Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | phenylethanolamine N-methyltransferase | Starlite/ChEMBL | References |
Bos taurus | Phenylethanolamine N-methyltransferase | Starlite/ChEMBL | References |
Rattus norvegicus | Adrenergic receptor alpha-2 | Starlite/ChEMBL | References |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | hypothetical protein | 0.0667 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0667 | 0.5 | 0.5 |
Loa Loa (eye worm) | NNMT/PNMT/TEMT family protein | 0.0667 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Kb (binding) | = 2.5 uM | Binding affinity to human dopamine D2 receptor | ChEMBL. | 26052807 |
Ki (binding) | = 5.14 | Inhibition of [3H]-clonidine binding to the rat alpha2-adrenoceptor | ChEMBL. | 10091706 |
Ki (binding) | = 5.87 | Inhibitory activity against bovine adrenal phenylethanolamine N-methyltransferase (PNMT) | ChEMBL. | 10091706 |
Ki (binding) | = 1.4 uM | In vitro inhibitory activity against bovine adrenal phenylethanolamine N-methyltransferase (PNMT) | ChEMBL. | 9888838 |
Ki (binding) | = 1.4 uM | In vitro inhibitory activity against bovine adrenal phenylethanolamine N-methyltransferase (PNMT) | ChEMBL. | 9888838 |
Ki (binding) | = 1.5 uM | Binding affinity to human PNMT | ChEMBL. | 17126018 |
Ki (binding) | = 1.5 uM | Inhibition of bovine PNMT by radiochemical assay | ChEMBL. | 18024134 |
Ki (binding) | = 1.5 uM | Binding affinity to human PNMT | ChEMBL. | 17126018 |
Ki (binding) | = 1.5 uM | Inhibition of bovine PNMT by radiochemical assay | ChEMBL. | 18024134 |
Ki (binding) | = 7.3 uM | In vitro inhibitory activity against Alpha-2 adrenergic receptor using [3H]-clonidine as radioligand in male Sparague-Dawley rats | ChEMBL. | 9888838 |
Ki (binding) | = 7.3 uM | Displacement of [3H]clonidine from adrenergic alpha2 receptor in Sprague-Dawley rat cortex membrane | ChEMBL. | 17126018 |
Ki (binding) | = 7.3 uM | In vitro inhibitory activity against Alpha-2 adrenergic receptor using [3H]-clonidine as radioligand in male Sparague-Dawley rats | ChEMBL. | 9888838 |
Ki (binding) | = 7.3 uM | Displacement of [3H]clonidine from adrenergic alpha2 receptor in Sprague-Dawley rat cortex membrane | ChEMBL. | 17126018 |
Log Ki (binding) | = 5.14 | Inhibition of [3H]-clonidine binding to the rat alpha2-adrenoceptor | ChEMBL. | 10091706 |
Log Ki (binding) | = 5.87 | Inhibitory activity against bovine adrenal phenylethanolamine N-methyltransferase (PNMT) | ChEMBL. | 10091706 |
Ratio Ki (binding) | = 21 | Ratio of Ki of drug to 1,2,3,4-tetrahydroisoquinoline for Sprague-Dawley rat adrenergic alpha2 receptor | ChEMBL. | 17126018 |
Ratio Ki (binding) | = 4.9 | Selectivity for human PNMT over Sprague-Dawley rat adrenergic alpha2 receptor | ChEMBL. | 17126018 |
Ratio Ki (binding) | = 21 | Ratio of Ki of drug to 1,2,3,4-tetrahydroisoquinoline for Sprague-Dawley rat adrenergic alpha2 receptor | ChEMBL. | 17126018 |
Selectivity (binding) | = 5.2 | Binding selectivity against PNMT and alpha2-adrenoceptors, measured as a ratio of respective in vitro Ki's. | ChEMBL. | 9888838 |
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.
5 literature references were collected for this gene.