General Information of the Protein
Protein ID
PT03075
Protein Name
Signal transducer and activator of transcription 1-alpha/beta
Gene Name
PDE9A
Sequence
MGSGSSSYRPKAIYLDIDGRIQKVIFSKYCNSSDIMDLFCIATGLPRNTTISLLTTDDAMVSIDPTMPANSERTPYKVRPVAIKQLSAGVEDKRTTSRGQSAERPLRDRRVVGLEQPRREGAFESGQVEPRPREPQGCYQEGQRIPPEREELIQSVLAQVAEQFSRAFKINELKAEVANHLAVLEKRVELEGLKVVEIEKCKSDIKKMREELAARSSRTNCPCKYSFLDNHKKLTPRRDVPTYPKYLLSPETIEALRKPTFDVWLWEPNEMLSCLEHMYHDLGLVRDFSINPVTLRRWLFCVHDNYRNNPFHNFRHCFCVAQMMYSMVWLCSLQEKFSQTDILILMTAAICHDLDHPGYNNTYQINARTELAVRYNDISPLENHHCAVAFQILAEPECNIFSNIPPDGFKQIRQGMITLILATDMARHAEIMDSFKEKMENFDYSNEEHMTLLKMILIKCCDISNEVRPMEVAEPWVDCLLEEYFMQSDREKSEGLPVAPFMDRDKVTKATAQIGFIKFVLIPMFETVTKLFPMVEEIMLQPLWESRDRYEELKRIDDAMKELQKKTDSLTSGATEKSRERSRDVKNSEGDCA
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Phosphodiesterase
>
Phosphodiesterase 9
>
Phosphodiesterase 9A
Function
Specifically hydrolyzes the second messenger cGMP, which is a key regulator of many important physiological processes. Highly specific: compared to other members of the cyclic nucleotide phosphodiesterase family, has the highest affinity and selectivity for cGMP (PubMed:9624146, PubMed:18757755, PubMed:21483814). Specifically regulates natriuretic-peptide-dependent cGMP signaling in heart, acting as a regulator of cardiac hypertrophy in myocytes and muscle. Does not regulate nitric oxide-dependent cGMP in heart (PubMed:25799991). Additional experiments are required to confirm whether its ability to hydrolyze natriuretic-peptide-dependent cGMP is specific to heart or is a general feature of the protein (Probable). In brain, involved in cognitive function, such as learning and long-term memory (By similarity).
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Uniprot ID
Primary ID:
O76083

Secondarily ID:
B2RBI5
B4DFI5
D3DSJ8
D3DSJ9
O75490
O75491
O95225
Q53Y40
Q5QD39
Q86SF7
Q86SI6
Q86SJ3
Q86WN3
Q86WN4
Q86WN5
Q86WN6
Q86WN7
Q86WN8
Q86WN9
Q86WP0
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Ensembl ID
ENSG00000160191
HGNC ID
HGNC:8795
Subcellular Location
Cell projection
Ruffle membrane
Cytoplasm
Perinuclear region
Golgi apparatus
Endoplasmic reticulum
Cell membrane
Sarcolemma
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: CL000013 , Sf9
Compound ID Compound Name Compound Formula
CP0398541
6-benzyl-1-cyclopentyl-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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C17H18N4O
 1
1
IC50 = 0.8 nM
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CP0271210
6-[(3S,4S)-1-[(4-fluorophenyl)methyl]-4-methylpyrrolidin-3-yl]-1-(oxan-4-yl)-5H-pyrazolo[3,4-d]pyrimidin-4-one
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C22H26FN5O2
 1
1
IC50 = 0.9 nM
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CP0487996
6-benzyl-1-(oxan-4-yl)-5H-pyrazolo[3,4-d]pyrimidin-4-one
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C17H18N4O2
 1
1
IC50 = 1 nM
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CP0486716
6-[(3S,4S)-1-[(3-fluorophenyl)methyl]-4-methylpyrrolidin-3-yl]-1-(oxan-4-yl)-5H-pyrazolo[3,4-d]pyrimidin-4-one
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C22H26FN5O2
 1
1
IC50 = 1.2 nM
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CP0487995
6-[(3S,4S)-1-benzyl-4-ethylpyrrolidin-3-yl]-1-(oxan-4-yl)-5H-pyrazolo[3,4-d]pyrimidin-4-one
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C23H29N5O2
 1
1
IC50 = 1.7 nM
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CP0958208
6-{1-[3-(quinoxalin-2-yloxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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C23H25N7O3
 1
1
IC50 = 2.94 nM
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CP0578902
6-[2-(2,3-dihydroindol-1-yl)-2-oxoethyl]-4-(4-methylphenyl)-2-oxo-8-propyl-1,5,7,8-tetrahydro-1,6-naphthyridine-3-carbonitrile
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C29H30N4O2
 1
1
IC50 = 3 nM
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CP0486714
6-[(3S,4S)-1-[(4-methoxyphenyl)methyl]-4-methylpyrrolidin-3-yl]-1-(oxan-4-yl)-5H-pyrazolo[3,4-d]pyrimidin-4-one
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C23H29N5O3
 1
1
IC50 = 3.4 nM
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CP0441922
6-[(3S,4S)-4-methyl-1-[(6-methylpyridin-3-yl)methyl]pyrrolidin-3-yl]-1-(oxan-4-yl)-5H-pyrazolo[3,4-d]pyrimidin-4-one
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C22H28N6O2
 1
1
IC50 = 3.8 nM
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CP0958209
1-cyclopentyl-6-(1-{3-[(4,6-dimethylpyrimidin-2-yl)oxy]azetidin-1-yl}ethyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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C21H27N7O2
 1
1
IC50 = 3.81 nM
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CP0875593
6-(1-{3-[(3-methylquinoxalin-2-yl)oxy]azetidin-1-yl}ethyl)-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-, 4-one
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C24H27N7O3
 1
1
IC50 = 4.56 nM
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CP0078267
6-[(3S,4S)-4-methyl-1-[(2-methylpyrimidin-5-yl)methyl]pyrrolidin-3-yl]-1-(oxan-4-yl)-5H-pyrazolo[3,4-d]pyrimidin-4-one
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C21H27N7O2
 1
1
IC50 = 4.6 nM
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CP0543310
6-[(3S,4S)-1-[(2-fluorophenyl)methyl]-4-methylpyrrolidin-3-yl]-1-(oxan-4-yl)-5H-pyrazolo[3,4-d]pyrimidin-4-one
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C22H26FN5O2
 1
1
IC50 = 4.6 nM
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CP0841616
6-{1-[3-(phthalazin-1-yloxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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C23H25N7O3
 1
1
IC50 = 4.63 nM
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CP0476999
6-[(3S,4S)-1-benzyl-4-methylpyrrolidin-3-yl]-1-(oxan-4-yl)-5H-pyrazolo[3,4-d]pyrimidin-4-one
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C22H27N5O2
 1
1
IC50 = 4.9 nM
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CP0910086
US9328120, 16
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C20H22F2N6O
 1
1
IC50 = 5 nM
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CP0928194
US9328120, 2
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C19H23N5O3
 1
1
IC50 = 5 nM
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CP0954007
US9328120, 18 (enantiomer 1)
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C18H20F2N6OS
 1
1
IC50 = 5 nM
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CP0688414
