General Information of the Protein
Protein ID
PT04908
Protein Name
Transient receptor potential cation channel subfamily M member 2
Secondarily
Protein Name
Estrogen-responsive element-associated gene 1 protein
Long transient receptor potential channel 2
Transient receptor potential channel 7
Transient receptor potential melastatin 2
Gene Name
TRPM2
Secondarily
Gene Name
EREG1
KNP3
LTRPC2
TRPC7
Sequence
MEPSALRKAGSEQEEGFEGLPRRVTDLGMVSNLRRSNSSLFKSWRLQCPFGNNDKQESLSSWIPENIKKKECVYFVESSKLSDAGKVVCQCGYTHEQHLEEATKPHTFQGTQWDPKKHVQEMPTDAFGDIVFTGLSQKVKKYVRVSQDTPSSVIYHLMTQHWGLDVPNLLISVTGGAKNFNMKPRLKSIFRRGLVKVAQTTGAWIITGGSHTGVMKQVGEAVRDFSLSSSYKEGELITIGVATWGTVHRREGLIHPTGSFPAEYILDEDGQGNLTCLDSNHSHFILVDDGTHGQYGVEIPLRTRLEKFISEQTKERGGVAIKIPIVCVVLEGGPGTLHTIDNATTNGTPCVVVEGSGRVADVIAQVANLPVSDITISLIQQKLSVFFQEMFETFTESRIVEWTKKIQDIVRRRQLLTVFREGKDGQQDVDVAILQALLKASRSQDHFGHENWDHQLKLAVAWNRVDIARSEIFMDEWQWKPSDLHPTMTAALISNKPEFVKLFLENGVQLKEFVTWDTLLYLYENLDPSCLFHSKLQKVLVEDPERPACAPAAPRLQMHHVAQVLRELLGDFTQPLYPRPRHNDRLRLLLPVPHVKLNVQGVSLRSLYKRSSGHVTFTMDPIRDLLIWAIVQNRRELAGIIWAQSQDCIAAALACSKILKELSKEEEDTDSSEEMLALAEEYEHRAIGVFTECYRKDEERAQKLLTRVSEAWGKTTCLQLALEAKDMKFVSHGGIQAFLTKVWWGQLSVDNGLWRVTLCMLAFPLLLTGLISFREKRLQDVGTPAARARAFFTAPVVVFHLNILSYFAFLCLFAYVLMVDFQPVPSWCECAIYLWLFSLVCEEMRQLFYDPDECGLMKKAALYFSDFWNKLDVGAILLFVAGLTCRLIPATLYPGRVILSLDFILFCLRLMHIFTISKTLGPKIIIVKRMMKDVFFFLFLLAVWVVSFGVAKQAILIHNERRVDWLFRGAVYHSYLTIFGQIPGYIDGVNFNPEHCSPNGTDPYKPKCPESDATQQRPAFPEWLTVLLLCLYLLFTNILLLNLLIAMFNYTFQQVQEHTDQIWKFQRHDLIEEYHGRPAAPPPFILLSHLQLFIKRVVLKTPAKRHKQLKNKLEKNEEAALLSWEIYLKENYLQNRQFQQKQRPEQKIEDISNKVDAMVDLLDLDPLKRSGSMEQRLASLEEQVAQTAQALHWIVRTLRASGFSSEADVPTLASQKAAEEPDAEPGGRKKTEEPGDSYHVNARHLLYPNCPVTRFPVPNEKVPWETEFLIYDPPFYTAERKDAAAMDPMGDTLEPLSTIQYNVVDGLRDRRSFHGPYTVQAGLPLNPMGRTGLRGRGSLSCFGPNHTLYPMVTRWRRNEDGAICRKSIKKMLEVLVVKLPLSEHWALPGGSREPGEMLPRKLKRILRQEHWPSFENLLKCGMEVYKGYMDDPRNTDNAWIETVAVSVHFQDQNDVELNRLNSNLHACDSGASIRWQVVDRRIPLYANHKTLLQKAAAEFGAHY
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Organism
Homo sapiens, Human
Protein Classification
Ion channel
>
Voltage-gated ion channel
>
Transient receptor potential channel
Function
Nonselective, voltage-independent cation channel that mediates Na(+) and Ca(2+) influx, leading to increased cytoplasmic Ca(2+) levels (PubMed:11960981, PubMed:12594222, PubMed:11385575, PubMed:11509734, PubMed:11804595, PubMed:15561722, PubMed:16601673, PubMed:19171771, PubMed:20660597, PubMed:25620041, PubMed:27383051, PubMed:27068538, PubMed:28775320, PubMed:29745897, PubMed:30467180). Functions as a ligand-gated ion channel (PubMed:19171771, PubMed:25620041, PubMed:28775320, PubMed:30467180). Binding of ADP-ribose to the cytoplasmic Nudix domain causes a conformation change; the channel is primed but still requires Ca(2+) binding to trigger channel opening (PubMed:19171771, PubMed:25620041, PubMed:28775320, PubMed:29745897, PubMed:30467180). Extracellular calcium passes through the channel and increases channel activity (PubMed:19171771). Contributes to Ca(2+) release from intracellular stores in response to ADP-ribose (PubMed:19454650). Plays a role in numerous processes that involve signaling via intracellular Ca(2+) levels (Probable). Besides, mediates the release of lysosomal Zn(2+) stores in response to reactive oxygen species, leading to increased cytosolic Zn(2+) levels (PubMed:25562606, PubMed:27068538). Activated by moderate heat (35 to 40 degrees Celsius) (PubMed:16601673). Activated by intracellular