Target Information
Target General Infomation | |||||
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Target ID |
T61744
|
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Former ID |
TTDS00280
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Target Name |
CAMP-specific 3',5'-cyclic phosphodiesterase 4A
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Gene Name |
PDE4A
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Synonyms |
DPDE2; PDE46; Type 4A cAMP phosphodiesterase; PDE4A
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Target Type |
Successful
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Disease | Asthma [ICD10: J45] | ||||
Acute bronchial asthma [ICD9: 493; ICD10: J45] | |||||
Asthma; Chronic obstructive pulmonary disease [ICD9: 490-492, 493, 494-496; ICD10: J40-J44, J47, J45] | |||||
Atopic dermatitis [ICD9: 691.8, 692.9; ICD10: L00-L99] | |||||
Allergy [ICD9: 995.3; ICD10: T78.4] | |||||
Cutaneous T-cell lymphoma [ICD9: 202.1, 202.2; ICD10: C84.0, C84.1] | |||||
Chronic lymphocytic leukaemia [ICD10: C91] | |||||
Crohn's disease [ICD9: 555; ICD10: K50] | |||||
Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47] | |||||
Cognitive disorders [ICD9: 290-294, 294.0, 780.09, 780.9, 780.93; ICD10: F01-F07, F04, F05, R41.3] | |||||
Chronic obstructive pulmonary disease; Asthma [ICD9: 490-492, 493, 494-496; ICD10: J40-J44, J47, J45] | |||||
Emphysema; Bronchitis; Chronic obstructive pulmonary disease [ICD9: 460-519, 466, 490, 490-492, 491, 492, 494-496; ICD10: J00-J99, J20-J21, J40-J44, J42, J43, J47] | |||||
Glomerulonephritis [ICD9: 580-582; ICD10: N00, N01, N03, N18] | |||||
Huntington's disease [ICD9: 294.1, 333.4; ICD10: F02.2, G10] | |||||
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25] | |||||
Lung inflammation [ICD10: D86] | |||||
Multiple scierosis [ICD9: 340; ICD10: G35] | |||||
Mood disorder [ICD10: F30-F39] | |||||
Peripheral vascular disease [ICD9: 443.9; ICD10: I73.9] | |||||
Parkinson's disease [ICD9: 332; ICD10: G20] | |||||
Psoriasis [ICD9: 696; ICD10: L40] | |||||
Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06] | |||||
Respiratory tract inflammation [ICD10: J00-J99] | |||||
Rhinitis [ICD9: 472.0, 477; ICD10: J00, J30, J31.0] | |||||
Xerophthalmia [ICD10: E50.6-E50.7] | |||||
Function |
Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes. .
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BioChemical Class |
Phosphoric diester hydrolases
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Target Validation |
T61744
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UniProt ID | |||||
EC Number |
EC 3.1.4.17
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Sequence |
MEPPTVPSERSLSLSLPGPREGQATLKPPPQHLWRQPRTPIRIQQRGYSDSAERAERERQ
PHRPIERADAMDTSDRPGLRTTRMSWPSSFHGTGTGSGGAGGGSSRRFEAENGPTPSPGR SPLDSQASPGLVLHAGAATSQRRESFLYRSDSDYDMSPKTMSRNSSVTSEAHAEDLIVTP FAQVLASLRSVRSNFSLLTNVPVPSNKRSPLGGPTPVCKATLSEETCQQLARETLEELDW CLEQLETMQTYRSVSEMASHKFKRMLNRELTHLSEMSRSGNQVSEYISTTFLDKQNEVEI PSPTMKEREKQQAPRPRPSQPPPPPVPHLQPMSQITGLKKLMHSNSLNNSNIPRFGVKTD QEELLAQELENLNKWGLNIFCVSDYAGGRSLTCIMYMIFQERDLLKKFRIPVDTMVTYML TLEDHYHADVAYHNSLHAADVLQSTHVLLATPALDAVFTDLEILAALFAAAIHDVDHPGV SNQFLINTNSELALMYNDESVLENHHLAVGFKLLQEDNCDIFQNLSKRQRQSLRKMVIDM VLATDMSKHMTLLADLKTMVETKKVTSSGVLLLDNYSDRIQVLRNMVHCADLSNPTKPLE LYRQWTDRIMAEFFQQGDRERERGMEISPMCDKHTASVEKSQVGFIDYIVHPLWETWADL VHPDAQEILDTLEDNRDWYYSAIRQSPSPPPEEESRGPGHPPLPDKFQFELTLEEEEEEE ISMAQIPCTAQEALTAQGLSGVEEALDATIAWEASPAQESLEVMAQEASLEAELEAVYLT QQAQSTGSAPVAPDEFSSREEFVVAVSHSSPSALALQSPLLPAWRTLSVSEHAPGLPGLP STAAEVEAQREHQAAKRACSACAGTFGEDTSALPAPGGGGSGGDPT |
