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 |
---|---|---|---|---|
AUC (ADMET) | = 79 ng.hr/ml | AUC (0-infinity) in Sprague-Dawley rat at 5 mg/kg, po | ChEMBL. | 17585749 |
AUC (ADMET) | = 340 ng.hr/ml | AUC (0-infinity) in Sprague-Dawley rat at 2 mg/kg, iv | ChEMBL. | 17585749 |
CL (ADMET) | = 2.9 L/hr.Kg | Clearance in Sprague-Dawley rat at 2 mg/kg, iv | ChEMBL. | 17585749 |
Cmax (ADMET) | = 34 ng/ml | Cmax in Sprague-Dawley rat at 5 mg/kg, po | ChEMBL. | 17585749 |
EC50 (functional) | > 4 uM | Agonist activity at TRPV1 expressed in CHO cells | ChEMBL. | 17585749 |
EC50 (functional) | > 4 uM | Agonist activity at TRPV1 expressed in CHO cells | ChEMBL. | 17585749 |
F (ADMET) | = 5 % | Bioavailability in Sprague-Dawley rat at 5 mg/kg, po | ChEMBL. | 17585749 |
IC50 (functional) | = 1.9 nM | Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx | ChEMBL. | 17585749 |
IC50 (functional) | = 1.9 nM | Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx | ChEMBL. | 17585749 |
IC50 (functional) | = 2 nM | Antagonist activty at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx | ChEMBL. | 17585749 |
IC50 (functional) | = 2 nM | Antagonist activty at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx | ChEMBL. | 17585749 |
IC50 (functional) | = 6.9 nM | Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of acid-induced calcium influx | ChEMBL. | 17585749 |
IC50 (functional) | = 6.9 nM | Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of acid-induced calcium influx | ChEMBL. | 17585749 |
IC50 (functional) | = 22 nM | Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of acid-induced calcium influx | ChEMBL. | 17585749 |
IC50 (functional) | = 22 nM | Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of acid-induced calcium influx | ChEMBL. | 17585749 |
t1/2 (ADMET) | = 1.6 hr | Half life in Sprague-Dawley rat at 2 mg/kg, iv | ChEMBL. | 17585749 |
Tmax (ADMET) | = 0.5 hr | Tmax in Sprague-Dawley rat at 5 mg/kg, po | ChEMBL. | 17585749 |
Vss (ADMET) | = 3.1 L/Kg | Volume of distribution at steady state in Sprague-Dawley rat at 2 mg/kg, iv | ChEMBL. | 17585749 |
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.