1-cyclopentyl-6-{(1S)-1-[3-(4-methylphenoxy)azetidin-1-yl]ethyl}-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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C22H27N5O2
 1
1
IC50 = 5.37 nM
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CP0851630
6-{1-[3-(1,8-naphthyridin-2-yloxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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C23H25N7O3
 1
1
IC50 = 5.41 nM
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CP0578680
4-(2-oxa-7-azaspiro[3.5]nonan-7-yl)-2-oxo-8-propyl-5,6,7,8-tetrahydro-1H-1,6-naphthyridine-3-carbonitrile;2,2,2-trifluoroacetic acid
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C21H27F3N4O4
 1
1
IC50 = 6 nM
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CP0523690
6-[(3S,4S)-4-methyl-1-(pyridin-2-ylmethyl)pyrrolidin-3-yl]-1-(oxan-4-yl)-5H-pyrazolo[3,4-d]pyrimidin-4-one
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C21H26N6O2
 1
1
IC50 = 6.3 nM
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CP0037251
(-)2-({(trans)-2-[(3-isopropyl-7-oxo-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)methyl]cyclohexyl}amino)-4-(trifluoromethyl)pyrimidine-5-carboxylic acid
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C21H24F3N7O3
 1
1
IC50 = 7 nM
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CP0862910
US9328120, 32
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C20H21F2N5O
 1
1
IC50 = 7 nM
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CP0928196
US9328120, 13
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C19H20F2N6O
 1
1
IC50 = 7 nM
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CP0804184
6-(1-{3-[(4,6-dimethylpyrimidin-2-yl)oxy]azetidin-1-yl}ethyl)-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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C21H27N7O3
 1
1
IC50 = 7.45 nM
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CP0243948
6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(oxan-4-yl)-5H-pyrazolo[3,4-d]pyrimidin-4-one
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C20H25N7O2
 1
1
IC50 = 8.3 nM
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CP0955029
1-Cyclopentyl-6-{(1R)-1-[3-(pyrimidin-2-yloxy)azetidin-1-yl]ethyl}-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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C19H23N7O2
 1
1
IC50 = 9.49 nM
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CP0037249
US8829000, Referential Example 1
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C15H15ClN4O
 1
1
IC50 = 10 nM
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CP0578896
4-(4-methylphenyl)-2-oxo-8-propyl-5,6,7,8-tetrahydro-1H-quinoline-3-carbonitrile
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C20H22N2O
 1
1
IC50 = 10 nM
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CP0368880
1-cyclopentyl-6-[(1S)-1-(3-phenoxyazetidin-1-yl)ethyl]-5H-pyrazolo[3,4-d]pyrimidin-4-one
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C21H25N5O2
 1
1
IC50 = 10.5 nM
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CP0686512
6-{(1R)-1-[3-(4-Fluorophenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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C21H24FN5O3
 1
1
IC50 = 10.7 nM
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CP0920695
US9328120, 29
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C19H21N5O2
 1
1
IC50 = 11 nM
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CP0243949
6-[(3S,4S)-4-methyl-1-[(5-methylpyrazin-2-yl)methyl]pyrrolidin-3-yl]-1-(oxan-4-yl)-5H-pyrazolo[3,4-d]pyrimidin-4-one
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C21H27N7O2
 1
1
IC50 = 12 nM
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CP0122342
1-(oxan-4-yl)-6-[(1R)-1-(3-phenoxyazetidin-1-yl)ethyl]-5H-pyrazolo[3,4-d]pyrimidin-4-one
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C21H25N5O3
 1
1
IC50 = 12.5 nM
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CP0920693
US9328120, 10
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C18H21N5O2S
 1
1
IC50 = 13 nM
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CP0578901
4-(2-oxa-8-azaspiro[4.5]decan-8-yl)-2-oxo-8-propyl-5,6,7,8-tetrahydro-1H-1,6-naphthyridine-3-carbonitrile;hydrochloride
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C20H29ClN4O2
 1
1
IC50 = 13 nM
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CP0579267
4-(7-azaspiro[3.5]nonan-7-yl)-2-oxo-8-propyl-5,6,7,8-tetrahydro-1H-1,6-naphthyridine-3-carbonitrile;hydrochloride
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C20H29ClN4O
 1
1
IC50 = 13 nM
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CP0069183
2-chloro-4-[1-[1-[1-(oxan-4-yl)-4-oxo-5H-pyrazolo[3,4-d]pyrimidin-6-yl]ethyl]azetidin-3-yl]oxybenzonitrile
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C22H23ClN6O3
 1
1
IC50 = 13.2 nM
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CP0576481
4-(4-methylphenyl)-8-propyl-5,6,7,8-tetrahydro-1H-quinazolin-2-one
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C18H22N2O
 1
1
IC50 = 13.4 nM
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CP0942946
6-{1-[3-(quinazolin-2-yloxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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C23H25N7O3
 1
1
IC50 = 13.8 nM
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CP0955027
6-{1-[3-(2-chloro-4-methylphenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
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C24H27ClF3N5O5
 1
1
IC50 = 14.2 nM
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CP0773276
6-{1-[3-(3-chlorophenoxy)azetidin-1-yl]ethyl}-1-cyclopentyl-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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C21H24ClN5O2
 1
1
IC50 = 15.6 nM
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CP0875594
6-{1-[3-(isoquinolin-5-yloxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
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C26H27F3N6O5
 1
1
IC50 = 15.6 nM
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CP0863066
6-{1-[3-(4-methylphenoxy)azetidin-1-yl]propyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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C23H29N5O3
 1
1
IC50 = 16.5 nM
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CP0128879
2-(oxan-4-yl)-N-[(1R,2S)-2-[(7-oxo-3-propan-2-yl-2,6-dihydropyrazolo[4,3-d]pyrimidin-5-yl)methyl]cyclohexyl]acetamide
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C22H33N5O3
 1
1
IC50 = 19 nM
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CP0954006
US9328120, 9
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C19H21F2N5OS
 1
1
IC50 = 19 nM
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CP0090870
2-fluoro-5-[1-[1-[1-(oxan-4-yl)-4-oxo-5H-pyrazolo[3,4-d]pyrimidin-6-yl]ethyl]azetidin-3-yl]oxybenzonitrile
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C22H23FN6O3
 1
1
IC50 = 20 nM
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CP0578737
4-(4-methylphenyl)-2-oxo-8-propyl-5,6,7,8-tetrahydro-1H-1,6-naphthyridine-3-carbonitrile;hydrochloride
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C19H22ClN3O
 1
1
IC50 = 20 nM
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CP0955057
6-{1-[3-(pyrido[2,3-d]pyrimidin-2-yloxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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C22H24N8O3
 1
1
IC50 = 20.2 nM
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CP0959843
US9328120, 22
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C18H18ClF2N5OS
 1
1
IC50 = 21 nM
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CP0955055
4-({1-[1-(1-cyclopentyl-4-oxo-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-6-yl)ethyl]azetidin-3-yl}oxy)benzonitrile
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C22H24N6O2
 1
1
IC50 = 21.1 nM
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CP0864903
6-{1-[3-(quinolin-7-yloxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
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C26H27F3N6O5
 1
1
IC50 = 21.4 nM
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CP0883342
6-{1-[3-(2,3-dichlorophenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
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C23H24Cl2F3N5O5
 1
1
IC50 = 22.3 nM
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CP0947353
6-{1-[3-(4-methylphenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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C22H27N5O3
 1
1
IC50 = 22.5 nM
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CP0773280
6-(1-{3-[(6-methylpyridazin-3-yl)oxy]azetidin-1-yl}ethyl)-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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C20H25N7O3
 1
1
IC50 = 22.8 nM
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CP0092375
3-isopropyl-5-(((1S, 2R)-2-(6-methylpyridazin-3-ylamino)cyclohexyl)methyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
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C20H27N7O
 1
1
IC50 = 23 nM
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CP0862909
US9328120, 23
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C18H20N6O2
 1
1
IC50 = 23 nM
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CP0928195
US9328120, 3
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C17H19N5O3
 1
1
IC50 = 23 nM
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CP0580070
4-(8-azaspiro[4.5]decan-8-yl)-2-oxo-8-propyl-5,6,7,8-tetrahydro-1H-1,6-naphthyridine-3-carbonitrile;hydrochloride
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C21H31ClN4O
 1
1
IC50 = 23 nM
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CP0787449
6-{1-[3-(4-chloro-3-methylphenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
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C24H27ClF3N5O5
 1
1
IC50 = 23.3 nM
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CP0688416
3-[(1-{1-[4-oxo-1-(tetrahydro-2H-pyran-4-yl)-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-6-yl]ethyl}azetidin-3-yl)oxy]benzonitrile
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C22H24N6O3
 1
1
IC50 = 24.1 nM
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CP0773279
6-[1-(3-phenoxyazetldin-1-yl)propyl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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C22H27N5O3
 1
1
IC50 = 24.5 nM
   TI
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CP0576757
4-(4-methylphenyl)-8-(2-methylpropyl)-2-oxo-5,6,7,8-tetrahydro-1H-quinoline-3-carbonitrile
   Show/Hide
C21H24N2O
 1
1
IC50 = 25 nM
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CP0875592
6-{(1R)-1-[3-(pyridin-2-yloxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
   Show/Hide
C20H24N6O3
 1
1
IC50 = 27.2 nM
   TI
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CP0804186
2-[(1-{1-[4-oxo-1-(tetrahydro-2H-pyran-4-yl)-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-6-yl]ethyl}azetidin-3-yl)oxy]benzonitrile, trifluoroacetate salt
   Show/Hide
C24H25F3N6O5
 1
1
IC50 = 28.3 nM
   TI
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CP0883424
2-chloro-3-fluoro-6-[(1-{1-[4-oxo-1-(tetrahydro-2H-pyran-4-yl)-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-6-yl]ethyl}azetidin-3-yl)oxy]benzonitrile, trifluoroacetate salt
   Show/Hide
C24H23ClF4N6O5
 1
1
IC50 = 30.1 nM
   TI
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CP0962541
6-{1-[3-(2,5-dichlorophenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C23H24Cl2F3N5O5
 1
1
IC50 = 30.9 nM
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CP0906396
US9328120, 20
   Show/Hide
C20H20N6OS
 1
1
IC50 = 31 nM
   TI
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CP0920692
US9328120, 7
   Show/Hide
C19H21F2N5O2
 1
1
IC50 = 31 nM
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CP0688415
6-[(1R)-1-(3-benzylazetidin-1-yl)ethyl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
   Show/Hide
C22H27N5O2
 1
1
IC50 = 31.4 nM
   TI
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CP0841612
6-[(3-phenoxyazetidin-1-yl)(phenyl)methyl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
   Show/Hide
C26H27N5O3
 1
1
IC50 = 32 nM
   TI
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CP0959846
US9328120, 26
   Show/Hide
C19H17N7O
 1
1
IC50 = 32 nM
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CP0942950
6-{1-[3-(3-fluoro-5-methoxyphenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C24H27F4N5O6
 1
1
IC50 = 32.4 nM
   TI
   LI
   LO
   TS
CP0851632
3-fluoro-4-[(1-{1-[4-oxo-1-(tetrahydro-2H-pyran-4-yl)-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-6-yl]ethyl}azetidin-3-yl)oxy]benzonitrile, trifluoroacetate salt
   Show/Hide
C24H24F4N6O5
 1
1
IC50 = 33.2 nM
   TI
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CP0851633
6-[1-[3-(2-chloro-5-methoxyphenoxy)azetidin-1-yl]ethyl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C24H27ClF3N5O6
 1
1
IC50 = 34.4 nM
   TI
   LI
   LO
   TS
CP0147026
2-fluoro-4-[1-[1-[1-(oxan-4-yl)-4-oxo-5H-pyrazolo[3,4-d]pyrimidin-6-yl]ethyl]azetidin-3-yl]oxybenzonitrile
   Show/Hide
C22H23FN6O3
 1
1
IC50 = 34.8 nM
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CP0037255
(-)3-Isopropyl-5-{[(trans)-2-(pyrimidin-2-ylamino)cyclohexyl]methyl}-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
