Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T21357 | Target Info | |||
| Target Name | Phosphodiesterase 3B (PDE3B) | ||||
| Synonyms |
cGMPinhibited 3',5'cyclic phosphodiesterase B; cGMP-inhibited 3',5'-cyclic phosphodiesterase B; Cyclic GMPinhibited phosphodiesterase B; Cyclic GMP-inhibited phosphodiesterase B; CGIPDE1; CGIPDE B; CGIP1; CGI-PDE B
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| Target Type | Patented-recorded Target | ||||
| Gene Name | PDE3B | ||||
| Biochemical Class | Phosphoric diester hydrolase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 16 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Tadalafil
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Approved | Compound Info | ||
| Synonyms |
ADCIRCA; Acdirca; Cialis; Tadanafil; Lilly brand of tadalafil; Tadalafil [USAN]; GF 196960; IC 351; ICOS 351; Ic351; Cialis (TN); GF-196960; IC-351; KS-1117; Tadalafil (JAN/USAN/INN); Cialis, GF 196960, IC 351, ICOS 351, Tadalafil; (6R,12aR)-2,3,6,7,12,12a-Hexahydro-2-methyl-6-(3,4-(methylenedioxy)phenyl) pyrazino(1',2':1,6)pyrido(3,4-b)indole-1,4-dione; (6R,12aR)-2,3,6,7,12,12a-Hexahydro-2-methyl-6-(3,4-methylenedioxyphenyl)pyrazino(1',2':1,6)pyrido(3,4-b)indole-1,4-dione; (6R-trans)-6-(1,3-Benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methyl-pyrazino(1',2':1,6)pyrido(3,4-b)indole-1,4-dione
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| Activity |
IC50 ~ 50000 nM
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[1] | |||
| Compound Name |
(2R,8R)-2-(2,4-Dichlorophenyl)-6-ethyl-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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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1650866; BDBM50335827
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| Activity |
IC50 ~ 50000 nM
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[1] | |||
| Compound Name |
(10R,15S)-10-(2,4-Dichlorophenyl)-13-ethyl-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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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1650676
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
4-[2-(2-Fluoroethoxy)ethoxy]-2-[[4-(2-methyl-4-pyridin-4-ylpyrazol-3-yl)phenoxy]methyl]quinoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3628996; BDBM50128237
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| Activity |
IC50 = 50100 nM
|
[2] | |||
| Compound Name |
4-[2-[2-(2-Fluoroethoxy)ethoxy]ethoxy]-2-[[4-(2-methyl-4-pyridin-4-ylpyrazol-3-yl)phenoxy]methyl]quinoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3628997; BDBM50128238
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| Activity |
IC50 = 51800 nM
|
[2] | |||
| Compound Name |
4-[2-[2-(2-Fluoroethoxy)ethoxy]ethoxy]-2-[[4-(1-methyl-4-pyridin-4-ylpyrazol-3-yl)phenoxy]methyl]quinoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3628719; BDBM50128270
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| Activity |
IC50 = 61900 nM
|
[2] | |||
| Compound Name |
3-Methoxy-2-[[4-[4-(4-pyridyl)-1-methyl-1H-pyrazole-3-yl]phenoxy]methyl]quinoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3218036; BDBM50496800
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| Activity |
IC50 = 82700 nM
|
[3] | |||
| Compound Name |
N-(4-Methoxybenzyl)-3-(cyclopentyloxy)-4-(difluoromethoxy)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3628685; BDBM50129817
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| Activity |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
N-(2-Chlorophenyl)-3-cyclopentyloxy-4-(difluoromethoxy)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3883753; BDBM50208310
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| Activity |
IC50 ~ 100000 nM
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[5] | |||
| Compound Name |
Chembl4206423
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Investigative | Compound Info | ||
| Synonyms |
BDBM50455384
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| Activity |
IC50 ~ 100000 nM
|
[6] | |||
| Compound Name |
Chembl4215772
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Investigative | Compound Info | ||
| Synonyms |
BDBM50455383
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| Activity |
IC50 ~ 100000 nM
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[6] | |||
| Compound Name |
3-(Cyclopropylmethoxy)-4-(difluoromethoxy)-N-pyridin-3-ylbenzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3884224; BDBM50208315
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| Activity |
IC50 ~ 100000 nM
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[5] | |||
| Compound Name |
3-Cyclopentyloxy-4-(difluoromethoxy)-N-pyridin-3-ylbenzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3885161; BDBM50208311
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| Activity |
IC50 ~ 100000 nM
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[5] | |||
| Compound Name |
N-(2-Chlorophenyl)-3(cyclopropylmethoxy)-4-(difluoromethoxy)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3884788; BDBM50208314
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| Activity |
IC50 ~ 100000 nM
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[5] | |||
| Compound Name |
4-Fluoro-2-[[4-(1-methyl-4-pyridin-4-ylpyrazol-3-yl)phenoxy]methyl]quinoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3628713; BDBM50128291
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| Activity |
IC50 = 103000 nM
|
[2] | |||
| Compound Name |
6-Fluoro-2-[[4-(2-methyl-4-pyridin-4-ylpyrazol-3-yl)phenoxy]methyl]quinoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3629001; BDBM50128266
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| Activity |
IC50 = 151000 nM
|
[2] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 2 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
(1-Methylbenzimidazol-2-yl)-[4-(3-pyridin-3-ylpyridin-2-yl)oxyphenyl]methanone
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3393204; BDBM50103183
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| Activity |
IC50 = 234000 nM
|
[7] | |||
| Compound Name |
4-(2-Fluoroethoxymethyl)-2-[[4-(2-methyl-4-pyridin-4-ylpyrazol-3-yl)phenoxy]methyl]quinoline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3628995; BDBM50128236
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| Activity |
IC50 > 1000000 nM
|
[2] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Synthesis and molecular modeling of novel tetrahydro--carboline derivatives with phosphodiesterase 5 inhibitory and anticancer properties. J Med Chem. 2011 Jan 27;54(2):495-509. | ||||
| REF 2 | Synthesis of Fluorine-Containing Phosphodiesterase 10A (PDE10A) Inhibitors and the In Vivo Evaluation of F-18 Labeled PDE10A PET Tracers in Rodent and Nonhuman Primate. J Med Chem. 2015 Nov 12;58(21):8584-600. | ||||
| REF 3 | Synthesis and in vitro biological evaluation of pyrazole group-containing analogues for PDE10A. Medchemcomm. 2013 Feb 1;4(2):443-449. | ||||
| 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 | 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 6 | 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 7 | Synthesis and in vitro characterization of cinnoline and benzimidazole analogues as phosphodiesterase 10A inhibitors. Bioorg Med Chem Lett. 2015 Feb 15;25(4):919-24. | ||||
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