General Information of the Protein
Protein ID
PT04758
Protein Name
P2X purinoceptor 1
Secondarily
Protein Name
ATP receptor
Purinergic receptor
Gene Name
P2RX1
Secondarily
Gene Name
P2X1
Sequence
MARRFQEELAAFLFEYDTPRMVLVRNKKVGVIFRLIQLVVLVYVIGWVFLYEKGYQTSSGLISSVSVKLKGLAVTQLPGLGPQVWDVADYVFPAQGDNSFVVMTNFIVTPKQTQGYCAEHPEGGICKEDSGCTPGKAKRKAQGIRTGKCVAFNDTVKTCEIFGWCPVEVDDDIPRPALLREAENFTLFIKNSISFPRFKVNRRNLVEEVNAAHMKTCLFHKTLHPLCPVFQLGYVVQESGQNFSTLAEKGGVVGITIDWHCDLDWHVRHCRPIYEFHGLYEEKNLSPGFNFRFARHFVENGTNYRHLFKVFGIRFDILVDGKAGKFDIIPTMTTIGSGIGIFGVATVLCDLLLLHILPKRHYYKQKKFKYAEDMGPGAAERDLAATSSTLGLQENMRTS
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Organism
Homo sapiens, Human
Protein Classification
Ion channel
>
Ligand-gated ion channel
>
P2X receptor
Function
Ligand-gated ion channel with relatively high calcium permeability. Binding to ATP mediates synaptic transmission between neurons and from neurons to smooth muscle. Seems to be linked to apoptosis, by increasing the intracellular concentration of calcium in the presence of ATP, leading to programmed cell death (By similarity).
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Uniprot ID
Primary ID:
P51575

Secondarily ID:
Q9UK84
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HGNC ID
HGNC:8533
Subcellular Location
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
CP0072340
N-[3,5-bis(trifluoromethyl)phenyl]-5-chloro-2-hydroxybenzamide
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C15H8ClF6NO2
 4
1
IC50 = 19.2 nM
   TI
   LI
   LO
   TS
2
IC50 = 570 nM
   TI
   LI
   LO
   TS
3
IC50 = 3640 nM
   TI
   LI
   LO
   TS
4
IC50 = 4730 nM
   TI
   LI
   LO
   TS
CP0479699
N-[3,5-bis(trifluoromethyl)phenyl]-4-chloro-2-hydroxybenzamide
   Show/Hide
C15H8ClF6NO2
 4
1
IC50 = 23.1 nM
   TI
   LI
   LO
   TS
2
IC50 = 1140 nM
   TI
   LI
   LO
   TS
3
IC50 = 4800 nM
   TI
   LI
   LO
   TS
4
IC50 = 5470 nM
   TI
   LI
   LO
   TS
CP0410779
5-chloro-N-(3,5-dichlorophenyl)-2-hydroxybenzamide
   Show/Hide
C13H8Cl3NO2
 4
1
IC50 = 29.3 nM
   TI
   LI
   LO
   TS
2
IC50 = 3030 nM
   TI
   LI
   LO
   TS
3
IC50 > 10000 nM
   TI
   LI
   LO
   TS
4
IC50 > 20000 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 = 31.6 nM
   TI
   LI
   LO
   TS
CP0479707
5-chloro-2-hydroxy-N-[4-(trifluoromethyl)phenyl]benzamide
   Show/Hide
C14H9ClF3NO2
 3
1
IC50 = 38.3 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
3
IC50 > 20000 nM
   TI
   LI
   LO
   TS
CP0479706
5-chloro-N-(3,5-difluorophenyl)-2-hydroxybenzamide
   Show/Hide
C13H8ClF2NO2
 4
1
IC50 = 50.5 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
3
IC50 >= 10000 nM
   TI
   LI
   LO
   TS
4
IC50 > 20000 nM
   TI
   LI
   LO
   TS
CP0487340
N-[3,5-bis(trifluoromethyl)phenyl]-3-chloro-2-hydroxybenzamide
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C15H8ClF6NO2
 1
1
IC50 = 58 nM
   TI
   LI
   LO
   TS
CP0387004
N-[3,5-bis(trifluoromethyl)phenyl]-3-fluoro-2-hydroxybenzamide
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C15H8F7NO2
 1
1
IC50 = 70.6 nM
   TI
   LI
   LO
   TS
CP0472736
5-chloro-N-(3-chlorophenyl)-2-hydroxybenzamide
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C13H9Cl2NO2
 1
1
IC50 = 75.6 nM
   TI
   LI
   LO
   TS
CP0472734
N-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxybenzamide
