Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T99802 | Target Info | |||
| Target Name | Phosphodiesterase 11A (PDE11A) | ||||
| Synonyms |
cAMP and cGMP phosphodiesterase 11A; Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A
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| Target Type | Literature-reported Target | ||||
| Gene Name | PDE11A | ||||
| Biochemical Class | Phosphoric diester hydrolase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 10 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 = 60000 nM
|
[1] | |||
| Compound Name |
US9388139, 12
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Patented | Compound Info | ||
| Synonyms |
SCHEMBL12493454; CHEMBL3899621; BDBM236643; US9388139, 12
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
6-(3,4-Dimethoxyphenyl)-3-(2-methoxyphenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine
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Investigative | Compound Info | ||
| Synonyms |
triazolothiadiazine, 21; MLS000040393; BMCL181297 Compound 5A; CHEMBL251785; cid_662965; SCHEMBL1773326; REGID_for_CID_662965; BDBM30027; HMS2427C11; ZINC4312962; STK877959; AKOS002046530; CCG-193287; MCULE-2949109211; NCGC00071837-02; NCGC00071837-03; NCGC00071837-05; SMR000043645; ST081704; SR-01000612138; SR-01000612138-3; BRD-K77507773-001-10-1
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| 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
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3770107; SCHEMBL8238925; BDBM50150238
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| Activity |
Ki = 72000 nM
|
[4] | |||
| Compound Name |
4-(4-((8-(3-(Difluoromethoxy)phenyl)quinolin-6-yl)methoxy)phenyl)-2-methylbutan-2-ol
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1221434; BDBM50325786; NCGC00249759; NCGC00249759-01; NCGC00249759-02
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| Activity |
IC50 ~ 95000 nM
|
[5] | |||
| 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
|
[6] | |||
| 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
|
[7] | |||
| Compound Name |
Chembl4206423
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Investigative | Compound Info | ||
| Synonyms |
BDBM50455384
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| Activity |
IC50 ~ 100000 nM
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[8] | |||
| Compound Name |
Chembl4215772
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Investigative | Compound Info | ||
| Synonyms |
BDBM50455383
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| Activity |
IC50 ~ 100000 nM
|
[8] | |||
| 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
|
[7] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 3 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
N-Cyclohexyl-7-(4-fluorophenyl)-N-methyl-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine
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Investigative | Compound Info | ||
| Synonyms |
Oprea1_300744; CHEMBL1555933; SCHEMBL14998922; BDBM189313; HMS1911A17; ZINC2714026; STK889914; AKOS002103474; MCULE-3926295648; NCGC00139159-01; ST50069854; SR-01000568543; US9173884, BC11-28-3; SR-01000568543-1; K405-1140; cyclohexyl[7-(4-fluorophenyl)-5-phenylpyrrolo[3,2-e]pyrimidin-4-yl]methylamine
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| Activity |
IC50 > 2000000 nM
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[9] | |||
| Compound Name |
N'-[7-(3-Chlorophenyl)-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-N,N-dimethylbenzene-1,4-diamine
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Investigative | Compound Info | ||
| Synonyms |
Oprea1_571522; CHEMBL1395950; SCHEMBL14998923; BDBM189312; HMS1911A05; ZINC2974760; AKOS002104215; MCULE-3784901894; NCGC00138967-01; SR-01000567848; US9173884, BC11-28-2; SR-01000567848-1; K405-0296
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| Activity |
IC50 > 2000000 nM
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[9] | |||
| Compound Name |
3-(3-Chlorophenyl)-8-methyl-2H-[1,3,5]triazino[2,1-b][1,3]benzothiazole-2,4(3H)-dione
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Investigative | Compound Info | ||
| Synonyms |
SMR000148070; MLS000556953; CHEMBL1318630; SCHEMBL14998930; BDBM189308; HMS1802I16; HMS2408N13; ZINC208896; STK320577; AKOS001683276; MCULE-6434945522; NCGC00100793-01; EU-0082087; US9173884, BC11-19-3; 3-(3-Chloro-phenyl)-7-methyl-9-thia-1,3,4a-triaza-fluorene-2,4-dione
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| Activity |
IC50 > 2000000 nM
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[9] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases. J Med Chem. 2005 May 19;48(10):3449-62. | ||||
| REF 2 | US patent application no. 9388139B2, Derivatives of celeboxib, use thereof and preparation thereof | ||||
| REF 3 | Identification of a potent new chemotype for the selective inhibition of PDE4. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1297-303. | ||||
| REF 4 | 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 5 | The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5502-5. | ||||
| REF 6 | 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 7 | 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 8 | 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 9 | US patent application no. 9173884B2, Inhibitors of phosphodiesterase 11 (PDE11) | ||||
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