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Structure |
2QYK; 3I8V; 3TVX
|
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Drugs and Mode of Action | |||||
Drug(s) | Dyphylline | Drug Info | Approved | Acute bronchial asthma | [538402], [542076], [551871] |
Enprofylline | Drug Info | Approved | Asthma | [537725] | |
DENBUFYLLINE | Drug Info | Phase 3 | Cognitive disorders | [525628] | |
SOTB07 | Drug Info | Phase 3 | Asthma | [524380] | |
AN-2898 | Drug Info | Phase 2 | Atopic dermatitis | [523369] | |
AWD-12-281 | Drug Info | Phase 2 | Rhinitis | [521859] | |
CC-1088 | Drug Info | Phase 2 | Crohn's disease | [521533] | |
GPD-1116 | Drug Info | Phase 2 | Asthma | [529143] | |
HT-0712 | Drug Info | Phase 2 | Cognitive disorders | [547671] | |
LIRIMILAST | Drug Info | Phase 2 | Chronic obstructive pulmonary disease | [551720] | |
MK-0873 | Drug Info | Phase 2 | Psoriasis | [521664] | |
Oglemilast | Drug Info | Phase 2 | Asthma | [522312] | |
OX-914 | Drug Info | Phase 2 | Asthma | [522443] | |
Piclamilast | Drug Info | Phase 2 | Rheumatoid arthritis | [525937] | |
Revamilast | Drug Info | Phase 2 | Asthma | [523630] | |
ROLIPRAM | Drug Info | Phase 2 | Discovery agent | [521483], [540724] | |
TA-7906 | Drug Info | Phase 2 | Atopic dermatitis | [548322] | |
TOFIMILAST | Drug Info | Phase 2 | Chronic obstructive pulmonary disease | [521675] | |
AVE-8112 | Drug Info | Phase 1 | Parkinson's disease | [524229] | |
GSK-356278 | Drug Info | Phase 1 | Huntington's disease | [522890] | |
MEM-1414 | Drug Info | Phase 1 | Mood disorder | [551843] | |
Ronomilast | Drug Info | Phase 1 | Chronic obstructive pulmonary disease | [547206] | |
Cilomilast | Drug Info | Discontinued in Phase 3 | Emphysema; Bronchitis; Chronic obstructive pulmonary disease | [536958], [542430] | |
CDP840 | Drug Info | Discontinued in Phase 2 | Chronic obstructive pulmonary disease | [545388] | |
CI-1018 | Drug Info | Discontinued in Phase 2 | Asthma | [546735] | |
Cilomilast | Drug Info | Discontinued in Phase 2 | Asthma; Chronic obstructive pulmonary disease | [536958], [542430] | |
Daxalipram | Drug Info | Discontinued in Phase 2 | Multiple scierosis | [547377] | |
GSK256066 | Drug Info | Discontinued in Phase 2 | Chronic obstructive pulmonary disease; Asthma | [548294] | |
KW-4490 | Drug Info | Discontinued in Phase 2 | Asthma | [547542] | |
LAS-37779 | Drug Info | Discontinued in Phase 2 | Psoriasis | [548191] | |
V-11294A | Drug Info | Discontinued in Phase 2 | Asthma | [547058] | |
D-4418 | Drug Info | Discontinued in Phase 1 | Cutaneous T-cell lymphoma | [546370] | |
SCH-351591 | Drug Info | Discontinued in Phase 1 | Chronic obstructive pulmonary disease | [546885] | |
YM-976 | Drug Info | Discontinued in Phase 1 | Asthma | [540755], [546870] | |
D-22888 | Drug Info | Terminated | Allergy | [546267] | |
GW-3600 | Drug Info | Terminated | Asthma | [546122] | |
NIK-616 | Drug Info | Terminated | Asthma; Chronic obstructive pulmonary disease | [547892] | |
TJN-598 | Drug Info | Terminated | Glomerulonephritis | [531152] | |
