General Information of the Protein
Protein ID
PT03065
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
MSFRAARLSMRNRRNDTLDSTRTLYSSASRSTDLSYSESDLVNFIQANFKKRECVFFTKDSKATENVCKCGYAQSQHMEGTQINQSEKWNYKKHTKEFPTDAFGDIQFETLGKKGKYIRLSCDTDAEILYELLTQHWHLKTPNLVISVTGGAKNFALKPRMRKIFSRLIYIAQSKGAWILTGGTHYGLMKYIGEVVRDNTISRSSEENIVAIGIAAWGMVSNRDTLIRNCDAEGYFLAQYLMDDFTRDPLYILDNNHTHLLLVDNGCHGHPTVEAKLRNQLEKYISERTIQDSNYGGKIPIVCFAQGGGKETLKAINTSIKNKIPCVVVEGSGQIADVIASLVEVEDALTSSAVKEKLVRFLPRTVSRLPEEETESWIKWLKEILECSHLLTVIKMEEAGDEIVSNAISYALYKAFSTSEQDKDNWNGQLKLLLEWNQLDLANDEIFTNDRRWESADLQEVMFTALIKDRPKFVRLFLENGLNLRKFLTHDVLTELFSNHFSTLVYRNLQIAKNSYNDALLTFVWKLVANFRRGFRKEDRNGRDEMDIELHDVSPITRHPLQALFIWAILQNKKELSKVIWEQTRGCTLAALGASKLLKTLAKVKNDINAAGESEELANEYETRAVELFTECYSSDEDLAEQLLVYSCEAWGGSNCLELAVEATDQHFIAQPGVQNFLSKQWYGEISRDTKNWKIILCLFIIPLVGCGFVSFRKKPVDKHKKLLWYYVAFFTSPFVVFSWNVVFYIAFLLLFAYVLLMDFHSVPHPPELVLYSLVFVLFCDEVRQWYVNGVNYFTDLWNVMDTLGLFYFIAGIVFRLHSSNKSSLYSGRVIFCLDYIIFTLRLIHIFTVSRNLGPKIIMLQRMLIDVFFFLFLFAVWMVAFGVARQGILRQNEQRWRWIFRSVIYEPYLAMFGQVPSDVDGTTYDFAHCTFTGNESKPLCVELDEHNLPRFPEWITIPLVCIYMLSTNILLVNLLVAMFGYTVGTVQENNDQVWKFQRYFLVQEYCSRLNIPFPFIVFAYFYMVVKKCFKCCCKEKNMESSVCCFKNEDNETLAWEGVMKENYLVKINTKANDTSEEMRHRFRQLDTKLNDLKGLLKEIANKIK
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Organism
Homo sapiens, Human
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 agonist 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. In prostate cancer cells, shows strong inward rectification and high calcium selectivity in contrast to its behavior in normal cells which is characterized by outward rectification and poor cationic selectivity. Plays a role in prostate cancer cell migration (PubMed:25559186). Isoform 2 and isoform 3 negatively regulate menthol- and cold-induced channel activity by stabilizing the closed state of the channel.
