General Information of the Protein
Protein ID
PT01914
Protein Name
Transient receptor potential cation channel subfamily V member 1
Secondarily
Protein Name
Capsaicin receptor
Osm-9-like TRP channel 1
Vanilloid receptor 1
Vanilloid receptor type 1-like
Gene Name
TRPV1
Secondarily
Gene Name
Vr1
Vr1l
Sequence
MEQRASLDSEESESPPQENSCLDPPDRDPNCKPPPVKPHIFTTRSRTRLFGKGDSEEASPLDCPYEEGGLASCPIITVSSVLTIQRPGDGPASVRPSSQDSVSAGEKPPRLYDRRSIFDAVAQSNCQELESLLPFLQRSKKRLTDSEFKDPETGKTCLLKAMLNLHNGQNDTIALLLDVARKTDSLKQFVNASYTDSYYKGQTALHIAIERRNMTLVTLLVENGADVQAAANGDFFKKTKGRPGFYFGELPLSLAACTNQLAIVKFLLQNSWQPADISARDSVGNTVLHALVEVADNTVDNTKFVTSMYNEILILGAKLHPTLKLEEITNRKGLTPLALAASSGKIGVLAYILQREIHEPECRHLSRKFTEWAYGPVHSSLYDLSCIDTCEKNSVLEVIAYSSSETPNRHDMLLVEPLNRLLQDKWDRFVKRIFYFNFFVYCLYMIIFTAAAYYRPVEGLPPYKLKNTVGDYFRVTGEILSVSGGVYFFFRGIQYFLQRRPSLKSLFVDSYSEILFFVQSLFMLVSVVLYFSQRKEYVASMVFSLAMGWTNMLYYTRGFQQMGIYAVMIEKMILRDLCRFMFVYLVFLFGFSTAVVTLIEDGKNNSLPMESTPHKCRGSACKPGNSYNSLYSTCLELFKFTIGMGDLEFTENYDFKAVFIILLLAYVILTYILLLNMLIALMGETVNKIAQESKNIWKLQRAITILDTEKSFLKCMRKAFRSGKLLQVGFTPDGKDDYRWCFRVDEVNWTTWNTNVGIINEDPGNCEGVKRTLSFSLRSGRVSGRNWKNFALVPLLRDASTRDRHATQQEEVQLKHYTGSLKPEDAEVFKDSMVPGEK
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Organism
Rattus norvegicus, Rat
Protein Classification
Ion channel
>
Voltage-gated ion channel
>
Transient receptor potential channel
Function
Ligand-activated non-selective calcium permeant cation channel involved in detection of noxious chemical and thermal stimuli. Seems to mediate proton influx and may be involved in intracellular acidosis in nociceptive neurons. Involved in mediation of inflammatory pain and hyperalgesia. Sensitized by a phosphatidylinositol second messenger system activated by receptor tyrosine kinases, which involves PKC isozymes and PCL. Activation by vanilloids, like capsaicin, and temperatures higher than 42 degrees Celsius, exhibits a time- and Ca(2+)-dependent outward rectification, followed by a long-lasting refractory state. Mild extracellular acidic pH (6.5) potentiates channel activation by noxious heat and vanilloids, whereas acidic conditions (pH <6) directly activate the channel. Can be activated by endogenous compounds, including 12-hydroperoxytetraenoic acid and bradykinin. Acts as ionotropic endocannabinoid receptor with central neuromodulatory effects. Triggers a form of long-term depression (TRPV1-LTD) mediated by the endocannabinoid anandamine in the hippocampus and nucleus accumbens by affecting AMPA receptors endocytosis.
