General Information of the Protein
Protein ID
PT01174
Protein Name
Polymerase acidic protein
Secondarily
Protein Name
RNA-directed RNA polymerase subunit P2
Gene Name
PA
Sequence
MEDFVRQCFNPMIVELAEKTMKEYGEDLKIETNKFAAICTHLEVCFMYSDFHFINEQGESIIVELGDPNALLKHRFEIIEGRDRTMAWTVVNSICNTTGAEKPKFLPDLYDYKENRFIEIGVTRREVHIYYLEKANKIKSEKTHIHIFSFTGEEMATKADYTLDEESRARIKTRLFTIRQEMASRGLWDSFRQSERGEETIEERFEITGTMRKLADQSLPPNFSSLENFRAYVDGFEPNGYIEGKLSQMSKEVNARIEPFLKTTPRPLRLPNGPPCSQRSKFLLMDALKLSIEDPSHEGEGIPLYDAIKCMRTFFGWKEPNVVKPHEKGINPNYLLSWKQVLAELQDIENEEKIPKTKNMKKTSQLKWALGENMAPEKVDFDDCKDVGDLKQYDSDEPELRSLASWIQNEFNKACELTDSSWIELDEIGEDVAPIEHIASMRRNYFTSEVSHCRATEYIMKGVYINTALLNASCAAMDDFQLIPMISKCRTKEGRRKTNLYGFIIKGRSHLRNDTDVVNFVSMEFSLTDPRLEPHKWEKYCVLEIGDMLIRSAIGQVSRPMFLYVRTNGTSKIKMKWGMEMRRCLLQSLQQIESMIEAESSVKEKDMTKEFFENKSETWPIGESPKGVEESSIGKVCRTLLAKSVFNSLYASPQLEGFSAESRKLLLIVQALRDNLEPGTFDLGGLYEAIEECLINDPWVLLNASWFNSFLTHALS
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Organism
Influenza A virus (strain A/Puerto Rico/8/1934 H1N1)
Protein Classification
Enzyme
>
Hydrolase
Function
Plays an essential role in viral RNA transcription and replication by forming the heterotrimeric polymerase complex together with PB1 and PB2 subunits. The complex transcribes viral mRNAs by using a unique mechanism called cap-snatching. It consists in the hijacking and cleavage of host capped pre-mRNAs. These short capped RNAs are then used as primers for viral mRNAs. The PB2 subunit is responsible for the binding of the 5' cap of cellular pre-mRNAs which are subsequently cleaved after 10-13 nucleotides by the PA subunit that carries the endonuclease activity.
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Uniprot ID
Primary ID:
P03433

Secondarily ID:
A4GXH3
Q20N31
Q8JUU6
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Subcellular Location
Host cytoplasm
Host nucleus
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: CL000031 , MDCK
Compound ID Compound Name Compound Formula
CP0687592
(Z)-4-[4-[(4-chlorophenyl)methyl]-1-(cyclohexylmethyl)piperidin-4-yl]-2-hydroxy-4-oxobut-2-enoic acid
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C23H30ClNO4
 1
1
EC50 = 800 nM
   TI
   LI
   LO
   TS
CP0109317
(Z)-4-[1-benzyl-4-[(4-chlorophenyl)methyl]piperidin-4-yl]-2-hydroxy-4-oxobut-2-enoic acid
   Show/Hide
C23H24ClNO4
 1
1
EC50 = 860 nM
   TI
   LI
   LO
   TS
CP0115435
4-hydroxy-2-oxo-4-(4-phenoxyphenyl)but-3-enoic acid
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C16H12O5
 1
1
EC50 = 1450 nM
   TI
   LI
   LO
   TS
CP0410191
5-hydroxy-6-oxo-N-[(1R)-1-phenylethyl]-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
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C17H15N5O3
 1
1
EC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0847636
4-hydroxy-2-oxo-4-(4-piperazin-1-ylphenyl)but-3-enoic acid
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C14H16N2O4
 1
1
EC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0036531
4-hydroxy-2-oxo-4-phenylbut-3-enoic acid
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C10H8O4
 1
1
EC50 = 2070 nM
   TI
   LI
   LO
   TS
CP0089024
2-hydroxy-4H-isoquinoline-1,3-dione
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C9H7NO3
 1
1
EC50 = 3220 nM
   TI
   LI
   LO
   TS
CP0271229
5-hydroxy-6-oxo-N-(1-phenylethyl)-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
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C17H15N5O3
 1
1
EC50 = 3500 nM
   TI
   LI
   LO
   TS
CP0271261
5-hydroxy-N-[(1S)-2-hydroxy-1-phenylethyl]-6-oxo-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
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C17H15N5O4
 1
1
EC50 = 3500 nM
   TI
   LI
   LO
   TS
CP0713308
2-Hydroxy-4-(biphenyl-4-yl)-4-oxobut-2-enoic acid
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C16H12O4
 1
1
EC50 = 3560 nM