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Uniprot ID
Primary ID:
Q7Z2W7

Secondarily ID:
A0AVG2
Q3YFM7
Q6QNH9
Q8TAC3
Q8TDX8
Q9BVK1
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HGNC ID
HGNC:17961
Subcellular Location
Cell membrane
Membrane raft
Endoplasmic reticulum 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: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0389427
N-[(S)-(3-fluoropyridin-2-yl)-[3-fluoro-4-(trifluoromethyl)phenyl]methyl]-6-oxo-1H-pyridine-3-carboxamide
   Show/Hide
C19H12F5N3O2
 1
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0389434
6-oxo-N-[(S)-[4-(trifluoromethyl)phenyl]-[3-(trifluoromethyl)pyridin-2-yl]methyl]-1H-pyridine-3-carboxamide
   Show/Hide
C20H13F6N3O2
 1
1
IC50 = 6 nM
   TI
   LI
   LO
   TS
CP0389437
4-hydroxy-N-[(S)-[4-(trifluoromethyl)phenyl]-[3-(trifluoromethyl)pyridin-2-yl]methyl]benzamide
   Show/Hide
C21H14F6N2O2
 1
1
IC50 = 8 nM
   TI
   LI
   LO
   TS
CP0365159
(4R)-8-chloro-4-hydroxy-N-[4-(trifluoromethoxy)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxamide
   Show/Hide
C21H20ClF3N2O4
 1
1
IC50 = 8.9 nM
   TI
   LI
   LO
   TS
CP0476724
N-[(S)-(3-fluoropyridin-2-yl)-[3-fluoro-4-(trifluoromethoxy)phenyl]methyl]-6-oxo-1H-pyridine-3-carboxamide
   Show/Hide
C19H12F5N3O3
 1
1
IC50 = 9 nM
   TI
   LI
   LO
   TS
CP0375227
(4R)-8-fluoro-4-hydroxy-N-[4-(trifluoromethoxy)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxamide
   Show/Hide
C21H20F4N2O4
 1
1
IC50 = 9.5 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 = 10 nM
   TI
   LI
   LO
   TS
CP0466273
6-[[(S)-[4-(trifluoromethyl)phenyl]-[3-(trifluoromethyl)pyridin-2-yl]methyl]carbamoyl]pyridine-3-carboxylic acid
   Show/Hide
C21H13F6N3O3
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0219345
6-[[(S)-(3-fluoropyridin-2-yl)-[3-fluoro-4-(trifluoromethoxy)phenyl]methyl]carbamoyl]pyridine-3-carboxylic acid
   Show/Hide
C20H12F5N3O4
 1
1
IC50 = 13 nM
   TI
   LI
   LO
   TS
CP0845991
(+/-)-8-Chloro-4-hydroxy-N-[4-(trifluoromethoxy)phenyl]-3,4-dihydro-1'H-spiro[chromene-2,4'-piperidine]-1'-carboxamide
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C21H20ClF3N2O4
 1
1
IC50 = 13.3 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 = 15 nM
   TI
   LI
   LO
   TS
CP0375224
(4R)-8-bromo-4-hydroxy-N-[4-(trifluoromethoxy)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxamide
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C21H20BrF3N2O4
 1
1
IC50 = 16.6 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 = 18 nM
   TI
   LI
   LO
   TS
CP0566817
8-bromo-N-[4-(trifluoromethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxamide
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C21H20BrF3N2O2
 1
1
IC50 = 18.9 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 = 19 nM
   TI
   LI
   LO
   TS
CP0873823
(+/-)-8-Bromo-4-hydroxy-N-[4-(trifluoromethoxy)phenyl]-3,4-dihydro-1'H-spiro[chromene-2,4'-piperidine]-1'-carboxamide
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C21H20BrF3N2O4
 1
1
IC50 = 19.5 nM
   TI
   LI
   LO
   TS
CP0446361
4-[[(S)-(3-fluoropyridin-2-yl)-[3-fluoro-4-(trifluoromethoxy)phenyl]methyl]carbamoyl]benzoic acid
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C21H13F5N2O4
 1
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0553575
N-[(S)-[4-(trifluoromethyl)phenyl]-[3-(trifluoromethyl)pyridin-2-yl]methyl]quinoline-6-carboxamide
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C24H15F6N3O
 1
1
IC50 = 20 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 = 22 nM
   TI
   LI
   LO
   TS
CP0963723
(+/-)-8-Fluoro-4-hydroxy-N-[4-(trifluoromethoxy)phenyl]-3,4-dihydro-1'H-spiro[chromene-2,4'-piperidine]-1'-carboxamide
   Show/Hide
C21H20F4N2O4
 1
1
IC50 = 22.5 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 = 27 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 = 27 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 = 35 nM
   TI
   LI
   LO
   TS
CP0539003
8-chloro-N-[4-(trifluoromethoxy)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxamide
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C21H20ClF3N2O3
 1
1
IC50 = 41.1 nM
   TI
   LI
   LO
   TS
CP0539002
8-bromo-4-hydroxy-N-[4-(trifluoromethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxamide
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C21H20BrF3N2O3
 1
1
IC50 = 44.5 nM
   TI
   LI
   LO
   TS
CP0375226
