General Information of the Protein
Protein ID
PT06117
Protein Name
Transient receptor potential cation channel subfamily M member 8
Secondarily
Protein Name
Long transient receptor potential channel 6
Transient receptor potential p8
Gene Name
TRPM8
Secondarily
Gene Name
Ltrpc6
Trpp8
Sequence
MSFEGARLSMRSRRNGTMGSTRTLYSSVSRSTDVSYSDSDLVNFIQANFKKRECVFFTRDSKAMENICKCGYAQSQHIEGTQINQNEKWNYKKHTKEFPTDAFGDIQFETLGKKGKYLRLSCDTDSETLYELLTQHWHLKTPNLVISVTGGAKNFALKPRMRKIFSRLIYIAQSKGAWILTGGTHYGLMKYIGEVVRDNTISRNSEENIVAIGIAAWGMVSNRDTLIRSCDDEGHFSAQYIMDDFTRDPLYILDNNHTHLLLVDNGCHGHPTVEAKLRNQLEKYISERTSQDSNYGGKIPIVCFAQGGGRETLKAINTSVKSKIPCVVVEGSGQIADVIASLVEVEDVLTSSMVKEKLVRFLPRTVSRLPEEEIESWIKWLKEILESSHLLTVIKMEEAGDEIVSNAISYALYKAFSTNEQDKDNWNGQLKLLLEWNQLDLASDEIFTNDRRWESADLQEVMFTALIKDRPKFVRLFLENGLNLQKFLTNEVLTELFSTHFSTLVYRNLQIAKNSYNDALLTFVWKLVANFRRSFWKEDRSSREDLDVELHDASLTTRHPLQALFIWAILQNKKELSKVIWEQTKGCTLAALGASKLLKTLAKVKNDINAAGESEELANEYETRAVELFTECYSNDEDLAEQLLVYSCEAWGGSNCLELAVEATDQHFIAQPGVQNFLSKQWYGEISRDTKNWKIILCLFIIPLVGCGLVSFRKKPIDKHKKLLWYYVAFFTSPFVVFSWNVVFYIAFLLLFAYVLLMDFHSVPHTPELILYALVFVLFCDEVRQWYMNGVNYFTDLWNVMDTLGLFYFIAGIVFRLHSSNKSSLYSGRVIFCLDYIIFTLRLIHIFTVSRNLGPKIIMLQRMLIDVFFFLFLFAVWMVAFGVARQGILRQNEQRWRWIFRSVIYEPYLAMFGQVPSDVDSTTYDFSHCTFSGNESKPLCVELDEHNLPRFPEWITIPLVCIYMLSTNILLVNLLVAMFGYTVGIVQENNDQVWKFQRYFLVQEYCNRLNIPFPFVVFAYFYMVVKKCFKCCCKEKNMESNACCFRNEDNETLAWEGVMKENYLVKINTKANDNSEEMRHRFRQLDSKLNDLKSLLKEIANNIK
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Organism
Mus musculus, Mouse
Protein Classification
Ion channel
>
Voltage-gated ion channel
>
Transient receptor potential channel
Function
Receptor-activated non-selective cation channel involved in detection of sensations such as coolness, by being activated by cold temperature below 25 degrees Celsius. Activated by icilin, eucalyptol, menthol, cold and modulation of intracellular pH. Involved in menthol sensation. Permeable for monovalent cations sodium, potassium, and cesium and divalent cation calcium. Temperature sensing is tightly linked to voltage-dependent gating. Activated upon depolarization, changes in temperature resulting in graded shifts of its voltage-dependent activation curves. The chemical agonists menthol functions as a gating modifier, shifting activation curves towards physiological membrane potentials. Temperature sensitivity arises from a tenfold difference in the activation energies associated with voltage-dependent opening and closing.
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Uniprot ID
Primary ID:
Q8R4D5

Secondarily ID:
E9Q165
Q148W9
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Subcellular Location
Cell membrane
Membrane raft
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: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0389437
4-hydroxy-N-[(S)-[4-(trifluoromethyl)phenyl]-[3-(trifluoromethyl)pyridin-2-yl]methyl]benzamide
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C21H14F6N2O2
 1
1
IC50 = 6 nM
   TI
   LI
   LO
   TS
CP0476724
N-[(S)-(3-fluoropyridin-2-yl)-[3-fluoro-4-(trifluoromethoxy)phenyl]methyl]-6-oxo-1H-pyridine-3-carboxamide
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C19H12F5N3O3
 1
1
IC50 = 9 nM
   TI
   LI
   LO
   TS
CP0389429
N-[(S)-(3-fluoropyridin-2-yl)-[4-(trifluoromethyl)phenyl]methyl]-6-oxo-1H-pyridine-3-carboxamide
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C19H13F4N3O2
 1
1
IC50 = 15 nM
   TI
   LI
   LO
   TS
CP0466273
6-[[(S)-[4-(trifluoromethyl)phenyl]-[3-(trifluoromethyl)pyridin-2-yl]methyl]carbamoyl]pyridine-3-carboxylic acid
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C21H13F6N3O3
 1
1
IC50 = 17 nM
   TI
   LI
   LO
   TS
CP0396486
6-methoxy-N-[(S)-[4-(trifluoromethyl)phenyl]-[3-(trifluoromethyl)pyridin-2-yl]methyl]pyridine-3-carboxamide
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C21H15F6N3O2
 1
1
IC50 = 24 nM
   TI
   LI
   LO
   TS
CP0389434
6-oxo-N-[(S)-[4-(trifluoromethyl)phenyl]-[3-(trifluoromethyl)pyridin-2-yl]methyl]-1H-pyridine-3-carboxamide
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C20H13F6N3O2
 1
1
IC50 = 27 nM
   TI
   LI
   LO
   TS
CP0390975
4-cyano-N-[(S)-[4-(trifluoromethyl)phenyl]-[3-(trifluoromethyl)pyridin-2-yl]methyl]benzamide
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C22H13F6N3O
 1
1
IC50 = 40 nM
   TI
   LI
   LO
   TS
CP0396485
N-[(S)-[3-fluoro-4-(trifluoromethyl)phenyl]-[3-(trifluoromethyl)pyridin-2-yl]methyl]benzamide
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C21H13F7N2O
 1
1
IC50 = 43 nM
   TI
   LI
   LO
   TS
CP0390976
N-[(S)-[3-fluoro-4-(trifluoromethyl)phenyl]-[3-(trifluoromethyl)pyridin-2-yl]methyl]quinoline-7-carboxamide
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C24H14F7N3O
 1
1
IC50 = 49 nM
   TI
   LI
   LO
   TS
CP0389426
N-[(S)-[4-(trifluoromethyl)phenyl]-[3-(trifluoromethyl)pyridin-2-yl]methyl]quinoline-7-carboxamide
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C24H15F6N3O
 1
1
IC50 = 53 nM
   TI
   LI
   LO
   TS
CP0396484
N-[(S)-[4-(trifluoromethyl)phenyl]-[3-(trifluoromethyl)pyridin-2-yl]methyl]pyridine-3-carboxamide
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C20H13F6N3O
 1
1
IC50 = 54 nM
   TI
   LI
   LO
   TS
CP0466390
N-[(S)-[4-(trifluoromethoxy)phenyl]-[3-(trifluoromethyl)pyridin-2-yl]methyl]quinoline-7-carboxamide
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C24H15F6N3O2
 1
1
IC50 = 67 nM
   TI
   LI
   LO
   TS
CP0389435
N-[(S)-quinolin-3-yl-[3-(trifluoromethyl)pyridin-2-yl]methyl]quinoline-7-carboxamide
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C26H17F3N4O
 1
1
IC50 = 119 nM
   TI
   LI
   LO
   TS
CP0466259
N-[(S)-(4-methylphenyl)-[3-(trifluoromethyl)pyridin-2-yl]methyl]quinoline-7-carboxamide
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C24H18F3N3O
 1
1
IC50 = 143 nM
