General Information of the Protein
Protein ID
PT01798
Protein Name
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A
Secondarily
Protein Name
Cyclic GMP-inhibited phosphodiesterase A
cGMP-inhibited cAMP phosphodiesterase
Gene Name
PDE3A
Sequence
MAVPGDAARVRDKPVHSGVSQAPTAGRDCHHRADPASPRDSGCRGCWGDLVLQPLRSSRKLSSALCAGSLSFLLALLVRLVRGEVGCDLEQCKEAAAAEEEEAAPGAEGGVFPGPRGGAPGGGARLSPWLQPSALLFSLLCAFFWMGLYLLRAGVRLPLAVALLAACCGGEALVQIGLGVGEDHLLSLPAAGVVLSCLAAATWLVLRLRLGVLMIALTSAVRTVSLISLERFKVAWRPYLAYLAGVLGILLARYVEQILPQSAEAAPREHLGSQLIAGTKEDIPVFKRRRRSSSVVSAEMSGCSSKSHRRTSLPCIPREQLMGHSEWDHKRGPRGSQSSGTSITVDIAVMGEAHGLITDLLADPSLPPNVCTSLRAVSNLLSTQLTFQAIHKPRVNPVTSLSENYTCSDSEESSEKDKLAIPKRLRRSLPPGLLRRVSSTWTTTTSATGLPTLEPAPVRRDRSTSIKLQEAPSSSPDSWNNPVMMTLTKSRSFTSSYAISAANHVKAKKQSRPGALAKISPLSSPCSSPLQGTPASSLVSKISAVQFPESADTTAKQSLGSHRALTYTQSAPDLSPQILTPPVICSSCGRPYSQGNPADEPLERSGVATRTPSRTDDTAQVTSDYETNNNSDSSDIVQNEDETECLREPLRKASACSTYAPETMMFLDKPILAPEPLVMDNLDSIMEQLNTWNFPIFDLVENIGRKCGRILSQVSYRLFEDMGLFEAFKIPIREFMNYFHALEIGYRDIPYHNRIHATDVLHAVWYLTTQPIPGLSTVINDHGSTSDSDSDSGFTHGHMGYVFSKTYNVTDDKYGCLSGNIPALELMALYVAAAMHDYDHPGRTNAFLVATSAPQAVLYNDRSVLENHHAAAAWNLFMSRPEYNFLINLDHVEFKHFRFLVIEAILATDLKKHFDFVAKFNGKVNDDVGIDWTNENDRLLVCQMCIKLADINGPAKCKELHLQWTDGIVNEFYEQGDEEASLGLPISPFMDRSAPQLANLQESFISHIVGPLCNSYDSAGLMPGKWVEDSDESGDTDDPEEEEEEAPAPNEEETCENNESPKKKTFKRRKIYCQITQHLLQNHKMWKKVIEEEQRLAGIENQSLDQTPQSHSSEQIQAIKEEEEEKGKPRGEEIPTQKPDQ
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Phosphodiesterase
>
Phosphodiesterase 3
>
Phosphodiesterase 3A
Function
Cyclic nucleotide phosphodiesterase with specificity for the second messengers cAMP and cGMP, which are key regulators of many important physiological processes (PubMed:1315035, PubMed:8695850, PubMed:8155697, PubMed:25961942). Has also activity toward cUMP (PubMed:27975297). Independently of its catalytic activity it is part of an E2/17beta-estradiol-induced pro-apoptotic signaling pathway. E2 stabilizes the PDE3A/SLFN12 complex in the cytosol, promoting the dephosphorylation of SLFN12 and activating its pro-apoptotic ribosomal RNA/rRNA ribonuclease activity. This apoptotic pathway might be relevant in tissues with high concentration of E2 and be for instance involved in placenta remodeling (PubMed:31420216, PubMed:34707099).
