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Target
cGMP-dependent 3',5'-cyclic phosphodiesterase
Ligand
BDBM284771
Substrate
n/a
Meas. Tech.
IMAP TR-FRET Assay
IC50
63.0±n/a nM
Citation
 Hoenke, C; Bertani, B; Ferrara, M; Fossati, G; Frattini, S; Giovannini, R; Hobson, 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:
BDBM284771
Synonyms:
US10023575, Example 62 | US10023575, Example 91a | US10023575, Example 91b | US10479794, Example 91b | US10875867, Example 62 | US11691977, Example 62
Type:
Small organic molecule
Emp. Form.:
C23H23F4N5O3
Mol. Mass.:
493.454
SMILES:
Cc1nn2cc(cnc2c1C(=O)NC1(CCOCC1(C)O)c1ncc(cc1F)C(F)(F)F)C1CC1
Structure:
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