   TI
   LI
   LO
   TS
CP0390973
1-[(S)-[4-(trifluoromethyl)phenyl]-[3-(trifluoromethyl)pyridin-2-yl]methyl]-3-[(2S)-1,1,1-trifluoropropan-2-yl]urea
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C18H14F9N3O
 1
1
IC50 = 145 nM
   TI
   LI
   LO
   TS
CP0390979
N-[(S)-[3-fluoro-4-(trifluoromethyl)phenyl]-[2-(trifluoromethyl)phenyl]methyl]quinoline-7-carboxamide
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C25H15F7N2O
 1
1
IC50 = 212 nM
   TI
   LI
   LO
   TS
CP0390977
N-[(S)-[3-(trifluoromethyl)phenyl]-[3-(trifluoromethyl)pyridin-2-yl]methyl]quinoline-7-carboxamide
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C24H15F6N3O
 1
1
IC50 = 218 nM
   TI
   LI
   LO
   TS
CP0555772
N-[(S)-(4-methoxyphenyl)-[3-(trifluoromethyl)pyridin-2-yl]methyl]quinoline-7-carboxamide
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C24H18F3N3O2
 1
1
IC50 = 224 nM
   TI
   LI
   LO
   TS
CP0548517
N-[(S)-(4-fluorophenyl)-[3-(trifluoromethyl)pyridin-2-yl]methyl]quinoline-7-carboxamide
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C23H15F4N3O
 1
1
IC50 = 225 nM
   TI
   LI
   LO
   TS
CP0446362
1-[(S)-(3-fluoropyridin-2-yl)-[4-(trifluoromethyl)phenyl]methyl]-3-[(2S)-1,1,1-trifluoropropan-2-yl]urea
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C17H14F7N3O
 1
1
IC50 = 234 nM
   TI
   LI
   LO
   TS
CP0390978
N-[(S)-(3-methylphenyl)-[3-(trifluoromethyl)pyridin-2-yl]methyl]quinoline-7-carboxamide
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C24H18F3N3O
 1
1
IC50 = 321 nM
   TI
   LI
   LO
   TS
CP0476725
N-[(S)-cyclohexyl-[3-(trifluoromethyl)pyridin-2-yl]methyl]quinoline-7-carboxamide
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C23H22F3N3O
 1
1
IC50 = 373 nM
   TI
   LI
   LO
   TS
CP0466371
N-[(S)-[4-(trifluoromethyl)phenyl]-[4-(trifluoromethyl)pyridin-3-yl]methyl]quinoline-7-carboxamide
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C24H15F6N3O
 1
1
IC50 = 663 nM
   TI
   LI
   LO
   TS
CP0493064
N-[(S)-phenyl-[3-(trifluoromethyl)pyridin-2-yl]methyl]quinoline-7-carboxamide
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C23H16F3N3O
 1
1
IC50 = 1260 nM
   TI
   LI
   LO
   TS
CP0446363
N-[(1S)-2-phenyl-1-[3-(trifluoromethyl)pyridin-2-yl]ethyl]quinoline-7-carboxamide
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C24H18F3N3O
 1
1
IC50 = 2050 nM
   TI
   LI
   LO
   TS
CP0466275
N-[(S)-pyridin-2-yl-[3-(trifluoromethyl)pyridin-2-yl]methyl]quinoline-7-carboxamide
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C22H15F3N4O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0492710
N-[(R)-1,3-thiazol-2-yl-[3-(trifluoromethyl)pyridin-2-yl]methyl]quinoline-7-carboxamide
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C20H13F3N4OS
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0396611
N-[(S)-(2-methylphenyl)-[3-(trifluoromethyl)pyridin-2-yl]methyl]quinoline-7-carboxamide
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C24H18F3N3O
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
   TS
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT00608 Transient receptor potential M8 protein Canis lupus familiaris, Dog, Canis familiaris
PT03065 Transient receptor potential cation channel subfamily M member 8 Homo sapiens, Human
PT05529 Transient receptor potential cation channel subfamily M member 8 Rattus norvegicus, Rat