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Uniprot ID
Primary ID:
Q14432

Secondarily ID:
O60865
Q13348
Q17RD1
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Ensembl ID
ENSG00000172572
HGNC ID
HGNC:8778
Subcellular Location
Membrane
Cytoplasm
Cytosol
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
CP0486314
2-amino-9-[3-[4-(2H-tetrazol-5-yl)phenoxy]propyl]-1H-purin-6-one
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C15H15N9O2
 1
1
IC50 = 1.89 nM
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CP0560476
9-[3-[4-(2H-tetrazol-5-yl)phenoxy]propyl]purin-6-amine
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C15H15N9O
 1
1
IC50 = 2.17 nM
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CP0553044
1-[4-[4-(2H-tetrazol-5-yl)phenoxy]butyl]pyrimidine-2,4-dione
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C15H16N6O3
 1
1
IC50 = 2.41 nM
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CP0060773
CHEBI:31401
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C20H27N5O2
 1
1
IC50 = 3.89 nM
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CP0565778
9-[4-[4-(2H-tetrazol-5-yl)phenoxy]butyl]purin-6-amine
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C16H17N9O
 1
1
IC50 = 3.91 nM
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CP0568706
1-[3-[4-(2H-tetrazol-5-yl)phenoxy]propyl]pyrimidine-2,4-dione
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C14H14N6O3
 1
1
IC50 = 4 nM
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CP0533421
1,3-dimethyl-7-[4-[4-(2H-tetrazol-5-yl)phenoxy]butyl]purine-2,6-dione
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C18H20N8O3
 1
1
IC50 = 4.74 nM
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CP0553043
2-[3-[4-(2H-tetrazol-5-yl)phenoxy]propyl]-1,2,4-triazine-3,5-dione
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C13H13N7O3
 1
1
IC50 = 5.08 nM
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CP0556018
2-[4-[4-(2H-tetrazol-5-yl)phenoxy]butylsulfanyl]-1H-pyrimidin-6-one
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C15H16N6O2S
 1
1
IC50 = 5.13 nM
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CP0568708
1,3-dimethyl-7-[3-[4-(2H-tetrazol-5-yl)phenoxy]propyl]purine-2,6-dione
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C17H18N8O3
 1
1
IC50 = 5.83 nM
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CP0568707
2-[3-[4-(2H-tetrazol-5-yl)phenoxy]propylsulfanyl]-1H-pyrimidin-6-one
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C14H14N6O2S
 1
1
IC50 = 6.22 nM
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CP0568710
3,7-dimethyl-1-[3-[4-(2H-tetrazol-5-yl)phenoxy]propyl]purine-2,6-dione
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C17H18N8O3
 1
1
IC50 = 6.29 nM
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CP0486316
3,7-dimethyl-1-[4-[4-(2H-tetrazol-5-yl)phenoxy]butyl]purine-2,6-dione
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C18H20N8O3
 1
1
IC50 = 6.5 nM
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CP0515576
2-[4-[4-(2H-tetrazol-5-yl)phenoxy]butyl]-1,2,4-triazine-3,5-dione
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C14H15N7O3
 1
1
IC50 = 6.78 nM
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CP0556019
2-amino-9-[4-[4-(2H-tetrazol-5-yl)phenoxy]butyl]-1H-purin-6-one
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C16H17N9O2
 1
1
IC50 = 7.15 nM
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CP0910630
(RS)-[3-(1H-Pyrrolo[2,3-b]pyridin-4-yl)-1-piperidyl]-(4,5,6,7-tetrahydrobenzothiophen-2-yl)methanone
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C21H23N3OS
 1
1
IC50 = 38 nM
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CP0535021
[3-[5-(difluoromethyl)-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl]piperidin-1-yl]-(4,5,6,7-tetrahydro-1-benzothiophen-2-yl)methanone
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C20H21F2N5OS
 1
1
IC50 = 56 nM
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CP0532944
4,5,6,7-tetrahydro-1-benzothiophen-2-yl-[(3S)-3-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperidin-1-yl]methanone
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C19H21N5OS
 1
1
IC50 = 89 nM
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CP0542603
[3-(5-propan-2-yl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperidin-1-yl]-(4,5,6,7-tetrahydro-1-benzothiophen-2-yl)methanone
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C22H27N5OS
 1
1
IC50 = 89 nM
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CP0555757
6-(1,3-dimethylpyrazol-4-yl)-3-[(1S)-1-quinolin-6-ylethyl]-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