(4S)-8-chloro-4-hydroxy-N-[4-(trifluoromethoxy)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxamide
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C21H20ClF3N2O4
 1
1
IC50 = 46.3 nM
   TI
   LI
   LO
   TS
CP0484709
8-chloro-N-[4-(trifluoromethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxamide
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C21H20ClF3N2O2
 1
1
IC50 = 48.5 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 = 51 nM
   TI
   LI
   LO
   TS
CP0466391
1-[(S)-(3-bromopyridin-2-yl)-[4-(trifluoromethyl)phenyl]methyl]-3-[(2S)-1,1,1-trifluoropropan-2-yl]urea
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C17H14BrF6N3O
 1
1
IC50 = 59 nM
   TI
   LI
   LO
   TS
CP0375225
(4S)-8-bromo-4-hydroxy-N-[4-(trifluoromethoxy)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxamide
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C21H20BrF3N2O4
 1
1
IC50 = 60 nM
   TI
   LI
   LO
   TS
CP0429060
8-chloro-4-hydroxy-N-[4-(trifluoromethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxamide
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C21H20ClF3N2O3
 1
1
IC50 = 65.9 nM
   TI
   LI
   LO
   TS
CP0389435
N-[(S)-quinolin-3-yl-[3-(trifluoromethyl)pyridin-2-yl]methyl]quinoline-7-carboxamide
   Show/Hide
C26H17F3N4O
 1
1
IC50 = 75 nM
   TI
   LI
   LO
   TS
CP0466259
N-[(S)-(4-methylphenyl)-[3-(trifluoromethyl)pyridin-2-yl]methyl]quinoline-7-carboxamide
   Show/Hide
C24H18F3N3O
 1
1
IC50 = 75 nM
   TI
   LI
   LO
   TS
CP0429061
8-fluoro-4-hydroxy-N-[4-(trifluoromethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxamide
   Show/Hide
C21H20F4N2O3
 1
1
IC50 = 90.1 nM
   TI
   LI
   LO
   TS
CP0390978
N-[(S)-(3-methylphenyl)-[3-(trifluoromethyl)pyridin-2-yl]methyl]quinoline-7-carboxamide
   Show/Hide
C24H18F3N3O
 1
1
IC50 = 92 nM
   TI
   LI
   LO
   TS
CP0375228
(4S)-8-fluoro-4-hydroxy-N-[4-(trifluoromethoxy)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxamide
   Show/Hide
C21H20F4N2O4
 1
1
IC50 = 94 nM
   TI
   LI
   LO
   TS
CP0555772
N-[(S)-(4-methoxyphenyl)-[3-(trifluoromethyl)pyridin-2-yl]methyl]quinoline-7-carboxamide
   Show/Hide
C24H18F3N3O2
 1
1
IC50 = 95 nM
   TI
   LI
   LO
   TS
CP0375230
8-fluoro-N-[4-(trifluoromethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxamide
   Show/Hide
C21H20F4N2O2
 1
1
IC50 = 97.3 nM
   TI
   LI
   LO
   TS
CP0541835
8-bromo-4-oxo-N-[4-(trifluoromethoxy)phenyl]spiro[3H-chromene-2,4'-piperidine]-1'-carboxamide
   Show/Hide
C21H18BrF3N2O4
 1
1
IC50 = 107.3 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 = 109 nM
   TI
   LI
   LO
   TS
CP0541836
8-chloro-4-oxo-N-[4-(trifluoromethoxy)phenyl]spiro[3H-chromene-2,4'-piperidine]-1'-carboxamide
   Show/Hide
C21H18ClF3N2O4
 1
1
IC50 = 111 nM
   TI
   LI
   LO
   TS
CP0426426
8-chloro-N-(6-fluoro-1,3-benzothiazol-2-yl)spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxamide
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C21H19ClFN3O2S
 1
1
IC50 = 113.1 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
   Show/Hide
C17H14F7N3O
 1
1
IC50 = 119 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 = 129 nM
   TI
   LI
   LO
   TS
CP0390977
N-[(S)-[3-(trifluoromethyl)phenyl]-[3-(trifluoromethyl)pyridin-2-yl]methyl]quinoline-7-carboxamide
   Show/Hide
C24H15F6N3O
 1
1
IC50 = 157 nM
   TI
   LI
   LO
   TS
CP0414937
8-chloro-N-[2-chloro-4-(trifluoromethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxamide
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C21H19Cl2F3N2O2
 1
1
IC50 = 177.8 nM
   TI
   LI
   LO
   TS
CP0407038
8-fluoro-4-oxo-N-[4-(trifluoromethoxy)phenyl]spiro[3H-chromene-2,4'-piperidine]-1'-carboxamide
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C21H18F4N2O4
 1
1
IC50 = 182.1 nM
   TI
   LI
   LO
   TS
CP0414936
8-chloro-4-oxo-N-[4-(trifluoromethyl)phenyl]spiro[3H-chromene-2,4'-piperidine]-1'-carboxamide
   Show/Hide
C21H18ClF3N2O3
 1
1
IC50 = 230.4 nM
   TI
   LI
   LO
   TS
CP0489781
8-chloro-N-[4-(trifluoromethyl)-1,3-thiazol-2-yl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxamide
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C18H17ClF3N3O2S
 1
1
IC50 = 265.8 nM
   TI
   LI
   LO
   TS
CP0429063
N-[4-(trifluoromethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxamide
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C21H21F3N2O2
 1
1
IC50 = 280.7 nM
   TI
   LI
   LO
   TS
CP0426427
