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Target
Isoform 4 of cAMP-specific 3',5'-cyclic phosphodiesterase 4A (RD1)
Ligand
BDBM285551
Substrate
n/a
Meas. Tech.
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays
IC50
5.04±n/a nM
Citation
 Chappie, TA; Patel, NC; Hayward, MM; Helal, CJ; Sciabola, S; LaChapelle, EA; Young, JM; Verhoest, 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:
BDBM285551
Synonyms:
4-[2-(azetidin-1-ylcarbonyl)imidazo[1,2-b]pyridazin-3-yl]-2,5-difluorobenzonitrile | US10077269, Example 24 | US10669279, Example 24 | US9598421, Example 24
Type:
Small organic molecule
Emp. Form.:
C17H11F2N5O
Mol. Mass.:
339.2989
SMILES:
Fc1cc(-c2c(nc3cccnn23)C(=O)N2CCC2)c(F)cc1C#N |(-2.3,-23.34,;-3.79,-23.74,;-4.19,-25.23,;-5.68,-25.62,;-6.08,-27.11,;-5.17,-28.36,;-6.08,-29.6,;-7.54,-29.13,;-8.87,-29.9,;-10.21,-29.13,;-10.21,-27.59,;-8.87,-26.82,;-7.54,-27.59,;-3.63,-28.36,;-2.86,-27.02,;-2.86,-29.69,;-3.26,-31.18,;-1.77,-31.58,;-1.37,-30.09,;-6.77,-24.54,;-8.25,-24.93,;-6.37,-23.05,;-4.88,-22.65,;-4.48,-21.16,;-4.16,-19.66,)|
Structure:
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