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DB01791 - Piclamilast


Identification
Name Piclamilast
Accession Number DB01791 (EXPT02600)
Type small molecule
Description Piclamilast (RP-73,401), is a selective PDE4 inhibitor. It is comparable to other PDE4 inhibitors for its anti-inflammatory effects. It has been investigated for its applications to the treatment of conditions such as chronic obstructive pulmonary disease, bronchopulmonary dysplasia and asthma. It is a second generation compound that exhibits structural functionalities of the PDE4 inhibitors cilomilast and roflumilast. The structure for piclamilast was first elucidated in a 1995 European patent application.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 381.253
Groups experimental
Monoisotopic Weight 380.069447866
Pharmacology
Indication Not Available
Mechanism of action Not Available
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions Not Available
Food Interactions Not Available

Targets


cAMP-specific 3',5'-cyclic phosphodiesterase 4A
Name cAMP-specific 3',5'-cyclic phosphodiesterase 4A
Gene Name PDE4A
Pharmacological action unknown
Actions Not Available
References
  • Beeh KM, Beier J, Lerch C, Schulz AK, Buhl R: Effects of piclamilast, a selective phosphodiesterase-4 inhibitor, on oxidative burst of sputum cells from mild asthmatics and stable COPD patients. Lung. 2004;182(6):369-77. - Pubmed
DTHybrid score Not Available
cAMP-specific 3',5'-cyclic phosphodiesterase 4B
Name cAMP-specific 3',5'-cyclic phosphodiesterase 4B
Gene Name PDE4B
Pharmacological action unknown
Actions Not Available
References
  • Beeh KM, Beier J, Lerch C, Schulz AK, Buhl R: Effects of piclamilast, a selective phosphodiesterase-4 inhibitor, on oxidative burst of sputum cells from mild asthmatics and stable COPD patients. Lung. 2004;182(6):369-77. - Pubmed
  • Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. - Pubmed
DTHybrid score Not Available
cAMP-specific 3',5'-cyclic phosphodiesterase 4C
Name cAMP-specific 3',5'-cyclic phosphodiesterase 4C
Gene Name PDE4C
Pharmacological action unknown
Actions Not Available
References
  • Beeh KM, Beier J, Lerch C, Schulz AK, Buhl R: Effects of piclamilast, a selective phosphodiesterase-4 inhibitor, on oxidative burst of sputum cells from mild asthmatics and stable COPD patients. Lung. 2004;182(6):369-77. - Pubmed
DTHybrid score Not Available
cAMP-specific 3',5'-cyclic phosphodiesterase 4D
Name cAMP-specific 3',5'-cyclic phosphodiesterase 4D
Gene Name PDE4D
Pharmacological action unknown
Actions Not Available
References
  • Beeh KM, Beier J, Lerch C, Schulz AK, Buhl R: Effects of piclamilast, a selective phosphodiesterase-4 inhibitor, on oxidative burst of sputum cells from mild asthmatics and stable COPD patients. Lung. 2004;182(6):369-77. - Pubmed
  • Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. - Pubmed
DTHybrid score Not Available

Predictions


Id Partner name Gene Name Score
485 cGMP-inhibited 3',5'-cyclic phosphodiesterase A PDE3A 0.1292
779 High-affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7A PDE7A 0.1228
691 cAMP-specific 3',5'-cyclic phosphodiesterase 7B PDE7B 0.1163
1178 Adenosine A2a receptor ADORA2A 0.1057
16 Adenosine A1 receptor ADORA1 0.1039
268 Adenosine A2b receptor ADORA2B 0.0725
6216 High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A PDE8A 0.0701
695 cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A PDE10A 0.0645
6217 High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B PDE8B 0.0588
204 cGMP-specific 3',5'-cyclic phosphodiesterase PDE5A 0.0492
2684 Histidine triad nucleotide-binding protein 1 HINT1 0.0463
1792 Tissue-type plasminogen activator PLAT 0.0456
527 Prostacyclin receptor PTGIR 0.0423
3806 cGMP-dependent 3',5'-cyclic phosphodiesterase PDE2A 0.0391
73 Prostaglandin E2 receptor, EP1 subtype PTGER1 0.0388
6040 6-phosphogluconate dehydrogenase, decarboxylating PGD 0.0375
478 Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C 0.037
6160 Solute carrier organic anion transporter family member 3A1 SLCO3A1 0.0367
6152 Solute carrier organic anion transporter family member 2A1 SLCO2A1 0.0365
1632 Solute carrier organic anion transporter family member 2B1 SLCO2B1 0.0297
4200 Cytochrome P450 1A2 CYP1A2 0.0275
1830 5'-nucleotidase NT5E 0.0266
492 Histamine H1 receptor HRH1 0.0244
4122 Histone deacetylase 2 HDAC2 0.0228
777 Tumor necrosis factor TNF 0.0205
3957 Adenosine deaminase ADA 0.0185
5360 High-affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A PDE9A 0.0149
6143 Solute carrier family 22 member 7 SLC22A7 0.0143
6013 Cytochrome P450 2E1 CYP2E1 0.0129
2256 cGMP-inhibited 3',5'-cyclic phosphodiesterase B PDE3B 0.0122
4512 Cytochrome P450 3A4 CYP3A4 0.0122
2347 Proto-oncogene serine/threonine-protein kinase Pim-1 PIM1 0.0113
6037 Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma PDE6G 0.011
851 5'-AMP-activated protein kinase subunit beta-2 PRKAB2 0.0105
388 AMP deaminase 1 AMPD1 0.0105
6136 Multidrug resistance-associated protein 5 ABCC5 0.0104
1291 cAMP response element-binding protein CREB1 0.0092
704 Long-chain-fatty-acid--CoA ligase 1 ACSL1 0.0091
386 Acetyl-coenzyme A synthetase, cytoplasmic ACSS2 0.0091
821 Acetyl-coenzyme A synthetase 2-like, mitochondrial ACSS1 0.0091
297 Adenylate cyclase type 1 ADCY1 0.0091
4198 Fructose-1,6-bisphosphatase 1 FBP1 0.0088
281 5'-AMP-activated protein kinase subunit beta-1 PRKAB1 0.0087
2164 Multidrug resistance-associated protein 4 ABCC4 0.0087
128 Adenine phosphoribosyltransferase APRT 0.0086
1898 Cytochrome P450 1B1 CYP1B1 0.0085
748 5'-AMP-activated protein kinase catalytic subunit alpha-1 PRKAA1 0.0084
6021 Adenosine kinase ADK 0.0081
10 Glycogen phosphorylase, liver form PYGL 0.0081
1588 Multidrug resistance protein 1 ABCB1 0.0077
6024 Cytochrome P450 1A1 CYP1A1 0.0069
5691 DTDP-4-DEHYDRORHAMNOSE 3,5-EPIMERASE RMLC rmlC 0.0067
3361 Serpin B5 SERPINB5 0.0067
5694 Transcription antiterminator licT licT 0.0067
4924 Cytochrome P450 2C8 CYP2C8 0.0061
4757 Cytochrome P450 2C9 CYP2C9 0.0056
4119 Cytochrome P450 2D6 CYP2D6 0.0055
56 Delta-aminolevulinic acid dehydratase ALAD 0.0054
2356 Delta-aminolevulinic acid dehydratase hemB 0.0054
3613 Delta-aminolevulinic acid dehydratase hemB 0.0054
3674 Delta-aminolevulinic acid dehydratase hemB 0.0054
2286 Isocitrate dehydrogenase [NADP] icd 0.0051
2302 Isocitrate dehydrogenase [NADP] icd 0.0051
2771 Isocitrate dehydrogenase [NADP] icd 0.0051
4534 Cytohesin-2 CYTH2 0.0048
814 Ryanodine receptor 1 RYR1 0.0048
3668 Maltose-binding periplasmic protein precursor malE 0.0047
5692 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B PDE1B 0.0042
2592 Beta-galactosidase lacZ 0.0042
315 Arginase-1 ARG1 0.004
24 Thymidylate synthase TMP1 0.0033
359 Thymidylate synthase TYMS 0.0033
2626 Thymidylate synthase thyA 0.0033
2729 Thymidylate synthase thyA 0.0033
5352 Thymidylate synthase THYA 0.0033
6263 cAMP-dependent protein kinase catalytic subunit alpha PRKACA 0.0032
6107 Cytochrome P450 3A7 CYP3A7 0.0021
4118 Cytochrome P450 3A5 CYP3A5 0.002
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