   TI
   LI
   LO
   TS
CP0338376
N-(cyclopropylmethyl)-5-hydroxy-6-oxo-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
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C13H13N5O3
 1
1
EC50 = 3660 nM
   TI
   LI
   LO
   TS
CP0338858
N-[(4-fluorophenyl)methyl]-5-hydroxy-6-oxo-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
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C16H12FN5O3
 1
1
EC50 = 3700 nM
   TI
   LI
   LO
   TS
CP0222790
5,6-dihydroxy-2-pyrazin-2-ylpyrimidine-4-carboxylic acid
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C9H6N4O4
 1
1
EC50 = 3800 nM
   TI
   LI
   LO
   TS
CP0529344
N-[(1R)-1-cyclohexylethyl]-5-hydroxy-6-oxo-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
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C17H21N5O3
 1
1
EC50 = 4851 nM
   TI
   LI
   LO
   TS
CP0153974
N-benzyl-5-hydroxy-6-oxo-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
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C16H13N5O3
 1
1
EC50 = 5410 nM
   TI
   LI
   LO
   TS
CP0160931
5-hydroxy-N-[(1R)-1-(4-methylphenyl)ethyl]-6-oxo-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
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C18H17N5O3
 1
1
EC50 = 5520 nM
   TI
   LI
   LO
   TS
CP0257766
5-hydroxy-6-oxo-2-pyridin-2-yl-1H-pyrimidine-4-carboxylic acid
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C10H7N3O4
 1
1
EC50 = 5920 nM
   TI
   LI
   LO
   TS
CP0711424
4-hydroxy-4-(4-methoxyphenyl)-2-oxobut-3-enoic acid
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C11H10O5
 1
1
EC50 = 6700 nM
   TI
   LI
   LO
   TS
CP0711425
4-hydroxy-2-oxo-4-(4-phenylmethoxyphenyl)but-3-enoic acid
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C17H14O5
 1
1
EC50 = 6800 nM
   TI
   LI
   LO
   TS
CP0711426
2-Hydroxy-4-oxo-4-o-tolylbut-2-enoic acid
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C11H10O4
 1
1
EC50 = 6800 nM
   TI
   LI
   LO
   TS
CP0338859
5-hydroxy-6-oxo-N-[(1S)-1-phenylethyl]-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
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C17H15N5O3
 1
1
EC50 = 7670 nM
   TI
   LI
   LO
   TS
CP0655462
4-hydroxy-2-oxo-4-(2,4,6-trimethylphenyl)but-3-enoic acid
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C13H14O4
 1
1
EC50 = 8170 nM
   TI
   LI
   LO
   TS
CP0338856
N-cyclohexyl-5-hydroxy-6-oxo-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
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C15H17N5O3
 1
1
EC50 = 11480 nM
   TI
   LI
   LO
   TS
CP0092193
5-hydroxy-2-(1-methylimidazol-4-yl)-6-oxo-1H-pyrimidine-4-carboxylic acid
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C9H8N4O4
 1
1
EC50 = 18090 nM
   TI
   LI
   LO
   TS
CP0338857
5-hydroxy-N-[(4-methylphenyl)methyl]-6-oxo-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
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C17H15N5O3
 1
1
EC50 = 22600 nM
   TI
   LI
   LO
   TS
CP0336538
5-hydroxy-6-oxo-2-pyrazin-2-yl-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1H-pyrimidine-4-carboxamide
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C19H17N5O3
 1
1
EC50 = 24300 nM
   TI
   LI
   LO
   TS
CP0339214
methyl 5-hydroxy-6-oxo-2-pyrazin-2-yl-1H-pyrimidine-4-carboxylate
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C10H8N4O4
 1
1
EC50 = 25460 nM
   TI
   LI
   LO
   TS
CP0436403
5-hydroxy-N-[(4-methoxyphenyl)methyl]-6-oxo-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
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C17H15N5O4
 1
1
EC50 = 35300 nM
   TI
   LI
   LO
   TS
CP0336536
2-(3-acetamidophenyl)-5-hydroxy-6-oxo-1H-pyrimidine-4-carboxylic acid
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C13H11N3O5
 1
1
EC50 = 58900 nM
   TI
   LI
   LO
   TS
CP0338032
5-hydroxy-6-oxo-3,7,13-triazatricyclo[7.4.0.02,7]trideca-1(9),2,4,10,12-pentaene-4-carboxylic acid
