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Target
cAMP-specific 3',5'-cyclic phosphodiesterase 4A [2-825]
Ligand
BDBM577152
Substrate
n/a
Meas. Tech.
Scintillation Proximity Assay
IC50
3.49±n/a nM
Citation
 Chappie, TA; Patel, NC; Verhoest, PR; Helal, CJ; Sciabola, S; LaChapelle, EA; Wager, TT; Chandrasekaran, RY Tricyclic compounds and their use as phosphodiesterase inhibitors US Patent  US11472805 Publication Date 10/18/2022 
Target
Name:
cAMP-specific 3',5'-cyclic phosphodiesterase 4A [2-825]
Synonyms:
DPDE2 | PDE4A | PDE4A_HUMAN | cAMP-specific 3',5'-cyclic phosphodiesterase (PDE4A3) (2-825)
Type:
Enzyme Catalytic Domain
Mol. Mass.:
92170.87
Organism:
Homo sapiens (Human)
Description:
aa 2-825
Residue:
824
Sequence:
EPPTVPSERSLSLSLPGPREGQATLKPPPQHLWRQPRTPIRIQQRGYSDSAERAERERQPHRPIERADAMDTSDRPGLRTTRMSWPSSFHGTGTGSGGAGGGSSRRFEAENGPTPSPGRSPLDSQASPGLVLHAGAATSQRRESFLYRSDSDYDMSPKTMSRNSSVTSEAHAEDLIVTPFAQVLASLRSVRSNFSLLTNVPVPSNKRSPLGGPTPVCKATLSEETCQQLARETLEELDWCLEQLETMQTYRSVSEMASHKFKRMLNRELTHLSEMSRSGNQVSEYISTTFLDKQNEVEIPSPTMKEREKQQAPRPRPSQPPPPPVPHLQPMSQITGLKKLMHSNSLNNSNIPRFGVKTDQEELLAQELENLNKWGLNIFCVSDYAGGRSLTCIMYMIFQERDLLKKFRIPVDTMVTYMLTLEDHYHADVAYHNSLHAADVLQSTHVLLATPALDAVFTDLEILAALFAAAIHDVDHPGVSNQFLINTNSELALMYNDESVLENHHLAVGFKLLQEDNCDIFQNLSKRQRQSLRKMVIDMVLATDMSKHMTLLADLKTMVETKKVTSSGVLLLDNYSDRIQVLRNMVHCADLSNPTKPLELYRQWTDRIMAEFFQQGDRERERGMEISPMCDKHTASVEKSQVGFIDYIVHPLWETWADLVHPDAQEILDTLEDNRDWYYSAIRQSPSPPPEEESRGPGHPPLPDKFQFELTLEEEEEEEISMAQIPCTAQEALTAQGLSGVEEALDATIAWEASPAQESLEVMAQEASLEAELEAVYLTQQAQSTGSAPVAPDEFSSREEFVVAVSHSSPSALALQSPLLPAWR
  
Inhibitor
Name:
BDBM577152
Synonyms:
10-(4-Chlorophenyl)-8-(5-methyl-1,2-oxazol-3-yl)-7,8-dihydropyrido[2',3':4,5]pyrrolo[1,2-a]pyrazin-9(6H)-one | US11472805, Example 57
Type:
Small organic molecule
Emp. Form.:
C20H15ClN4O2
Mol. Mass.:
378.812
SMILES:
Cc1cc(no1)N1CCn2c(c(-c3ccc(Cl)cc3)c3ncccc23)C1=O
Structure:
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