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C19H17N7S
 1
1
IC50 = 100 nM
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CP0498445
[3-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperidin-1-yl]-(4,5,6,7-tetrahydro-1-benzothiophen-2-yl)methanone
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C20H23N5OS
 1
1
IC50 = 112 nM
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CP0484310
4,5,6,7-tetrahydro-1-benzothiophen-2-yl-[(2S)-2-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)morpholin-4-yl]methanone
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C18H19N5O2S
 1
1
IC50 = 178 nM
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CP0553125
6-(1,3-dimethylpyrazol-4-yl)-3-[(1R)-1-quinolin-6-ylethyl]-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
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C19H17N7S
 1
1
IC50 = 200 nM
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CP0099911
4-[8''-chloro-2''-oxospiro[cyclohexane-1,4''-(1'',2'',3'',4''-tetrahydroquinazoline)]-6-yl]benzamide
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C20H20ClN3O2
 1
1
IC50 = 280 nM
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CP0542605
(1-methylsulfonylindol-5-yl)-[(3S)-3-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperidin-1-yl]methanone
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C20H20N6O3S
 1
1
IC50 = 282 nM
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CP0535019
1-[5-[3-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperidine-1-carbonyl]indol-1-yl]ethanone
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C21H20N6O2
 1
1
IC50 = 331 nM
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CP0542607
2,3-dihydro-1,4-benzodioxin-6-yl-[(3S)-3-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperidin-1-yl]methanone
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C19H19N5O3
 1
1
IC50 = 398 nM
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CP0532945
[(3S)-3-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperidin-1-yl]-[4-(trifluoromethyl)phenyl]methanone
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C18H16F3N5O
 1
1
IC50 = 436 nM
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CP0015057
6-(1-methylpyrazol-4-yl)-3-[(1S)-1-quinolin-6-ylethyl]-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
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C18H15N7S
 1
1
IC50 = 500 nM
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CP0553921
(4-methoxyphenyl)-[(3S)-3-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperidin-1-yl]methanone
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C18H19N5O2
 1
1
IC50 = 537 nM
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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
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C26H30N8O5
 1
1
IC50 = 750 nM
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CP0498444
(1-methylsulfonylindol-5-yl)-[3-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperidin-1-yl]methanone
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C20H20N6O3S
 1
1
IC50 = 776 nM
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CP0542606
5-(difluoromethyl)-7-[(3S,4R)-4-methyl-1-(4-phenylpyridin-2-yl)piperidin-3-yl]-[1,2,4]triazolo[1,5-a]pyrimidine
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C23H22F2N6
 1
1
IC50 = 813 nM
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CP0484240
[(3S,4R)-3-[5-(difluoromethyl)-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl]-4-methylpiperidin-1-yl]-(3,4-dimethoxyphenyl)methanone
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C21H23F2N5O3
 1
1
IC50 = 912 nM
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CP0540141
1-benzofuran-5-yl-[(3S,4R)-3-[5-(difluoromethyl)-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl]-4-methylpiperidin-1-yl]methanone
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C21H19F2N5O2
 1
1
IC50 = 1290 nM
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CP0484309
(3-methoxyphenyl)-[(3S)-3-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperidin-1-yl]methanone
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C18H19N5O2
 1
1
IC50 = 1513 nM
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CP0484311
7-[(3S,4R)-1-(4-tert-butylpyridin-2-yl)-4-methylpiperidin-3-yl]-5-(difluoromethyl)-[1,2,4]triazolo[1,5-a]pyrimidine
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C21H26F2N6
 1
1
IC50 = 1660 nM
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CP0879689
[5-(4-Chloro-phenyl)-3-methyl-3H-[1,3,4]thiadiazol-2-ylidene]-[3-(1H-tetrazol-5-yl)-phenyl]-amine
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C16H12ClN7S