   Show/Hide
C19H25N7O
 1
1
IC50 = 35 nM
   TI
   LI
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CP0568847
8-butyl-4-(4-methylphenyl)-2-oxo-5,6,7,8-tetrahydro-1H-quinoline-3-carbonitrile
   Show/Hide
C21H24N2O
 1
1
IC50 = 35 nM
   TI
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   TS
CP0256873
N-[(1R,2S)-2-[(7-oxo-3-propan-2-yl-2,6-dihydropyrazolo[4,3-d]pyrimidin-5-yl)methyl]cyclohexyl]-2-pyrrolidin-1-ylacetamide
   Show/Hide
C21H32N6O2
 1
1
IC50 = 36 nM
   TI
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CP0864904
2-chloro-6-fluoro-3-[(1-{1-[4-oxo-1-(tetrahydro-2H-pyran-4-yl)-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-6-yl]ethyl}azetidin-3-yl)oxy]benzonitrile, trifluoroacetate salt
   Show/Hide
C24H23ClF4N6O5
 1
1
IC50 = 36.2 nM
   TI
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CP0816866
1-Cyclobutyl-6-{(1R)-1-[3-(pyrimidin-2-yloxy)azetidin-1-yl]ethyl}-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
   Show/Hide
C18H21N7O2
 1
1
IC50 = 37.3 nM
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CP0686515
6-{1-[3-(pyrazin-2-yloxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
   Show/Hide
C19H23N7O3
 1
1
IC50 = 39.9 nM
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CP0708063
6-(1-{3-[(7-chloroquinolin-4-yl)oxy]azetldin-1-yl}ethyl)-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C26H26ClF3N6O5
 1
1
IC50 = 40.4 nM
   TI
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CP0773283
6-{1-[3-(3,5-difluorophenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C23H24F5N5O5
 1
1
IC50 = 40.4 nM
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CP0037254
3-isopropyl-5-(2-(2-morpholinoethoxy)benzyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
   Show/Hide
C21H27N5O3
 1
1
IC50 = 41 nM
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CP0942948
3-chloro-4-[(1-{1-[4-oxo-1-(tetrahydro-2H-pyran-4-yl)-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-6-yl]ethyl}azetidin-3-yl)oxy]benzonitrile, trifluoroacetate salt
   Show/Hide
C24H24ClF3N6O5
 1
1
IC50 = 42.6 nM
   TI
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CP0914444
1-isopropyl-6-{1-[3-(4-methylphenoxy)azetidin-1-yl]ethyl}-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
   Show/Hide
C20H25N5O2
 1
1
IC50 = 42.9 nM
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CP0967405
1-(tetrahydro-2H-pyran-4-yl)-6-(1-{3-[3-(trifluoromethyl)phenoxy]azetidin-1-yl}ethyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C24H25F6N5O5
 1
1
IC50 = 43.6 nM
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CP0914447
5-chloro-2-[(1-{1-[4-oxo-1-(tetrahydro-2H-pyran-4-yl)-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-6-yl]ethyl}azetidin-3-yl)oxy]benzonitrile, trifluoroacetate salt
   Show/Hide
C24H24ClF3N6O5
 1
1
IC50 = 44.7 nM
   TI
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CP0688418
6-{1-[3-(3-chloro-2-fluorophenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C23H24ClF4N5O5
 1
1
IC50 = 44.9 nM
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CP0545563
4-(4,4-dimethylpiperidin-1-yl)-2-oxo-8-propyl-5,6,7,8-tetrahydro-1H-1,6-naphthyridine-3-carbonitrile;hydrochloride
   Show/Hide
C19H29ClN4O
 1
1
IC50 = 45 nM
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CP0675505
6-{1-[3-(Pyrimidin-2-yloxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
   Show/Hide
C19H23N7O3
 1
1
IC50 = 45.3 nM
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CP0071234
1-{(1R,2S)-2-[(3-isopropyl-7-oxo-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)methyl]cyclohexyl}-3-(3-morpholin-4-ylpropyl)urea
   Show/Hide
C23H37N7O3
 1
1
IC50 = 46 nM
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CP0957847
1-cyclopentyl-6-(1-{3-[4-(trifluoromethyl)phenoxy]azetidin-1-yl}ethyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
   Show/Hide
C22H24F3N5O2
 1
1
IC50 = 47 nM
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CP0686518
6-{1-[3-(2,3-difluoro-4-methylphenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C24H26F5N5O5
 1
1
IC50 = 47.2 nM
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CP0871236
6-{1-[3-(2-chloro-3,4-difluorophenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C23H23ClF5N5O5
 1
1
IC50 = 48.8 nM
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CP0921110
1-(tetrahydro-2H-pyran-4-yl)-6-(1-{3-[3-(trifluoromethoxy)phenoxy]azetidin-1-yl}ethyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C24H25F6N5O6
 1
1
IC50 = 48.9 nM
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   LO
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CP0883340
6-[(1R)-1-(3-benzyl-3-fluoroazetidin-1-yl)ethyl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
   Show/Hide
C22H26FN5O2
 1
1
IC50 = 50.3 nM
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CP0831183
1-(tetrahydro-2H-pyran-4-yl)-6-(1-{3-[3,4,5-trifluorophenoxy]azetidin-1-yl}ethyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C23H23F6N5O5
 1
1
IC50 = 51.4 nM
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CP0838686
6-{1-[3-(2-chlorophenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C23H25ClF3N5O5
 1
1
IC50 = 52.1 nM
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   TS
CP0042235
3-isopropyl-5-(2-(trifluoromethoxy)benzyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
   Show/Hide
C16H15F3N4O2
 1
1
IC50 = 56 nM
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CP0796482
6-{1-[3-(quinolin-2-yloxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
   Show/Hide
C24H26N6O3
 1
1
IC50 = 57.2 nM
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CP0942949
6-{1-[3-(2,5-difluorophenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C23H24F5N5O5
 1
1
IC50 = 57.4 nM
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CP0941862
US9328120, 6
   Show/Hide
C19H21F2N5O2
 1
1
IC50 = 58 nM
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CP0851634
6-{1-[3-(isoquinolin-7-yloxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C26H27F3N6O5
 1
1
IC50 = 58.3 nM
   TI
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CP0955056
6-{1-[3-(pyrimidin-4-yloxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
   Show/Hide
C19H23N7O3
 1
1
IC50 = 59.4 nM
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CP0862907
US9328120, 5
   Show/Hide
C20H23F2N5O2
 1
1
IC50 = 60 nM
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CP0578775
8-ethyl-4-(4-methylphenyl)-2-oxo-5,6,7,8-tetrahydro-1H-quinoline-3-carbonitrile
   Show/Hide
C19H20N2O
 1
1
IC50 = 60 nM
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CP0705291
