Target
Isoform 4 of cAMP-specific 3',5'-cyclic phosphodiesterase 4A (RD1)
Ligand
BDBM285628
Substrate
n/a
Meas. Tech.
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays
IC50
26.6±n/a nM
Citation
 Chappie, TAPatel, NCHayward, MMHelal, CJSciabola, SLaChapelle, EAYoung, JMVerhoest, PR Imidazopyridazine compounds US Patent  US10077269 Publication Date 9/18/2018 
Target
Name:
Isoform 4 of cAMP-specific 3',5'-cyclic phosphodiesterase 4A (RD1)
Synonyms:
DPDE2 | PDE4A | PDE4A1 | PDE4A_HUMAN | Phosphodiesterase 4A (PDE4A1) | Phosphodiesterase 4A1 | cAMP-specific 3',5'-cyclic phosphodiesterase 4A (RD1) | cAMP-specific 3',5'-cyclic phosphodiesterase 4A Isoform 4
Type:
Enzyme Catalytic Domain
Mol. Mass.:
72186.86
Organism:
Homo sapiens (Human)
Description:
P27815-4
Residue:
647
Sequence:
MPLVDFFCETCSKPWLVGWWDQFKRMLNRELTHLSEMSRSGNQVSEYISTTFLDKQNEVEIPSPTMKEREKQQAPRPRPSQPPPPPVPHLQPMSQITGLKKLMHSNSLNNSNIPRFGVKTDQEELLAQELENLNKWGLNIFCVSDYAGGRSLTCIMYMIFQERDLLKKFRIPVDTMVTYMLTLEDHYHADVAYHNSLHAADVLQSTHVLLATPALDAVFTDLEILAALFAAAIHDVDHPGVSNQFLINTNSELALMYNDESVLENHHLAVGFKLLQEDNCDIFQNLSKRQRQSLRKMVIDMVLATDMSKHMTLLADLKTMVETKKVTSSGVLLLDNYSDRIQVLRNMVHCADLSNPTKPLELYRQWTDRIMAEFFQQGDRERERGMEISPMCDKHTASVEKSQVGFIDYIVHPLWETWADLVHPDAQEILDTLEDNRDWYYSAIRQSPSPPPEEESRGPGHPPLPDKFQFELTLEEEEEEEISMAQIPCTAQEALTAQGLSGVEEALDATIAWEASPAQESLEVMAQEASLEAELEAVYLTQQAQSTGSAPVAPDEFSSREEFVVAVSHSSPSALALQSPLLPAWRTLSVSEHAPGLPGLPSTAAEVEAQREHQAAKRACSACAGTFGEDTSALPAPGGGGSGGDPT
  
Inhibitor
Name:
BDBM285628
Synonyms:
3-(4-cyano-5-fluoro-2-methyl-phenyl)-N-ethylimidazo[1,2-b]pyridazine-2-carboxamide | US10077269, Example 98 | US10669279, Example 98 | US9598421, Example 98
Type:
Small organic molecule
Emp. Form.:
C17H14FN5O
Mol. Mass.:
323.3244
SMILES:
CCNC(=O)c1nc2cccnn2c1-c1cc(F)c(cc1C)C#N |(4.83,-5.68,;4.06,-4.34,;2.52,-4.34,;1.75,-3.01,;2.52,-1.67,;.21,-3.01,;-.7,-4.25,;-2.16,-3.78,;-3.49,-4.55,;-4.83,-3.78,;-4.83,-2.24,;-3.49,-1.47,;-2.16,-2.24,;-.7,-1.76,;-.3,-.27,;1.19,.12,;1.59,1.61,;3.08,2.01,;.49,2.8,;-.99,2.3,;-1.39,.81,;-2.87,.42,;.87,4.29,;1.25,5.78,)|
Structure:
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