 1
1
IC50 = 1710 nM
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CP0007669
3-[[4-ethoxy-3-(3-ethyl-1-methyl-7-oxo-6H-pyrazolo[4,3-d]pyrimidin-5-yl)phenyl]methyl]-N-hydroxycyclobutane-1-carboxamide
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C22H27N5O4
 1
1
IC50 = 1800 nM
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CP0847555
3-{3-[5-(4-Chloro-phenyl)-3-methyl-3H-[1,3,4]thiadiazol-(2Z)-ylideneamino]-phenyl}-[1,2,4]oxadiazol-5-ol
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C17H12ClN5O2S
 1
1
IC50 = 1890 nM
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CP0500072
1-benzofuran-5-yl-[3-[5-(difluoromethyl)-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl]-4-methylpiperidin-1-yl]methanone
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C21H19F2N5O2
 1
1
IC50 = 2240 nM
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CP0484238
[3-[5-methyl-2-(trifluoromethyl)-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl]piperidin-1-yl]-(4,5,6,7-tetrahydro-1-benzothiophen-2-yl)methanone
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C21H22F3N5OS
 1
1
IC50 = 2291 nM
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CP0540142
(3,4-dimethoxyphenyl)-[3-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperidin-1-yl]methanone
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C19H21N5O3
 1
1
IC50 = 2399 nM
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CP0374540
3-[5-(4-Chloro-phenyl)-3-methyl-3H-[1,3,4]thiadiazol-(2Z)-ylideneamino]-benzamide
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C16H13ClN4OS
 1
1
IC50 = 2650 nM
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CP0450884
N-(1-methylpyrazol-4-yl)-3-[(1S)-1-quinolin-6-ylethyl]-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-6-amine
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C18H16N8S
 1
1
IC50 = 3000 nM
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CP0535020
4,5,6,7-tetrahydro-1-benzothiophen-2-yl-[3-[5-(trifluoromethyl)-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl]piperidin-1-yl]methanone
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C20H20F3N5OS
 1
1
IC50 = 3236 nM
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CP0532946
7-[1-(1-benzofuran-5-ylmethyl)piperidin-3-yl]-5-(difluoromethyl)-[1,2,4]triazolo[1,5-a]pyrimidine
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C20H19F2N5O
 1
1
IC50 = 3467 nM
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CP0540143
4,5,6,7-tetrahydro-1-benzothiophen-2-yl-[3-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)azepan-1-yl]methanone
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C20H23N5OS
 1
1
IC50 = 3631 nM
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CP0474856
6-methyl-N-[(1R)-1-[4-(trifluoromethoxy)phenyl]propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
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C18H17F3N4O2
 1
1
IC50 = 4200 nM
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CP0535016
phenyl-[(3S)-3-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperidin-1-yl]methanone
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C17H17N5O
 1
1
IC50 = 4266 nM
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CP0484312
4-[(3S)-3-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperidine-1-carbonyl]benzonitrile
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C18H16N6O
 1
1
IC50 = 4786 nM
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CP0484308
2-(3,4-dimethoxyphenyl)-1-[(3S)-3-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperidin-1-yl]ethanone
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C20H23N5O3
 1
1
IC50 = 4898 nM
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CP0421160
5-[5-(4-Chloro-phenyl)-3-methyl-3H-[1,3,4]thiadiazol-(2Z)-ylideneamino]-2-hydroxy-benzoic acid
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C16H12ClN3O3S
 1
1
IC50 = 5580 nM
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CP0535023
5-(difluoromethyl)-7-[1-[(3,4-dimethoxyphenyl)methyl]piperidin-3-yl]-[1,2,4]triazolo[1,5-a]pyrimidine
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C20H23F2N5O2
 1
1
IC50 = 5623 nM
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CP0420018
3-[5-(4-Chloro-phenyl)-3-methyl-3H-[1,3,4]thiadiazol-(2Z)-ylideneamino]-phenol
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C15H12ClN3OS
 1
1
IC50 = 6130 nM
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CP0484239
7-[(3S)-1-[(2-chloro-6-methylpyridin-4-yl)methyl]piperidin-3-yl]-5-(difluoromethyl)-[1,2,4]triazolo[1,5-a]pyrimidine
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C18H19ClF2N6
