Details of the Target

General Information of Target

Target ID LDTP09168
Target Name Transient receptor potential cation channel subfamily V member 1 (TRPV1)
Gene Name TRPV1
Gene ID 7442
Synonyms
VR1; Transient receptor potential cation channel subfamily V member 1; TrpV1; Capsaicin receptor; Osm-9-like TRP channel 1; OTRPC1; Vanilloid receptor 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MKKWSSTDLGAAADPLQKDTCPDPLDGDPNSRPPPAKPQLSTAKSRTRLFGKGDSEEAFP
VDCPHEEGELDSCPTITVSPVITIQRPGDGPTGARLLSQDSVAASTEKTLRLYDRRSIFE
AVAQNNCQDLESLLLFLQKSKKHLTDNEFKDPETGKTCLLKAMLNLHDGQNTTIPLLLEI
ARQTDSLKELVNASYTDSYYKGQTALHIAIERRNMALVTLLVENGADVQAAAHGDFFKKT
KGRPGFYFGELPLSLAACTNQLGIVKFLLQNSWQTADISARDSVGNTVLHALVEVADNTA
DNTKFVTSMYNEILMLGAKLHPTLKLEELTNKKGMTPLALAAGTGKIGVLAYILQREIQE
PECRHLSRKFTEWAYGPVHSSLYDLSCIDTCEKNSVLEVIAYSSSETPNRHDMLLVEPLN
RLLQDKWDRFVKRIFYFNFLVYCLYMIIFTMAAYYRPVDGLPPFKMEKTGDYFRVTGEIL
SVLGGVYFFFRGIQYFLQRRPSMKTLFVDSYSEMLFFLQSLFMLATVVLYFSHLKEYVAS
MVFSLALGWTNMLYYTRGFQQMGIYAVMIEKMILRDLCRFMFVYIVFLFGFSTAVVTLIE
DGKNDSLPSESTSHRWRGPACRPPDSSYNSLYSTCLELFKFTIGMGDLEFTENYDFKAVF
IILLLAYVILTYILLLNMLIALMGETVNKIAQESKNIWKLQRAITILDTEKSFLKCMRKA
FRSGKLLQVGYTPDGKDDYRWCFRVDEVNWTTWNTNVGIINEDPGNCEGVKRTLSFSLRS
SRVSGRHWKNFALVPLLREASARDRQSAQPEEVYLRQFSGSLKPEDAEVFKSPAASGEK
Target Type
Successful
Target Bioclass
Transporter and channel
Family
Transient receptor (TC 1.A.4) family, TrpV subfamily, TRPV1 sub-subfamily
Subcellular location
Postsynaptic cell membrane
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.
TTD ID
T83193
Uniprot ID
Q8NER1
DrugMap ID
TT50OG3
Ensemble ID
ENST00000399756.8
HGNC ID
HGNC:12716
ChEMBL ID
CHEMBL4794

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
DEL SNV: p.P619A .
HDMYZ SNV: p.P619A .
HUPT3 SNV: p.N629T .
IGR1 SNV: p.T259I; p.R368K .
KATOIII SNV: p.R622S .
KMCH1 SNV: p.E360D .
MCC13 SNV: p.G492R .
MFE319 SNV: p.I174T .
MOLT4 SNV: p.D129Y .
NCIH1155 SNV: p.S6N .
NCIH196 SNV: p.N420S .
RL952 SNV: p.A36T; p.E799D .
RVH421 SNV: p.P463L .
SF295 SNV: p.F522L .
TF1 SNV: p.T634A .