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C15H9F6NO2
 1
1
IC50 = 76.9 nM
   TI
   LI
   LO
   TS
CP0472737
5-chloro-2-hydroxy-N-[3-(trifluoromethyl)phenyl]benzamide
   Show/Hide
C14H9ClF3NO2
 1
1
IC50 = 91 nM
   TI
   LI
   LO
   TS
CP0525426
5-chloro-2-hydroxy-N-(3-nitrophenyl)benzamide
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C13H9ClN2O4
 1
1
IC50 = 172 nM
   TI
   LI
   LO
   TS
CP0516611
5-chloro-N-(4-chlorophenyl)-2-hydroxybenzamide
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C13H9Cl2NO2
 1
1
IC50 = 199 nM
   TI
   LI
   LO
   TS
CP0472731
3-chloro-2-hydroxy-N-[3-nitro-5-(trifluoromethyl)phenyl]benzamide
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C14H8ClF3N2O4
 1
1
IC50 = 219 nM
   TI
   LI
   LO
   TS
CP0564264
N-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxy-5-methylbenzamide
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C16H11F6NO2
 1
1
IC50 = 236 nM
   TI
   LI
   LO
   TS
CP0651325
SID50106714
   Show/Hide
C41H24N6Na8O29S8
 1
1
IC50 = 236 nM
   TI
   LI
   LO
   TS
CP0479702
5-chloro-N-(3,5-dimethylphenyl)-2-hydroxybenzamide
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C15H14ClNO2
 1
1
IC50 = 323 nM
   TI
   LI
   LO
   TS
CP0545240
5-chloro-2-hydroxy-N-[3-(trifluoromethylsulfonyl)phenyl]benzamide
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C14H9ClF3NO4S
 1
1
IC50 = 335 nM
   TI
   LI
   LO
   TS
CP0402500
N-[3,5-bis(trifluoromethyl)phenyl]-1-hydroxynaphthalene-2-carboxamide
   Show/Hide
C19H11F6NO2
 1
1
IC50 = 341 nM
   TI
   LI
   LO
   TS
CP0387011
N-[3,5-bis(trifluoromethyl)phenyl]-5-chloro-2-hydroxybenzenesulfonamide
   Show/Hide
C14H8ClF6NO3S
 4
1
IC50 = 439 nM
   TI
   LI
   LO
   TS
2
IC50 = 3130 nM
   TI
   LI
   LO
   TS
3
IC50 > 10000 nM
   TI
   LI
   LO
   TS
4
IC50 > 20000 nM
   TI
   LI
   LO
   TS
CP0068867
1H-Benzoimidazole-2-carboxylic acid [(R)-1-((1S,2R,3S)-1-cyclohexylmethyl-3-cyclopropyl-2,3-dihydroxy-propylcarbamoyl)-2-thiazol-4-yl-ethyl]-amide
   Show/Hide
C27H35N5O4S
 1
1
IC50 = 496 nM
   TI
   LI
   LO
   TS
CP0526822
5-chloro-N-(3-cyanophenyl)-2-hydroxybenzamide
   Show/Hide
C14H9ClN2O2
 1
1
IC50 = 522 nM
   TI
   LI
   LO
   TS
CP0437452
N-(3-tert-butylphenyl)-5-chloro-2-hydroxybenzamide
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C17H18ClNO2
 1
1
IC50 = 567 nM
   TI
   LI
   LO
   TS
CP0487341
N-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxy-3-methylbenzamide
   Show/Hide
C16H11F6NO2
 1
1
IC50 = 655 nM
   TI
   LI
   LO
   TS
CP0472771
N-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxy-5-methoxybenzamide
   Show/Hide
C16H11F6NO3
 1
1
IC50 = 755 nM
   TI
   LI
   LO
   TS
CP0479695
N-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxy-3-nitrobenzamide
   Show/Hide
C15H8F6N2O4
 1
1
IC50 = 869 nM
   TI
   LI
   LO
   TS
CP0479696
5-chloro-N-(4-fluorophenyl)-2-hydroxybenzamide
   Show/Hide
C13H9ClFNO2
 1
1
IC50 = 907 nM
   TI
   LI
   LO
   TS
CP0524384
5-chloro-N-(3,5-dimethoxyphenyl)-2-hydroxybenzamide
   Show/Hide
C15H14ClNO4
 1
1
IC50 = 915 nM
   TI
   LI
   LO
   TS
CP0472637
Salfluverine
   Show/Hide
C14H10F3NO2
 1
1
IC50 = 1300 nM
   TI
   LI
   LO
   TS
CP0526821
5-chloro-N-(3-ethynylphenyl)-2-hydroxybenzamide
   Show/Hide
C15H10ClNO2
 1
1
IC50 = 1340 nM
   TI
   LI
   LO
   TS
CP0525427