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C11H7N3O4
 1
1
EC50 = 67400 nM
   TI
   LI
   LO
   TS
CP0336537
methyl 5-hydroxy-2-(1-methylimidazol-4-yl)-6-oxo-1H-pyrimidine-4-carboxylate
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C10H10N4O4
 1
1
EC50 = 71300 nM
   TI
   LI
   LO
   TS
CP0338854
N-butyl-5-hydroxy-6-oxo-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
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C13H15N5O3
 1
1
EC50 = 88120 nM
   TI
   LI
   LO
   TS
CP0477033
1-(4-chlorophenyl)-2-[4-[1-(4-chlorophenyl)-4,5-dihydroimidazol-2-yl]phenyl]-4,5-dihydroimidazole
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C24H20Cl2N4
 1
1
IC50 = 5000 nM
   TI
   LI
   LO
   TS
CP0076946
(alpha-methyl-1-adamantyl)methylamine
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C12H21N
 1
1
IC50 = 11000 nM
   TI
   LI
   LO
   TS
CP0545298
1-(4-fluorophenyl)-2-[4-[1-(4-fluorophenyl)-4,5-dihydroimidazol-2-yl]phenyl]-4,5-dihydroimidazole
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C24H20F2N4
 1
1
IC50 = 12000 nM
   TI
   LI
   LO
   TS
CP0438845
1-(4-methoxyphenyl)-2-[4-[1-(4-methoxyphenyl)-4,5-dihydroimidazol-2-yl]phenyl]-4,5-dihydroimidazole
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C26H26N4O2
 1
1
IC50 = 16000 nM
   TI
   LI
   LO
   TS
CP0466718
2-[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-1-phenyl-4,5-dihydroimidazole
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C18H18N4
 1
1
IC50 = 30000 nM
   TI
   LI
   LO
   TS
CP0423707
2-[2-[4-(1-pyridin-2-yl-4,5-dihydroimidazol-2-yl)phenyl]-4,5-dihydroimidazol-1-yl]pyridine
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C22H20N6
 1
1
IC50 = 35000 nM
   TI
   LI
   LO
   TS
CP0558031
2-[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-1-(4-methoxyphenyl)-4,5-dihydroimidazole
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C19H20N4O
 1
1
IC50 = 44000 nM
   TI
   LI
   LO
   TS
CP0420850
2-[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-1-(4-fluorophenyl)-4,5-dihydroimidazole
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C18H17FN4
 1
1
IC50 = 65000 nM
   TI
   LI
   LO
   TS
CP0423708
3-[2-[4-(1-pyridin-3-yl-4,5-dihydroimidazol-2-yl)phenyl]-4,5-dihydroimidazol-1-yl]pyridine
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C22H20N6
 1
1
IC50 = 68000 nM
   TI
   LI
   LO
   TS
CP0420851
1-phenyl-2-[4-(1-phenyl-4,5-dihydroimidazol-2-yl)phenyl]-4,5-dihydroimidazole
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C24H22N4
 1
1
IC50 = 77000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0687592
(Z)-4-[4-[(4-chlorophenyl)methyl]-1-(cyclohexylmethyl)piperidin-4-yl]-2-hydroxy-4-oxobut-2-enoic acid
   Show/Hide
C23H30ClNO4
 4
1 IC50 = 320 nM
2 IC50 = 330 nM
3 IC50 = 710 nM
4 Ki = 84 nM
CP0109317
(Z)-4-[1-benzyl-4-[(4-chlorophenyl)methyl]piperidin-4-yl]-2-hydroxy-4-oxobut-2-enoic acid
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C23H24ClNO4
 4
1 IC50 = 350 nM
2 IC50 = 430 nM
3 IC50 = 2210 nM
4 Ki = 90 nM
CP0713308
2-Hydroxy-4-(biphenyl-4-yl)-4-oxobut-2-enoic acid
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C16H12O4
 2
1 IC50 = 3700 nM
2 Ki = 960 nM
CP0089024
2-hydroxy-4H-isoquinoline-1,3-dione
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C9H7NO3
 2
1 IC50 = 15000 nM
2 Ki = 850 nM
CP0036531
CHEMBL467389
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C10H8O4
 2
1 IC50 = 21300 nM
2 Ki = 480 nM
CP0115435
CHEMBL573638
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C16H12O5
 1
1 Ki = 280 nM
CP0410191
5-hydroxy-6-oxo-N-[(1R)-1-phenylethyl]-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
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C17H15N5O3
 1
1 Ki = 290 nM
CP0847636
CHEMBL2040552
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C14H16N2O4