6-{1-[3-(3-chloro-4-fluorophenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C23H24ClF4N5O5
 1
1
IC50 = 63.8 nM
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   TS
CP0957496
6-[1-[3-(2-chloro-4,5-difluorophenoxy)azetidin-1-yl]ethyl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C23H23ClF5N5O5
 1
1
IC50 = 64.6 nM
   TI
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CP0942947
5-fluoro-2-[(1-{1-[4-oxo-1-(tetrahydro-2H-pyran-4-yl)-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-6-yl]ethyl}azetidin-3-yl)oxy]benzonitrile, trifluoroacetate salt
   Show/Hide
C24H24F4N6O5
 1
1
IC50 = 69.4 nM
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   TS
CP0955058
6-(1-{3-[(4-fluoro-2,3-dihydro-1-benzofuran-7-yl)oxy]azetidin-1-yl}ethyl)-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C25H27F4N5O6
 1
1
IC50 = 70.1 nM
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CP0169565
4-[1-[1-[1-(oxan-4-yl)-4-oxo-5H-pyrazolo[3,4-d]pyrimidin-6-yl]ethyl]azetidin-3-yl]oxybenzonitrile
   Show/Hide
C22H24N6O3
 1
1
IC50 = 70.2 nM
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CP0883341
6-{1-[3-(2-chloro-4-fluorophenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C23H24ClF4N5O5
 1
1
IC50 = 74.5 nM
   TI
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   LO
   TS
CP0831870
6-{1-[3-(3,4-difluoro-2-methylphenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C24H26F5N5O5
 1
1
IC50 = 78.7 nM
   TI
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   TS
CP0910085
US9328120, 12
   Show/Hide
C18H20F2N6OS
 1
1
IC50 = 80 nM
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CP0914441
1-Isopropyl-6-[1-(3-phenoxyazetidin-1-yl)ethyl]-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
   Show/Hide
C19H23N5O2
 1
1
IC50 = 81.7 nM
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   TS
CP0039447
5-(2-(benzyloxy)benzyl)-3-isopropyl-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
   Show/Hide
C22H22N4O2
 1
1
IC50 = 82 nM
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   TS
CP0914442
6-[(1R)-1-(3-Phenylazetidin-1-yl)ethyl]-1-tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
   Show/Hide
C21H25N5O2
 1
1
IC50 = 82.4 nM
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   TS
CP0957511
6-{1-[3-(4-chloro-2-methylphenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C24H27ClF3N5O5
 1
1
IC50 = 84.5 nM
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CP0910084
US9328120, 8
   Show/Hide
C20H20N6O2
 1
1
IC50 = 85 nM
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CP0576476
8-ethoxy-4-(4-methylphenyl)-2-oxo-5,6,7,8-tetrahydro-1H-quinoline-3-carbonitrile
   Show/Hide
C19H20N2O2
 1
1
IC50 = 85 nM
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   TS
CP0665654
6-{1-[3-(3-chlorophenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C23H25ClF3N5O5
 1
1
IC50 = 85.6 nM
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   TS
CP0154317
3-isopropyl-5-{[(1S,2R)-2-(2-morpholin-4-ylethoxy)cyclohexyl]methyl}-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
   Show/Hide
C21H33N5O3
 1
1
IC50 = 87 nM
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   TS
CP0838687
6-{1-[3-(4-chlorophenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C23H25ClF3N5O5
 1
1
IC50 = 88.2 nM
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CP0487994
6-[(3S,4S)-4-methylpyrrolidin-3-yl]-1-(oxan-4-yl)-5H-pyrazolo[3,4-d]pyrimidin-4-one
   Show/Hide
C15H21N5O2
 1
1
IC50 = 89 nM
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   TS
CP0578900
4-(2,2-difluoro-6-azaspiro[2.5]octan-6-yl)-2-oxo-8-propyl-5,6,7,8-tetrahydro-1H-1,6-naphthyridine-3-carbonitrile;hydrochloride
   Show/Hide
C19H25ClF2N4O
 1
1
IC50 = 89 nM
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   TS
CP0864902
6-[(1R)-1-(3-benzyl-3-hydroxyazetidin-1-yl)ethyl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
   Show/Hide
C22H27N5O3
 1
1
IC50 = 89.2 nM
   TI
   LI
   LO
   TS
CP0688417
6-{1-[3-(2-fluoro-5-methylphenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C24H27F4N5O5
 1
1
IC50 = 90.8 nM
   TI
   LI
   LO
   TS
CP0967404
6-{1-[3-(2-chloro-6-fluorophenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dlhydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C23H24ClF4N5O5
 1
1
IC50 = 91.1 nM
   TI
   LI
   LO
   TS
CP0580147
4-(4-cyanopiperidin-1-yl)-2-oxo-8-propyl-5,6,7,8-tetrahydro-1H-1,6-naphthyridine-3-carbonitrile;hydrochloride
   Show/Hide
C18H24ClN5O
 1
1
IC50 = 92 nM
   TI
   LI
   LO
   TS
CP0688860
6-{1-[3-(4-chloro-2-fluorophenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C23H24ClF4N5O5
 1
1
IC50 = 99.1 nM
   TI
   LI
   LO
   TS
CP0576485
4-(8,8-difluoro-6-azaspiro[2.5]octan-6-yl)-2-oxo-8-propyl-5,6,7,8-tetrahydro-1H-1,6-naphthyridine-3-carbonitrile;hydrochloride
   Show/Hide
C19H25ClF2N4O
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0708064
1-(tetrahydro-2H-pyran-4-yl)-6-{1-[3-(2,4,5-trifluorophenoxy)azetidin-1-yl]ethyl}-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C23H23F6N5O5
 1
1
IC50 = 102 nM
   TI
   LI
   LO
   TS
CP0688419
1-(tetrahydro-2H-pyran-4-yl)-6-(1-{3-[4-(trifluoromethyl)phenoxy]azetidin-1-yl}ethyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C24H25F6N5O5
 1
1
IC50 = 107 nM
   TI
   LI
   LO
   TS
CP0773284
1-(tetrahydro-2H-pyran-4-yl)-6-{1-[3-(2,3,4-trifluorophenoxy)azetidin-1-yl]ethyl}-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C23H23F6N5O5
 1
1
IC50 = 110 nM
   TI
   LI
   LO
   TS
CP0838685
6-{1-[3-(2,6-difluorophenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C23H24F5N5O5
 1
1
IC50 = 112 nM
   TI
   LI
   LO
   TS
CP0831869
6-{1-[3-(5-fluoro-2-methylphenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C24H27F4N5O5
 1
1
IC50 = 119 nM
   TI
   LI
   LO
   TS
CP0543875
4-(4-methylphenyl)-2-oxo-8-propan-2-yl-5,6,7,8-tetrahydro-1H-quinoline-3-carbonitrile
   Show/Hide
C20H22N2O
 1
1
IC50 = 130 nM
   TI
   LI
   LO
   TS
CP0942924
1-cyclopentyl-6-{(1R)-1-[(3R)-3-phenylpyrrolidin-1-yl]propyl}-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
   Show/Hide
C23H29N5O
 1
1
IC50 = 136 nM
   TI
   LI
   LO
   TS
CP0579265
4-(4-methylphenyl)-2-oxo-8-(2,2,2-trifluoroethyl)-5,6,7,8-tetrahydro-1H-quinoline-3-carbonitrile
   Show/Hide
C19H17F3N2O
 1
1
IC50 = 140 nM
   TI
   LI
   LO
   TS
CP0705290
6-{1-[3-(2-chlorophenyl)pyrrolidin-1-yl]ethyl}-1-cyclopentyl-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C24H27ClF3N5O3
 1
1
IC50 = 148 nM
   TI
   LI
   LO
   TS
CP0967403
6-{1-[3-(2-fluorophenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4Hpyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C23H25F4N5O5
