Reaction Details |
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Target | cGMP-specific 3',5'-cyclic phosphodiesterase |
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Ligand | BDBM50397838 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_876326 (CHEMBL2185800) |
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IC50 | >10000±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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cGMP-specific 3',5'-cyclic phosphodiesterase |
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Name: | cGMP-specific 3',5'-cyclic phosphodiesterase |
Synonyms: | 3',5'-cyclic phosphodiesterase | CGB-PDE | PDE5 | PDE5A | PDE5A_HUMAN | Phosphodiesterase 2 and 5 (PDE2 and PDE5) | Phosphodiesterase 5 (PDE5) | Phosphodiesterase 5A | Phosphodiesterase 5A (PDE5A) | cGMP-binding cGMP-specific phosphodiesterase | cGMP-specific 3',5'-cyclic phosphodiesterase |
Type: | Protein |
Mol. Mass.: | 99975.83 |
Organism: | Homo sapiens (Human) |
Description: | O76074 |
Residue: | 875 |
Sequence: | MERAGPSFGQQRQQQQPQQQKQQQRDQDSVEAWLDDHWDFTFSYFVRKATREMVNAWFAE
RVHTIPVCKEGIRGHTESCSCPLQQSPRADNSAPGTPTRKISASEFDRPLRPIVVKDSEG
TVSFLSDSEKKEQMPLTPPRFDHDEGDQCSRLLELVKDISSHLDVTALCHKIFLHIHGLI
SADRYSLFLVCEDSSNDKFLISRLFDVAEGSTLEEVSNNCIRLEWNKGIVGHVAALGEPL
NIKDAYEDPRFNAEVDQITGYKTQSILCMPIKNHREEVVGVAQAINKKSGNGGTFTEKDE
KDFAAYLAFCGIVLHNAQLYETSLLENKRNQVLLDLASLIFEEQQSLEVILKKIAATIIS
FMQVQKCTIFIVDEDCSDSFSSVFHMECEELEKSSDTLTREHDANKINYMYAQYVKNTME
PLNIPDVSKDKRFPWTTENTGNVNQQCIRSLLCTPIKNGKKNKVIGVCQLVNKMEENTGK
VKPFNRNDEQFLEAFVIFCGLGIQNTQMYEAVERAMAKQMVTLEVLSYHASAAEEETREL
QSLAAAVVPSAQTLKITDFSFSDFELSDLETALCTIRMFTDLNLVQNFQMKHEVLCRWIL
SVKKNYRKNVAYHNWRHAFNTAQCMFAALKAGKIQNKLTDLEILALLIAALSHDLDHRGV
NNSYIQRSEHPLAQLYCHSIMEHHHFDQCLMILNSPGNQILSGLSIEEYKTTLKIIKQAI
LATDLALYIKRRGEFFELIRKNQFNLEDPHQKELFLAMLMTACDLSAITKPWPIQQRIAE
LVATEFFDQGDRERKELNIEPTDLMNREKKNKIPSMQVGFIDAICLQLYEALTHVSEDCF
PLLDGCRKNRQKWQALAEQQEKMLINGESGQAKRN
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BDBM50397838 |
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n/a |
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Name | BDBM50397838 |
Synonyms: | CHEMBL2179105 | PF-04447943 | US10513524, Reference compound disclosed in WO2008/139293 | US11608342, Reference compound disclosed in WO2008/139293 |
Type | Small organic molecule |
Emp. Form. | C20H25N7O2 |
Mol. Mass. | 395.4582 |
SMILES | C[C@@H]1CN(Cc2ncccn2)C[C@H]1c1nc2n(ncc2c(=O)[nH]1)C1CCOCC1 |r| |
Structure |
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