Reaction Details |
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Target | cGMP-dependent 3',5'-cyclic phosphodiesterase |
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Ligand | BDBM50402940 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_885312 (CHEMBL2215175) |
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IC50 | >10000±n/a nM |
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Citation | Rzasa, RM; Hu, E; Rumfelt, S; Chen, N; Andrews, KL; Chmait, S; Falsey, JR; Zhong, W; Jones, AD; Porter, A; Louie, SW; Zhao, X; Treanor, JJ; Allen, JR Discovery of selective biaryl ethers as PDE10A inhibitors: improvement in potency and mitigation of Pgp-mediated efflux. Bioorg Med Chem Lett22:7371-5 (2012) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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cGMP-dependent 3',5'-cyclic phosphodiesterase |
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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
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BDBM50402940 |
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n/a |
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Name | BDBM50402940 |
Synonyms: | CHEMBL2206218 |
Type | Small organic molecule |
Emp. Form. | C23H24N6O2 |
Mol. Mass. | 416.4757 |
SMILES | OCC1CCN(CC1)c1nccnc1Oc1ccc(Nc2nc3ccccc3[nH]2)cc1 |
Structure |
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