Probe(s) Labeling This Target

PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STS-1
 Probe Info  		N.A.  LDD0136  [1]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 9 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Acetaminophen Small molecular drug DB00316
Alpha-linolenic Acid Small molecular drug DB00132
Camphor Small molecular drug DB01744
Cannabidiol Small molecular drug DB09061
Capsaicin Small molecular drug D0U5CE
Icosapent Small molecular drug DB00159
Tramadol Small molecular drug DB00193
Capsicum Oleoresin . DB11131
Zucapsaicin . DB09120
Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cntx-4975 . D0XW8Y
Phase 2
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Resiniferatoxin Small molecular drug D05XJW
Sb-705498 Small molecular drug D0VJ5N
Dwp-05195 . D0FC8O
Grc-15300 . D0A3EX
Pac-14028 . D09BDE
Xen-d0501 . D04VQH
Phase 1
Click To Hide/Show 8 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Abt-102 Small molecular drug D00CMV
Grc-6211 Small molecular drug D00MAN
Jnj-39439335 Small molecular drug D0EM4S
Phe-377 Small molecular drug D0EK1C
Ca-011 . D0KK9D
Mr-1817 . D01SZA
Pf-3864086 . D02XGC
Sar-115740 . D0W8NP
Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
A-425619 Small molecular drug D07LRT
Investigative
Click To Hide/Show 83 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(5e,8e,11e,14e)-icosa-5,8,11,14-tetraenal Small molecular drug D0DL4Y
(E)-3-(4-tert-butyl-phenyl)-n-phenyl-acrylamide Small molecular drug D0Y7QY
(E)-octadec-9-enal Small molecular drug D0E4FJ
(R)-1-(1h-indazol-4-yl)-3-(1-p-tolylethyl)Urea Small molecular drug D09SXM
(S)-1-(1h-indazol-4-yl)-3-(1-p-tolylethyl)Urea Small molecular drug D0H6TX
1,3-dibenzyl Urea Small molecular drug D0GL2X
1-(4-bromo-benzyl)-3-quinazolin-8-yl-urea Small molecular drug D0D0DW
1-(Isoquinolin-5-yl)-3-(1-phenylpropyl)Urea Small molecular drug D0X8XU
1-(Isoquinolin-5-yl)-3-(4-morpholinobenzyl)Urea Small molecular drug D0J3VX
1-benzhydryl-3-(Isoquinolin-5-yl)Urea Small molecular drug D0SH1L
12s-hpete Small molecular drug D0F9NL
15s-hpete Small molecular drug D0KH9W
2-(4-pentylphenyl)-n-(Pyridin-3-yl)Acetamide Small molecular drug D09WYF
2-apb Small molecular drug D00HCI
4-(3-methylpyridin-2-yl)-n-p-tolylbenzamide Small molecular drug D09AZO
4-(Butyl(Methyl)Amino)-n-(Quinolin-3-yl)Benzamide Small molecular drug D0N8EI
4-(Cyclohexylamino)-n-(Quinolin-3-yl)Benzamide Small molecular drug D01WDS
4-(Hexyl(Methyl)Amino)-n-(Quinolin-3-yl)Benzamide Small molecular drug D08KYH
4-(Methyl(Nonyl)Amino)-n-(Quinolin-3-yl)Benzamide Small molecular drug D0WK3N
4-(Methyl(Octyl)Amino)-n-(Quinolin-3-yl)Benzamide Small molecular drug D06MRN
4-butyl-n-(7-hydroxynaphthalen-1-yl)Benzamide Small molecular drug D0DJ6G
4-butyl-n-(Isoquinolin-5-yl)Benzamide Small molecular drug D0BB7F
4-butyl-n-(Pyridin-3-yl)Benzamide Small molecular drug D00XZZ
4-butyl-n-(Quinolin-3-yl)Benzamide Small molecular drug D00ZWU
4-butyl-n-phenylbenzamide Small molecular drug D07LCG
4-decyl-n-(Pyridin-3-yl)Benzamide Small molecular drug D0C3XF
4-heptyl-n-(Pyridin-3-yl)Benzamide Small molecular drug D0H6GW
4-heptyl-n-(Quinolin-3-yl)Benzamide Small molecular drug D0Y9EU
4-hexyl-n-(Quinolin-3-yl)Benzamide Small molecular drug D0T8DR
4-nonyl-n-(Quinolin-3-yl)Benzamide Small molecular drug D08KRX
4-octyl-n-(Pyridin-3-yl)Benzamide Small molecular drug D0Q2ZO
4-octyl-n-(Quinolin-3-yl)Benzamide Small molecular drug D0D4SO
4-pentyl-n-pyridin-3-yl Benzamide Small molecular drug D08WAW
4-propyl-n-(Quinolin-3-yl)Benzamide Small molecular drug D0D9MW
4-pyridin-2-yl-piperazine-1-carboxylic Acid Amide Small molecular drug D00ESG
4-tert-butyl-n-(Quinolin-3-yl)Benzamide Small molecular drug D00RDS
5s-hete Small molecular drug D07CJR
