Target
cGMP-dependent 3',5'-cyclic phosphodiesterase
Ligand
BDBM284764
Substrate
n/a
Meas. Tech.
IMAP TR-FRET Assay
IC50
5.90±n/a nM
Citation
 Hoenke, CBertani, BFerrara, MFossati, GFrattini, SGiovannini, RHobson, S Cyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxyamide US Patent  US10479794 Publication Date 11/19/2019 
Target
Name:
cGMP-dependent 3',5'-cyclic phosphodiesterase
Synonyms:
CGS-PDE | Cyclic GMP-stimulated phosphodiesterase | Homo sapiens phosphodiesterase 2A (PDE2A) | NM_002599 | PDE2A | PDE2A_HUMAN | cGSPDE
Type:
Enzyme Catalytic Domain
Mol. Mass.:
105691.58
Organism:
Homo sapiens (Human)
Description:
O00408
Residue:
941
Sequence:
MGQACGHSILCRSQQYPAARPAEPRGQQVFLKPDEPPPPPQPCADSLQDALLSLGSVIDISGLQRAVKEALSAVLPRVETVYTYLLDGESQLVCEDPPHELPQEGKVREAIISQKRLGCNGLGFSDLPGKPLARLVAPLAPDTQVLVMPLADKEAGAVAAVILVHCGQLSDNEEWSLQAVEKHTLVALRRVQVLQQRGPREAPRAVQNPPEGTAEDQKGGAAYTDRDRKILQLCGELYDLDASSLQLKVLQYLQQETRASRCCLLLVSEDNLQLSCKVIGDKVLGEEVSFPLTGCLGQVVEDKKSIQLKDLTSEDVQQLQSMLGCELQAMLCVPVISRATDQVVALACAFNKLEGDLFTDEDEHVIQHCFHYTSTVLTSTLAFQKEQKLKCECQALLQVAKNLFTHLDDVSVLLQEIITEARNLSNAEICSVFLLDQNELVAKVFDGGVVDDESYEIRIPADQGIAGHVATTGQILNIPDAYAHPLFYRGVDDSTGFRTRNILCFPIKNENQEVIGVAELVNKINGPWFSKFDEDLATAFSIYCGISIAHSLLYKKVNEAQYRSHLANEMMMYHMKVSDDEYTKLLHDGIQPVAAIDSNFASFTYTPRSLPEDDTSMAILSMLQDMNFINNYKIDCPTLARFCLMVKKGYRDPPYHNWMHAFSVSHFCYLLYKNLELTNYLEDIEIFALFISCMCHDLDHRGTNNSFQVASKSVLAALYSSEGSVMERHHFAQAIAILNTHGCNIFDHFSRKDYQRMLDLMRDIILATDLAHHLRIFKDLQKMAEVGYDRNNKQHHRLLLCLLMTSCDLSDQTKGWKTTRKIAELIYKEFFSQGDLEKAMGNRPMEMMDREKAYIPELQISFMEHIAMPIYKLLQDLFPKAAELYERVASNREHWTKVSHKFTIRGLPSNNSLDFLDEEYEVPDLDGTRAPINGCCSLDAE
  
Inhibitor
Name:
BDBM284764
Synonyms:
US10023575, Example 55 | US10023575, Example 83a | US10023575, Example 83b | US10023575, Example 84a | US10023575, Example 84b | US10479794, Example 84b | US10875867, Example 55 | US11691977, Example 55
Type:
Small organic molecule
Emp. Form.:
C21H20F4N4O3
Mol. Mass.:
452.4021
SMILES:
Cc1cnc2c(cnn2c1)C(=O)NC1(CCOCC1(C)O)c1ccc(cc1F)C(F)(F)F
Structure:
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