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 |
---|---|---|---|---|
Activity (functional) | Agonist activity at human VR1 expressed in HEK293 cells upto 4 uM | ChEMBL. | 16870426 | |
Activity (functional) | 0 | Agonist activity at human VR1 expressed in HEK293 cells upto 4 uM | ChEMBL. | 16870426 |
CL (ADMET) | = 23 ml/min.kg | Clearance in rat at 3 mg/kg, iv | ChEMBL. | 16870426 |
F (ADMET) | = 99 % | Bioavailability in rat at 3 mg/kg, iv | ChEMBL. | 16870426 |
IC50 (functional) | = 0.8 nM | Antagonist activity at human TRPV1 receptor assessed as inhibition of capsaicin-induced activation | ChEMBL. | 18662872 |
IC50 (functional) | = 1.1 nM | Antagonist activity against capsaicin-activated human VR1 by FLIPR assay | ChEMBL. | 16870426 |
IC50 (functional) | = 1.1 nM | Antagonist activity against capsaicin-activated human VR1 by FLIPR assay | ChEMBL. | 16870426 |
IC50 (functional) | = 1.1 nM | Antagonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as inhibition of capsazepine-induced calcium mobilization by FLIPR assay | ChEMBL. | 20307063 |
IC50 (binding) | = 1.1 nM | Inhibition of human TRPV1 | ChEMBL. | 20307063 |
IC50 (functional) | = 1.4 nM | Antagonist activity against low pH(5.0-5.5)-activated rat VR1 | ChEMBL. | 16870426 |
IC50 (functional) | = 1.4 nM | Antagonist activity against low pH(5.0-5.5)-activated rat VR1 | ChEMBL. | 16870426 |
Inhibition (binding) | = 8 % | Inhibition of human ERG potassium channel expressed in african green monkey COS7 cells at 3 uM by whole cell assay | ChEMBL. | 18662872 |
Inhibition (binding) | = 8 % | Inhibition of human ERG expressed in COS7 cells at 3 uM by electrophysiology assay | ChEMBL. | 20307063 |
T1/2 (ADMET) | = 8.1 hr | Half life in rat at 3 mg/kg, iv | ChEMBL. | 16870426 |
Tmax (ADMET) | = 0.7 hr | Tmax in rat at 3 mg/kg, iv | ChEMBL. | 16870426 |
Vdss (ADMET) | = 12.5 L/Kg | Volume of distribution in rat at 3 mg/kg, iv | ChEMBL. | 16870426 |
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.
3 literature references were collected for this gene.