Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | transient receptor potential cation channel, subfamily V, member 1 | Starlite/ChEMBL | References |
Rattus norvegicus | Vanilloid receptor | Starlite/ChEMBL | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (binding) | Agonist activity at rat TRPV1 expressed in CHO cells assessed as stimulation of Ca2+ uptake | ChEMBL. | 23981530 | |
EC50 (binding) | Agonist activity at human TRPV1 expressed in CHO cells assessed as stimulation of Ca2+ uptake | ChEMBL. | 23981530 | |
EC50 (functional) | = 4.7 pM | Agonist activity at human TRPV1 expressed in HEK293 cells assessed as increase in intracellular calcium level | ChEMBL. | 19951840 |
Ki (binding) | = 1.66 nM | Displacement of [3H]RTX from rat TRPV1 expressed in CHO cells | ChEMBL. | 23981530 |
Ki (binding) | = 2.23 nM | Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-stimulated Ca2+ uptake | ChEMBL. | 23981530 |
Ki (binding) | = 49 nM | Displacement of [3H]RTX from human TRPV1 expressed in CHO cells | ChEMBL. | 23981530 |
Ki (binding) | = 189 nM | Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-stimulated Ca2+ uptake | ChEMBL. | 23981530 |
Ratio Ki (binding) | = 5 | Ratio of I-RTX Ki to compound Ki for rat TRPV1 expressed in CHO cells | ChEMBL. | 23981530 |
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.