 1
1
IC50 = 148 nM
   TI
   LI
   LO
   TS
CP0486715
6-[(3R,4R)-1-benzyl-4-methylpyrrolidin-3-yl]-1-(oxan-4-yl)-5H-pyrazolo[3,4-d]pyrimidin-4-one
   Show/Hide
C22H27N5O2
 1
1
IC50 = 152 nM
   TI
   LI
   LO
   TS
CP0579266
4-(4-methylpiperidin-1-yl)-2-oxo-8-propyl-5,6,7,8-tetrahydro-1H-1,6-naphthyridine-3-carbonitrile
   Show/Hide
C18H26N4O
 1
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
CP0773282
1-cyclopentyl-6-{1-[(3R)-3-(2-methoxyphenoxy)pyrrolidin-1-yl]ethyl}-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C25H30F3N5O5
 1
1
IC50 = 211 nM
   TI
   LI
   LO
   TS
CP0787422
1-cyclopentyl-6-{(1R)-1-[(3R)-3-phenylpyrrolidin-1-yl]ethyl}-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
   Show/Hide
C22H27N5O
 1
1
IC50 = 211 nM
   TI
   LI
   LO
   TS
CP0914446
6-{1-[3-(2,4-difluorophenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C23H24F5N5O5
 1
1
IC50 = 211 nM
   TI
   LI
   LO
   TS
CP0957653
6-{1-[3-(2-chloro-6-methylphenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C24H27ClF3N5O5
 1
1
IC50 = 215 nM
   TI
   LI
   LO
   TS
CP0787448
1-isopropyl-6-{1-[3-(4-methylphenoxy)azetidin-1-yl]propyl}-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
   Show/Hide
C21H27N5O2
 1
1
IC50 = 216 nM
   TI
   LI
   LO
   TS
CP0919514
1-cyclopentyl-6-{(1R)-1-[3-(4-methylphenoxy)azetidin-1-yl]ethyl}-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
   Show/Hide
C22H27N5O2
 1
1
IC50 = 222 nM
   TI
   LI
   LO
   TS
CP0773281
1-cyclopentyl-6-[1-(3-phenylpyrrolidin-1-yl)ethyl]-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C24H28F3N5O3
 1
1
IC50 = 230 nM
   TI
   LI
   LO
   TS
CP0941863
US9328120, 11
   Show/Hide
C20H24F2N6OS
 1
1
IC50 = 233 nM
   TI
   LI
   LO
   TS
CP0686519
6-{1-[3-(4-tert-butylphenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dlhydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C27H34F3N5O5
 1
1
IC50 = 234 nM
   TI
   LI
   LO
   TS
CP0913595
US9328120, 4
   Show/Hide
C18H20F2N6O2
 1
1
IC50 = 242 nM
   TI
   LI
   LO
   TS
CP0883338
6-{1-[3-(pyridin-2-yloxy)azetidin-1-yl]propyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
   Show/Hide
C21H26N6O3
 1
1
IC50 = 245 nM
   TI
   LI
   LO
   TS
CP0952682
1-isopropyl-6-[1-(3-phenoxyazetidin-1-yl)propyl]-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
   Show/Hide
C20H25N5O2
 1
1
IC50 = 256 nM
   TI
   LI
   LO
   TS
CP0914445
6-{1-[3-(pyridin-3-yloxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4Hpyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C22H25F3N6O5
 1
1
IC50 = 310 nM
   TI
   LI
   LO
   TS
CP0576482
4-(4,4-dimethylpiperidin-1-yl)-2-oxo-1H-1,5-naphthyridine-3-carbonitrile
   Show/Hide
C16H18N4O
 1
1
IC50 = 330 nM
   TI
   LI
   LO
   TS
CP0851631
1-cyclopentyl-6-[1-(3-pyridin-4-ylpyrrolidin-1-yl)ethyl]-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C23H27F3N6O3
 1
1
IC50 = 382 nM
   TI
   LI
   LO
   TS
CP0578899
4-(3-ethyl-1,2-oxazol-5-yl)-2-oxo-8-propyl-5,6,7,8-tetrahydro-1H-1,6-naphthyridine-3-carbonitrile;hydrochloride
   Show/Hide
C17H21ClN4O2
 1
1
IC50 = 410 nM
   TI
   LI
   LO
   TS
CP0578504
4-(4-cyanophenyl)-2-oxo-8-propyl-5,6,7,8-tetrahydro-1H-1,6-naphthyridine-3-carbonitrile;hydrochloride
   Show/Hide
C19H19ClN4O
 1
1
IC50 = 430 nM
   TI
   LI
   LO
   TS
CP0926809
US9328120, 21
   Show/Hide
C17H18F2N6O2
 1
1
IC50 = 433 nM
   TI
   LI
   LO
   TS
CP0953088
US9328120, 1
   Show/Hide
C19H21F2N5O2
 1
1
IC50 = 450 nM
   TI
   LI
   LO
   TS
CP0163475
3-isopropyl-1-methyl-5-(2-(2-morpholinoethoxy)benzyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one
   Show/Hide
C22H29N5O3
 1
1
IC50 = 530 nM
   TI
   LI
   LO
   TS
CP0572328
4-(4-methylphenyl)-2-oxo-5,6,7,8-tetrahydro-1H-quinoline-3-carbonitrile
   Show/Hide
C17H16N2O
 1
1
IC50 = 530 nM
   TI
   LI
   LO
   TS
CP0568057
4-(5-ethylpyridin-2-yl)-2-oxo-8-propyl-5,6,7,8-tetrahydro-1H-1,6-naphthyridine-3-carbonitrile;hydrochloride
   Show/Hide
C19H23ClN4O
 1
1
IC50 = 570 nM
   TI
   LI
   LO
   TS
CP0946221
6-(1-azetidin-1-ylethyl)-1-cyclopentyl-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, trifluoroacetate salt
   Show/Hide
C17H22F3N5O3
 1
1
IC50 = 593 nM
   TI
   LI
   LO
   TS
CP0580236
4-(5-ethyl-1,3-thiazol-2-yl)-2-oxo-8-propyl-5,6,7,8-tetrahydro-1H-1,6-naphthyridine-3-carbonitrile;hydrochloride
   Show/Hide
C17H21ClN4OS
 1
1
IC50 = 600 nM
   TI
   LI
   LO
   TS
CP0577383
4-(4,4-dimethylpiperidin-1-yl)-8-ethyl-2-oxo-1H-1,5-naphthyridine-3-carbonitrile
   Show/Hide
C18H22N4O
 1
1
IC50 = 610 nM
   TI
   LI
   LO
   TS
CP0578898
4-(6-methylpyridin-3-yl)-2-oxo-8-propyl-5,6,7,8-tetrahydro-1H-1,6-naphthyridine-3-carbonitrile;hydrochloride
   Show/Hide
C18H21ClN4O
 1
1
IC50 = 630 nM
   TI
   LI
   LO
   TS
CP0580145
2-oxo-8-propyl-4-pyridin-4-yl-5,6,7,8-tetrahydro-1H-1,6-naphthyridine-3-carbonitrile;dihydrochloride
   Show/Hide
C17H20Cl2N4O
 1
1
IC50 = 640 nM
   TI
   LI
   LO
   TS
CP0580146
4-(4-methylphenyl)-2-oxo-1H-1,5-naphthyridine-3-carbonitrile
   Show/Hide
C16H11N3O
 1
1
IC50 = 725 nM
   TI
   LI
   LO
   TS
CP0579563
8-methyl-4-(4-methylphenyl)-2-oxo-5,6,7,8-tetrahydro-1H-1,5-naphthyridine-3-carbonitrile;hydrochloride
   Show/Hide
C17H18ClN3O
 1
1
IC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0385143
2-[4-[4-ethoxy-3-(3-ethyl-1-methyl-7-oxo-6H-pyrazolo[4,3-d]pyrimidin-5-yl)phenoxy]piperidin-1-yl]-N-hydroxypyrimidine-5-carboxamide
   Show/Hide
C26H30N8O5
 1
1
IC50 = 4800 nM
   TI
   LI
   LO
   TS
CP0578897
8-methyl-4-(4-methylphenyl)-2-oxo-5,6,7,8-tetrahydro-1H-1,7-naphthyridine-3-carbonitrile;hydrochloride
   Show/Hide
C17H18ClN3O
 1
1
IC50 = 7000 nM
   TI
   LI
   LO
   TS
CP0414199
4-[[1-(2-chlorophenyl)-4-methyl-[1,2,4]triazolo[4,3-a]quinoxalin-8-yl]methyl]morpholine
   Show/Hide
C21H20ClN5O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0090153
4-[[1-(5-butoxypyridin-3-yl)-4-methyl-[1,2,4]triazolo[4,3-a]quinoxalin-8-yl]methyl]morpholine
   Show/Hide
C24H28N6O2
 1
1
IC50 > 10000 nM
   TI
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   TS
CP0147040
US11419874, Example 28
   Show/Hide
C15H10ClN5
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0006487
2-oxo-N-[1-[4-(trifluoromethoxy)phenyl]propyl]-1,3-dihydropyrido[2,3-b]pyrazine-4-carboxamide
   Show/Hide
C18H17F3N4O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0248670
5,8-dimethyl-2-(2-phenylimidazo[1,2-a]pyrimidin-7-yl)-[1,2,4]triazolo[1,5-a]pyrazine
   Show/Hide
C19H15N7
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0366792
5,8-Dimethyl-2-(2-phenyl-1H-benzimidazol-5-yl)[1,2,4]triazolo[1,5-a]pyrazine
   Show/Hide
C20H16N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0389044
5,8-dimethyl-2-(2-pyridin-3-yl-3H-benzimidazol-5-yl)-[1,2,4]triazolo[1,5-a]pyrazine
   Show/Hide
C19H15N7
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0389045
2-[2-(5-chlorothiophen-2-yl)-3H-benzimidazol-5-yl]-5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazine
   Show/Hide
C18H13ClN6S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0396021
5,8-dimethyl-2-(2-thiophen-2-yl-3H-benzimidazol-5-yl)-[1,2,4]triazolo[1,5-a]pyrazine
   Show/Hide
C18H14N6S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0396022
5-[6-(5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazin-2-yl)-1H-benzimidazol-2-yl]-1,3-thiazole
   Show/Hide
C17H13N7S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0396025
2-[2-(2-methoxyphenyl)imidazo[1,2-a]pyrimidin-7-yl]-5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazine
   Show/Hide
C20H17N7O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0408074
2-[2-(3-bromophenyl)-3H-benzimidazol-5-yl]-5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazine
   Show/Hide
C20H15BrN6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0408075
2-[2-(4-fluorophenyl)imidazo[1,2-a]pyrimidin-7-yl]-5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazine
   Show/Hide
C19H14FN7
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0408076
2-[2-(3-chlorophenyl)imidazo[1,2-a]pyrimidin-7-yl]-5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazine
   Show/Hide
C19H14ClN7
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0412213
2-[6-(5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazin-2-yl)-1H-benzimidazol-2-yl]-5-methyl-1,3-thiazole
   Show/Hide
C18H15N7S
 1
1
IC50 > 10000 nM
   TI
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   LO
   TS
CP0412218
US10138245, Example 56
   Show/Hide
C19H15N7
 1
1
IC50 > 10000 nM
   TI
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   TS
CP0412219
US10138245, Example 2
   Show/Hide
C20H15FN6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0412220
2-[2-(2-Methoxyphenyl)-1H-benzimidazol-5-yl]-5,8-dimethyl[1,2,4]triazolo[1,5-a]pyrazine
   Show/Hide
C21H18N6O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0482326
5,7-Dimethyl-2-(2-phenyl-1H-benzo[d]imidazol-5-yl)-[1,2,4]triazolo-[1,5-a]pyrimidine
   Show/Hide
C20H16N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0482327
5,8-Dimethyl-2-[2-(1,3-thiazol-2-yl)-1H-benz-imidazol-5-yl][1,2,4]triazolo[1,5-a]pyrazine
   Show/Hide
C17H13N7S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0482328
2-[2-(4-FLuorophenyl)-1H-benzimidazol-5-yl]-5,8-dimethyl[1,2,4]triazolo[1,5-a]pyrazine
   Show/Hide
C20H15FN6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0482329
2-[6-(5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazin-2-yl)-1H-benzimidazol-2-yl]-4-methyl-1,3-thiazole
   Show/Hide
C18H15N7S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0513387
5,8-Dimethyl-2-[2-(pyridin-2-yl)-1H-benzimidazol-5-yl][1,2,4]triazolo[1,5-a]pyrazine
   Show/Hide
C19H15N7
 1
1
IC50 > 10000 nM
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CP0513391
2-[2-(3-methoxypyridin-2-yl)-3H-benzimidazol-5-yl]-5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazine
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C20H17N7O
 1
1
IC50 > 10000 nM
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CP0555893
2-[2-(furan-2-yl)-3H-benzimidazol-5-yl]-5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazine
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C18H14N6O
 1
1
IC50 > 10000 nM
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CP0862252
2-(2-Bromophenyl)-7-{5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazin-2-yl}imidazo[1,2-a]pyrimidine
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C19H14BrN7
 1
1
IC50 > 10000 nM
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CP0865138
2-(7-{5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazin-2-yl}imidazo[1,2-a]pyrimidin-2-yl)pyridine
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C18H14N8
 1
1
IC50 > 10000 nM
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CP0865140
6-{5,8-Dimethyl-[1,2,4]triazolo[1,5-a]pyrazin-2-yl}-2-(3-fluoropyridin-2-yl)-1H-1,3-benzodiazole
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C19H14FN7
 1
1
IC50 > 10000 nM
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CP0905292
2-(7-{5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazin-2-yl}imidazo[1,2-a]pyrimidin-2-yl)-1,3-thiazole
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C16H12N8S
 1
1
IC50 > 10000 nM
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CP0012519
5-[[4-ethoxy-3-(1-methyl-7-oxo-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-5-yl)phenyl]methyl]-N-hydroxythiophene-2-carboxamide
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C23H25N5O4S
 1
1
IC50 > 10000 nM
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CP0000847
(2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,17-triazatetracyclo[8.7.0.0^{3,8}.0^{11,16}]heptadeca-1(10),11(16),12,14-tetraene-4,7-dione
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C22H19N3O4
 1
1
IC50 > 10000 nM
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CP0010658
5-[2-ethoxy-5-(4-methyl-1-piperazinylsulfonyl)phenyl]-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
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C22H30N6O4S
 1
1
IC50 > 10000 nM
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CP0384486
N-[3-(4,5-diethyl-6-oxo-1H-pyrimidin-2-yl)-4-propoxyphenyl]-2-(4-methylpiperazin-1-yl)acetamide
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C24H35N5O3
 1
1
IC50 > 10000 nM
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CP0486657
[3-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperidin-1-yl]-(3,4,5-trimethoxyphenyl)methanone
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C20H23N5O4
 1
1
IC50 > 10000 nM
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CP0176508
[4-[3-(3-fluoro-4-methoxyphenyl)-5-(2-methylphenyl)-3,4-dihydropyrazol-2-yl]phenyl]-(4-methylpiperazin-1-yl)methanone
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C29H31FN4O2
 1
1
IC50 > 10000 nM
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CP0365459
[4-[5-tert-butyl-3-(3,5-difluoro-4-methoxyphenyl)-3,4-dihydropyrazol-2-yl]phenyl]-(4-methylpiperazin-1-yl)methanone
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C26H32F2N4O2
 1
1
IC50 > 10000 nM
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CP0419692
N-(2-hydroxyethyl)-4-[3-(4-methoxyphenyl)-5-(2-methylphenyl)-3,4-dihydropyrazol-2-yl]benzamide
