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Target
Isoform 7 of cAMP-specific 3',5'-cyclic phosphodiesterase 4A (PDE4A8)
Ligand
BDBM399965
Substrate
n/a
Meas. Tech.
cintillation Proximity Assay (SPA)
IC50
64.0±n/a nM
Citation
 Chappie, TA; Patel, NC; Verhoest, PR; Helal, CJ; Sciabola, S; LaChapelle, EA; Wager, TT; Hayward, MM 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxamide compounds US Patent  US10323042 Publication Date 6/18/2019 
Target
Name:
Isoform 7 of cAMP-specific 3',5'-cyclic phosphodiesterase 4A (PDE4A8)
Synonyms:
DPDE2 | NP_001104779 | PDE4A | PDE4A3 | PDE4A_HUMAN | cAMP-specific 3',5'-cyclic phosphodiesterase 4A (PDE4A8) | cAMP-specific 3',5'-cyclic phosphodiesterase 4A isoform 3
Type:
Enzyme Catalytic Domain
Mol. Mass.:
91289.34
Organism:
Homo sapiens (Human)
Description:
P27815-7
Residue:
825
Sequence:
MRSGAAPRARPRPPALALPPTGPESLTHFPFSDEDTRRHPPGRSVSFEAENGPTPSPGRSPLDSQASPGLVLHAGAATSQRRESFLYRSDSDYDMSPKTMSRNSSVTSEAHAEDLIVTPFAQVLASLRSVRSNFSLLTNVPVPSNKRSPLGGPTPVCKATLSEETCQQLARETLEELDWCLEQLETMQTYRSVSEMASHKFKRMLNRELTHLSEMSRSGNQVSEYISTTFLDKQNEVEIPSPTMKEREKQQAPRPRPSQPPPPPVPHLQPMSQITGLKKLMHSNSLNNSNIPRFGVKTDQEELLAQELENLNKWGLNIFCVSDYAGGRSLTCIMYMIFQERDLLKKFRIPVDTMVTYMLTLEDHYHADVAYHNSLHAADVLQSTHVLLATPALDAVFTDLEILAALFAAAIHDVDHPGVSNQFLINTNSELALMYNDESVLENHHLAVGFKLLQEDNCDIFQNLSKRQRQSLRKMVIDMVLATDMSKHMTLLADLKTMVETKKVTSSGVLLLDNYSDRIQVLRNMVHCADLSNPTKPLELYRQWTDRIMAEFFQQGDRERERGMEISPMCDKHTASVEKSQVGFIDYIVHPLWETWADLVHPDAQEILDTLEDNRDWYYSAIRQSPSPPPEEESRGPGHPPLPDKFQFELTLEEEEEEEISMAQIPCTAQEALTAQGLSGVEEALDATIAWEASPAQESLEVMAQEASLEAELEAVYLTQQAQSTGSAPVAPDEFSSREEFVVAVSHSSPSALALQSPLLPAWRTLSVSEHAPGLPGLPSTAAEVEAQREHQAAKRACSACAGTFGEDTSALPAPGGGGSGGDPT
  
Inhibitor
Name:
BDBM399965
Synonyms:
US10323042, Example 45 | US10738063, Example 45
Type:
Small organic molecule
Emp. Form.:
C16H15ClFN3O2
Mol. Mass.:
335.761
SMILES:
Fc1ccc(cc1Cl)-c1c2OCCCn2nc1C(=O)NC1CC1
Structure:
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