 1
1
IC50 = 6166 nM
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CP0498043
3-[5-(4-Chloro-phenyl)-3-methyl-3H-[1,3,4]thiadiazol-(2Z)-ylideneamino]-benzoic acid
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C16H12ClN3O2S
 1
1
IC50 = 7470 nM
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CP0414199
4-[[1-(2-chlorophenyl)-4-methyl-[1,2,4]triazolo[4,3-a]quinoxalin-8-yl]methyl]morpholine
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C21H20ClN5O
 1
1
IC50 = 7760 nM
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CP0564294
6-(1-methylpyrazol-4-yl)-3-[(1R)-1-quinolin-6-ylethyl]-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
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C18H15N7S
 1
1
IC50 = 7900 nM
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CP0176069
3-[difluoro(quinolin-6-yl)methyl]-N-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-6-amine
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C17H12F2N8S
 1
1
IC50 = 8067 nM
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CP0483612
2-[3-[[5-(4-chlorophenyl)-3-methyl-1,3,4-thiadiazol-2-ylidene]amino]phenyl]acetic acid
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C17H14ClN3O2S
 1
1
IC50 = 8570 nM
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CP0573429
2-[3-[5-(difluoromethyl)-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl]-4-methylpiperidin-1-yl]-N-methylpyridine-4-carboxamide
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C19H21F2N7O
 1
1
IC50 = 9120 nM
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   TS
CP0378339
3-[5-(4-Chloro-phenyl)-3-methyl-3H-[1,3,4]thiadiazol-(2Z)-ylideneamino]-2-hydroxy-benzoic acid
   Show/Hide
C16H12ClN3O3S
 1
1
IC50 = 9830 nM
   TI
   LI
   LO
   TS
CP0484242
1-[4-(4,5,6,7-tetrahydro-1-benzothiophene-2-carbonyl)-2-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperazin-1-yl]ethanone
   Show/Hide
C20H22N6O2S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0484314
(1-methylsulfonylindol-5-yl)-[(3R)-3-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperidin-1-yl]methanone
   Show/Hide
C20H20N6O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0484316
5-(difluoromethyl)-7-[(3S)-1-[(2,6-dimethylpyridin-4-yl)methyl]piperidin-3-yl]-[1,2,4]triazolo[1,5-a]pyrimidine
   Show/Hide
C19H22F2N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0486657
[3-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperidin-1-yl]-(3,4,5-trimethoxyphenyl)methanone
   Show/Hide
C20H23N5O4
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0529994
cyclopropyl-[(3S)-3-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperidin-1-yl]methanone
   Show/Hide
C14H17N5O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0529995
4,5,6,7-tetrahydro-1-benzothiophen-2-yl-[3-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperazin-1-yl]methanone
   Show/Hide
C18H20N6OS
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0535017
[3-(2,5-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperidin-1-yl]-(4,5,6,7-tetrahydro-1-benzothiophen-2-yl)methanone
   Show/Hide
C21H25N5OS
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0176508
[4-[3-(3-fluoro-4-methoxyphenyl)-5-(2-methylphenyl)-3,4-dihydropyrazol-2-yl]phenyl]-(4-methylpiperazin-1-yl)methanone
   Show/Hide
C29H31FN4O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0365459
[4-[5-tert-butyl-3-(3,5-difluoro-4-methoxyphenyl)-3,4-dihydropyrazol-2-yl]phenyl]-(4-methylpiperazin-1-yl)methanone
   Show/Hide
C26H32F2N4O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0419692
N-(2-hydroxyethyl)-4-[3-(4-methoxyphenyl)-5-(2-methylphenyl)-3,4-dihydropyrazol-2-yl]benzamide
   Show/Hide
C26H27N3O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0419693
[4-[5-tert-butyl-3-(2,3-difluoro-4-methoxyphenyl)-3,4-dihydropyrazol-2-yl]phenyl]-(4-methylpiperazin-1-yl)methanone
   Show/Hide
C26H32F2N4O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0444327
[4-[3-(4-methoxyphenyl)-5-(2-methylphenyl)-3,4-dihydropyrazol-2-yl]phenyl]-(4-methylpiperazin-1-yl)methanone
   Show/Hide
C29H32N4O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0487171
5-[8''-chloro-2''-oxospiro[cyclohexane-1,4''-(1'',2'',3'',4''-tetrahydroquinazoline)]-5-yloxymethyl]-2-furoic acid
   Show/Hide
C19H19ClN2O5
 1
1
IC50 = 10800 nM
   TI
   LI
   LO
   TS
CP0298895
8''-chloro-6''-(4-pyridyl)spiro[cyclohexane-1,4''-(1'',2'',3'',4''-tetrahydroquinazoline)]-2''-one
   Show/Hide
C18H18ClN3O
 1
1
IC50 = 11200 nM
   TI
   LI
   LO
   TS
CP0487261
8''-chloro-5''-(1H-1,2,3,4-tetraazol-5-ylmethoxy)spiro[cyclohexane-1,4''-(1'',2'',3'',4''-tetrahydroquinazoline)]-2''-one
   Show/Hide
C15H17ClN6O2
