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Target
Isoform 4 of cAMP-specific 3',5'-cyclic phosphodiesterase 4A (RD1)
Ligand
BDBM285612
Substrate
n/a
Meas. Tech.
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays
IC50
12.0±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:
BDBM285612
Synonyms:
3-(4-chloro-3-fluorophenyl)-N-(1H-pyrazol-4-yl)imidazo[1,2-b]pyridazine-2-carboxamide | US10077269, Example 82 | US10669279, Example 82 | US9598421, Example 82
Type:
Small organic molecule
Emp. Form.:
C16H10ClFN6O
Mol. Mass.:
356.742
SMILES:
Fc1cc(ccc1Cl)-c1c(nc2cccnn12)C(=O)Nc1cn[nH]c1
Structure:
Search PDB for entries with ligand similarity: