General Information of the Protein
Protein ID
PT03393
Protein Name
P2X purinoceptor 3
Secondarily
Protein Name
ATP receptor
Purinergic receptor
Gene Name
P2RX3
Sequence
MNCISDFFTYETTKSVVVKSWTIGIINRVVQLLIISYFVGWVFLHEKAYQVRDTAIESSVVTKVKGSGLYANRVMDVSDYVTPPQGTSVFVIITKMIVTENQMQGFCPESEEKYRCVSDSQCGPERLPGGGILTGRCVNYSSVLRTCEIQGWCPTEVDTVETPIMMEAENFTIFIKNSIRFPLFNFEKGNLLPNLTARDMKTCRFHPDKDPFCPILRVGDVVKFAGQDFAKLARTGGVLGIKIGWVCDLDKAWDQCIPKYSFTRLDSVSEKSSVSPGYNFRFAKYYKMENGSEYRTLLKAFGIRFDVLVYGNAGKFNIIPTIISSVAAFTSVGVGTVLCDIILLNFLKGADQYKAKKFEEVNETTLKIAALTNPVYPSDQTTAEKQSTDSGAFSIGH
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Organism
Homo sapiens, Human
Protein Classification
Ion channel
>
Ligand-gated ion channel
>
P2X receptor
Function
Receptor for ATP that acts as a ligand-gated cation channel (PubMed:27626375). Plays a role in sensory perception. Required for normal perception of pain. Required for normal taste perception (By similarity).
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Uniprot ID
Primary ID:
P56373

Secondarily ID:
Q6DK37
Q9UQB6
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Ensembl ID
ENSG00000109991
HGNC ID
HGNC:8534
Subcellular Location
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
CP0402500
N-[3,5-bis(trifluoromethyl)phenyl]-1-hydroxynaphthalene-2-carboxamide
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C19H11F6NO2
 1
1
IC50 = 195 nM
   TI
   LI
   LO
   TS
CP0093745
[4-[[3-[1-[4-chloro-3-(trifluoromethyl)benzoyl]piperidin-4-yl]-2,5-dioxoimidazolidin-4-yl]methyl]phenyl] isoquinoline-5-sulfonate
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C32H26ClF3N4O6S
 1
1
IC50 = 600 nM
   TI
   LI
   LO
   TS
CP0429999
[[(2R,3aR,4R,6R,6aR)-4-(6-aminopurin-9-yl)-2-phenyl-3a,4,6,6a-tetrahydrofuro[3,4-d][1,3]dioxol-6-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate;azane
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C17H32N9O13P3
 1
1
IC50 = 611 nM
   TI
   LI
   LO
   TS
CP0389792
[4-[3-[1-[4-(dimethylamino)benzoyl]piperidin-4-yl]imidazol-4-yl]phenyl] isoquinoline-5-sulfonate
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C32H31N5O4S
 1
1
IC50 = 800 nM
   TI
   LI
   LO
   TS
CP0149500
[[(3aR,4R,6R,6aR)-4-(6-aminopurin-9-yl)spiro[3a,4,6,6a-tetrahydrofuro[3,4-d][1,3]dioxole-2,1'-cyclohexane]-6-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate;azane
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C16H36N9O13P3
 1
1
IC50 = 883 nM
   TI
   LI
   LO
   TS
CP0455718
[4-[3-[1-[4-(dimethylamino)benzoyl]piperidin-4-yl]imidazol-4-yl]phenyl] 3-(cyclopropylcarbamoyl)benzenesulfonate
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C33H35N5O5S
 1
1
IC50 = 910 nM
   TI
   LI
   LO
   TS
CP0852911
tetrasodium 4-[[3-[[3,5-bis[(4-sulfonatophenyl)carbamoyl]phenyl]carbamoylamino]-5-[(4-sulfonatophenyl)carbamoyl]benzoyl]amino]benzenesulfonate
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C41H28N6Na4O17S4
 2
1
IC50 = 1580 nM
   TI
   LI
   LO
   TS
2
IC50 = 1600 nM
   TI
   LI
   LO
   TS
CP0038813
(1S,2R,10S,11S,14S,15S)-14-acetyl-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-en-5-one
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C21H30O2
 1
1
IC50 = 1600 nM
   TI
   LI
   LO
   TS
CP0451123
[4-[[6-[4-[4-(dimethylamino)benzoyl]piperazin-1-yl]-2,4-dioxopyrimidin-1-yl]methyl]phenyl] isoquinoline-5-sulfonate
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C33H32N6O6S
 1
1
IC50 = 2660 nM
   TI
   LI
   LO
   TS
CP0466664
2-(1-adamantyl)-N-[2-(4-methoxyphenyl)quinolin-5-yl]acetamide
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C28H30N2O2
 1
1
IC50 = 3000 nM
   TI
   LI
   LO
   TS
CP0232343
[[(3aR,4R,6R,6aR)-4-(6-aminopurin-9-yl)-2,2-dimethyl-3a,4,6,6a-tetrahydrofuro[3,4-d][1,3]dioxol-6-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate;azane
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C13H32N9O13P3
 1
1
IC50 = 4110 nM
   TI
   LI
   LO
   TS
CP0347185
[[(2S,3aR,4R,6R,6aR)-4-(6-aminopurin-9-yl)-2-phenyl-3a,4,6,6a-tetrahydrofuro[3,4-d][1,3]dioxol-6-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate;azane
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C17H32N9O13P3
 1
1
IC50 = 5830 nM
   TI
   LI
   LO
   TS
CP0246925
N,N-di(propan-2-yl)benzo[b][1]benzazepine-11-carboxamide
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C21H24N2O
 1
1
IC50 = 7180 nM
   TI
   LI
   LO
   TS
CP0167727
benzo[b][1]benzazepin-11-yl(piperidin-1-yl)methanone
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C20H20N2O
 1
1
IC50 = 7980 nM
   TI
   LI
   LO
   TS
CP0072340
N-[3,5-bis(trifluoromethyl)phenyl]-5-chloro-2-hydroxybenzamide
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C15H8ClF6NO2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0387003