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Uniprot ID
Primary ID:
O35433

Secondarily ID:
Q920B3
Q920B4
Q9JLM0
Q9JM56
Q9JM57
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Subcellular Location
Postsynaptic cell membrane
Cell projection
Dendritic spine membrane
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000094 , 1321N1
Compound ID Compound Name Compound Formula
CP0462526
A-784168
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C19H15F6N3O3S
 1
1
IC50 = 17 nM
   TI
   LI
   LO
   TS
CP0522903
(R)-1-(1H-indazol-4-yl)-3-(5-(piperidin-1-yl)-2,3-dihydro-1H-inden-1-yl)urea
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C22H25N5O
 1
1
IC50 = 30 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0407471
3-[(4-tert-butylphenyl)methyl]-1-[(1R)-1-(4-methanesulfonamidophenyl)ethyl]thiourea
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C21H29N3O2S2
 1
1 EC50 > 100000 nM
CP0050997
N-[2-(4-chlorophenyl)ethyl]-7,8-dihydroxy-1,3,4,5-tetrahydro-2-benzazepine-2-carbothioamide
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C19H21ClN2O2S
 3
1 IC50 = 4 nM
2 IC50 = 365 nM
3 Ki = 1300 nM
CP0049976
(6E)-N-[(4-hydroxy-3-methoxyphenyl)methyl]-8-methylnon-6-enamide
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C18H27NO3
 2
1 IC50 = 19 nM
2 Ki = 1800 nM
CP0082813
1-Isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea
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C18H14F3N3O
 1
1 IC50 = 24 nM
CP0222429
RESINIFERATOXIN
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C37H40O9
 2
1 IC50 = 180 nM
2 Ki = 0.023 nM
CP0312254
US9120756, 17
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C24H28ClFN4O3S
 1
1 Ki = 0.1 nM
CP0451014
US9120756, 26
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C21H19ClF4N4O3S
 1
1 Ki = 0.1 nM
CP0396411
[(2S)-2-[(3,4-dimethylphenyl)methyl]-3-[[(1R)-1-[4-(methanesulfonamido)phenyl]ethyl]carbamothioylamino]propyl] 2,2-dimethylpropanoate
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C27H39N3O4S2
 1
1 Ki = 2.12 nM
CP0396410
[2-[(3,4-dimethylphenyl)methyl]-3-[[(1R)-1-[4-(methanesulfonamido)phenyl]ethyl]carbamothioylamino]propyl] 2,2-dimethylpropanoate
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C27H39N3O4S2
 1
1 Ki = 6.1 nM
CP0434050
2,2-Dimethyl-propionic acid 2-(4-tert-butyl-benzyl)-3-[3-(4-hydroxy-3-methoxy-benzyl)-thioureido]-propyl ester
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C28H40N2O4S
 1
1 Ki = 6.35 nM
CP0086120
[(2S)-2-[(4-tert-butylphenyl)methyl]-3-[[(1R)-1-[4-(methanesulfonamido)phenyl]ethyl]carbamothioylamino]propyl] 2,2-dimethylpropanoate
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C29H43N3O4S2
 1
1 Ki = 6.75 nM
CP0468548
[2-[(4-tert-butylphenyl)methyl]-3-[[(1R)-1-[4-(methanesulfonamido)phenyl]ethyl]carbamothioylamino]propyl] 2,2-dimethylpropanoate
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C29H43N3O4S2
 1
1 Ki = 10 nM
CP0086118
[(2R)-2-[(3,4-dimethylphenyl)methyl]-3-[[(1R)-1-[4-(methanesulfonamido)phenyl]ethyl]carbamothioylamino]propyl] 2,2-dimethylpropanoate
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C27H39N3O4S2
 1
1 Ki = 15.2 nM
CP0326468
2,2-Dimethyl-propionic acid 2-(3,4-dimethyl-benzyl)-3-[3-(4-hydroxy-3-methoxy-benzyl)-thioureido]-propyl ester
