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Target
Isoform 7 of cAMP-specific 3',5'-cyclic phosphodiesterase 4A (PDE4A8)
Ligand
BDBM399970
Substrate
n/a
Meas. Tech.
cintillation Proximity Assay (SPA)
IC50
40.8±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:
BDBM399970
Synonyms:
US10323042, Example 50 | US10738063, Example 50
Type:
Small organic molecule
Emp. Form.:
C17H14F2N4O2
Mol. Mass.:
344.3155
SMILES:
Fc1cc(-c2c3OCCCn3nc2C(=O)N2CCC2)c(F)cc1C#N |(3.49,2.29,;2,1.89,;1.6,.4,;.11,0,;-.29,-1.49,;-1.75,-1.96,;-3.08,-1.19,;-4.42,-1.96,;-4.42,-3.5,;-3.08,-4.27,;-1.75,-3.5,;-.29,-3.98,;.62,-2.73,;2.16,-2.73,;2.93,-1.4,;2.93,-4.07,;2.53,-5.55,;4.02,-5.95,;4.42,-4.46,;-.98,1.09,;-2.46,.69,;-.58,2.58,;.93,3.03,;1.32,4.52,;1.72,6,)|
Structure:
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