8-chloro-N-(4-methylphenyl)spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxamide
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C21H23ClN2O2
 1
1
IC50 = 289.6 nM
   TI
   LI
   LO
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CP0429062
8-fluoro-4-oxo-N-[4-(trifluoromethyl)phenyl]spiro[3H-chromene-2,4'-piperidine]-1'-carboxamide
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C21H18F4N2O3
 1
1
IC50 = 295.2 nM
   TI
   LI
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CP0476725
N-[(S)-cyclohexyl-[3-(trifluoromethyl)pyridin-2-yl]methyl]quinoline-7-carboxamide
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C23H22F3N3O
 1
1
IC50 = 301 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 = 311 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 = 389 nM
   TI
   LI
   LO
   TS
CP0552668
quinolin-6-yl-[(1R)-1-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-isoquinolin-2-yl]methanone
   Show/Hide
C26H19F3N2O
 1
1
IC50 = 390 nM
   TI
   LI
   LO
   TS
CP0566816
8-chloro-6-fluoro-N-[4-(trifluoromethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxamide
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C21H19ClF4N2O2
 1
1
IC50 = 457.2 nM
   TI
   LI
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CP0375229
8-chloro-N-(4-cyanophenyl)spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxamide
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C21H20ClN3O2
 1
1
IC50 = 543.7 nM
   TI
   LI
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   TS
CP0426425
8-bromo-4-oxo-N-[4-(trifluoromethyl)phenyl]spiro[3H-chromene-2,4'-piperidine]-1'-carboxamide
   Show/Hide
C21H18BrF3N2O3
 1
1
IC50 = 656.9 nM
   TI
   LI
   LO
   TS
CP0541069
6-fluoro-N-[4-(trifluoromethyl)phenyl]spiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxamide
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C21H20F4N2O2
 1
1
IC50 = 666.9 nM
   TI
   LI
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   TS
CP0446363
N-[(1S)-2-phenyl-1-[3-(trifluoromethyl)pyridin-2-yl]ethyl]quinoline-7-carboxamide
   Show/Hide
C24H18F3N3O
 1
1
IC50 = 1140 nM
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CP0375231
N-phenylspiro[3,4-dihydrochromene-2,4'-piperidine]-1'-carboxamide
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C20H22N2O2
 1
1
IC50 = 2423 nM
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CP0019489
US9108905, 1
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C12H14FNO
 1
1
IC50 > 10000 nM
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CP0262006
4-[3-(3-methoxypropoxy)phenyl]-2-sulfanylidene-3,4-dihydro-1H-indeno[1,2-d]pyrimidin-5-one
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C21H20N2O3S
 1
1
IC50 > 10000 nM
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CP0402704
US9186360, 85
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C21H15F4N5O3S
 1
1
IC50 > 10000 nM
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CP0402705
US9186360, 24
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C21H16ClFN4O3S
 1
1
IC50 > 10000 nM
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CP0412454
US9186360, 22
   Show/Hide
C26H28N4O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0412557
US9186360, 21
   Show/Hide
C22H16ClF3N4O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0412575
US9186360, 49
   Show/Hide
C23H19F5N4O4S2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0412578
US9186360, 70
   Show/Hide
C21H16F4N4O5S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0412582
US9186360, 18
   Show/Hide
C22H16F4N4O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0412583
US9186360, 30
   Show/Hide
C22H17ClF2N4O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0412586
US9186360, 75
   Show/Hide
C24H24Cl2N4O5S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0412587
US9186360, 82
   Show/Hide
C19H13F4N5O4S2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0412588
US9186360, 11
   Show/Hide
C22H17F3N4O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0412589
US9186360, 14
   Show/Hide
C24H24N4O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0412592
US9186360, 56
   Show/Hide
C22H17F5N4O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0412617
US9186360, 17
   Show/Hide
C23H22N4O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0412618
US9186360, 28
   Show/Hide
C22H15F5N4O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0412619
US9186360, 39
   Show/Hide
C20H17F3N6O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0413535
US9186360, 58
   Show/Hide
C20H14F4N4O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0413536
US9186360, 77
   Show/Hide
C19H12F5N5O3S2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0413540
US9186360, 69
   Show/Hide
C21H16F4N4O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0413541
US9186360, 87
   Show/Hide
C21H14F5N5O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0419511
US9186360, 31
   Show/Hide
C22H15F5N4O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0419512
US9186360, 73
   Show/Hide
C21H16ClF3N4O5S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0419513
US9186360, 94
   Show/Hide
C21H18F5N6O7PS
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0419515
US9186360, 6
   Show/Hide
C22H20N4O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0419516
US9186360, 20
   Show/Hide
C22H16F4N4O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0423872
US9186360, 27
   Show/Hide
C21H16F2N4O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0441106
US9186360, 86
   Show/Hide
C22H16F5N5O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0441108
US9186360, 95
   Show/Hide
C27H27ClF3N5O7S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0441109
US9186360, 1
   Show/Hide
C19H16BrN7O2S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0441110
US9186360, 4
   Show/Hide
C21H16Cl2N4O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0441111
US9186360, 9
   Show/Hide
C21H17ClN4O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0441112
US9186360, 19
   Show/Hide
C22H16F4N4O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0441113
US9186360, 23
   Show/Hide
C25H26N4O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0441114
US9186360, 25
   Show/Hide
C21H16ClFN4O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0441115
US9186360, 41
   Show/Hide
C20H16F4N6O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0441116
US9186360, 62
   Show/Hide
C22H17F5N4O5S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0463397
US9186360, 3
   Show/Hide
C21H17BrN4O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0463398
US9186360, 12
   Show/Hide
C25H26N4O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0463399
US9186360, 15
   Show/Hide
C21H16ClFN4O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0463400
US9186360, 16
   Show/Hide
C22H18F3N5O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0463403
US9186360, 60
   Show/Hide
C21H15ClF4N4O5S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0463405
US9186360, 48
   Show/Hide
C22H18F4N4O4S2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0470141
US9186360, 67
   Show/Hide
C21H16F4N4O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0470143
US9186360, 92
   Show/Hide
C19H12F5N5O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0470699
US9186360, 68
   Show/Hide
C21H16F4N4O5S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0470719
US9186360, 47
   Show/Hide
C20H16Cl2N4O3S2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0472819
US9186360, 38
   Show/Hide
C20H16F4N6O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0478201
US9186360, 34
   Show/Hide
C20H16F3N5O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0478205
US9186360, 54
   Show/Hide
C20H14F4N4O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0478206
US9186360, 63
   Show/Hide
C21H16ClF3N4O5S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0478207
US9186360, 71
   Show/Hide
C21H16ClF3N4O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0478208
US9186360, 79
   Show/Hide
C19H13F4N5O3S2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0478209
US9186360, 83
   Show/Hide
C19H13F4N5O3S2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0479347
US9186360, 32
   Show/Hide
C23H17F5N4O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0479348
US9186360, 36
   Show/Hide
C20H15F4N5O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0479349
US9186360, 37
   Show/Hide
C23H24Cl2N6O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0479354
US9186360, 50
   Show/Hide
C22H18F4N4O3S2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0482710
US9186360, 65
   Show/Hide
C21H16F4N4O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0482711
US9186360, 62
   Show/Hide
C25H26F2N4O5S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0482713
US9186360, 35