ADP-ribose, beta-NAD (NAD(+)) and similar compounds, and by oxidative stress caused by reactive oxygen or nitrogen species (PubMed:11960981, PubMed:11385575, PubMed:11509734, PubMed:11804595, PubMed:15561722, PubMed:16601673, PubMed:19171771, PubMed:25620041, PubMed:27383051, PubMed:27068538, PubMed:30467180). The precise physiological activators are under debate; the true, physiological activators may be ADP-ribose and ADP-ribose-2'-phosphate (PubMed:20650899, PubMed:25918360). Activation by ADP-ribose and beta-NAD is strongly increased by moderate heat (35 to 40 degrees Celsius) (PubMed:16601673). Likewise, reactive oxygen species lower the threshold for activation by moderate heat (37 degrees Celsius) (PubMed:22493272). Plays a role in mediating behavorial and physiological responses to moderate heat and thereby contributes to body temperature homeostasis. Plays a role in insulin secretion, a process that requires increased cytoplasmic Ca(2+) levels (By similarity). Required for normal IFNG and cytokine secretion and normal innate immune immunity in response to bacterial infection. Required for normal phagocytosis and cytokine release by macrophages exposed to zymosan (in vitro). Plays a role in dendritic cell differentiation and maturation, and in dendritic cell chemotaxis via its role in regulating cytoplasmic Ca(2+) levels (By similarity). Plays a role in the regulation of the reorganization of the actin cytoskeleton and filopodia formation in response to reactive oxygen species via its role in increasing cytoplasmic Ca(2+) and Zn(2+) levels (PubMed:27068538). Confers susceptibility to cell death following oxidative stress (PubMed:12594222, PubMed:25562606).
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Uniprot ID
Primary ID:
O94759

Secondarily ID:
D3DSL6
Q5KTC2
Q6J3P5
Q96KN6
Q96Q93
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Ensembl ID
ENSG00000142185
HGNC ID
HGNC:12339
Subcellular Location
Cell membrane
Perikaryon
Cell projection
Cytoplasmic vesicle
Lysosome
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: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0897887
N-(6-oxo-5,6-dihydrophenanthridin-2-yl)-(N,N-dimethylamino)acetamide hydrochloride hydrate
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C17H20ClN3O3
 1
1
IC50 = 25 nM
   TI
   LI
   LO
   TS
CP0008872
Scalaradial
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C27H40O4
 1
1
IC50 = 210 nM
   TI
   LI
   LO
   TS
CP0409040
2-[[(E)-3-(4-pentylphenyl)prop-2-enoyl]amino]benzoic acid
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C21H23NO3
 3
1
IC50 = 320 nM
   TI
   LI
   LO
   TS
2
IC50 = 1700 nM
   TI
   LI
   LO
   TS
3
IC50 = 4500 nM
   TI
   LI
   LO
   TS
CP0088659
3,4-dihydro-5-(4-(1-piperidinyl)butoxy)-1(2H)-isoquinolinone
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C18H26N2O2
 1
1
IC50 = 600 nM
   TI
   LI
   LO
   TS
CP0083490
2-(Diphenylboryloxy)Ethanamine
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C14H16BNO
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0908454
COPPER
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Cu
 1
1
IC50 = 2600 nM
   TI
   LI
   LO
   TS
CP0869337
{[(2R,3S,5R)-5-(6-amino-8-phenyl-9H-purin-9-yl)-3-hydroxyoxolan-2-yl]methoxy}({[hydroxy({[(2R,3S,4R)-3,4,5-trihydroxyoxolan-2-yl]methoxy})phosphoryl]oxy})phosphinic acid
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C21H27N5O13P2
 1
1
IC50 = 3000 nM