 1
1
IC50 = 11800 nM
   TI
   LI
   LO
   TS
CP0485017
3-[8''-chloro-2''-oxospiro[cyclohexane-1,4''-(1'',2'',3'',4''-tetrahydroquinazoline)]-5-yloxy]-1-propanesulfonic acid
   Show/Hide
C16H21ClN2O5S
 1
1
IC50 = 12700 nM
   TI
   LI
   LO
   TS
CP0104740
8''-chloro-6''-(3-pyridyl)spiro[cyclohexane-1,4''-(1'',2'',3'',4''-tetrahydroquinazoline)]-2''-one
   Show/Hide
C18H18ClN3O
 1
1
IC50 = 14800 nM
   TI
   LI
   LO
   TS
CP0279262
3-[8''-chloro-2''-oxospiro[cyclohexane-1,4''-(1'',2'',3'',4''-tetrahydroquinazoline)]-6-yl]benzoic acid
   Show/Hide
C20H19ClN2O3
 1
1
IC50 = 16700 nM
   TI
   LI
   LO
   TS
CP0464638
5-[5-(4-Chloro-phenyl)-3-methyl-3H-[1,3,4]thiadiazol-(2Z)-ylideneamino]-2-fluoro-benzoic acid
   Show/Hide
C16H11ClFN3O2S
 1
1
IC50 = 16980 nM
   TI
   LI
   LO
   TS
CP0378338
2-[5-(4-Chloro-phenyl)-3-methyl-3H-[1,3,4]thiadiazol-(2Z)-ylideneamino]-3-methyl-benzoic acid
   Show/Hide
C17H14ClN3O2S
 1
1
IC50 = 20540 nM
   TI
   LI
   LO
   TS
CP0168455
4-[8''-chloro-2''-oxospiro[cyclohexane-1,4''-(1'',2'',3'',4''-tetrahydroquinazoline)]-6-yl]benzoic acid
   Show/Hide
C20H19ClN2O3
 1
1
IC50 = 21300 nM
   TI
   LI
   LO
   TS
CP0485988
8''-chloro-5''-(5-hydroxy-1,2,4-oxadiazol-3-ylmethoxy)spiro[cyclohexane-1,4''-(1'',2'',3'',4''-tetrahydroquinazoline)]-2''-one
   Show/Hide
C16H17ClN4O4
 1
1
IC50 = 21900 nM
   TI
   LI
   LO
   TS
CP0282220
4-[8''-chloro-2''-oxospiro[cyclohexane-1,4''-(1'',2'',3'',4''-tetrahydroquinazoline)]-6-yl]phenyl-4-methylhexahydro-1-pyrazinylmethanone
   Show/Hide
C25H29ClN4O2
 1
1
IC50 = 29300 nM
   TI
   LI
   LO
   TS
CP0013428
N-[(1S)-1-[3-fluoro-4-(trifluoromethoxy)phenyl]-2-methoxyethyl]-7-methoxy-2-oxo-1,3-dihydropyrido[2,3-b]pyrazine-4-carboxamide
   Show/Hide
C19H18F4N4O5
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0378336
4-[5-(4-Chloro-phenyl)-3-methyl-3H-[1,3,4]thiadiazol-(2Z)-ylideneamino]-benzoic acid
   Show/Hide
C16H12ClN3O2S
 1
1
IC50 = 30680 nM
   TI
   LI
   LO
   TS
CP0099891
3-[8''-chloro-2''-oxospiro[cyclohexane-1,4''-(1'',2'',3'',4''-tetrahydroquinazoline)]-6-yl]phenyl-4-methylhexahydro-1-pyrazinylmethanone
   Show/Hide
C25H29ClN4O2
 1
1
IC50 = 31600 nM
   TI
   LI
   LO
   TS
CP0099912
1N-(2-dimethylaminoethyl)-4-[8''-chloro-2''-oxospiro[cyclohexane-1,4''-(1'',2'',3'',4''-tetrahydroquinazoline)]-6-yl]benzamide
   Show/Hide
C24H29ClN4O2
 1
1
IC50 = 42200 nM
   TI
   LI
   LO
   TS
CP0178683
1N-(3-dimethylaminopropyl)-4-[8''-chloro-2''-oxospiro[cyclohexane-1,4''-(1'',2'',3'',4''-tetrahydroquinazoline)]-6-yl]benzamide
   Show/Hide
C25H31ClN4O2
 1
1
IC50 = 44500 nM
   TI
   LI
   LO
   TS
CP0287257
8''-chloro-6''-(2-pyridyl)spiro[cyclohexane-1,4''-(1'',2'',3'',4''-tetrahydroquinazoline)]-2''-one
   Show/Hide
C18H18ClN3O
 1
1
IC50 = 45100 nM
   TI
   LI
   LO
   TS
CP0374539
3-[5-(4-Chloro-phenyl)-3-methyl-3H-[1,3,4]thiadiazol-(2Z)-ylideneamino]-benzonitrile
   Show/Hide
C16H11ClN4S
 1
1
IC50 = 47210 nM
   TI
   LI
   LO
   TS
CP0378337
2-[5-(4-Chloro-phenyl)-3-methyl-3H-[1,3,4]thiadiazol-(2Z)-ylideneamino]-3-hydroxy-benzoic acid
   Show/Hide
C16H12ClN3O3S
 1
1
IC50 = 49420 nM
   TI
   LI
   LO
   TS
CP0395076
2-[8''-chloro-2''-oxospiro[cyclohexane-1,4''-(1'',2'',3'',4''-tetrahydroquinazoline)]-5-yloxy]acetic acid
   Show/Hide
C15H17ClN2O4
 1
1
IC50 > 68000 nM
   TI
   LI
   LO
   TS
CP0378341
8''-chloro-5''-(2-hydroxyethoxy)spiro[cyclohexane-1,4''-(1'',2'',3'',4''-tetrahydroquinazoline)]-2''-one
   Show/Hide
C15H19ClN2O3
 1
1
IC50 > 73000 nM
   TI
   LI
   LO
   TS
CP0378342
ethyl 5-[(8-chloro-2-oxospiro[1,3-dihydroquinazoline-4,1'-cyclohexane]-5-yl)oxymethyl]furan-2-carboxylate
   Show/Hide
C21H23ClN2O5
 1
1
IC50 = 78000 nM
   TI
   LI
   LO
   TS
CP0319822
1N-(3-dimethylaminopropyl)-3-[8''-chloro-2''-oxospiro[cyclohexane-1,4''-(1'',2'',3'',4''-tetrahydroquinazoline)]-6-yl]benzamide
   Show/Hide
C25H31ClN4O2
 1
1
IC50 = 78100 nM
   TI
   LI
   LO
   TS
CP0151419
1N-(2-dimethylaminoethyl)-3-[8''-chloro-2''-oxospiro[cyclohexane-1,4''-(1'',2'',3'',4''-tetrahydroquinazoline)]-6-yl]benzamide
   Show/Hide
C24H29ClN4O2
 1
1
IC50 > 79900 nM
   TI
   LI
   LO
   TS
CP0277375
2-[8''-chloro-2''-oxospiro[cyclohexane-1,4''-(1'',2'',3'',4''-tetrahydroquinazoline)]-6-yl]phenyl-4-methylhexahydro-1-pyrazinylmethanone
   Show/Hide
C25H29ClN4O2
 1
1
IC50 > 92000 nM
   TI
   LI
   LO
   TS
CP0391246
2-[8''-chloro-2''-oxospiro[cyclohexane-1,4''-(1'',2'',3'',4''-tetrahydroquinazoline)]-5-yloxy]acetonitrile
   Show/Hide
C15H16ClN3O2
 1
1
IC50 = 94000 nM
   TI
   LI
   LO
   TS
CP0205820
(R)-6,7-Dimethoxy-4-[3-(naphthalen-1-yloxy)-pyrrolidin-1-yl]-quinazoline
   Show/Hide
C24H23N3O3
 1
1
Ki = 48 nM
   TI
   LI
   LO
   TS
CP0091866
