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Target
Isoform 7 of cAMP-specific 3',5'-cyclic phosphodiesterase 4A (PDE4A8)
Ligand
BDBM399936
Substrate
n/a
Meas. Tech.
cintillation Proximity Assay (SPA)
IC50
36.7±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:
BDBM399936
Synonyms:
US10323042, Example 16 | US10738063, Example 16
Type:
Small organic molecule
Emp. Form.:
C16H14ClF2N3O2
Mol. Mass.:
353.751
SMILES:
Fc1cc(-c2c3OCCCn3nc2C(=O)NC2CC2)c(F)cc1Cl |(2.79,2.47,;1.31,2.07,;.91,.59,;-.58,.19,;-.98,-1.3,;-2.44,-1.78,;-3.78,-1.01,;-5.11,-1.78,;-5.11,-3.32,;-3.78,-4.09,;-2.44,-3.32,;-.98,-3.79,;-.07,-2.55,;1.47,-2.55,;2.24,-1.21,;2.24,-3.88,;3.78,-3.88,;5.11,-4.65,;5.11,-3.11,;-1.67,1.28,;-3.16,.88,;-1.27,2.76,;.22,3.16,;.62,4.65,)|
Structure:
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