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C26H36N2O4S
 1
1 Ki = 17.4 nM
CP0302906
[(2R)-2-[(4-tert-butylphenyl)methyl]-3-[[(1R)-1-[4-(methanesulfonamido)phenyl]ethyl]carbamothioylamino]propyl] 2,2-dimethylpropanoate
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C29H43N3O4S2
 1
1 Ki = 17.9 nM
CP0168119
[(2S)-2-benzyl-3-[[(1R)-1-[4-(methanesulfonamido)phenyl]ethyl]carbamothioylamino]propyl] 2,2-dimethylpropanoate
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C25H35N3O4S2
 1
1 Ki = 19.4 nM
CP0061655
[(2R)-2-benzyl-3-[[(1R)-1-[4-(methanesulfonamido)phenyl]ethyl]carbamothioylamino]propyl] 2,2-dimethylpropanoate
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C25H35N3O4S2
 1
1 Ki = 22.7 nM
CP0245890
2,2-Dimethyl-propionic acid 2-(4-tert-butyl-benzyl)-3-[3-(4-methanesulfonylamino-3-methoxy-benzyl)-thioureido]-propyl ester
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C29H43N3O5S2
 1
1 Ki = 25.2 nM
CP0118931
2,2-Dimethyl-propionic acid 2-(3,4-dimethyl-benzyl)-3-[3-(4-methanesulfonylamino-benzyl)-thioureido]-propyl ester
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C26H37N3O4S2
 1
1 Ki = 29.3 nM
CP0302904
[(2R)-2-[(3,4-dimethylphenyl)methyl]-3-[[4-(methanesulfonamido)phenyl]methylcarbamothioylamino]propyl] 2,2-dimethylpropanoate
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C26H37N3O4S2
 1
1 Ki = 29.3 nM
CP0116650
[2-[(3,4-dimethylphenyl)methyl]-3-[1-[4-(methanesulfonamido)phenyl]ethylcarbamothioylamino]propyl] 2,2-dimethylpropanoate
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C27H39N3O4S2
 1
1 Ki = 37.2 nM
CP0302905
[2-[(4-tert-butylphenyl)methyl]-3-[1-[4-(methanesulfonamido)phenyl]ethylcarbamothioylamino]propyl] 2,2-dimethylpropanoate
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C29H43N3O4S2
 1
1 Ki = 42.7 nM
CP0118920
2,2-Dimethyl-propionic acid 2-(3,4-dimethyl-benzyl)-3-[3-(4-methanesulfonylamino-3-methoxy-benzyl)-thioureido]-propyl ester
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C27H39N3O5S2
 1
1 Ki = 49 nM
CP0245749
2-[(3,4-dimethylphenyl)methyl]-3-({[(3-fluoro-4-methanesulfonamidophenyl)methyl]carbamothioyl}amino)propyl 2,2-dimethylpropanoate
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C26H36FN3O4S2
 1
1 Ki = 54 nM
CP0363530
2,2-Dimethyl-propionic acid 2-(4-tert-butyl-benzyl)-3-[3-(4-methanesulfonylamino-benzyl)-thioureido]-propyl ester
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C28H41N3O4S2
 1
1 Ki = 64 nM
CP0282395
[(2R)-2-[(4-tert-butylphenyl)methyl]-3-[[4-(methanesulfonamido)phenyl]methylcarbamothioylamino]propyl] 2,2-dimethylpropanoate
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C28H41N3O4S2
 1
1 Ki = 64 nM
CP0402446
Benzoic acid 2-(4-tert-butyl-benzyl)-3-[3-(4-methanesulfonylamino-3-methoxy-benzyl)-thioureido]-propyl ester
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C31H39N3O5S2
 1
1 Ki = 77.2 nM
CP0147525
2,2-Dimethyl-propionic acid 2-(3,4-dimethyl-benzyl)-3-[3-(4-ethanesulfonylamino-benzyl)-thioureido]-propyl ester
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C27H39N3O4S2
 1
1 Ki = 108 nM
CP0340076
Benzoic acid 2-(3,4-dimethyl-benzyl)-3-[3-(4-methanesulfonylamino-3-methoxy-benzyl)-thioureido]-propyl ester
