Target
High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A
Ligand
BDBM50397842
Substrate
n/a
Meas. Tech.
ChEMBL_876339 (CHEMBL2185813)
IC50
6.3±n/a nM
Citation
 Verhoest, PRFonseca, KRHou, XProulx-Lafrance, CCorman, MHelal, CJClaffey, MMTuttle, JBCoffman, KJLiu, SNelson, FKleiman, RJMenniti, FSSchmidt, CJVanase-Frawley, MLiras, 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 
Target
Name:
High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A
Synonyms:
3',5'-cyclic phosphodiesterase | PDE9A | PDE9A_HUMAN | Phosphodiesterase 9A | Phosphodiesterase 9A (PDE9) | Phosphodiesterase 9A (PDE9A)
Type:
Protein
Mol. Mass.:
68488.40
Organism:
Homo sapiens (Human)
Description:
O76083
Residue:
593
Sequence:
MGSGSSSYRPKAIYLDIDGRIQKVIFSKYCNSSDIMDLFCIATGLPRNTTISLLTTDDAMVSIDPTMPANSERTPYKVRPVAIKQLSAGVEDKRTTSRGQSAERPLRDRRVVGLEQPRREGAFESGQVEPRPREPQGCYQEGQRIPPEREELIQSVLAQVAEQFSRAFKINELKAEVANHLAVLEKRVELEGLKVVEIEKCKSDIKKMREELAARSSRTNCPCKYSFLDNHKKLTPRRDVPTYPKYLLSPETIEALRKPTFDVWLWEPNEMLSCLEHMYHDLGLVRDFSINPVTLRRWLFCVHDNYRNNPFHNFRHCFCVAQMMYSMVWLCSLQEKFSQTDILILMTAAICHDLDHPGYNNTYQINARTELAVRYNDISPLENHHCAVAFQILAEPECNIFSNIPPDGFKQIRQGMITLILATDMARHAEIMDSFKEKMENFDYSNEEHMTLLKMILIKCCDISNEVRPMEVAEPWVDCLLEEYFMQSDREKSEGLPVAPFMDRDKVTKATAQIGFIKFVLIPMFETVTKLFPMVEEIMLQPLWESRDRYEELKRIDDAMKELQKKTDSLTSGATEKSRERSRDVKNSEGDCA
  
Inhibitor
Name:
BDBM50397842
Synonyms:
CHEMBL2179101
Type:
Small organic molecule
Emp. Form.:
C21H26N6O2
Mol. Mass.:
394.4701
SMILES:
C[C@@H]1CN(Cc2ccccn2)C[C@H]1c1nc2n(ncc2c(=O)[nH]1)C1CCOCC1 |r|
Structure:
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