Proteins > Transient receptor potential cation channel subfamily V member 4
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Transient receptor potential cation channel subfamily V member 4
A transient receptor potential cation channel TRPV4 that is encoded in the genome of rat. [OMA:Q9ERZ8, PRO:DNx]
Synonyms
TrpV4;
Osm-9-like TRP channel 4;
OTRPC4;
Vanilloid receptor-related osmotically-activated channel;
VR-OAC
Research
Bioassay Publications (13)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 3 (23.08) | 18.2507 |
| 2000's | 5 (38.46) | 29.6817 |
| 2010's | 3 (23.08) | 24.3611 |
| 2020's | 2 (15.38) | 2.80 |
Compounds (15)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| haloperidol | Rattus norvegicus (Norway rat) | Ki | 0.0050 | 1 | 1 |
| cannabidiol | Rattus norvegicus (Norway rat) | IC50 | 5.9000 | 1 | 1 |
| capsazepine | Rattus norvegicus (Norway rat) | IC50 | 162.9750 | 4 | 4 |
| hc-067047 | Rattus norvegicus (Norway rat) | IC50 | 0.1487 | 3 | 3 |
| rn 1734 | Rattus norvegicus (Norway rat) | IC50 | 3.2000 | 2 | 2 |
| iodoresiniferatoxin | Rattus norvegicus (Norway rat) | IC50 | 4.0000 | 1 | 1 |
| kjm 429 | Rattus norvegicus (Norway rat) | IC50 | 0.1100 | 2 | 2 |
| jyl 1421 | Rattus norvegicus (Norway rat) | IC50 | 0.0370 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| cannabinol | Rattus norvegicus (Norway rat) | EC50 | 16.1000 | 1 | 1 |
| nonivamide | Rattus norvegicus (Norway rat) | EC50 | 0.5500 | 2 | 2 |
| dihydrocapsaicin | Rattus norvegicus (Norway rat) | EC50 | 0.1900 | 1 | 1 |
| cannabidiol | Rattus norvegicus (Norway rat) | EC50 | 0.9000 | 1 | 1 |
| capsaicin | Rattus norvegicus (Norway rat) | EC50 | 0.2460 | 4 | 5 |
| capsazepine | Rattus norvegicus (Norway rat) | EC50 | 100.0000 | 1 | 1 |
| N-octylhomovanillamide | Rattus norvegicus (Norway rat) | EC50 | 0.3000 | 1 | 1 |
| olvanil | Rattus norvegicus (Norway rat) | EC50 | 0.1700 | 2 | 2 |
| ne 21610 | Rattus norvegicus (Norway rat) | EC50 | 0.2500 | 1 | 1 |
Analogues of capsaicin with agonist activity as novel analgesic agents; structure-activity studies. 2. The amide bond "B-region".Journal of medicinal chemistry, , Aug-06, Volume: 36, Issue:16, 1993
Analogues of capsaicin with agonist activity as novel analgesic agents; structure-activity studies. 3. The hydrophobic side-chain "C-region".Journal of medicinal chemistry, , Aug-06, Volume: 36, Issue:16, 1993
N-4-Substituted-benzyl-N'-tert-butylbenzyl thioureas as vanilloid receptor ligands: investigation on the role of methanesulfonamido group in antagonistic activity.Bioorganic & medicinal chemistry letters, , Feb-09, Volume: 14, Issue:3, 2004
Analogues of capsaicin with agonist activity as novel analgesic agents: structure-activity studies. 4. Potent, orally active analgesics.Journal of medicinal chemistry, , Dec-06, Volume: 39, Issue:25, 1996
Analogues of capsaicin with agonist activity as novel analgesic agents; structure-activity studies. 3. The hydrophobic side-chain "C-region".Journal of medicinal chemistry, , Aug-06, Volume: 36, Issue:16, 1993
Analogues of capsaicin with agonist activity as novel analgesic agents; structure-activity studies. 2. The amide bond "B-region".Journal of medicinal chemistry, , Aug-06, Volume: 36, Issue:16, 1993
N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands.Bioorganic & medicinal chemistry letters, , Apr-05, Volume: 14, Issue:7, 2004
N-4-Substituted-benzyl-N'-tert-butylbenzyl thioureas as vanilloid receptor ligands: investigation on the role of methanesulfonamido group in antagonistic activity.Bioorganic & medicinal chemistry letters, , Feb-09, Volume: 14, Issue:3, 2004
Synthesis of N,N',N"-trisubstituted thiourea derivatives and their antagonist effect on the vanilloid receptor.Bioorganic & medicinal chemistry letters, , Feb-24, Volume: 13, Issue:4, 2003
Chain-branched acyclic phenethylthiocarbamates as vanilloid receptor antagonists.Bioorganic & medicinal chemistry letters, , May-05, Volume: 13, Issue:9, 2003
Modulation of TRPV4 and BKCa for treatment of brain diseases.Bioorganic & medicinal chemistry, , 08-15, Volume: 28, Issue:16, 2020
Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.ACS medicinal chemistry letters, , May-11, Volume: 8, Issue:5, 2017
Pharmacological evaluation of novel (6-aminopyridin-3-yl)(4-(pyridin-2-yl)piperazin-1-yl) methanone derivatives as TRPV4 antagonists for the treatment of pain.Bioorganic & medicinal chemistry, , 04-01, Volume: 25, Issue:7, 2017
Modulation of TRPV4 and BKCa for treatment of brain diseases.Bioorganic & medicinal chemistry, , 08-15, Volume: 28, Issue:16, 2020
Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.ACS medicinal chemistry letters, , May-11, Volume: 8, Issue:5, 2017
Analogues of capsaicin with agonist activity as novel analgesic agents: structure-activity studies. 4. Potent, orally active analgesics.Journal of medicinal chemistry, , Dec-06, Volume: 39, Issue:25, 1996
Analogues of capsaicin with agonist activity as novel analgesic agents; structure-activity studies. 3. The hydrophobic side-chain "C-region".Journal of medicinal chemistry, , Aug-06, Volume: 36, Issue:16, 1993
N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands.Bioorganic & medicinal chemistry letters, , Apr-05, Volume: 14, Issue:7, 2004
N-4-Substituted-benzyl-N'-tert-butylbenzyl thioureas as vanilloid receptor ligands: investigation on the role of methanesulfonamido group in antagonistic activity.Bioorganic & medicinal chemistry letters, , Feb-09, Volume: 14, Issue:3, 2004