Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | acetylcholinesterase (Yt blood group) | Starlite/ChEMBL | References |
Cavia porcellus | Serotonin 4 (5-HT4) receptor | Starlite/ChEMBL | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (functional) | = 20 % | Agonist activity at HA-tagged 5-HT4R (unknown origin) expressed in COS7 cells assessed as cAMP accumulation by HTRF assay | ChEMBL. | 25793650 |
IC50 (binding) | = 118 nM | Inhibition of human erythrocyte AChE pre-incubated for 5 mins before acetylthiocholine iodide substrate by Ellman' method | ChEMBL. | 25793650 |
Inhibition (binding) | = 26 % | Inhibition of equine serum BuChE at 10 uM pre-incubated for 5 mins before butyrylthiocholine iodide substrate by Ellman' method | ChEMBL. | 25793650 |
Inhibition (binding) | = 30 % | Inhibition of propidium iodide binding to peripheral anionic site of electric eel AChE at 10 uM incubated for 6 hrs by propidium competition assay | ChEMBL. | 25793650 |
Inhibition (binding) | = 69 % | Displacement of [3H]GR113808 from human 5-HT4R at 10 nM by radioligand binding assay | ChEMBL. | 25793650 |
Inhibition (binding) | = 100 % | Displacement of [3H]GR113808 from human 5-HT4R at 1 uM by radioligand binding assay | ChEMBL. | 25793650 |
Ki (binding) | = 2.5 nM | Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay | ChEMBL. | 25793650 |
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.