5s-hpete Small molecular drug D0Q2LG
6'-iodononivamide Small molecular drug D05NTO
6-iodo-nordihydrocapsaicin Small molecular drug D08WTR
A-795614 Small molecular drug D07BKU
A778317 Small molecular drug D0BY9X
Agatoxin 489 Small molecular drug D0M7TC
Amg 9810 Small molecular drug D0XO2G
Amg-628 Small molecular drug D0W8UW
Amg-8563 Small molecular drug D04FFY
Arvanil Small molecular drug D0D7QH
Aspartame Small molecular drug DB00168
Atc-120 Small molecular drug D0SO5A
Bctc Small molecular drug D0P7VQ
Capsazepine Small molecular drug D0G8BN
Diphenylboronic Anhydride Small molecular drug D03TWR
Jnj-17203212 Small molecular drug D0DY4E
Kjm429 Small molecular drug D0VM5U
Lassbio-881 Small molecular drug D0F4LI
N-(4-iodophenyl)-4-(Trifluoromethoxy)Benzamide Small molecular drug D0W6TX
N-(4-iodophenyl)-4-(Trifluoromethyl)Benzamide Small molecular drug D0F4NA
N-(4-tert-butylphenyl)-4-(Pyridin-2-yl)Benzamide Small molecular drug D0W3VM
N-methyl-4-pentyl-n-(Pyridin-3-yl)Benzamide Small molecular drug D09BEW
N-[2-(5-hydroxy-1h-indol-3-yl)Ethyl]Lauramide Small molecular drug D0R8XX
N-[2-(5-hydroxy-1h-indol-3-yl)Ethyl]Linoleamide Small molecular drug D0E2XP
N-[2-(5-hydroxy-1h-indol-3-yl)Ethyl]Undecanamide Small molecular drug D03SJY
Nabiximols Small molecular drug DB14011
Nada Small molecular drug D07YQG
Ne-28345 Small molecular drug D0P0MN
Phenylacetylrinvanil Small molecular drug D02ANZ
Ppahv Small molecular drug D06CDW
Pyrrolidin-1-yl-thiourea Small molecular drug D03KQG
Sb-782443 Small molecular drug D0L9DR
Sb452533 Small molecular drug D0U3WK
Sc-0030 Small molecular drug D0X7AM
[125i]Resiniferatoxin Small molecular drug D04IJB
[3h]A778317 Small molecular drug D0D2FP
(S)-camphor . DB11345
A-993610 . D0M7NA
Abt-116 . D05APW
Asp-8370 . D0J8NC
Cannabidivarin . DB14050
Kmj-372 . D02GNL
Medical Cannabis . DB14009
Nonivamide . DB11324
Propacetamol . DB09288
Ricinoleic Acid . DB02955
Patented
Click To Hide/Show 162 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid25666693-compound-1 Small molecular drug D0KB2Z
Pmid25666693-compound-10 Small molecular drug D0C1MZ
Pmid25666693-compound-100 Small molecular drug D0Y1SI
Pmid25666693-compound-101 Small molecular drug D0F3HP
Pmid25666693-compound-102 Small molecular drug D0IK1S
Pmid25666693-compound-103 Small molecular drug D01LGQ
Pmid25666693-compound-104 Small molecular drug D01RUK
Pmid25666693-compound-105 Small molecular drug D0ZP2C
Pmid25666693-compound-106 Small molecular drug D0R2VB
Pmid25666693-compound-107 Small molecular drug D0ZE1M
Pmid25666693-compound-108 Small molecular drug D0D4NX
Pmid25666693-compound-109 Small molecular drug D0MY3K
Pmid25666693-compound-11 Small molecular drug D0HE7X
Pmid25666693-compound-110 Small molecular drug D0E0SA
Pmid25666693-compound-111 Small molecular drug D08YAL
Pmid25666693-compound-112 Small molecular drug D0PT0U
Pmid25666693-compound-113 Small molecular drug D0A8LU
Pmid25666693-compound-114 Small molecular drug D0C5NT
Pmid25666693-compound-115 Small molecular drug D0D2CF
Pmid25666693-compound-116 Small molecular drug D05SMP
Pmid25666693-compound-117 Small molecular drug D07FWF
Pmid25666693-compound-118 Small molecular drug D0EH2T
Pmid25666693-compound-119 Small molecular drug D07XVL
Pmid25666693-compound-12 Small molecular drug D0C8ZZ
Pmid25666693-compound-120 Small molecular drug D0WX4W
Pmid25666693-compound-121 Small molecular drug D00KTN
Pmid25666693-compound-122 Small molecular drug D0R2QV
Pmid25666693-compound-123 Small molecular drug D08CLA
Pmid25666693-compound-124 Small molecular drug D0DT7M
Pmid25666693-compound-125 Small molecular drug D0U5ON
Pmid25666693-compound-126 Small molecular drug D02EKO
Pmid25666693-compound-127 Small molecular drug D07MNI
