Reaction Details Report a problem with these data
Target
Isoform 7 of cAMP-specific 3',5'-cyclic phosphodiesterase 4A (PDE4A8)
Ligand
BDBM399928
Substrate
n/a
Meas. Tech.
cintillation Proximity Assay (SPA)
IC50
5.29±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:
BDBM399928
Synonyms:
3-(4-Chloro-2-methylphenyl)-N-cyclopropyl-6,6-difluoro-6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxamide | US10323042, Example 8 | US10738063, Example 8
Type:
Small organic molecule
Emp. Form.:
C17H16ClF2N3O2
Mol. Mass.:
367.778
SMILES:
Cc1cc(Cl)ccc1-c1c2OCC(F)(F)Cn2nc1C(=O)NC1CC1 |(1.97,-5.49,;3.45,-5.09,;3.85,-3.6,;5.34,-3.21,;5.74,-1.72,;6.43,-4.29,;6.03,-5.78,;4.54,-6.18,;4.14,-7.67,;2.68,-8.14,;1.35,-7.37,;.01,-8.14,;.01,-9.68,;-.76,-11.02,;-1.53,-9.68,;1.35,-10.45,;2.68,-9.68,;4.14,-10.16,;5.05,-8.91,;6.59,-8.91,;7.36,-7.58,;7.36,-10.25,;8.9,-10.25,;10.23,-11.02,;10.23,-9.48,)|
Structure:
Search PDB for entries with ligand similarity: