| Reaction Details |
|---|
 | Report a problem with these data |
| Target | cGMP-dependent 3',5'-cyclic phosphodiesterase |
|---|
| Ligand | BDBM50166893 |
|---|
| Substrate/Competitor | n/a |
|---|
| Meas. Tech. | ChEMBL_1690400 (CHEMBL4040970) |
|---|
| IC50 | 0.860000±n/a nM |
|---|
| Citation |  Mikami, S; Sasaki, S; Asano, Y; Ujikawa, O; Fukumoto, S; Nakashima, K; Oki, H; Kamiguchi, N; Imada, H; Iwashita, H; Taniguchi, T Discovery of an Orally Bioavailable, Brain-Penetrating, in Vivo Active Phosphodiesterase 2A Inhibitor Lead Series for the Treatment of Cognitive Disorders. J Med Chem60:7658-7676 (2017) [PubMed] Article |
|---|
| More Info.: | Get all data from this article, Assay Method |
|---|
| |
| cGMP-dependent 3',5'-cyclic phosphodiesterase |
|---|
| 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: | MGQACGHSILCRSQQYPAARPAEPRGQQVFLKPDEPPPPPQPCADSLQDALLSLGSVIDI
SGLQRAVKEALSAVLPRVETVYTYLLDGESQLVCEDPPHELPQEGKVREAIISQKRLGCN
GLGFSDLPGKPLARLVAPLAPDTQVLVMPLADKEAGAVAAVILVHCGQLSDNEEWSLQAV
EKHTLVALRRVQVLQQRGPREAPRAVQNPPEGTAEDQKGGAAYTDRDRKILQLCGELYDL
DASSLQLKVLQYLQQETRASRCCLLLVSEDNLQLSCKVIGDKVLGEEVSFPLTGCLGQVV
EDKKSIQLKDLTSEDVQQLQSMLGCELQAMLCVPVISRATDQVVALACAFNKLEGDLFTD
EDEHVIQHCFHYTSTVLTSTLAFQKEQKLKCECQALLQVAKNLFTHLDDVSVLLQEIITE
ARNLSNAEICSVFLLDQNELVAKVFDGGVVDDESYEIRIPADQGIAGHVATTGQILNIPD
AYAHPLFYRGVDDSTGFRTRNILCFPIKNENQEVIGVAELVNKINGPWFSKFDEDLATAF
SIYCGISIAHSLLYKKVNEAQYRSHLANEMMMYHMKVSDDEYTKLLHDGIQPVAAIDSNF
ASFTYTPRSLPEDDTSMAILSMLQDMNFINNYKIDCPTLARFCLMVKKGYRDPPYHNWMH
AFSVSHFCYLLYKNLELTNYLEDIEIFALFISCMCHDLDHRGTNNSFQVASKSVLAALYS
SEGSVMERHHFAQAIAILNTHGCNIFDHFSRKDYQRMLDLMRDIILATDLAHHLRIFKDL
QKMAEVGYDRNNKQHHRLLLCLLMTSCDLSDQTKGWKTTRKIAELIYKEFFSQGDLEKAM
GNRPMEMMDREKAYIPELQISFMEHIAMPIYKLLQDLFPKAAELYERVASNREHWTKVSH
KFTIRGLPSNNSLDFLDEEYEVPDLDGTRAPINGCCSLDAE
|
|
|
|---|
| BDBM50166893 |
|---|
| n/a |
|---|
| Name | BDBM50166893 |
|---|
| Synonyms: | 2-(3,4-Dimethoxy-benzyl)-7-[(R)-1-((R)-1-hydroxy-ethyl)-4-phenyl-butyl]-5-methyl-3H-imidazo[5,1-f][1,2,4]triazin-4-one | BAY-60-7550 | CHEMBL370962 | US10105349, Bay 60-7550 | US10543194, Example Bay 60-7550 | US11419874, BAY 60-7550 |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C27H32N4O4 |
|---|
| Mol. Mass. | 476.5674 |
|---|
| SMILES | COc1ccc(Cc2nn3c(nc(C)c3c(=O)[nH]2)[C@@H](CCCc2ccccc2)[C@@H](C)O)cc1OC |
|---|
| Structure | 
|
|---|
Search and Browse