Torbafylline | Drug Info | Terminated | Peripheral vascular disease | [532864] | |
Inhibitor | (2,5-Diphenyl-furan-3-yl)-phenyl-methanone | Drug Info | [525447] | ||
(R)-Rolipram | Drug Info | [537166] | |||
(S)-Rolipram | Drug Info | [537166] | |||
1-Butyl-3-methyl-3,7-dihydro-purine-2,6-dione | Drug Info | [526756] | |||
1-Methyl-3-propyl-3,7-dihydro-purine-2,6-dione | Drug Info | [526756] | |||
2,5-Bis-(3,4-dimethoxy-phenyl)-furan | Drug Info | [525447] | |||
2,5-Bis-(3-cyclopentyloxy-4-methoxy-phenyl)-furan | Drug Info | [525447] | |||
3-Isobutyl-1-methyl-3,9-dihydro-purine-2,6-dione | Drug Info | [533395] | |||
4-(2,5-Diphenyl-furan-3-yl)-morpholine | Drug Info | [525447] | |||
6-Azido-8-(3-iodo-phenyl)-quinoline | Drug Info | [525895] | |||
6-Imidazol-1-ylmethyl-8-phenyl-quinoline | Drug Info | [525895] | |||
8-(3-Azido-phenyl)-6-iodo-quinoline | Drug Info | [525895] | |||
8-(3-Azido-phenyl)-6-pyridin-4-ylmethyl-quinoline | Drug Info | [525895] | |||
8-(3-Nitro-phenyl)-6-phenyl-[1,7]naphthyridine | Drug Info | [525700] | |||
8-(3-Nitro-phenyl)-6-pyridin-4-ylmethyl-quinoline | Drug Info | [525895] | |||
AL-59640 | Drug Info | [543404] | |||
AN-2898 | Drug Info | [532329] | |||
ASP-3258 | Drug Info | [543404] | |||
AVE-8112 | Drug Info | [544367] | |||
AWD-12-281 | Drug Info | [527926] | |||
Benzyl-(2-imidazol-1-yl-quinazolin-4-yl)-amine | Drug Info | [533684] | |||
Benzyl-(2-phenyl-quinazolin-4-yl)-amine | Drug Info | [533684] | |||
Benzyl-(2-pyridin-3-yl-quinazolin-4-yl)-amine | Drug Info | [533684] | |||
Benzyl-(2-pyridin-4-yl-quinazolin-4-yl)-amine | Drug Info | [533684] | |||
Benzyl-(2-thiophen-2-yl-quinazolin-4-yl)-amine | Drug Info | [533684] | |||
CC-1088 | Drug Info | [534801] | |||
CD-160130 | Drug Info | [543404] | |||
CDP840 | Drug Info | [527742] | |||
CH-3697 | Drug Info | [543404] | |||
CHF-5480 | Drug Info | [543404] | |||
CI-1018 | Drug Info | [527082] | |||
CI-1044 | Drug Info | [525932] | |||
Cilomilast | Drug Info | [536958] | |||
D-22888 | Drug Info | [534736] | |||
D-4418 | Drug Info | [529616] | |||
Daxalipram | Drug Info | [532832] | |||
DENBUFYLLINE | Drug Info | [526336] | |||
Dyphylline | Drug Info | [537894] | |||
Enprofylline | Drug Info | [537725] | |||
GPD-1116 | Drug Info | [529143] | |||
GSK-356278 | Drug Info | [532759] | |||
GSK256066 | Drug Info | [550963] | |||
GW-3600 | Drug Info | [534617] | |||
HT-0712 | Drug Info | [543404] | |||
KF-66490 | Drug Info | [529747] | |||
KURAIDIN | Drug Info | [526395] | |||
KURARINOL | Drug Info | [526395] | |||
KW-4490 | Drug Info | [529433] | |||
L-454560 | Drug Info | [531102] | |||
L-791943 | Drug Info | [526342] | |||
L-869298 | Drug Info | [528081] | |||
LAS-37779 | Drug Info | [548192] | |||
LIRIMILAST | Drug Info | [544060] | |||
MEM-1414 | Drug Info | [533010] | |||
MK-0873 | Drug Info | [529356] | |||
NIK-616 | Drug Info | [550628] | |||
NIS-62949 | Drug Info | [537177] | |||
NITRAQUAZONE | Drug Info | [525939] | |||
OCID-2987 | Drug Info | [543404] | |||
Oglemilast | Drug Info | [544060] | |||
OX-914 | Drug Info | [549827] | |||
PDE4 inhibitors | Drug Info | [543404] | |||
PDE4 inhibitors | Drug Info | [543404] | |||
Piclamilast | Drug Info | [551373] | |||
Revamilast | Drug Info | [550161] | |||
ROLIPRAM | Drug Info | [551282] | |||
Ronomilast | Drug Info | [550312] | |||
RS-14491 | Drug Info | [534389] | |||
