Reaction Details |
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Target | Dual specificity calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C |
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Ligand | BDBM50397844 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_876338 (CHEMBL2185812) |
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IC50 | 165±n/a nM |
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Citation | Verhoest, PR; Fonseca, KR; Hou, X; Proulx-Lafrance, C; Corman, M; Helal, CJ; Claffey, MM; Tuttle, JB; Coffman, KJ; Liu, S; Nelson, F; Kleiman, RJ; Menniti, FS; Schmidt, CJ; Vanase-Frawley, M; Liras, S Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disorders. J Med Chem55:9045-54 (2012) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Dual specificity calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C |
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Name: | Dual specificity calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C |
Synonyms: | 3',5'-cyclic-AMP phosphodiesterase | 3',5'-cyclic-GMP phosphodiesterase | Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C | Cam-PDE 1C | Hcam3 | PDE1C | PDE1C_HUMAN | Phosphodiesterase 1 | Phosphodiesterase 1C | Phosphodiesterase, PDE1/PDE5 |
Type: | Enzyme |
Mol. Mass.: | 80778.58 |
Organism: | Homo sapiens (Human) |
Description: | Q14123 |
Residue: | 709 |
Sequence: | MESPTKEIEEFESNSLKYLQPEQIEKIWLRLRGLRKYKKTSQRLRSLVKQLERGEASVVD
LKKNLEYAATVLESVYIDETRRLLDTEDELSDIQSDAVPSEVRDWLASTFTRQMGMMLRR
SDEKPRFKSIVHAVQAGIFVERMYRRTSNMVGLSYPPAVIEALKDVDKWSFDVFSLNEAS
GDHALKFIFYELLTRYDLISRFKIPISALVSFVEALEVGYSKHKNPYHNLMHAADVTQTV
HYLLYKTGVANWLTELEIFAIIFSAAIHDYEHTGTTNNFHIQTRSDPAILYNDRSVLENH
HLSAAYRLLQDDEEMNILINLSKDDWREFRTLVIEMVMATDMSCHFQQIKAMKTALQQPE
AIEKPKALSLMLHTADISHPAKAWDLHHRWTMSLLEEFFRQGDREAELGLPFSPLCDRKS
TMVAQSQVGFIDFIVEPTFTVLTDMTEKIVSPLIDETSQTGGTGQRRSSLNSISSSDAKR
SGVKTSGSEGSAPINNSVISVDYKSFKATWTEVVHINRERWRAKVPKEEKAKKEAEEKAR
LAAEEQQKEMEAKSQAEEGASGKAEKKTSGETKNQVNGTRANKSDNPRGKNSKAEKSSGE
QQQNGDFKDGKNKTDKKDHSNIGNDSKKTDGTKQRSHGSPAPSTSSTCRLTLPVIKPPLR
HFKRPAYASSSYAPSVSKKTDEHPARYKMLDQRIKMKKIQNISHNWNRK
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BDBM50397844 |
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n/a |
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Name | BDBM50397844 |
Synonyms: | CHEMBL2179099 |
Type | Small organic molecule |
Emp. Form. | C22H26FN5O2 |
Mol. Mass. | 411.4725 |
SMILES | C[C@@H]1CN(Cc2ccc(F)cc2)C[C@H]1c1nc2n(ncc2c(=O)[nH]1)C1CCOCC1 |r| |
Structure |
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