Target
Isoform 4 of cAMP-specific 3',5'-cyclic phosphodiesterase 4A (RD1)
Ligand
BDBM285580
Substrate
n/a
Meas. Tech.
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays
IC50
17.8±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:
BDBM285580
Synonyms:
US10077269, Example 53 | US10669279, Example 53 | US9598421, Example 53 | azetidin-1-yl[3-(4-fluoro-3,5-dimethylphenyl)imidazo[1,2-b]pyridazin-2-yl]methanone
Type:
Small organic molecule
Emp. Form.:
C18H17FN4O
Mol. Mass.:
324.3522
SMILES:
Cc1cc(cc(C)c1F)-c1c(nc2cccnn12)C(=O)N1CCC1
Structure:
Search PDB for entries with ligand similarity: