receptor by cell-based calcium influx assay | ChEMBL. | 23075067 |
IC50 (functional) | = 6.52 uM | Antagonist activity at human P2X1 receptor by cell-based calcium influx assay | ChEMBL. | 23075067 |
IC50 (functional) | > 10 uM | Antagonist activity at human P2X7 receptor by cell-based calcium influx assay | ChEMBL. | 23075067 |
IC50 (functional) | = 10 uM | Antagonist activity at human P2X3 receptor by cell-based calcium influx assay | ChEMBL. | 23075067 |
IC50 (functional) | > 10 uM | Antagonist activity at human P2X2 receptor by cell-based calcium influx assay | ChEMBL. | 23075067 |
Inhibition (functional) | = 77 % | Antagonist activity at human P2X4 receptor expressed in 1321N1 cells assessed as inhibition of ATP-induced cytosolic calcium influx preincubated at 10 uM for 30 mins before ATP treatment by Fluo-4 AM fluorescence method | ChEMBL. | 23075067 |
Inhibition (binding) | = 77 % | Antagonist activity at human P2X4 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced cytosolic calcium influx at 100 uM preincubated for 30 mins followed by ATP addition by Fluo-4 AM dye-based fluorescence assay | ChEMBL. | 24411477 |
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.
2 literature references were collected for this gene.