Reaction Details
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cGMP-dependent 3',5'-cyclic phosphodiesterase [574-941]
Ligand
BDBM14361
Substrate
BDBM10851
Meas. Tech.
Phosphodiesterase (PDE) Inhibition Assay
pH
7.5000±n/a
Temperature
303.1500±n/a K
IC50
>200000±n/a nM
Citation
Card, GL; England, BP; Suzuki, Y; Fong, D; Powell, B; Lee, B; Luu, C; Tabrizizad, M; Gillette, S; Ibrahim, PN; Artis, DR; Bollag, G; Milburn, MV; Kim, SH; Schlessinger, J; Zhang, KY Structural basis for the activity of drugs that inhibit phosphodiesterases. Structure 12:2233-47 (2004) [PubMed] Article More Info.:
Target
Name:
cGMP-dependent 3',5'-cyclic phosphodiesterase [574-941]
Synonyms:
PDE2A_HUMAN | PDE2A | CGS-PDE | Cyclic GMP-stimulated phosphodiesterase | cGMP-dependent 3,5-cyclic phosphodiesterase | cGSPDE | Phosphodiesterase Type 2 (PDE2A)
Type:
Enzyme
Mol. Mass.:
42724.46
Organism:
Human
Description:
Recombinant catalytic domain (H574-E941) of human PDE2A.
Residue:
368
Sequence:
HMKVSDDEYTKLLHDGIQPVAAIDSNFASFTYTPRSLPEDDTSMAILSMLQDMNFINNYKIDCPTLARFCLMVKKGYRDPPYHNWMHAFSVSHFCYLLYKNLELTNYLEDIEIFALFISCMCHDLDHRGTNNSFQVASKSVLAALYSSEGSVMERHHFAQAIAILNTHGCNIFDHFSRKDYQRMLDLMRDIILATDLAHHLRIFKDLQKMAEVGYDRNNKQHHRLLLCLLMTSCDLSDQTKGWKTTRKIAELIYKEFFSQGDLEKAMGNRPMEMMDREKAYIPELQISFMEHIAMPIYKLLQDLFPKAAELYERVASNREHWTKVSHKFTIRGLPSNNSLDFLDEEYEVPDLDGTRAPINGCCSLDAE
Inhibitor
Name:
BDBM14361
Synonyms:
Adeo | 4-(3-cyclopentyloxy-4-methoxy-phenyl)pyrrolidin-2-one | (R,S)-Rolipram | 4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrrolidin-2-one | CHEMBL63 | Rolipram
Type:
Small organic molecule
Emp. Form.:
C16H21NO3
Mol. Mass.:
275.15
SMILES:
COc1ccc(cc1OC2CCCC2)[C@H]3CC(=O)NC3
Substrate
Name:
BDBM10851
Synonyms:
(4aR,6R,7R,7aS)-6-(6-amino-9H-purin-9-yl)tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinine-2,7-diol 2-oxide | cid_23902375 | Cyclic adenosine monophosphate | (4aR,6R,7R,7aS)-6-(6-amino-9H-purin-9-yl)-2,7-dihydroxy-hexahydro-1,3,5,2-furo[3,2-d][1,3,2]dioxaphosphinin-2-one | ADENOSINE-3 ,5 -CYCLIC-MONOPHOSPHATE | cAMP
Type:
Small organic molecule
Emp. Form.:
C10H12N5O6P
Mol. Mass.:
329.05
SMILES:
Nc1ncnc2n(cnc12)[C@@H]1O[C@@H]2COP(O)(=O)O[C@H]2[C@H]1O