 1
1 Ki = 300 nM
CP0271229
5-hydroxy-6-oxo-N-(1-phenylethyl)-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
   Show/Hide
C17H15N5O3
 1
1 Ki = 720 nM
CP0338376
N-(cyclopropylmethyl)-5-hydroxy-6-oxo-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
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C13H13N5O3
 1
1 Ki = 990 nM
CP0271261
5-hydroxy-N-[(1S)-2-hydroxy-1-phenylethyl]-6-oxo-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
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C17H15N5O4
 1
1 Ki = 1000 nM
CP0222790
5,6-dihydroxy-2-pyrazin-2-ylpyrimidine-4-carboxylic acid
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C9H6N4O4
 1
1 Ki = 1100 nM
CP0338858
N-[(4-fluorophenyl)methyl]-5-hydroxy-6-oxo-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
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C16H12FN5O3
 1
1 Ki = 1200 nM
CP0529344
N-[(1R)-1-cyclohexylethyl]-5-hydroxy-6-oxo-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
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C17H21N5O3
 1
1 Ki = 1392 nM
CP0160931
5-hydroxy-N-[(1R)-1-(4-methylphenyl)ethyl]-6-oxo-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
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C18H17N5O3
 1
1 Ki = 1610 nM
CP0153974
N-benzyl-5-hydroxy-6-oxo-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
   Show/Hide
C16H13N5O3
 1
1 Ki = 1650 nM
CP0257766
5-hydroxy-6-oxo-2-pyridin-2-yl-1H-pyrimidine-4-carboxylic acid
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C10H7N3O4
 1
1 Ki = 1840 nM
CP0711424
CHEMBL2040553
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C11H10O5
 1
1 Ki = 1970 nM
CP0711425
CHEMBL492768
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C17H14O5
 1
1 Ki = 1990 nM
CP0711426
2-Hydroxy-4-oxo-4-o-tolylbut-2-enoic acid
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C11H10O4
 1
1 Ki = 2000 nM
CP0338859
5-hydroxy-6-oxo-N-[(1S)-1-phenylethyl]-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
   Show/Hide
C17H15N5O3
 1
1 Ki = 2280 nM
CP0655462
CHEMBL2040555
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C13H14O4
 1
1 Ki = 2440 nM
CP0338856
N-cyclohexyl-5-hydroxy-6-oxo-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
   Show/Hide
C15H17N5O3
 1
1 Ki = 3556 nM
CP0092193
5-hydroxy-2-(1-methylimidazol-4-yl)-6-oxo-1H-pyrimidine-4-carboxylic acid
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C9H8N4O4
 1
1 Ki = 5010 nM
CP0338857
5-hydroxy-N-[(4-methylphenyl)methyl]-6-oxo-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
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C17H15N5O3
 1
1 Ki = 7100 nM
CP0339214
methyl 5-hydroxy-6-oxo-2-pyrazin-2-yl-1H-pyrimidine-4-carboxylate
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C10H8N4O4
 1
1 Ki = 8000 nM
CP0436403
5-hydroxy-N-[(4-methoxyphenyl)methyl]-6-oxo-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
   Show/Hide
C17H15N5O4
 1
1 Ki = 11200 nM
CP0336536
2-(3-acetamidophenyl)-5-hydroxy-6-oxo-1H-pyrimidine-4-carboxylic acid
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C13H11N3O5
 1
1 Ki = 18700 nM
CP0336537
methyl 5-hydroxy-2-(1-methylimidazol-4-yl)-6-oxo-1H-pyrimidine-4-carboxylate
   Show/Hide
C10H10N4O4
 1
1 Ki = 20300 nM
CP0338032
5-hydroxy-6-oxo-3,7,13-triazatricyclo[7.4.0.02,7]trideca-1(9),2,4,10,12-pentaene-4-carboxylic acid
   Show/Hide
C11H7N3O4
 1
1 Ki = 21600 nM
CP0336538
5-hydroxy-6-oxo-2-pyrazin-2-yl-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1H-pyrimidine-4-carboxamide
   Show/Hide
C19H17N5O3
 1
1 Ki = 24300 nM
CP0338854
N-butyl-5-hydroxy-6-oxo-2-pyrazin-2-yl-1H-pyrimidine-4-carboxamide
   Show/Hide
C13H15N5O3
 1
1 Ki = 28570 nM
Clinical Information about the Protein
Target 1 ( Influenza Polymerase acidic endonuclease (Influ PA) )
Target Type Successful Target