Reaction Details
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Isoform 3 of cAMP-specific 3',5'-cyclic phosphodiesterase 4D (hPDE4D3) 0-562]
Ligand
BDBM399924
Substrate
n/a
Meas. Tech.
Scintillation Proximity Assay (SPA)
IC50
>17800±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 US10738063 Publication Date 8/11/2020 More Info.:
Target
Name:
Isoform 3 of cAMP-specific 3',5'-cyclic phosphodiesterase 4D (hPDE4D3) 0-562]
Synonyms:
DPDE3 | PDE4D | PDE4D_HUMAN | cAMP-specific 3',5'-cyclic phosphodiesterase 4D (PDE4D3)(50-672) | cAMP-specific 3',5'-cyclic phosphodiesterase 4D (hPDE4D3) [50-562]
Type:
Enzyme Catalytic Domain
Mol. Mass.:
71001.79
Organism:
Homo sapiens (Human)
Description:
aa 50-672
Residue:
624
Sequence:
QRRESFLYRSDSDYDLSPKSMSRNSSIASDIHGDDLIVTPFAQVLASLRTVRNNFAALTNLQDRAPSKRSPMCNQPSINKATITEEAYQKLASETLEELDWCLDQLETLQTRHSVSEMASNKFKRMLNRELTHLSEMSRSGNQVSEFISNTFLDKQHEVEIPSPTQKEKEKKKRPMSQISGVKKLMHSSSLTNSSIPRFGVKTEQEDVLAKELEDVNKWGLHVFRIAELSGNRPLTVIMHTIFQERDLLKTFKIPVDTLITYLMTLEDHYHADVAYHNNIHAADVVQSTHVLLSTPALEAVFTDLEILAAIFASAIHDVDHPGVSNQFLINTNSELALMYNDSSVLENHHLAVGFKLLQEENCDIFQNLTKKQRQSLRKMVIDIVLATDMSKHMNLLADLKTMVETKKVTSSGVLLLDNYSDRIQVLQNMVHCADLSNPTKPLQLYRQWTDRIMEEFFRQGDRERERGMEISPMCDKHNASVEKSQVGFIDYIVHPLWETWADLVHPDAQDILDTLEDNREWYQSTIPQSPSPAPDDPEEGRQGQTEKFQFELTLEEDGESDTEKDSGSQVEEDTSCSDSKTLCTQDSESTEIPLDEQVEEEAVGEEEESQPEACVIDDRSPDT
Inhibitor
Name:
BDBM399924
Synonyms:
Azetidin-1-yl[3-(4-chloro-2,3-difluorophenyl)-6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazin-2-yl]methanone | US10323042, Example 4 | US10738063, Example 4
Type:
Small organic molecule
Emp. Form.:
C16H14ClF2N3O2
Mol. Mass.:
353.751
SMILES:
Fc1c(Cl)ccc(-c2c3OCCCn3nc2C(=O)N2CCC2)c1F |(4.22,-13.7,;5.31,-14.79,;6.8,-14.39,;7.2,-12.9,;7.89,-15.48,;7.49,-16.96,;6,-17.36,;5.6,-18.85,;4.14,-19.33,;2.8,-18.56,;1.47,-19.33,;1.47,-20.87,;2.8,-21.64,;4.14,-20.87,;5.6,-21.34,;6.51,-20.1,;8.05,-20.1,;8.82,-18.76,;8.82,-21.43,;8.42,-22.92,;9.91,-23.32,;10.31,-21.83,;4.91,-16.27,;3.43,-16.67,)|
Structure:
