Target Information
Target General Infomation | |||||
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Target ID |
T88975
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Former ID |
TTDS00390
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Target Name |
CGMP-inhibited 3',5'-cyclic phosphodiesterase A
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Gene Name |
PDE3A
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Synonyms |
CGI-PDE A; Cyclic GMP inhibited phosphodiesterase A; Phosphodiesterase 3A; PDE3A
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Target Type |
Successful
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Disease | Asthma [ICD10: J45] | ||||
Bronchial asthma [ICD9: 493; ICD10: J45] | |||||
Cardiovascular disorder [ICD10: I00-I99] | |||||
Cardiac failure [ICD10: I50] | |||||
Heart failure [ICD9: 428; ICD10: I50] | |||||
Thrombocythemia [ICD9: 289.9; ICD10: D75.8] | |||||
Function |
Cyclic nucleotide phosphodiesterase with a dual- specificity for the second messengers cAMP and cGMP, which are key regulators of many important physiological processes.
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BioChemical Class |
Phosphoric diester hydrolases
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Target Validation |
T88975
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UniProt ID | |||||
EC Number |
EC 3.1.4.17
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Sequence |
MAVPGDAARVRDKPVHSGVSQAPTAGRDCHHRADPASPRDSGCRGCWGDLVLQPLRSSRK
LSSALCAGSLSFLLALLVRLVRGEVGCDLEQCKEAAAAEEEEAAPGAEGGVFPGPRGGAP GGGARLSPWLQPSALLFSLLCAFFWMGLYLLRAGVRLPLAVALLAACCGGEALVQIGLGV GEDHLLSLPAAGVVLSCLAAATWLVLRLRLGVLMIALTSAVRTVSLISLERFKVAWRPYL AYLAGVLGILLARYVEQILPQSAEAAPREHLGSQLIAGTKEDIPVFKRRRRSSSVVSAEM SGCSSKSHRRTSLPCIPREQLMGHSEWDHKRGPRGSQSSGTSITVDIAVMGEAHGLITDL LADPSLPPNVCTSLRAVSNLLSTQLTFQAIHKPRVNPVTSLSENYTCSDSEESSEKDKLA IPKRLRRSLPPGLLRRVSSTWTTTTSATGLPTLEPAPVRRDRSTSIKLQEAPSSSPDSWN NPVMMTLTKSRSFTSSYAISAANHVKAKKQSRPGALAKISPLSSPCSSPLQGTPASSLVS KISAVQFPESADTTAKQSLGSHRALTYTQSAPDLSPQILTPPVICSSCGRPYSQGNPADE PLERSGVATRTPSRTDDTAQVTSDYETNNNSDSSDIVQNEDETECLREPLRKASACSTYA PETMMFLDKPILAPEPLVMDNLDSIMEQLNTWNFPIFDLVENIGRKCGRILSQVSYRLFE DMGLFEAFKIPIREFMNYFHALEIGYRDIPYHNRIHATDVLHAVWYLTTQPIPGLSTVIN DHGSTSDSDSDSGFTHGHMGYVFSKTYNVTDDKYGCLSGNIPALELMALYVAAAMHDYDH PGRTNAFLVATSAPQAVLYNDRSVLENHHAAAAWNLFMSRPEYNFLINLDHVEFKHFRFL VIEAILATDLKKHFDFVAKFNGKVNDDVGIDWTNENDRLLVCQMCIKLADINGPAKCKEL HLQWTDGIVNEFYEQGDEEASLGLPISPFMDRSAPQLANLQESFISHIVGPLCNSYDSAG LMPGKWVEDSDESGDTDDPEEEEEEAPAPNEEETCENNESPKKKTFKRRKIYCQITQHLL QNHKMWKKVIEEEQRLAGIENQSLDQTPQSHSSEQIQAIKEEEEEKGKPRGEEIPTQKPD Q |
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Drugs and Mode of Action | |||||
Drug(s) | Aminophylline | Drug Info | Approved | Bronchial asthma | [538346] |
Anagrelide | Drug Info | Approved | Thrombocythemia | [536361], [542121] | |
VESNARINONE | Drug Info | Approved | Cardiac failure | [551871] | |
Aminophylline | Drug Info | Phase 2 | Asthma | [533467] | |
BEMORADAN | Drug Info | Phase 2 | Heart failure | [526254] | |
CI-930 | Drug Info | Discontinued in Phase 2 | Discovery agent | [544562] | |
EMD-53998 | Drug Info | Discontinued in Phase 1 | Cardiovascular disorder | [544631] | |
BMY-20844 | Drug Info | Terminated | Discovery agent | [544630] | |
IMAZODAN | Drug Info | Terminated | Discovery agent | [544637] | |
LAS-31180 | Drug Info | Terminated | Heart failure | [525948] | |
Inhibitor | 1,3,9,9a-Tetrahydro-imidazo[4,5-b]quinolin-2-one | Drug Info | [528087] | ||
1,3-Dihydro-imidazo[4,5-b]quinolin-2-one | Drug Info | [528087] | |||
1,3-Dihydro-naphtho[2,3-d]imidazol-2-one | Drug Info | [528087] | |||
1,5-Dihydro-imidazo[2,1-b]quinazolin-2-one | Drug Info | [533367] | |||
2-Morpholin-4-yl-8-phenylethynyl-chromen-4-one | Drug Info | [527870] | |||
2-morpholino-7-(2-phenylethynyl)-4H-chromen-4-one | Drug Info | [527870] | |||
2-morpholino-7-phenyl-4H-chromen-4-one | Drug Info | [527870] | |||
3-Isobutyl-1-methyl-3,9-dihydro-purine-2,6-dione | Drug Info | [533395] | |||
5-Methyl-1,3-dihydro-imidazo[4,5-b]quinolin-2-one | Drug Info | [528087] | |||
6-(2-Imidazol-1-yl-vinyl)-1H-quinolin-2-one | Drug Info | [526726] | |||
6-Imidazol-1-yl-3,4-dihydro-1H-quinolin-2-one | Drug Info | [526726] | |||
6-Pyridin-3-yl-3,4-dihydro-1H-quinolin-2-one | Drug Info | [526726] | |||
7-Chloro-1,3-dihydro-imidazo[4,5-b]quinolin-2-one | Drug Info | [528087] | |||
7-Ethoxy-1,3-dihydro-imidazo[4,5-b]quinolin-2-one | Drug Info | [528087] | |||
7-Fluoro-1,3-dihydro-imidazo[4,5-b]quinolin-2-one | Drug Info | [528087] | |||
7-Iodo-1,5-dihydro-imidazo[2,1-b]quinazolin-2-one | Drug Info | [533367] | |||
7-Methyl-1,3-dihydro-imidazo[4,5-b]quinolin-2-one | Drug Info | [528087] | |||
8-Chloro-1,3-dihydro-imidazo[4,5-b]quinolin-2-one | Drug Info | [528087] | |||
8-Methyl-1,3-dihydro-imidazo[4,5-b]quinolin-2-one | Drug Info | [528087] | |||
8-methyl-2-morpholino-7-phenoxy-4H-chromen-4-one | Drug Info | [527870] | |||
8-methyl-2-morpholino-7-phenyl-4H-chromen-4-one | Drug Info | [527870] | |||
Aminophylline | Drug Info | [535425], [536386] | |||
Anagrelide | Drug Info | [536112] | |||
BEMORADAN | Drug Info | [551871] | |||
BENZOYLENUREA | Drug Info | [529219] | |||
BMY-20844 | Drug Info | [526741] | |||
CI-930 | Drug Info | [533015] | |||
EMD-53998 | Drug Info | [551871] | |||
FENOXIMONE | Drug Info | [533411] | |||
IMAZODAN | Drug Info | [526726] | |||
KURAIDIN | Drug Info | [526395] | |||
KURARINOL | Drug Info | [526395] | |||
OPC-13013 | Drug Info | [533395] | |||
SOPHOFLAVESCENOL | Drug Info | [526395] | |||
TETRAHYDROBENXIMIDAZOLE | Drug Info | [533015] | |||
VESNARINONE | Drug Info | [530575] | |||
Modulator | LAS-31180 | Drug Info | [525948] | ||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
References | |||||
Ref 525948 | Pharmacological profile of LAS 31180, a new inotropic/vasodilator quinolone derivative. Arzneimittelforschung. 2000 Nov;50(11):980-6. | ||||
Ref 526254 | Evaluation of the excretion, and metabolism of the cardiotonic agent bemoradan in male rats and female beagle dogs. Eur J Drug Metab Pharmacokinet. 2001 Oct-Dec;26(4):263-71. | ||||