   TI
   LI
   LO
   TS
CP0865093
6-Bromo-8-methyl-2-(3-(naphthalen-1-yl)-1H-pyrazol-4-yl)-2,3-dihydroquinazolin-4(1H)-one
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C22H17BrN4O
 1
1
IC50 = 3700 nM
   TI
   LI
   LO
   TS
CP0851718
6-Chloro-8-methyl-2-(3-(naphthalen-1-yl)-1H-pyrazol-4-yl)-2,3-dihydroquinazolin-4(1H)-one
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C22H17ClN4O
 1
1
IC50 = 4000 nM
   TI
   LI
   LO
   TS
CP0851719
6-Bromo-8-methyl-2-(3-phenyl-1H-pyrazol-4-yl)-2,3-dihydroquinazolin-4(1H)-one
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C18H15BrN4O
 1
1
IC50 = 4600 nM
   TI
   LI
   LO
   TS
CP0899372
6-Chloro-8-methyl-2-(3-phenyl-1H-pyrazol-4-yl)-2,3-dihydroquinazolin-4(1H)-one
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C18H15ClN4O
 1
1
IC50 = 5100 nM
   TI
   LI
   LO
   TS
CP0338965
[[(2R,3S,4R,5R)-5-(6-amino-8-phenylpurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] [(2R,3S,4R)-3,4,5-trihydroxyoxolan-2-yl]methyl hydrogen phosphate
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C21H27N5O14P2
 1
1
IC50 = 11000 nM
   TI
   LI
   LO
   TS
CP0873804
Cyclopentyl-8-phenyladenosine-diphosphate
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C21H27N5O10P2
 1
1
IC50 = 15000 nM
   TI
   LI
   LO
   TS
CP0461943
[[(2R,3S,4R,5R)-5-[8-(3-acetylphenyl)-6-aminopurin-9-yl]-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] [(2R,3S,4R)-3,4,5-trihydroxyoxolan-2-yl]methyl hydrogen phosphate
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C23H29N5O15P2
 1
1
IC50 = 49000 nM
   TI
   LI
   LO
   TS
CP0483818
[[(2R,3S,4R,5R)-5-(6-amino-8-thiophen-3-ylpurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] [(2R,3S,4R)-3,4,5-trihydroxyoxolan-2-yl]methyl hydrogen phosphate
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C19H25N5O14P2S
 1
1
IC50 = 51000 nM
   TI
   LI
   LO
   TS
CP0280422
2-(3-methylanilino)benzoic acid
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C14H13NO2
 1
1
IC50 = 76000 nM
   TI
   LI
   LO
   TS
CP0037867
((2R,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl 2-hydroxybenzoylsulfamate
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C17H18N6O8S
 1
1
IC50 = 100000 nM
   TI
   LI
   LO
   TS
CP0429030
[4-(6-aminopurin-9-yl)butoxy-hydroxyphosphoryl] [(2R,3S,4R)-3,4,5-trihydroxyoxolan-2-yl]methyl hydrogen phosphate
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C14H23N5O11P2
 1
1
IC50 = 100000 nM
   TI
   LI
   LO
   TS
CP0481449
2-amino-3-[4-[6-amino-9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(phosphonooxymethyl)oxolan-2-yl]purin-8-yl]phenyl]propanoic acid
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C19H23N6O9P
 1
1
IC50 = 100000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0036697
2-{[3-(trifluoromethyl)phenyl]amino}benzoic acid
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C14H10F3NO2
 1
1 IC50 = 70000 nM
CP0030899
1-[(2-chlorophenyl)-diphenylmethyl]imidazole
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C22H17ClN2
 1
1 IC50 < 3000 nM
CP0057530
ECONAZOLE
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C18H15Cl3N2O
 1
1 IC50 < 3000 nM
Clinical Information about the Protein
Target 1 ( Long transient receptor potential channel 2 (TRPM2) )
Target Type Literature-reported Target
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT07452 Transient receptor potential cation channel subfamily M member 2 Rattus norvegicus, Rat