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C29H35N3O5S2
 1
1 Ki = 148 nM
CP0065232
2,2-Dimethyl-propionic acid 2-(3,4-dimethyl-benzyl)-3-{3-[4-(propane-2-sulfonylamino)-benzyl]-thioureido}-propyl ester
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C28H41N3O4S2
 1
1 Ki = 227 nM
CP0396409
[(2S)-2-benzyl-3-[[4-(methanesulfonamido)phenyl]methylcarbamothioylamino]propyl] 2,2-dimethylpropanoate
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C24H33N3O4S2
 1
1 Ki = 236 nM
CP0154431
Benzoic acid 2-(4-tert-butyl-benzyl)-3-[3-(4-methanesulfonylamino-benzyl)-thioureido]-propyl ester
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C30H37N3O4S2
 1
1 Ki = 239 nM
CP0248038
[(2R)-2-benzyl-3-[[4-(methanesulfonamido)phenyl]methylcarbamothioylamino]propyl] 2,2-dimethylpropanoate
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C24H33N3O4S2
 1
1 Ki = 252 nM
CP0556639
[(2S)-2-[[(1R)-1-[4-(methanesulfonamido)phenyl]ethyl]carbamothioylamino]-3-phenylpropyl] 2,2-dimethylpropanoate
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C24H33N3O4S2
 1
1 Ki = 272 nM
CP0065226
2,2-Dimethyl-propionic acid 2-(3,4-dimethyl-benzyl)-3-{3-[4-(propane-1-sulfonylamino)-benzyl]-thioureido}-propyl ester
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C28H41N3O4S2
 1
1 Ki = 313 nM
CP0222332
2,2-Dimethyl-propionic acid 2-(3,4-dimethyl-benzyl)-3-[3-(3-methanesulfonylamino-benzyl)-thioureido]-propyl ester
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C26H37N3O4S2
 1
1 Ki = 355 nM
CP0366899
Benzoic acid 2-(3,4-dimethyl-benzyl)-3-[3-(4-methanesulfonylamino-benzyl)-thioureido]-propyl ester
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C28H33N3O4S2
 1
1 Ki = 410 nM
CP0508053
[(2R)-2-[[(1R)-1-[4-(methanesulfonamido)phenyl]ethyl]carbamothioylamino]-3-phenylpropyl] 2,2-dimethylpropanoate
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C24H33N3O4S2
 1
1 Ki = 420 nM
CP0061656
[(2S)-2-benzyl-3-[[(1S)-1-[4-(methanesulfonamido)phenyl]ethyl]carbamothioylamino]propyl] 2,2-dimethylpropanoate
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C25H35N3O4S2
 1
1 Ki = 710 nM
CP0248039
[(2R)-2-benzyl-3-[[(1S)-1-[4-(methanesulfonamido)phenyl]ethyl]carbamothioylamino]propyl] 2,2-dimethylpropanoate
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C25H35N3O4S2
 1
1 Ki = 1140 nM
CP0333259
2-[4-(2-Amino-ethoxy)-3-methoxy-phenyl]-N-[3-(3,4-dimethyl-phenyl)-propyl]-acetamide
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C22H30N2O3
 1
1 Ki = 1400 nM
CP0221907
2,2-Dimethyl-propionic acid 3-[3-(4-acetylamino-benzyl)-thioureido]-2-(3,4-dimethyl-benzyl)-propyl ester
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C27H37N3O3S
 1
1 Ki = 1700 nM
CP0079191
2,2-Dimethyl-propionic acid 2-(3,4-dimethyl-benzyl)-3-[3-(4-isobutyrylamino-benzyl)-thioureido]-propyl ester
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C29H41N3O3S
 1
1 Ki = 2600 nM
CP0038427
2,2-Dimethyl-propionic acid 2-(3,4-dimethyl-benzyl)-3-{3-[4-(methanesulfonylamino-methyl)-benzyl]-thioureido}-propyl ester
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C27H39N3O4S2
 1
1 Ki = 3000 nM
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT05119 Transient receptor potential cation channel subfamily V member 1 Mus musculus, Mouse