Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T81637 | Target Info | |||
| Target Name | Phosphodiesterase 1A (PDE1A) | ||||
| Synonyms |
hCam-1; Cam-PDE 1A; Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A; 61 kDa Cam-PDE
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| Target Type | Literature-reported Target | ||||
| Gene Name | PDE1A | ||||
| Biochemical Class | Phosphoric diester hydrolase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 11 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
ROLIPRAM
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Phase 2 | Compound Info | ||
| Synonyms |
61413-54-5; ZK 62711; Rolipramum; Rolipramum [Latin]; 4-[3-(Cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidinone; Adeo; Rolipram [USAN:INN]; 4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrrolidin-2-one; 4-(3-(cyclopentyloxy)-4-methoxyphenyl)pyrrolidin-2-one; 4-(3-(Cyclopentyloxy)-4-methoxyphenyl)-2-pyrrolidinone; (R,S)-rolipram; ZK-62711; CHEMBL63; EINECS 262-771-1; BRN 1588548; MLS000069691; CHEBI:104872; HJORMJIFDVBMOB-UHFFFAOYSA-N; 4-(3-Cyclopentyloxy-4-methoxyphenyl)-2-pyrrolidone; [3H]rolipram
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| Activity |
IC50 ~ 50000 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
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[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
|
[1] | |||
| 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 ~ 58000 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
|
[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
|
[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
|
[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
|
[5] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Identification of a potent new chemotype for the selective inhibition of PDE4. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1297-303. | ||||
| REF 2 | US patent application no. 9388139B2, Derivatives of celeboxib, use thereof and preparation thereof | ||||
| REF 3 | The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5502-5. | ||||
| 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. | ||||
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