(R)-4-[3-(3-Ethoxy-phenoxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
   Show/Hide
C22H25N3O4
 1
1
Ki = 61 nM
   TI
   LI
   LO
   TS
CP0038130
(R)-6,7-Dimethoxy-4-[3-(pyridin-2-yloxy)-pyrrolidin-1-yl]-quinazoline
   Show/Hide
C19H20N4O3
 1
1
Ki = 77 nM
   TI
   LI
   LO
   TS
CP0091864
(R)-2-[1-(6,7-Dimethoxy-quinazolin-4-yl)-pyrrolidin-3-yloxy]-benzonitrile
   Show/Hide
C21H20N4O3
 1
1
Ki < 100 nM
   TI
   LI
   LO
   TS
CP0091868
(R)-6,7-Dimethoxy-4-[3-(2-methoxy-phenoxy)-pyrrolidin-1-yl]-quinazoline
   Show/Hide
C21H23N3O4
 1
1
Ki < 100 nM
   TI
   LI
   LO
   TS
CP0103705
(R)-6,7-Dimethoxy-4-(3-o-tolyloxy-pyrrolidin-1-yl)-quinazoline
   Show/Hide
C21H23N3O3
 1
1
Ki < 100 nM
   TI
   LI
   LO
   TS
CP0103710
(R)-6,7-Dimethoxy-4-[3-(2-trifluoromethyl-phenoxy)-pyrrolidin-1-yl]-quinazoline
   Show/Hide
C21H20F3N3O3
 1
1
Ki < 100 nM
   TI
   LI
   LO
   TS
CP0160131
(R)-4-[3-(2-Chloro-phenoxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
   Show/Hide
C20H20ClN3O3
 1
1
Ki < 100 nM
   TI
   LI
   LO
   TS
CP0109409
(R)-6,7-Dimethoxy-4-[3-(quinolin-6-yloxy)-pyrrolidin-1-yl]-quinazoline
   Show/Hide
C23H22N4O3
 1
1
Ki = 104 nM
   TI
   LI
   LO
   TS
CP0103707
(R)-4-[3-(3,4-Dimethoxy-phenoxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
   Show/Hide
C22H25N3O5
 1
1
Ki = 121 nM
   TI
   LI
   LO
   TS
CP0109410
(R)-4-[3-(Indan-5-yloxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
   Show/Hide
C23H25N3O3
 1
1
Ki = 141 nM
   TI
   LI
   LO
   TS
CP0038129
(R)-4-[3-(Isoquinolin-3-yloxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
   Show/Hide
C23H22N4O3
 1
1
Ki = 151 nM
   TI
   LI
   LO
   TS
CP0103703
(R)-6,7-Dimethoxy-4-[3-(2-methyl-quinolin-6-yloxy)-pyrrolidin-1-yl]-quinazoline
   Show/Hide
C24H24N4O3
 1
1
Ki = 152 nM
   TI
   LI
   LO
   TS
CP0160129
(R)-4-[3-(4-Ethoxy-phenoxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
   Show/Hide
C22H25N3O4
 1
1
Ki = 161 nM
   TI
   LI
   LO
   TS
CP0156978
(R)-4-[3-(5-Chloro-pyrimidin-2-yloxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
   Show/Hide
C18H18ClN5O3
 1
1
Ki = 162 nM
   TI
   LI
   LO
   TS
CP0091873
(R)-6,7-Dimethoxy-4-[3-(6-methoxy-naphthalen-2-yloxy)-pyrrolidin-1-yl]-quinazoline
   Show/Hide
C25H25N3O4
 1
1
Ki = 199 nM
   TI
   LI
   LO
   TS
CP0117972
(R)-6,7-Dimethoxy-4-[3-(quinolin-7-yloxy)-pyrrolidin-1-yl]-quinazoline
   Show/Hide
C23H22N4O3
 1
1
Ki = 209 nM
   TI
   LI
   LO
   TS
CP0117968
(R)-6,7-Dimethoxy-4-[3-(quinoxalin-2-yloxy)-pyrrolidin-1-yl]-quinazoline
   Show/Hide
C22H21N5O3
 1
1
Ki = 211 nM
   TI
   LI
   LO
   TS
CP0103708
(R)-4-[1-(6,7-Dimethoxy-quinazolin-4-yl)-pyrrolidin-3-yloxy]-benzonitrile
   Show/Hide
C21H20N4O3
 1
1
Ki = 214 nM
   TI
   LI
   LO
   TS
CP0156977
(R)-6,7-Dimethoxy-4-[3-(pyridin-4-yloxy)-pyrrolidin-1-yl]-quinazoline
   Show/Hide
C19H20N4O3
 1
1
Ki = 226 nM
   TI
   LI
   LO
   TS
CP0202707
(R)-4-[3-(Biphenyl-3-yloxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
   Show/Hide
C26H25N3O3
 1
1
Ki = 271 nM
   TI
   LI
   LO
   TS
CP0038124
(R)-6,7-Dimethoxy-4-[3-(7-methoxy-naphthalen-2-yloxy)-pyrrolidin-1-yl]-quinazoline
   Show/Hide
C25H25N3O4
 1
1
Ki = 273 nM
   TI
   LI
   LO
   TS
CP0083432
1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoquinoline
   Show/Hide
C20H21NO4
 1
1
Ki = 279 nM
   TI
   LI
   LO
   TS
CP0117969
(R)-6,7-Dimethoxy-4-[3-(naphthalen-2-yloxy)-pyrrolidin-1-yl]-quinazoline
   Show/Hide
C24H23N3O3
 1
1
Ki = 283 nM
   TI
   LI
   LO
   TS
CP0038128
(R)-6,7-Dimethoxy-4-[3-(pyridin-3-yloxy)-pyrrolidin-1-yl]-quinazoline
   Show/Hide
C19H20N4O3
 1
1
Ki = 302 nM
   TI
   LI
   LO
   TS
CP0419676
(R)-4-[3-(3-Isopropyl-phenoxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
   Show/Hide
C23H27N3O3
 1
1
Ki = 370 nM
   TI
   LI
   LO
   TS
CP0091870
(R)-4-[3-(4-tert-Butyl-phenoxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
   Show/Hide
C24H29N3O3
 1
1
Ki = 720 nM
   TI
   LI
   LO
   TS
CP0428130
(R)-6,7-Dimethoxy-4-[3-(4-trifluoromethoxy-phenoxy)-pyrrolidin-1-yl]-quinazoline
   Show/Hide
C21H20F3N3O4
 1
1
Ki = 739 nM
   TI
   LI
   LO
   TS
CP0502730
(S)-6,7-Dimethoxy-4-[3-(2-methoxy-phenoxy)-pyrrolidin-1-yl]-quinazoline
   Show/Hide
C21H23N3O4
 1
1
Ki > 100 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0561858
2-amino-4-(3-benzyl-2-ethylsulfanylimidazol-4-yl)-6-(4-bromophenyl)pyridine-3-carbonitrile
   Show/Hide
C24H20BrN5S
 1
1 IC50 = 3.76 nM
CP0083432
1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoquinoline
   Show/Hide
C20H21NO4
 4
1 IC50 = 284 nM
2 IC50 = 287 nM
3 IC50 = 917 nM
4 IC50 = 1300 nM
CP0205820
(R)-6,7-Dimethoxy-4-[3-(naphthalen-1-yloxy)-pyrrolidin-1-yl]-quinazoline
