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Target
Dual specificity calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C
Ligand
BDBM50300099
Substrate
n/a
Meas. Tech.
ChEMBL_876338 (CHEMBL2185812)
IC50
0.400000±n/a nM
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 Chem 55:9045-54 (2012) [PubMed] Article
More Info.:
Target
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:
Human
Description:
Q14123
Residue:
709
Sequence:
MESPTKEIEEFESNSLKYLQPEQIEKIWLRLRGLRKYKKTSQRLRSLVKQLERGEASVVDLKKNLEYAATVLESVYIDETRRLLDTEDELSDIQSDAVPSEVRDWLASTFTRQMGMMLRRSDEKPRFKSIVHAVQAGIFVERMYRRTSNMVGLSYPPAVIEALKDVDKWSFDVFSLNEASGDHALKFIFYELLTRYDLISRFKIPISALVSFVEALEVGYSKHKNPYHNLMHAADVTQTVHYLLYKTGVANWLTELEIFAIIFSAAIHDYEHTGTTNNFHIQTRSDPAILYNDRSVLENHHLSAAYRLLQDDEEMNILINLSKDDWREFRTLVIEMVMATDMSCHFQQIKAMKTALQQPEAIEKPKALSLMLHTADISHPAKAWDLHHRWTMSLLEEFFRQGDREAELGLPFSPLCDRKSTMVAQSQVGFIDFIVEPTFTVLTDMTEKIVSPLIDETSQTGGTGQRRSSLNSISSSDAKRSGVKTSGSEGSAPINNSVISVDYKSFKATWTEVVHINRERWRAKVPKEEKAKKEAEEKARLAAEEQQKEMEAKSQAEEGASGKAEKKTSGETKNQVNGTRANKSDNPRGKNSKAEKSSGEQQQNGDFKDGKNKTDKKDHSNIGNDSKKTDGTKQRSHGSPAPSTSSTCRLTLPVIKPPLRHFKRPAYASSSYAPSVSKKTDEHPARYKMLDQRIKMKKIQNISHNWNRK
Inhibitor
Name:
BDBM50300099
Synonyms:
6-benzyl-1-cyclopentyl-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one | 6-benzyl-1-cyclopentyl-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one | CHEMBL572934
Type:
Small organic molecule
Emp. Form.:
C17H18N4O
Mol. Mass.:
294.351
SMILES:
O=c1[nH]c(Cc2ccccc2)nc2n(ncc12)C1CCCC1