Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Rattus norvegicus | Vanilloid receptor | Starlite/ChEMBL | References |
Homo sapiens | transient receptor potential cation channel, subfamily V, member 1 | Starlite/ChEMBL | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
CL (ADMET) | > 4000 ml/hr.kg | Clearance in iv dosed rat | ChEMBL. | 18299195 |
IC50 (functional) | = 0.65 nM | Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilization | ChEMBL. | 18299195 |
IC50 (functional) | = 0.65 nM | Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilization | ChEMBL. | 18299195 |
IC50 (functional) | = 4.8 nM | Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilization | ChEMBL. | 18299195 |
IC50 (functional) | = 4.8 nM | Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilization | ChEMBL. | 18299195 |
Solubility | < 0.0001 mg/ml | Solubility in phosphate buffered saline at pH 7.4 | ChEMBL. | 18299195 |
Solubility | = 0.003 mg/ml | Solubility in aqueous 0.01 N HCL | ChEMBL. | 18299195 |
Solubility | = 0.01 mg/ml | Solubility in simulated intestinal fluid at pH 6.8 | ChEMBL. | 18299195 |
t1/2 (ADMET) | = 0.7 hr | Half life in iv dosed rat | ChEMBL. | 18299195 |
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.