   Show/Hide
C24H23N3O3
 1
1 Ki = 48 nM
CP0091866
(R)-4-[3-(3-Ethoxy-phenoxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
   Show/Hide
C22H25N3O4
 1
1 Ki = 61 nM
CP0038130
(R)-6,7-Dimethoxy-4-[3-(pyridin-2-yloxy)-pyrrolidin-1-yl]-quinazoline
   Show/Hide
C19H20N4O3
 1
1 Ki = 77 nM
CP0091864
(R)-2-[1-(6,7-Dimethoxy-quinazolin-4-yl)-pyrrolidin-3-yloxy]-benzonitrile
   Show/Hide
C21H20N4O3
 1
1 Ki < 100 nM
CP0091868
(R)-6,7-Dimethoxy-4-[3-(2-methoxy-phenoxy)-pyrrolidin-1-yl]-quinazoline
   Show/Hide
C21H23N3O4
 1
1 Ki < 100 nM
CP0103705
(R)-6,7-Dimethoxy-4-(3-o-tolyloxy-pyrrolidin-1-yl)-quinazoline
   Show/Hide
C21H23N3O3
 1
1 Ki < 100 nM
CP0103710
(R)-6,7-Dimethoxy-4-[3-(2-trifluoromethyl-phenoxy)-pyrrolidin-1-yl]-quinazoline
   Show/Hide
C21H20F3N3O3
 1
1 Ki < 100 nM
CP0160131
(R)-4-[3-(2-Chloro-phenoxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
   Show/Hide
C20H20ClN3O3
 1
1 Ki < 100 nM
CP0109409
(R)-6,7-Dimethoxy-4-[3-(quinolin-6-yloxy)-pyrrolidin-1-yl]-quinazoline
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C23H22N4O3
 1
1 Ki = 104 nM
CP0103707
(R)-4-[3-(3,4-Dimethoxy-phenoxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
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C22H25N3O5
 1
1 Ki = 121 nM
CP0109410
(R)-4-[3-(Indan-5-yloxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
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C23H25N3O3
 1
1 Ki = 141 nM
CP0038129
(R)-4-[3-(Isoquinolin-3-yloxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
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C23H22N4O3
 1
1 Ki = 151 nM
CP0103703
(R)-6,7-Dimethoxy-4-[3-(2-methyl-quinolin-6-yloxy)-pyrrolidin-1-yl]-quinazoline
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C24H24N4O3
 1
1 Ki = 152 nM
CP0160129
(R)-4-[3-(4-Ethoxy-phenoxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
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C22H25N3O4
 1
1 Ki = 161 nM
CP0156978
(R)-4-[3-(5-Chloro-pyrimidin-2-yloxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
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C18H18ClN5O3
 1
1 Ki = 162 nM
CP0091873
(R)-6,7-Dimethoxy-4-[3-(6-methoxy-naphthalen-2-yloxy)-pyrrolidin-1-yl]-quinazoline
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C25H25N3O4
 1
1 Ki = 199 nM
CP0117972
(R)-6,7-Dimethoxy-4-[3-(quinolin-7-yloxy)-pyrrolidin-1-yl]-quinazoline
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C23H22N4O3
 1
1 Ki = 209 nM
CP0117968
(R)-6,7-Dimethoxy-4-[3-(quinoxalin-2-yloxy)-pyrrolidin-1-yl]-quinazoline
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C22H21N5O3
 1
1 Ki = 211 nM
CP0103708
(R)-4-[1-(6,7-Dimethoxy-quinazolin-4-yl)-pyrrolidin-3-yloxy]-benzonitrile
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C21H20N4O3
 1
1 Ki = 214 nM
CP0156977
(R)-6,7-Dimethoxy-4-[3-(pyridin-4-yloxy)-pyrrolidin-1-yl]-quinazoline
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C19H20N4O3
 1
1 Ki = 226 nM
CP0202707
(R)-4-[3-(Biphenyl-3-yloxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
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C26H25N3O3
 1
1 Ki = 271 nM
CP0038124
(R)-6,7-Dimethoxy-4-[3-(7-methoxy-naphthalen-2-yloxy)-pyrrolidin-1-yl]-quinazoline
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C25H25N3O4
 1
1 Ki = 273 nM
CP0117969
(R)-6,7-Dimethoxy-4-[3-(naphthalen-2-yloxy)-pyrrolidin-1-yl]-quinazoline
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C24H23N3O3
 1
1 Ki = 283 nM
CP0038128
(R)-6,7-Dimethoxy-4-[3-(pyridin-3-yloxy)-pyrrolidin-1-yl]-quinazoline
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C19H20N4O3
 1
1 Ki = 302 nM
CP0091870
(R)-4-[3-(4-tert-Butyl-phenoxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline
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C24H29N3O3
 1
1 Ki = 720 nM
Clinical Information about the Protein
Target 1 ( Phosphodiesterase 3A (PDE3A) )
Target Type Successful Target
Disease 7 Target-related Diseases  7
1 Bronchial asthma [ICD-11: CA23]
2 Thrombocythemia [ICD-11: 3B63]
3 Intermittent claudication [ICD-11: BD40.00]
4 Congestive heart failure [ICD-11: BD10]
5 Cardiac failure [ICD-11: BD10-BD13]
6 Heart failure [ICD-11: BD10-BD13]
7 Cardiovascular disease [ICD-11: BA00-BE2Z]
Approved Drug(s) 5 Approved Drugs  5
1 Aminophylline Approved
Bronchial asthma
2 Anagrelide Approved
Thrombocythemia
3 Cilostazol Approved
Intermittent claudication
4 Enoximone Approved
Congestive heart failure
5 VESNARINONE Approved
Cardiac failure
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 BEMORADAN Phase 2
Heart failure
Discontinued Drug(s) 1 Discontinued Drug  1
1 EMD-53998 Discontinued in Phase 1
Cardiovascular disease