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Target
cGMP-dependent 3',5'-cyclic phosphodiesterase [574-941]
Ligand
BDBM14769
Substrate
BDBM10851
Meas. Tech.
Phosphodiesterase (PDE) Inhibition Assay
pH
7.5±n/a
Temperature
303.15±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:
CGS-PDE | Cyclic GMP-stimulated phosphodiesterase | PDE2A | PDE2A_HUMAN | Phosphodiesterase Type 2 (PDE2A) | cGMP-dependent 3,5-cyclic phosphodiesterase | cGSPDE
Type:
Enzyme
Mol. Mass.:
42724.46
Organism:
Homo sapiens (Human)
Description:
Recombinant catalytic domain (H574-E941) of human PDE2A.
Residue:
368
Sequence:
HMKVSDDEYTKLLHDGIQPVAAIDSNFASFTYTPRSLPEDDTSMAILSMLQDMNFINNYKIDCPTLARFCLMVKKGYRDPPYHNWMHAFSVSHFCYLLYKNLELTNYLEDIEIFALFISCMCHDLDHRGTNNSFQVASKSVLAALYSSEGSVMERHHFAQAIAILNTHGCNIFDHFSRKDYQRMLDLMRDIILATDLAHHLRIFKDLQKMAEVGYDRNNKQHHRLLLCLLMTSCDLSDQTKGWKTTRKIAELIYKEFFSQGDLEKAMGNRPMEMMDREKAYIPELQISFMEHIAMPIYKLLQDLFPKAAELYERVASNREHWTKVSHKFTIRGLPSNNSLDFLDEEYEVPDLDGTRAPINGCCSLDAE
Inhibitor
Name:
BDBM14769
Synonyms:
6-(3,4-Dimethoxy-phenyl)-4,5-dimethyl-4,5-dihydro-2H-pyridazin-3-one | 6-(4-(difluoromethoxy)-3-methoxyphenyl)pyridazin-3(2H)-one | 6-(4-Difluoromethoxy-3-methoxy-phenyl)-2H-pyridazin-3-one | 6-[4-(difluoromethoxy)-3-methoxyphenyl]-2,3-dihydropyridazin-3-one | CHEMBL313842 | Zaradaverine | Zardaverine
Type:
Small organic molecule
Emp. Form.:
C12H10F2N2O3
Mol. Mass.:
268.2162
SMILES:
COc1cc(ccc1OC(F)F)-c1ccc(=O)[nH]n1
Substrate
Name:
BDBM10851
Synonyms:
(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 | (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 | ADENOSINE-3 ,5 -CYCLIC-MONOPHOSPHATE | Cyclic adenosine monophosphate | cAMP | cid_23902375
Type:
Small organic molecule
Emp. Form.:
C10H12N5O6P
Mol. Mass.:
329.2059
SMILES:
Nc1ncnc2n(cnc12)[C@@H]1O[C@@H]2COP(O)(=O)O[C@H]2[C@H]1O