5-chloro-2-hydroxy-N-[3-nitro-5-(trifluoromethyl)phenyl]benzamide
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C14H8ClF3N2O4
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0387004
N-[3,5-bis(trifluoromethyl)phenyl]-3-fluoro-2-hydroxybenzamide
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C15H8F7NO2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0410779
5-chloro-N-(3,5-dichlorophenyl)-2-hydroxybenzamide
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C13H8Cl3NO2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0472734
N-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxybenzamide
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C15H9F6NO2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0472736
5-chloro-N-(3-chlorophenyl)-2-hydroxybenzamide
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C13H9Cl2NO2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0472737
5-chloro-2-hydroxy-N-[3-(trifluoromethyl)phenyl]benzamide
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C14H9ClF3NO2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0479699
N-[3,5-bis(trifluoromethyl)phenyl]-4-chloro-2-hydroxybenzamide
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C15H8ClF6NO2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0479706
5-chloro-N-(3,5-difluorophenyl)-2-hydroxybenzamide
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C13H8ClF2NO2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0479707
5-chloro-2-hydroxy-N-[4-(trifluoromethyl)phenyl]benzamide
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C14H9ClF3NO2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0487340
N-[3,5-bis(trifluoromethyl)phenyl]-3-chloro-2-hydroxybenzamide
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C15H8ClF6NO2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0134749
N,N-diethylbenzo[b][1]benzazepine-11-carboxamide
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C19H20N2O
 1
1
IC50 = 14200 nM
   TI
   LI
   LO
   TS
CP0054493
N,N-dipropylbenzo[b][1]benzazepine-11-carboxamide
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C21H24N2O
 1
1
IC50 = 15200 nM
   TI
   LI
   LO
   TS
CP0149504
[(3aR,4R,6R,6aR)-4-(6-aminopurin-9-yl)spiro[3a,4,6,6a-tetrahydrofuro[3,4-d][1,3]dioxole-2,1'-cyclohexane]-6-yl]methoxy-[[hydroxy(phosphonooxy)phosphoryl]methyl]phosphinic acid;azane
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C17H38N9O12P3
 1
1
IC50 = 17500 nM
   TI
   LI
   LO
   TS
CP0246924
N-cyclohexylbenzo[b][1]benzazepine-11-carboxamide
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C21H22N2O
 1
1
IC50 = 28000 nM
   TI
   LI
   LO
   TS
CP0054492
benzo[b][1]benzazepin-11-yl(pyrrolidin-1-yl)methanone
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C19H18N2O
 1
1
IC50 = 29800 nM
   TI
   LI
   LO
   TS
CP0430000
5-[[(3aR,4R,6R,6aR)-4-(6-aminopurin-9-yl)-2,2-dimethyl-3a,4,6,6a-tetrahydrofuro[3,4-d][1,3]dioxol-6-yl]methoxycarbonyl]benzene-1,2,4-tricarboxylic acid
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C23H21N5O11
 1
1
IC50 >= 100000 nM
   TI
   LI
   LO
   TS
CP0487903
[[(3aR,4R,6R,6aR)-4-(6-aminopurin-9-yl)-3a,4,6,6a-tetrahydrofuro[3,4-d][1,3]dioxol-6-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate;azane
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C11H28N9O13P3
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0493771
(2S)-2-[[(3aR,4R,6S,6aS)-4-(6-aminopurin-9-yl)-2,2-dimethyl-3a,4,6,6a-tetrahydrofuro[3,4-d][1,3]dioxole-6-carbonyl]amino]pentanedioic acid
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C18H22N6O8
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0826581
(S)-3-(3-(4-chlorobenzyl)-2,6-dioxo-4-(4-(pyridin-2-yloxy)phenylimino)-1,3,5-triazinan-1-yl)-2-methylpropanoic acid
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C25H22ClN5O5
 1
1 IC50 = 4.2 nM
CP0031968
3-[4-(3-chloro-4-propan-2-yloxyanilino)-3-[(4-methylphenyl)methyl]-2,6-dioxo-1,3,5-triazin-1-yl]propanoic acid
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C23H25ClN4O5
 1
1 IC50 = 16.1 nM
CP0573448
US9150546, I-355
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C22H22Cl2N4O5
 1
1 IC50 = 19.6 nM
CP0465690
US9150546, I-200
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C22H25ClN4O3
 1
1 IC50 = 128 nM
CP0344193
1-[(4-methoxyphenyl)methyl]-3-prop-2-enyl-6-[3-(trifluoromethyl)anilino]-1,3,5-triazine-2,4-dione
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C21H19F3N4O3
 1
1 IC50 = 1200 nM
Clinical Information about the Protein
Target 1 ( P2X purinoceptor 3 (P2RX3) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Cough [ICD-11: MD12]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 Gefapixant Phase 3
Cough