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Target
Isoform 4 of cAMP-specific 3',5'-cyclic phosphodiesterase 4A (RD1)
Ligand
BDBM285539
Substrate
n/a
Meas. Tech.
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays
IC50
14.4±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:
BDBM285539
Synonyms:
3-(4-chloro-2-methyl-phenyl)-N-cyclopropyl-imidazo[1,2-b]pyridazine-2-carboxamide | US10077269, Example 12 | US10669279, Example 12 | US9598421, Example 12
Type:
Small organic molecule
Emp. Form.:
C17H15ClN4O
Mol. Mass.:
326.78
SMILES:
Cc1cc(Cl)ccc1-c1c(nc2cccnn12)C(=O)NC1CC1 |(2.81,-8.2,;4.3,-7.8,;4.7,-6.31,;6.19,-5.91,;6.58,-4.43,;7.27,-7,;6.88,-8.49,;5.39,-8.89,;4.99,-10.38,;5.89,-11.62,;4.99,-12.87,;3.52,-12.39,;2.19,-13.16,;.86,-12.39,;.86,-10.85,;2.19,-10.08,;3.52,-10.85,;7.44,-11.62,;8.21,-10.29,;8.21,-12.96,;9.75,-12.96,;11.08,-13.73,;11.08,-12.19,)|
Structure:
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