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Target
cGMP-dependent 3',5'-cyclic phosphodiesterase
Ligand
BDBM50059061
Substrate
n/a
Meas. Tech.
ChEMBL_156304 (CHEMBL760825)
IC50
3100±n/a nM
Citation
Ahn, HS; Bercovici, A; Boykow, G; Bronnenkant, A; Chackalamannil, S; Chow, J; Cleven, R; Cook, J; Czarniecki, M; Domalski, C; Fawzi, A; Green, M; Gündes, A; Ho, G; Laudicina, M; Lindo, N; Ma, K; Manna, M; McKittrick, B; Mirzai, B; Nechuta, T; Neustadt, B; Puchalski, C; Pula, K; Zhang, H Potent tetracyclic guanine inhibitors of PDE1 and PDE5 cyclic guanosine monophosphate phosphodiesterases with oral antihypertensive activity. J Med Chem 40:2196-210 (1997) [PubMed] Article
More Info.:
Target
Name:
cGMP-dependent 3',5'-cyclic phosphodiesterase
Synonyms:
PDE2A | PDE2A_BOVIN | Phosphodiesterase 2A
Type:
PROTEIN
Mol. Mass.:
103200.18
Organism:
Bos taurus
Description:
ChEMBL_154420
Residue:
921
Sequence:
MRRQPAASRDLFAQEPVPPGSGDGALQDALLSLGSVIDVAGLQQAVKEALSAVLPKVETVYTYLLDGESRLVCEEPPHELPQEGKVREAVISRKRLGCNGLGPSDLPGKPLARLVAPLAPDTQVLVIPLVDKEAGAVAAVILVHCGQLSDNEEWSLQAVEKHTLVALKRVQALQQRESSVAPEATQNPPEEAAGDQKGGVAYTNQDRKILQLCGELYDLDASSLQLKVLQYLQQETQASRCCLLLVSEDNLQLSCKVIGDKVLEEEISFPLTTGRLGQVVEDKKSIQLKDLTSEDMQQLQSMLGCEVQAMLCVPVISRATDQVVALACAFNKLGGDLFTDQDEHVIQHCFHYTSTVLTSTLAFQKEQKLKCECQALLQVAKNLFTHLDDVSVLLQEIITEARNLSNAEICSVFLLDQNELVAKVFDGGVVEDESYEIRIPADQGIAGHVATTGQILNIPDAYAHPLFYRGVDDSTGFRTRNILCFPIKNENQEVIGVAELVNKINGPWFSKFDEDLATAFSIYCGISIAHSLLYKKVNEAQYRSHLANEMMMYHMKVSDDEYTKLLHDGIQPVAAIDSNFASFTYTPRSLPEDDTSMAILSMLQDMNFINNYKIDCPTLARFCLMVKKGYRDPPYHNWMHAFSVSHFCYLLYKNLELTNYLEDMEIFALFISCMCHDLDHRGTNNSFQVASKSVLAALYSSEGSVMERHHFAQAIAILNTHGCNIFDHFSRKDYQRMLDLMRDIILATDLAHHLRIFKDLQKMAEVGYDRTNKQHHSLLLCLLMTSCDLSDQTKGWKTTRKIAELIYKEFFSQGDLEKAMGNRPMEMMDREKAYIPELQISFMEHIAMPIYKLLQDLFPKAAELYERVASNREHWTKVSHKFTIRGLPSNNSLDFLDEEYEVPDLDGARAPINGCCSLDAE
Inhibitor
Name:
BDBM50059061
Synonyms:
(6aR,9aS)-5,6a,7,8,9,9a-Hexahydro-5-methyl-2-(phenylethynyl)-3-(phenylmethyl)cyclopent[4,5]imidazo[2,1-b]purin-4(3H)-one | CHEMBL305618
Type:
Small organic molecule
Emp. Form.:
C26H23N5O
Mol. Mass.:
421.4937
SMILES:
CN1C2=N[C@@H]3CCC[C@@H]3N2c2nc(C#Cc3ccccc3)n(Cc3ccccc3)c2C1=O |t:2|