RS-25344 | Drug Info | [534698] | |||
SCH-351591 | Drug Info | [526350] | |||
SOPHOFLAVESCENOL | Drug Info | [526395] | |||
SOTB07 | Drug Info | [543404] | |||
TA-7906 | Drug Info | [526360] | |||
TAS-203 | Drug Info | [543404] | |||
TJN-598 | Drug Info | [531152] | |||
TOFIMILAST | Drug Info | [531324] | |||
Torbafylline | Drug Info | [532864] | |||
UCB-101333-3 | Drug Info | [527990] | |||
V-11294A | Drug Info | [526464] | |||
YM-976 | Drug Info | [526009] | |||
ZL-N-91 | Drug Info | [543404] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Purine metabolism | ||||
cAMP signaling pathway | |||||
Morphine addiction | |||||
Reactome | DARPP-32 events | ||||
G alpha (s) signalling events | |||||
WikiPathways | G Protein Signaling Pathways | ||||
References | |||||
Ref 521483 | ClinicalTrials.gov (NCT00011375) Rolipram to Treat Multiple Sclerosis. U.S. National Institutes of Health. | ||||
Ref 521533 | ClinicalTrials.gov (NCT00045786) Study to Determine the Safety and Preliminary Efficacy of CC-1088 in the Treatment of Myelodysplastic Syndromes. U.S. National Institutes of Health. | ||||
Ref 521664 | ClinicalTrials.gov (NCT00132730) An Investigational Drug Study In Patients With COPD (Chronic Obstructive Pulmonary Disease) (MK-0873-005). U.S. National Institutes of Health. | ||||
Ref 521675 | ClinicalTrials.gov (NCT00150397) A Study of the Safety and Efficacy of Tofimilast in Adult Asthmatics. U.S. National Institutes of Health. | ||||
Ref 521859 | ClinicalTrials.gov (NCT00354510) Topical GW842470X In Adults Patients With Moderate Atopic Dermatitis. U.S. National Institutes of Health. | ||||
Ref 522312 | ClinicalTrials.gov (NCT00671073) Study To Assess Efficacy and Safety of Oglemilast in Patients With Chronic Obstructive Pulmonary Disease (COPD). U.S. National Institutes of Health. | ||||
Ref 522443 | ClinicalTrials.gov (NCT00758446) Efficacy and Safety Study of BLX-028914 in Subjects With Allergic Rhinitis. U.S. National Institutes of Health. | ||||
Ref 522890 | ClinicalTrials.gov (NCT01031186) First Time in Human Study. U.S. National Institutes of Health. | ||||
Ref 523369 | ClinicalTrials.gov (NCT01301508) Efficacy and Safety of AN2898 and AN2728 Topical Ointments to Treat Mild-to-Moderate Atopic Dermatitis. U.S. National Institutes of Health. | ||||
Ref 523630 | ClinicalTrials.gov (NCT01436890) A Clinical Trial to Study the Effects of Revamilast in Patients With Chronic Persistent Asthma. U.S. National Institutes of Health. | ||||
Ref 524229 | ClinicalTrials.gov (NCT01803945) A Multiple Ascending Dose Study to Assess the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of AVE8112 in Patients With Parkinson's Disease. U.S. National Institutes of Health. | ||||
Ref 524380 | ClinicalTrials.gov (NCT01907763) Study Phase III Study to Assess the Efficacy and Safety of SOTB07 in Asthma Patients. U.S. National Institutes of Health. | ||||
Ref 525628 | Denbufylline in dementia: a double-blind controlled study. Dement Geriatr Cogn Disord. 1999 Nov-Dec;10(6):505-10. | ||||
Ref 525937 | Effect of food and gender on the pharmacokinetics of RP 73401, a phosphodiesterase IV inhibitor. Int J Clin Pharmacol Ther. 2000 Dec;38(12):588-94. | ||||
Ref 529143 | Phosphodiesterase 4 inhibitor GPD-1116 markedly attenuates the development of cigarette smoke-induced emphysema in senescence-accelerated mice P1 strain. Am J Physiol Lung Cell Mol Physiol. 2008 Feb;294(2):L196-204. Epub 2007 Nov 9. | ||||
