Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T05904 | Target Info | |||
| Target Name | Phosphodiesterase 8 (PDE8) | ||||
| Synonyms |
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
Click to Show/Hide
|
||||
| Target Type | Patented-recorded Target | ||||
| Gene Name | PDE8A | ||||
| Biochemical Class | Phosphoric diester hydrolase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 21 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Rhucin
Click to Show/Hide
|
Approved | Compound Info | ||
| Synonyms |
sildenafil; 139755-83-2; VIAGRA; Sildenafil [INN:BAN]; UK-92480; UNII-3M7OB98Y7H; UK-92,480-10; C22H30N6O4S; HSDB 7305; CHEMBL192; UK 92480-10; CHEBI:9139; 3M7OB98Y7H; 1-((3-(4,7-Dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo(4,3-d)pyrimidin-5-yl)-4-ethoxyphenyl)sulfonyl)-4-methylpiperazine; BNRNXUUZRGQAQC-UHFFFAOYSA-N; 5-(2-Ethoxy-5-((4-methylpiperazin-1-yl)sulfonyl)phenyl)-1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one; Sildenafil
Click to Show/Hide
|
||||
| Activity |
IC50 = 100000 nM
|
[1] | |||
| Compound Name |
AC1MOZOL
Click to Show/Hide
|
Patented | Compound Info | ||
| Synonyms |
686770-82-1; AC1MOZOL; CHEMBL3919432; SCHEMBL16200742; BDBM86644; AKOS024584761; MCULE-1812319467; BC11-38-2; EU-0022203; SR-01000120183; SR-01000120183-1; F0579-0063; 2-(sec-butylthio)-3-phenyl-6,7-dihydrothieno[3,2-d]pyrimidin-4(3H)-one; 2-butan-2-ylsulfanyl-3-phenyl-6,7-dihydrothieno[3,2-d]pyrimidin-4-one
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(6Ar,9aS)-5,6a,7,8,9,9a-hexahydro-5-methyl-3-(phenylamino)-2-(4-trifluoromethyl-benzyl)-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3769461; SCHEMBL4919408; BDBM50150239
Click to Show/Hide
|
||||
| Activity |
Ki = 54000 nM
|
[3] | |||
| Compound Name |
N-(4-Methoxybenzyl)-3-(cyclopentyloxy)-4-(difluoromethoxy)benzamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3628685; BDBM50129817
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
(2S)-2-[[1-(2-Chlorophenyl)-4-oxo-5H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]-N-(4-methoxyphenyl)propanamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3360413; BDBM50034649
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
N-(2-Chlorophenyl)-3-cyclopentyloxy-4-(difluoromethoxy)benzamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3883753; BDBM50208310
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
Chembl4206423
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50455384
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
N~2~-(1-Cyclopentyl-4-Oxo-4,7-Dihydro-1h-Pyrazolo[3,4-D]pyrimidin-6-Yl)-N-(4-Methoxyphenyl)-D-Alaninamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3360415; BDBM50034641; Q27453556
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
Chembl4215772
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50455383
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
3-(Cyclopropylmethoxy)-4-(difluoromethoxy)-N-pyridin-3-ylbenzamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3884224; BDBM50208315
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
N,N-Diethyl-3-methyl-1-(2-methylphenyl)-6-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridine-4-carboxamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3972355; SCHEMBL14999000; BDBM86639; HMS1786A16; ZINC3293408; AKOS034464439; BC11-15; MCULE-3880495348; Z56898051
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(11R,15S)-5-Anilino-8-methyl-4-[[6-(trifluoromethyl)pyridin-3-yl]methyl]-1,3,4,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2,5,9-trien-7-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3770107; SCHEMBL8238925; BDBM50150238
Click to Show/Hide
|
||||
| Activity |
Ki ~ 100000 nM
|
[3] | |||
| Compound Name |
(2R)-2-[[1-(2-Chlorophenyl)-4-oxo-5H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]-N-(4-methoxyphenyl)propanamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3360412; BDBM50034647
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
(2S)-2-[(1-Cyclopentyl-4-oxo-5H-pyrazolo[3,4-d]pyrimidin-6-yl)amino]-N-(4-methoxyphenyl)propanamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3360416; BDBM50034642
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[5] | |||
| Compound Name |
2-(Butylthio)-3-phenyl-6,7-dihydrothieno[3,2-d]pyrimidin-4(3H)-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3955950; SCHEMBL16200699; BDBM86643; ZINC2719706; AKOS024584760; MCULE-1273250191; BC11-38-1; EU-0022193; SR-01000120181; SR-01000120181-1; F0579-0062
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
2-(Propylthio)-3-(p-tolyl)-6,7-dihydrothieno[3,2-d]pyrimidin-4(3H)-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3950652; SCHEMBL16200731; BDBM86645; ZINC2459466; AKOS024584842; MCULE-6274932978; BC11-38-3; EU-0088907; SR-01000120189; SR-01000120189-1; F0579-0160
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
3-Phenyl-[1,3,5]triazino[2,1-b][1,3]benzothiazole-2,4-dione
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM86640; Maybridge4_000373; Oprea1_392751; CHEMBL3974407; SCHEMBL14998934; BDBM60808; HMS1522A21; ZINC134330; CCG-51916; BC11-19; MCULE-1137806289; IDI1_030955; NCGC00177650-01; US9173884, BC11-19; SR-01000641186-1; BRD-K04557143-001-01-6
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
2-[[1-(2-Chlorophenyl)-4-oxo-5H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]-N-(4-methoxyphenyl)propanamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2178115; SCHEMBL16981747; BDBM50398649
Click to Show/Hide
|
||||
| Activity |
IC50 = 100000 nM
|
[8] | |||
| Compound Name |
3-Cyclopentyloxy-4-(difluoromethoxy)-N-pyridin-3-ylbenzamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3885161; BDBM50208311
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
N-(2-Chlorophenyl)-3(cyclopropylmethoxy)-4-(difluoromethoxy)benzamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3884788; BDBM50208314
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
Click to Show/Hide
|
Compound Info | |||
| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of novel pyrazolopyrimidinone analogs as potent inhibitors of phosphodiesterase type-5. Bioorg Med Chem. 2015 May 1;23(9):2121-8. | ||||
| REF 2 | US patent application no. 9173884B2, Inhibitors of phosphodiesterase 11 (PDE11) | ||||
| REF 3 | Discovery of Potent and Selective Inhibitors of Phosphodiesterase 1 for the Treatment of Cognitive Impairment Associated with Neurodegenerative and Neuropsychiatric Diseases. J Med Chem. 2016 Feb 11;59(3):1149-64. | ||||
| REF 4 | Catecholic amides as potential selective phosphodiesterase 4D inhibitors: Design, synthesis, pharmacological evaluation and structure-activity relationships. Bioorg Med Chem. 2015 Nov 15;23(22):7332-9. | ||||
| REF 5 | Discovery of a phosphodiesterase 9A inhibitor as a potential hypoglycemic agent. J Med Chem. 2014 Dec 26;57(24):10304-13. | ||||
| REF 6 | Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings. Eur J Med Chem. 2016 Nov 29;124:372-379. | ||||
| REF 7 | Structure-based design and structure-activity relationships of 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors. Bioorg Med Chem Lett. 2018 Apr 15;28(7):1188-1193. | ||||
| REF 8 | Structure-based discovery of highly selective phosphodiesterase-9A inhibitors and implications for inhibitor design. J Med Chem. 2012 Oct 11;55(19):8549-58. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.