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-5-chloro-2-hydroxybenzamide
   Show/Hide
C16H10ClF6NO2
 1
1
IC50 = 1530 nM
   TI
   LI
   LO
   TS
CP0564279
N-[3,5-bis(trifluoromethyl)phenyl]-5-fluoro-2-hydroxybenzamide
   Show/Hide
C15H8F7NO2
 1
1
IC50 = 1660 nM
   TI
   LI
   LO
   TS
CP0564266
2-[3,5-bis(trifluoromethyl)anilino]-1-(5-chloro-2-hydroxyphenyl)ethanone
   Show/Hide
C16H10ClF6NO2
 1
1
IC50 = 1790 nM
   TI
   LI
   LO
   TS
CP0472766
N-[3,5-bis(trifluoromethyl)phenyl]benzamide
   Show/Hide
C15H9F6NO
 4
1
IC50 = 2100 nM
   TI
   LI
   LO
   TS
2
IC50 = 2220 nM
   TI
   LI
   LO
   TS
3
IC50 = 5570 nM
   TI
   LI
   LO
   TS
4
IC50 >= 20000 nM
   TI
   LI
   LO
   TS
CP0451239
N-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxy-5-nitrobenzamide
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C15H8F6N2O4
 1
1
IC50 = 2530 nM
   TI
   LI
   LO
   TS
CP0479704
N-(3-bromophenyl)-2-hydroxybenzamide
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C13H10BrNO2
 1
1
IC50 = 2690 nM
   TI
   LI
   LO
   TS
CP0565372
N-[3,5-bis(trifluoromethyl)phenyl]-2,5-dihydroxybenzamide
   Show/Hide
C15H9F6NO3
 1
1
IC50 = 3410 nM
   TI
   LI
   LO
   TS
CP0387010
2-[[3,5-bis(trifluoromethyl)anilino]methyl]-4-chlorophenol
   Show/Hide
C15H10ClF6NO
 1
1
IC50 = 3820 nM
   TI
   LI
   LO
   TS
CP0526757
N-[3,5-bis(trifluoromethyl)phenyl]-5-chloro-2-hydroxy-N-methylbenzamide
   Show/Hide
C16H10ClF6NO2
 1
1
IC50 = 4060 nM
   TI
   LI
   LO
   TS
CP0014670
CHEMBL3040216
   Show/Hide
C51H40N6O23S6
 2
1
IC50 = 4270 nM
   TI
   LI
   LO
   TS
2
IC50 = 4300 nM
   TI
   LI
   LO
   TS
CP0545241
5-chloro-N-(3,5-dinitrophenyl)-2-hydroxybenzamide
   Show/Hide
C13H8ClN3O6
 1
1
IC50 = 4350 nM
   TI
   LI
   LO
   TS
CP0054493
N,N-dipropylbenzo[b][1]benzazepine-11-carboxamide
   Show/Hide
C21H24N2O
 1
1
IC50 = 4550 nM
   TI
   LI
   LO
   TS
CP0479694
N-[3,5-bis(trifluoromethyl)phenyl]-3-hydroxybenzamide
   Show/Hide
C15H9F6NO2
 1
1
IC50 = 4910 nM
   TI
   LI
   LO
   TS
CP0472772
N-[3,5-bis(trifluoromethyl)phenyl]-3-hydroxypyridine-4-carboxamide
   Show/Hide
C14H8F6N2O2
 1
1
IC50 = 5250 nM
   TI
   LI
   LO
   TS
CP0246925
N,N-di(propan-2-yl)benzo[b][1]benzazepine-11-carboxamide
   Show/Hide
C21H24N2O
 1
1
IC50 = 5320 nM
   TI
   LI
   LO
   TS
CP0387005
N-[3,5-bis(trifluoromethyl)phenyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C16H8F9NO
 1
1
IC50 = 7180 nM
   TI
   LI
   LO
   TS
CP0487383
5-chloro-2-hydroxy-N-[3-(trifluoromethoxy)phenyl]benzamide
   Show/Hide
C14H9ClF3NO3
 1
1
IC50 = 7620 nM
   TI
   LI
   LO
   TS
CP0387006
N-[3,5-bis(trifluoromethyl)phenyl]-2,6-dihydroxybenzamide
   Show/Hide
C15H9F6NO3
 1
1
IC50 = 8000 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
   Show/Hide
C16H36N9O13P3
 1
1
IC50 = 8060 nM
   TI
   LI
   LO
   TS
CP0479693
N-[3,5-bis(trifluoromethyl)phenyl]-2-nitrobenzamide
   Show/Hide
C15H8F6N2O3
 1
1
IC50 = 8600 nM
   TI
   LI
   LO
   TS
CP0525424
2-amino-N-[3,5-bis(trifluoromethyl)phenyl]benzamide
   Show/Hide
C15H10F6N2O
 1
1
IC50 = 9930 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
   Show/Hide
C17H32N9O13P3
 1
1
IC50 >= 10000 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
   Show/Hide
C23H21N5O11
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0472732
2-hydroxy-N-pyridin-3-ylbenzamide