Ref 531152 | Effects of TJN-598, a new selective phosphodiesterase type IV inhibitor on anti-Thy1 nephritis in rats. Clin Exp Nephrol. 2011 Feb;15(1):14-24. | ||||
Ref 532864 | Phosphodiesterase (PDE) inhibitor torbafylline (HWA 448) attenuates burn-induced rat skeletal muscle proteolysis through the PDE4/cAMP/EPAC/PI3K/Akt pathway. Mol Cell Endocrinol. 2014 Aug 5;393(1-2):152-63. | ||||
Ref 537725 | Effects of enprofylline, a new xanthine derivate, on human pregnant myometrium. Am J Obstet Gynecol. 1987 Apr;156(4):958-62. | ||||
Ref 538402 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 007794. | ||||
Ref 540724 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5260). | ||||
Ref 540755 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5292). | ||||
Ref 542076 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7070). | ||||
Ref 542430 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7407). | ||||
Ref 545388 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003087) | ||||
Ref 546122 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006447) | ||||
Ref 546267 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007179) | ||||
Ref 546370 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007757) | ||||
Ref 546735 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010034) | ||||
Ref 546870 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010783) | ||||
Ref 546885 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010874) | ||||
Ref 547058 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012597) | ||||
Ref 547206 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013990) | ||||
Ref 547377 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015672) | ||||
Ref 547542 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017153) | ||||
Ref 547671 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018324) | ||||
Ref 547892 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020194) | ||||
Ref 548191 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022894) | ||||
Ref 548294 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024245) | ||||
Ref 548322 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024588) | ||||
Ref 525447 | Bioorg Med Chem Lett. 1999 Feb 8;9(3):323-6.Substituted furans as inhibitors of the PDE4 enzyme. | ||||
Ref 525700 | J Med Chem. 2000 Feb 24;43(4):675-82.Palladium-catalyzed cross-coupling reactions for the synthesis of 6, 8-disubstituted 1,7-naphthyridines: a novel class of potent and selective phosphodiesterase type 4D inhibitors. | ||||
Ref 525895 | J Med Chem. 2000 Oct 19;43(21):3820-3.Hunting the emesis and efficacy targets of PDE4 inhibitors: identification of the photoaffinity probe 8-(3-azidophenyl)-6- [(4-iodo-1H-1-imidazolyl)methyl]quinoline (APIIMQ). | ||||
Ref 525932 | J Med Chem. 2000 Dec 14;43(25):4850-67.Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discoveryof potent, selective phosphodiesterase type 4 inhibitors. | ||||
Ref 525939 | Bioorg Med Chem Lett. 2000 Dec 4;10(23):2661-4.Synthesis and biological evaluation of 2,5-dihydropyrazol. | ||||
Ref 526009 | Antiasthmatic effect of YM976, a novel PDE4 inhibitor, in guinea pigs. J Pharmacol Exp Ther. 2001 Apr;297(1):165-73. | ||||