Ref 533467 | Adenosine receptors: development of selective agonists and antagonists. Prog Clin Biol Res. 1987;230:41-63. | ||||
Ref 536361 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. | ||||
Ref 538346 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 081142. | ||||
Ref 542121 | (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: 7114). | ||||
Ref 544562 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000144) | ||||
Ref 544630 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000364) | ||||
Ref 544631 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000367) | ||||
Ref 525948 | Pharmacological profile of LAS 31180, a new inotropic/vasodilator quinolone derivative. Arzneimittelforschung. 2000 Nov;50(11):980-6. | ||||
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 526726 | J Med Chem. 1992 Feb 21;35(4):620-8.3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase. | ||||
Ref 526741 | J Med Chem. 1992 Jul 10;35(14):2688-96.Inhibitors of blood platelet cAMP phosphodiesterase. 3. 1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives with enhanced aqueous solubility. | ||||
Ref 527870 | Bioorg Med Chem Lett. 2006 Feb 15;16(4):969-73. Epub 2005 Nov 15.Analysis of anti-PDE3 activity of 2-morpholinochromone derivatives reveals multiple mechanisms of anti-platelet activity. | ||||
Ref 528087 | J Med Chem. 1991 Sep;34(9):2906-16.1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-ones--inhibitors of blood platelet cAMP phosphodiesterase and induced aggregation. | ||||
Ref 529219 | Eur J Med Chem. 2008 Jul;43(7):1349-59. Epub 2007 Dec 21.CODES, a novel procedure for ligand-based virtual screening: PDE7 inhibitors as an application example. | ||||
Ref 530575 | Bioorg Med Chem. 2010 Jan 15;18(2):855-62. Epub 2009 Nov 26.Design, synthesis and biological evaluation of 6-(benzyloxy)-4-methylquinolin-2(1H)-one derivatives as PDE3 inhibitors. | ||||
Ref 533015 | J Med Chem. 1989 Feb;32(2):342-50.Cardiotonic agents. 9. Synthesis and biological evaluation of a series of (E)-4,5-dihydro-6-[2-[4-(1H-imidazol-1-yl)phenyl]ethenyl]-3 (2H)-pyridazinones: a novel class of compounds with positive inotropic, antithrombotic, and vasodilatory activities for the treatment of congestive heart failure. | ||||
Ref 533367 | J Med Chem. 1988 Nov;31(11):2136-45.Inhibitors of cyclic AMP phosphodiesterase. 3. Synthesis and biological evaluation of pyrido and imidazolyl analogues of 1,2,3,5-tetrahydro-2-oxoimidazo[2,1-b]quinazoline. | ||||
Ref 533395 | J Med Chem. 1985 May;28(5):537-45.A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity. | ||||
Ref 533411 | J Med Chem. 1987 Feb;30(2):303-18.Inhibitors of cyclic AMP phosphodiesterase. 2. Structural variations of N-cyclohexyl-N-methyl-4-[(1,2,3,5-tetrahydro- 2-oxoimidazo[2,1-b]quinazolin-7-yl)-oxy]butyramide (RS-82856). | ||||
Ref 535425 | Spasmolytic effects of colforsin daropate on serotonin-induced pulmonary hypertension and bronchoconstriction in dogs. Acta Anaesthesiol Scand. 2002 Mar;46(3):297-302. |
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