   Show/Hide
C22H18Cl2F3N5O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0483920
US9186360, 33
   Show/Hide
C22H15F5N4O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0485488
US9186360, 81
   Show/Hide
C19H13F4N5O3S2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0489890
US9186360, 10
   Show/Hide
C27H28N4O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0490192
US9186360, 88
   Show/Hide
C21H15F4N5O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0490193
US9186360, 16
   Show/Hide
C22H17F3N4O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0495054
US9186360, 26
   Show/Hide
C22H17F3N4O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0495055
US9186360, 29
   Show/Hide
C22H16F4N4O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0499846
US9186360, 78
   Show/Hide
C19H13F4N5O3S2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0512070
US9186360, 57
   Show/Hide
C21H15Cl2F3N4O5S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0512071
US9186360, 72
   Show/Hide
C21H15F5N4O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0512072
US9186360, 61
   Show/Hide
C21H16F4N4O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0512088
US9186360, 5
   Show/Hide
C21H17IN4O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0512093
US9186360, 8
   Show/Hide
C21H18ClN5O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0516824
US9186360, 93
   Show/Hide
C22H19ClF3N4O9PS
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0516825
US9186360, 76
   Show/Hide
C21H15F5N4O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0516826
US9186360, 53
   Show/Hide
C23H22F2N4O5S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0518910
US9186360, 55
   Show/Hide
C20H14F4N4O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0518928
US9186360, 59
   Show/Hide
C20H14F4N4O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0518929
US9186360, 74
   Show/Hide
C22H18ClF3N4O5S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0518944
US9186360, 2
   Show/Hide
C23H25N7O2S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0519543
US9186360, 13
   Show/Hide
C21H16F2N4O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0544901
US9186360, 64
   Show/Hide
C21H15F5N4O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0544902
US9186360, 84
   Show/Hide
C19H12F5N5O3S2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0548934
US9186360, 80
   Show/Hide
C19H13ClF3N5O4S2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0466275
N-[(S)-pyridin-2-yl-[3-(trifluoromethyl)pyridin-2-yl]methyl]quinoline-7-carboxamide
   Show/Hide
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
   Show/Hide
C20H13F3N4OS
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0396611
N-[(S)-(2-methylphenyl)-[3-(trifluoromethyl)pyridin-2-yl]methyl]quinoline-7-carboxamide
   Show/Hide
C24H18F3N3O
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
   TS
CP0521618
US9186360, 46
   Show/Hide
C23H20F4N4O3S2
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0094059
3-(2-hydroxyphenyl)-6-(3-nitrophenyl)-3,4-dihydropyrimidin-2(1H)-one
   Show/Hide
C16H13N3O4
 1
1 EC50 = 60 nM
CP0067499
4-[[4-fluoro-3-(trifluoromethyl)phenyl]methyl-(3-methyl-1-benzothiophen-2-yl)sulfamoyl]benzoic acid
   Show/Hide
C24H17F4NO4S2
 1
1 IC50 = 4 nM
CP0284406
N-(3-aminopropyl)-2-[(3-methylphenyl)methoxy]-N-(thiophen-2-ylmethyl)benzamide
   Show/Hide
C23H26N2O2S
 1
1 IC50 = 4 nM
CP0024847
3-[[[(1R)-1-(4-fluorophenyl)ethyl]-(quinoline-3-carbonyl)amino]methyl]benzoic acid
   Show/Hide
C26H21FN2O3
 6
1 IC50 = 181 nM
2 IC50 ~ 13.8 nM
3 IC50 ~ 29.6 nM
4 IC50 ~ 103 nM
5 IC50 ~ 181 nM
6 IC50 ~ 480 nM
Clinical Information about the Protein
Target 1 ( Long transient receptor potential channel 8 (TRPM8) )
Target Type Successful Target
Disease 3 Target-related Diseases  3
1 Throat irritation [ICD-11: CA0Y]
2 Pain [ICD-11: MG30-MG3Z]
3 Neuropathic pain [ICD-11: 8E43.0]
Approved Drug(s) 1 Approved Drug  1
1 Menthol Approved
Throat irritation
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 PF-05105679 Phase 1
Pain
Investigative Drug(s) 1 Investigative Drug  1
1 RQ-00203078 Investigative
Neuropathic pain
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
PT05529 Transient receptor potential cation channel subfamily M member 8 Rattus norvegicus, Rat
PT06117 Transient receptor potential cation channel subfamily M member 8 Mus musculus, Mouse