Ref 526336 | J Med Chem. 2002 May 23;45(11):2342-5.Pyrazolopyrimidine-2,4-dione sulfonamides: novel and selective calcitonin inducers. | ||||
Ref 526342 | Bioorg Med Chem Lett. 2002 Jun 3;12(11):1457-61.Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 inhibitor. | ||||
Ref 526350 | Bioorg Med Chem Lett. 2002 Jun 17;12(12):1621-3.Synthesis and profile of SCH351591, a novel PDE4 inhibitor. | ||||
Ref 526360 | Potential role of phosphodiesterase 7 in human T cell function: comparative effects of two phosphodiesterase inhibitors. Clin Exp Immunol. 2002 Jun;128(3):460-6. | ||||
Ref 526395 | Bioorg Med Chem Lett. 2002 Sep 2;12(17):2313-6.A prenylated flavonol, sophoflavescenol: a potent and selective inhibitor of cGMP phosphodiesterase 5. | ||||
Ref 526464 | Pharmacokinetic and pharmacodynamic profile following oral administration of the phosphodiesterase (PDE)4 inhibitor V11294A in healthy volunteers. Br J Clin Pharmacol. 2002 Nov;54(5):478-84. | ||||
Ref 526756 | J Med Chem. 1992 Oct 30;35(22):4039-44.Effects of alkyl substitutions of xanthine skeleton on bronchodilation. | ||||
Ref 527082 | Bioorg Med Chem Lett. 2004 Jun 21;14(12):3303-6.New substituted triaza-benzo[cd]azulen-9-ones as promising phosphodiesterase-4 inhibitors. | ||||
Ref 527742 | Bioorg Med Chem Lett. 2005 Dec 1;15(23):5241-6. Epub 2005 Sep 15.Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor. | ||||
Ref 527926 | The phosphodiesterase 4 inhibitor AWD 12-281 is active in a new guinea-pig model of allergic skin inflammation predictive of human skin penetration and suppresses both Th1 and Th2 cytokines in mice. J Pharm Pharmacol. 2005 Dec;57(12):1609-17. | ||||
Ref 527990 | Bioorg Med Chem Lett. 2006 Apr 1;16(7):1834-9. Epub 2006 Jan 24.First dual M3 antagonists-PDE4 inhibitors: synthesis and SAR of 4,6-diaminopyrimidine derivatives. | ||||
Ref 528081 | J Med Chem. 2006 Mar 23;49(6):1867-73.Enantiomer discrimination illustrated by the high resolution crystal structures of type 4 phosphodiesterase. | ||||
Ref 529143 | Phosphodiesterase 4 inhibitor GPD-1116 markedly attenuates the development of cigarette smoke-induced emphysema in senescence-accelerated mice P1 strain. Am J Physiol Lung Cell Mol Physiol. 2008 Feb;294(2):L196-204. Epub 2007 Nov 9. | ||||
Ref 529356 | MK-0873, a PDE4 inhibitor, does not influence the pharmacokinetics of theophylline in healthy male volunteers. Pulm Pharmacol Ther. 2008;21(3):573-7. | ||||
Ref 529433 | Pharmacokinetics and metabolism of KW-4490, a selective phosphodiesterase 4 inhibitor: difference in excretion of KW-4490 and acylglucuronide metabolites between rats and cynomolgus monkeys. Xenobiotica. 2008 May;38(5):511-26. | ||||
Ref 529616 | Can the anti-inflammatory potential of PDE4 inhibitors be realized: guarded optimism or wishful thinking. Br J Pharmacol. 2008 Oct;155(3):288-90. | ||||
Ref 529747 | Effect of orally administered KF66490, a phosphodiesterase 4 inhibitor, on dermatitis in mouse models. Int Immunopharmacol. 2009 Jan;9(1):55-62. | ||||
Ref 531102 | Bioorg Med Chem Lett. 2010 Sep 15;20(18):5502-5. Epub 2010 Jul 21.The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors. | ||||
Ref 531152 | Effects of TJN-598, a new selective phosphodiesterase type IV inhibitor on anti-Thy1 nephritis in rats. Clin Exp Nephrol. 2011 Feb;15(1):14-24. | ||||
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