Target
Isoform 4 of cAMP-specific 3',5'-cyclic phosphodiesterase 4A (RD1)
Ligand
BDBM285595
Substrate
n/a
Meas. Tech.
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays
IC50
10.6±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:
BDBM285595
Synonyms:
3-(4-chloro-2-fluorophenyl)-N-[(1R,2S)-2-fluorocyclopro-pyl]imidazo[1,2-b]pyridazine-2-carboxamide | US10077269, Example 68 | US10669279, Example 68 | US9598421, Example 68
Type:
Small organic molecule
Emp. Form.:
C16H11ClF2N4O
Mol. Mass.:
348.735
SMILES:
F[C@H]1C[C@H]1NC(=O)c1nc2cccnn2c1-c1ccc(Cl)cc1F |r,wU:3.4,1.0,(5.5,-1.78,;4.73,-3.11,;4.73,-4.65,;3.39,-3.88,;1.85,-3.88,;1.08,-2.55,;1.85,-1.21,;-.46,-2.55,;-1.36,-3.79,;-2.83,-3.32,;-4.16,-4.09,;-5.5,-3.32,;-5.5,-1.78,;-4.16,-1.01,;-2.83,-1.78,;-1.36,-1.3,;-.96,.19,;.52,.59,;.92,2.07,;-.17,3.16,;.23,4.65,;-1.66,2.76,;-2.05,1.28,;-3.54,.88,)|
Structure:
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