Pmid25666693-compound-128 Small molecular drug D09SMA
Pmid25666693-compound-129 Small molecular drug D0PJ8O
Pmid25666693-compound-13 Small molecular drug D08ICT
Pmid25666693-compound-130 Small molecular drug D0DI1R
Pmid25666693-compound-131 Small molecular drug D07RYM
Pmid25666693-compound-132 Small molecular drug D0WT1W
Pmid25666693-compound-133 Small molecular drug D01GEK
Pmid25666693-compound-134 Small molecular drug D07XZR
Pmid25666693-compound-135 Small molecular drug D08UEC
Pmid25666693-compound-136 Small molecular drug D0O3TG
Pmid25666693-compound-137 Small molecular drug D0KM0W
Pmid25666693-compound-138 Small molecular drug D0CR0H
Pmid25666693-compound-139 Small molecular drug D0RC7L
Pmid25666693-compound-14 Small molecular drug D0R8GA
Pmid25666693-compound-140 Small molecular drug D02JQB
Pmid25666693-compound-141 Small molecular drug D0K0ZI
Pmid25666693-compound-142 Small molecular drug D0NH2M
Pmid25666693-compound-143 Small molecular drug D0G6IQ
Pmid25666693-compound-144 Small molecular drug D0Z5HH
Pmid25666693-compound-145 Small molecular drug D03VXP
Pmid25666693-compound-146 Small molecular drug D0N0QN
Pmid25666693-compound-147 Small molecular drug D0JT8B
Pmid25666693-compound-148 Small molecular drug D0K3KM
Pmid25666693-compound-149 Small molecular drug D00OLY
Pmid25666693-compound-15 Small molecular drug D0F4YX
Pmid25666693-compound-150 Small molecular drug D01DNH
Pmid25666693-compound-151 Small molecular drug D0YU9B
Pmid25666693-compound-152 Small molecular drug D0ZS3E
Pmid25666693-compound-153 Small molecular drug D0AQ3U
Pmid25666693-compound-154 Small molecular drug D04TIU
Pmid25666693-compound-155 Small molecular drug D0K3KE
Pmid25666693-compound-156 Small molecular drug D0N0TF
Pmid25666693-compound-157 Small molecular drug D0NV2M
Pmid25666693-compound-158 Small molecular drug D01HED
Pmid25666693-compound-159 Small molecular drug D0I3ZW
Pmid25666693-compound-16 Small molecular drug D0SD4G
Pmid25666693-compound-160 Small molecular drug D0Z4QQ
Pmid25666693-compound-161 Small molecular drug D0XX8R
Pmid25666693-compound-162 Small molecular drug D0LA0Q
Pmid25666693-compound-17 Small molecular drug D07JNJ
Pmid25666693-compound-18 Small molecular drug D0ZM8H
Pmid25666693-compound-19 Small molecular drug D0NM3D
Pmid25666693-compound-2 Small molecular drug D00YXA
Pmid25666693-compound-20 Small molecular drug D0HS1D
Pmid25666693-compound-21 Small molecular drug D0YR4E
Pmid25666693-compound-22 Small molecular drug D0JK2N
Pmid25666693-compound-23 Small molecular drug D02QJE
Pmid25666693-compound-24 Small molecular drug D0N2UQ
Pmid25666693-compound-25 Small molecular drug D0A3XC
Pmid25666693-compound-26 Small molecular drug D0EV3G
Pmid25666693-compound-27 Small molecular drug D0IR7H
Pmid25666693-compound-28 Small molecular drug D05SWL
Pmid25666693-compound-29 Small molecular drug D0M4WY
Pmid25666693-compound-3 Small molecular drug D06VYF
Pmid25666693-compound-30 Small molecular drug D0F4DI
Pmid25666693-compound-31 Small molecular drug D0JC8L
Pmid25666693-compound-32 Small molecular drug D0R9RP
Pmid25666693-compound-33 Small molecular drug D0W4AA
Pmid25666693-compound-34 Small molecular drug D0A0YI
Pmid25666693-compound-35 Small molecular drug D0NB5M
Pmid25666693-compound-36 Small molecular drug D0V3PI
Pmid25666693-compound-37 Small molecular drug D06JHW
Pmid25666693-compound-38 Small molecular drug D0TZ2W
Pmid25666693-compound-39 Small molecular drug D0X1OO
Pmid25666693-compound-4 Small molecular drug D0GZ4G
Pmid25666693-compound-40 Small molecular drug D09ZWU
Pmid25666693-compound-41 Small molecular drug D07EAV
Pmid25666693-compound-42 Small molecular drug D0DE5K
Pmid25666693-compound-43 Small molecular drug D0P9KJ
Pmid25666693-compound-44 Small molecular drug D04FRL
Pmid25666693-compound-45 Small molecular drug D0U8YZ
Pmid25666693-compound-46 Small molecular drug D0K4SZ
Pmid25666693-compound-47 Small molecular drug D0MU3S
Pmid25666693-compound-48 Small molecular drug D0IN5E
Pmid25666693-compound-49 Small molecular drug D0P5SB
Pmid25666693-compound-5 Small molecular drug D02OAH
Pmid25666693-compound-50 Small molecular drug D07FIY
Pmid25666693-compound-51 Small molecular drug D0B0WJ
Pmid25666693-compound-52 Small molecular drug D0IU1H
Pmid25666693-compound-53 Small molecular drug D0OA1P
Pmid25666693-compound-54 Small molecular drug D0U5CQ
Pmid25666693-compound-55 Small molecular drug D0G3UV
Pmid25666693-compound-56 Small molecular drug D07EGF
Pmid25666693-compound-57 Small molecular drug D0P0MR
Pmid25666693-compound-58 Small molecular drug D01PLJ
Pmid25666693-compound-59 Small molecular drug D0J9CS
Pmid25666693-compound-6 Small molecular drug D0O7IQ
Pmid25666693-compound-60 Small molecular drug D00QEZ
Pmid25666693-compound-61 Small molecular drug D03QAW
Pmid25666693-compound-62 Small molecular drug D0JX4I
Pmid25666693-compound-63 Small molecular drug D0O9GI
Pmid25666693-compound-64 Small molecular drug D0Y9ST
Pmid25666693-compound-65 Small molecular drug D0F5NQ
Pmid25666693-compound-66 Small molecular drug D0GV5G
Pmid25666693-compound-67 Small molecular drug D0YM1M
Pmid25666693-compound-68 Small molecular drug D0ZZ8F
Pmid25666693-compound-69 Small molecular drug D0E8UP
Pmid25666693-compound-7 Small molecular drug D0N9FJ
Pmid25666693-compound-70 Small molecular drug D03EEA
Pmid25666693-compound-71 Small molecular drug D03YFL
Pmid25666693-compound-72 Small molecular drug D0H6CX
Pmid25666693-compound-73 Small molecular drug D03FSF
Pmid25666693-compound-74 Small molecular drug D0DC4O
Pmid25666693-compound-75 Small molecular drug D0OC6A
Pmid25666693-compound-76 Small molecular drug D0CX4C
Pmid25666693-compound-77 Small molecular drug D0B4NI
Pmid25666693-compound-78 Small molecular drug D0DE5I
Pmid25666693-compound-79 Small molecular drug D09QXC
Pmid25666693-compound-8 Small molecular drug D0ON4M
Pmid25666693-compound-80 Small molecular drug D0H4TR
Pmid25666693-compound-81 Small molecular drug D0QP4N
Pmid25666693-compound-82 Small molecular drug D0EC3Z
Pmid25666693-compound-83 Small molecular drug D0UE9K
Pmid25666693-compound-84 Small molecular drug D08ZBB
Pmid25666693-compound-85 Small molecular drug D07BZW
Pmid25666693-compound-86 Small molecular drug D0O0UG
Pmid25666693-compound-87 Small molecular drug D0C9FN
Pmid25666693-compound-88 Small molecular drug D03SHM
Pmid25666693-compound-89 Small molecular drug D0V9RM
Pmid25666693-compound-9 Small molecular drug D0IP5E
Pmid25666693-compound-90 Small molecular drug D05ZWR
Pmid25666693-compound-91 Small molecular drug D0WJ8R
Pmid25666693-compound-92 Small molecular drug D0O6VU
Pmid25666693-compound-93 Small molecular drug D04HCS
Pmid25666693-compound-94 Small molecular drug D0IT4N
Pmid25666693-compound-95 Small molecular drug D00ODY
Pmid25666693-compound-96 Small molecular drug D0ZQ2W
Pmid25666693-compound-97 Small molecular drug D03ZOZ
Pmid25666693-compound-98 Small molecular drug D0KF3A
Pmid25666693-compound-99 Small molecular drug D05RBF
Discontinued
Click To Hide/Show 8 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Amg-517 Small molecular drug D0L5XI
Amg-8562 Small molecular drug D07IEM
Azd1386 Small molecular drug D04PMM
Da-5018 Small molecular drug D06GDH
Ngd-8243 Small molecular drug D0Z0PB
Bl-1872 . D01QIA
Jts-653 . D06PYP
Nuvanil . D00FJC

References

1 Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling. Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8551-6. doi: 10.1002/anie.201300683. Epub 2013 Jun 10.