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C26H27N3O3
 1
1
IC50 > 10000 nM
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CP0419693
[4-[5-tert-butyl-3-(2,3-difluoro-4-methoxyphenyl)-3,4-dihydropyrazol-2-yl]phenyl]-(4-methylpiperazin-1-yl)methanone
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C26H32F2N4O2
 1
1
IC50 > 10000 nM
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CP0444327
[4-[3-(4-methoxyphenyl)-5-(2-methylphenyl)-3,4-dihydropyrazol-2-yl]phenyl]-(4-methylpiperazin-1-yl)methanone
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C29H32N4O2
 1
1
IC50 > 10000 nM
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CP0013428
N-[(1S)-1-[3-fluoro-4-(trifluoromethoxy)phenyl]-2-methoxyethyl]-7-methoxy-2-oxo-1,3-dihydropyrido[2,3-b]pyrazine-4-carboxamide
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C19H18F4N4O5
 1
1
IC50 > 30000 nM
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CP0580144
1-methyl-4-(4-methylphenyl)-2-oxo-8-propyl-5,6,7,8-tetrahydro-1,6-naphthyridine-3-carbonitrile
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C20H23N3O
 1
1
IC50 > 10 nM
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CP0257911
(10S,15S)-13-ethyl-10-(5-ethylfuran-2-yl)-8,11,13-triazatetracyclo[7.7.0.02,7.011,15]hexadeca-1(9),2,4,6-tetraene-12,14-dione
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C21H21N3O3
 1
1
IC50 > 3000 nM
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CP0268684
(2S,8R)-2-(5-ethylthiophen-2-yl)-6-methyl-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dione
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C21H21N3O2S
 1
1
IC50 > 4000 nM
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0037249
US8829000, Referential Example 1
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C15H15ClN4O
 1
1 IC50 = 8 nM
CP0243948
6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(oxan-4-yl)-5H-pyrazolo[3,4-d]pyrimidin-4-one
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C20H25N7O2
 3
1 IC50 = 8 nM
2 IC50 = 8.3 nM
3 IC50 = 49 nM
CP0958208
6-{1-[3-(quinoxalin-2-yloxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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C23H25N7O3
 1
1 IC50 = 8.47 nM
CP0686512
6-{(1R)-1-[3-(4-Fluorophenoxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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C21H24FN5O3
 1
1 IC50 = 12.18 nM
CP0688415
6-[(1R)-1-(3-benzylazetidin-1-yl)ethyl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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C22H27N5O2
 1
1 IC50 = 13.2 nM
CP0523690
6-[(3S,4S)-4-methyl-1-(pyridin-2-ylmethyl)pyrrolidin-3-yl]-1-(oxan-4-yl)-5H-pyrazolo[3,4-d]pyrimidin-4-one
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C21H26N6O2
 1
1 IC50 = 14 nM
CP0271210
6-[(3S,4S)-1-[(4-fluorophenyl)methyl]-4-methylpyrrolidin-3-yl]-1-(oxan-4-yl)-5H-pyrazolo[3,4-d]pyrimidin-4-one
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C22H26FN5O2
 1
1 IC50 = 17 nM
CP0069183
2-chloro-4-[1-[1-[1-(oxan-4-yl)-4-oxo-5H-pyrazolo[3,4-d]pyrimidin-6-yl]ethyl]azetidin-3-yl]oxybenzonitrile
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C22H23ClN6O3
 1
1 IC50 = 19 nM
CP0122342
1-(oxan-4-yl)-6-[(1R)-1-(3-phenoxyazetidin-1-yl)ethyl]-5H-pyrazolo[3,4-d]pyrimidin-4-one
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C21H25N5O3
 2
1 IC50 = 22 nM
2 IC50 = 22.5 nM
CP0914442
6-[(1R)-1-(3-Phenylazetidin-1-yl)ethyl]-1-tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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C21H25N5O2
 1
1 IC50 = 25.4 nM
CP0078267
6-[(3S,4S)-4-methyl-1-[(2-methylpyrimidin-5-yl)methyl]pyrrolidin-3-yl]-1-(oxan-4-yl)-5H-pyrazolo[3,4-d]pyrimidin-4-one
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C21H27N7O2
 1
1 IC50 = 36 nM
CP0147026
2-fluoro-4-[1-[1-[1-(oxan-4-yl)-4-oxo-5H-pyrazolo[3,4-d]pyrimidin-6-yl]ethyl]azetidin-3-yl]oxybenzonitrile
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C22H23FN6O3
 1
1 IC50 = 43 nM
CP0090870
2-fluoro-5-[1-[1-[1-(oxan-4-yl)-4-oxo-5H-pyrazolo[3,4-d]pyrimidin-6-yl]ethyl]azetidin-3-yl]oxybenzonitrile
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C22H23FN6O3
 1
1 IC50 = 47 nM
CP0243949
6-[(3S,4S)-4-methyl-1-[(5-methylpyrazin-2-yl)methyl]pyrrolidin-3-yl]-1-(oxan-4-yl)-5H-pyrazolo[3,4-d]pyrimidin-4-one
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C21H27N7O2
 1
1 IC50 = 59 nM
CP0675505
6-{1-[3-(Pyrimidin-2-yloxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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C19H23N7O3
 1
1 IC50 = 63 nM
CP0919514
1-cyclopentyl-6-{(1R)-1-[3-(4-methylphenoxy)azetidin-1-yl]ethyl}-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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C22H27N5O2
 1
1 IC50 = 67.1 nM
CP0169565
4-[1-[1-[1-(oxan-4-yl)-4-oxo-5H-pyrazolo[3,4-d]pyrimidin-6-yl]ethyl]azetidin-3-yl]oxybenzonitrile
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C22H24N6O3
 1
1 IC50 = 70 nM
CP0686515
6-{1-[3-(pyrazin-2-yloxy)azetidin-1-yl]ethyl}-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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C19H23N7O3
 1
1 IC50 = 73.5 nM
CP0952932
4-[[(3S,4S)-3-(1-cyclopentyl-4-oxo-5H-pyrazolo[3,4-d]pyrimidin-6-yl)-4-methyl-pyrrolidin-1-yl]methyl]benzenecarbohydroxamic acid
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C23H28N6O3
 1
1 IC50 = 107 nM
CP0368880
1-cyclopentyl-6-[(1S)-1-(3-phenoxyazetidin-1-yl)ethyl]-5H-pyrazolo[3,4-d]pyrimidin-4-one
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C21H25N5O2
 1
1 IC50 = 986 nM
CP0010658
5-[2-ethoxy-5-(4-methyl-1-piperazinylsulfonyl)phenyl]-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
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C22H30N6O4S
 4
1 IC50 = 3400 nM
2 IC50 = 3600 nM
3 IC50 = 5600 nM
4 IC50 > 10000 nM
CP0000847
(2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,17-triazatetracyclo[8.7.0.0^{3,8}.0^{11,16}]heptadeca-1(10),11(16),12,14-tetraene-4,7-dione
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C22H19N3O4
 1
1 IC50 > 10000 nM
Clinical Information about the Protein
Target 1 ( Phosphodiesterase 9 (PDE9) )
Target Type Clinical trial Target
Disease 4 Target-related Diseases  4
1 Psychiatric disorder [ICD-11: 6E8Z]
2 Sickle-cell disorder [ICD-11: 3A51]
3 Alzheimer disease [ICD-11: 8A20]
4 Cognitive impairment [ICD-11: 6D71]
Clinical Trial Drug(s) 3 Clinical Trial Drugs  3
1 BI-409306 Phase 2
Psychiatric disorder
2 IMR-687 Phase 2
Sickle-cell disorder
3 PF-4447943 Phase 2
Alzheimer disease
Investigative Drug(s) 1 Investigative Drug  1
1 PF-4181366 Investigative
Cognitive impairment