Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Rattus norvegicus | P2X purinoceptor 2 | 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 2 | 472 aa | 449 aa | 25.2 % |
Echinococcus multilocularis | p2X purinoceptor 4 | P2X purinoceptor 2 | 472 aa | 463 aa | 26.4 % |
Echinococcus granulosus | p2X purinoceptor 4 | P2X purinoceptor 2 | 472 aa | 439 aa | 25.7 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Trichomonas vaginalis | ral, putative | 0.0121 | 1 | 0.5 |
Trichomonas vaginalis | dexras1, putative | 0.0121 | 1 | 0.5 |
Schistosoma mansoni | P2X receptor subunit | 0.0082 | 0.5752 | 1 |
Trichomonas vaginalis | GTP-binding protein rit, putative | 0.0121 | 1 | 0.5 |
Loa Loa (eye worm) | Ras protein let-60 | 0.0121 | 1 | 1 |
Echinococcus multilocularis | p2X purinoceptor 4 | 0.0082 | 0.5752 | 0.5752 |
Schistosoma mansoni | P2X receptor subunit | 0.0082 | 0.5752 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0121 | 1 | 1 |
Echinococcus multilocularis | p2X purinoceptor 4 | 0.0082 | 0.5752 | 0.5752 |
Entamoeba histolytica | Ras family GTPase | 0.0121 | 1 | 0.5 |
Echinococcus multilocularis | ras gtpase | 0.0121 | 1 | 1 |
Onchocerca volvulus | Bile acid receptor homolog | 0.0029 | 0 | 0.5 |
Schistosoma mansoni | P2X receptor subunit | 0.0082 | 0.5752 | 1 |
Onchocerca volvulus | Steroid hormone receptor family member cnr14 homolog | 0.0029 | 0 | 0.5 |
Echinococcus granulosus | ras gtpase | 0.0121 | 1 | 1 |
Entamoeba histolytica | ras-1, putative | 0.0121 | 1 | 0.5 |
Echinococcus granulosus | p2X purinoceptor 4 | 0.0082 | 0.5752 | 0.5752 |
Trichomonas vaginalis | ras-dva small GTPase, putative | 0.0121 | 1 | 0.5 |
Onchocerca volvulus | 0.0029 | 0 | 0.5 | |
Trichomonas vaginalis | rap1 and, putative | 0.0121 | 1 | 0.5 |
Echinococcus multilocularis | p2X purinoceptor 4 | 0.0082 | 0.5752 | 0.5752 |
Onchocerca volvulus | Protein ultraspiracle homolog | 0.0029 | 0 | 0.5 |
Schistosoma mansoni | P2X receptor subunit | 0.0082 | 0.5752 | 1 |
Echinococcus granulosus | p2X purinoceptor 4 | 0.0082 | 0.5752 | 0.5752 |
Echinococcus granulosus | p2X purinoceptor 4 | 0.0082 | 0.5752 | 0.5752 |
Trichomonas vaginalis | rheb, putative | 0.0121 | 1 | 0.5 |
Brugia malayi | Ras-related protein R-Ras2 | 0.0121 | 1 | 1 |
Entamoeba histolytica | Ras family GTPase | 0.0121 | 1 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (functional) | Antagonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization up to 300 uM by FLUOstar plate reader | ChEMBL. | 18630897 | |
IC50 (functional) | = 4.4 | Antagonist activity against rat P2X2 receptor expressed in Xenopus laevis oocyte assessed as inhibition of alpha, beta-meATP-induced inward current by two-electrode voltage-clamp electrophysiology | ChEMBL. | 21207957 |
IC50 (functional) | = 4 uM | Antagonist activity against rat P2X2 receptor expressed in Xenopus laevis oocyte assessed as inhibition of alpha, beta-meATP-induced inward current by two-electrode voltage-clamp electrophysiology | ChEMBL. | 21207957 |
IC50 (functional) | = 69 uM | Antagonist activity at human P2Y6 receptor expressed in human 1321N1 cells assessed as inhibition of UDP-induced intracellular calcium mobilization by NOVOstar plate reader | ChEMBL. | 18630897 |
IC50 (functional) | = 73 uM | Antagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate reader | ChEMBL. | 18630897 |
Ki (binding) | Inhibition of human NTPDase 8 expressed in COS7 cells | ChEMBL. | 18630897 | |
Ki (binding) | = 44.2 uM | Inhibition of rat NTPDase 2 | ChEMBL. | 18630897 |
Ki (binding) | = 46 uM | Inhibition of rat NTPDase 1 | ChEMBL. | 18630897 |
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.