   Show/Hide
C12H10N2O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0479697
5-chloro-N-(4-cyanophenyl)-2-hydroxybenzamide
   Show/Hide
C14H9ClN2O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0479698
2-hydroxy-N-(1H-indol-6-yl)benzamide
   Show/Hide
C15H12N2O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0479701
N-[3,5-bis(trifluoromethyl)phenyl]-2-oxo-1H-pyridine-3-carboxamide
   Show/Hide
C14H8F6N2O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0516612
2-hydroxy-N-(3-sulfamoylphenyl)benzamide
   Show/Hide
C13H12N2O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0525425
5-chloro-2-hydroxy-N-[2-(trifluoromethyl)phenyl]benzamide
   Show/Hide
C14H9ClF3NO2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0525862
N-[3,5-bis(trifluoromethyl)phenyl]-3-methyl-2-oxoimidazolidine-1-carboxamide
   Show/Hide
C13H11F6N3O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0539764
N-[3,5-bis(trifluoromethyl)phenyl]-2-(hydroxymethyl)benzamide
   Show/Hide
C16H11F6NO2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0564265
N-[3,5-bis(trifluoromethyl)phenyl]-4-oxo-1H-pyridine-3-carboxamide
   Show/Hide
C14H8F6N2O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0565371
5-chloro-N-(3,5-dihydroxyphenyl)-2-hydroxybenzamide
   Show/Hide
C13H10ClNO4
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0568619
2-hydroxy-N-quinolin-6-ylbenzamide
   Show/Hide
C16H12N2O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0866597
5-chloro-2-hydroxy-N-(4-nitrophenyl)benzamide
   Show/Hide
C13H9ClN2O4
 1
1
IC50 >= 10000 nM
   TI
   LI
   LO
   TS
CP0907005
N-(5-Chloro-2-hydroxyphenyl)-3,5-Bis(trifluoromethyl)benzamide
   Show/Hide
C15H8ClF6NO2
 1
1
IC50 >= 10000 nM
   TI
   LI
   LO
   TS
CP0516610
N-[3,5-bis(trifluoromethyl)phenyl]-8-hydroxy-3,4-dihydro-2H-quinoline-1-carboxamide
   Show/Hide
C18H14F6N2O2
 1
1
IC50 = 10400 nM
   TI
   LI
   LO
   TS
CP0516613
5-chloro-N-(4-chloro-3-nitrophenyl)-2-hydroxybenzamide
   Show/Hide
C13H8Cl2N2O4
 1
1
IC50 = 13500 nM
   TI
   LI
   LO
   TS
CP0167727
benzo[b][1]benzazepin-11-yl(piperidin-1-yl)methanone
   Show/Hide
C20H20N2O
 1
1
IC50 = 20700 nM
   TI
   LI
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   TS
CP0134749
N,N-diethylbenzo[b][1]benzazepine-11-carboxamide
   Show/Hide
C19H20N2O
 1
1
IC50 = 25200 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
   Show/Hide
C13H32N9O13P3
 1
1
IC50 = 41100 nM
   TI
   LI
   LO
   TS
CP0054492
benzo[b][1]benzazepin-11-yl(pyrrolidin-1-yl)methanone
   Show/Hide
C19H18N2O
 1
1
IC50 = 68800 nM
   TI
   LI
   LO
   TS
CP0246924
N-cyclohexylbenzo[b][1]benzazepine-11-carboxamide
   Show/Hide
C21H22N2O
 1
1
IC50 = 69600 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
   Show/Hide
C17H38N9O12P3
 1
1
IC50 > 100000 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
   Show/Hide
C17H32N9O13P3
 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
CP0487343
N-[3,5-bis(trifluoromethyl)phenyl]-5-chloro-2-methoxybenzamide
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C16H10ClF6NO2
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
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 > 30000 nM
Clinical Information about the Protein
Target 1 ( P2X purinoceptor 1 (P2RX1) )
Target Type Literature-reported Target