Reaction Details |
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Target | cGMP-specific 3',5'-cyclic phosphodiesterase |
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Ligand | BDBM50318143 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_632175 (CHEMBL1106508) |
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IC50 | 3.3±n/a nM |
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Citation | Tollefson, MB; Acker, BA; Jacobsen, EJ; Hughes, RO; Walker, JK; Fox, DN; Palmer, MJ; Freeman, SK; Yu, Y; Bond, BR 1-(2-(2,2,2-trifluoroethoxy)ethyl-1H-pyrazolo[4,3-d]pyrimidines as potent phosphodiesterase 5 (PDE5) inhibitors. Bioorg Med Chem Lett20:3125-8 (2010) [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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BDBM50318143 |
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n/a |
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Name | BDBM50318143 |
Synonyms: | 3-ethyl-N-(4-methylpyridin-2-yl)-5-(piperazin-1-yl)-1-(2-(2,2,2-trifluoroethoxy)ethyl)-1H-pyrazolo[4,3-d]pyrimidin-7-amine | CHEMBL1095405 |
Type | Small organic molecule |
Emp. Form. | C21H27F3N8O |
Mol. Mass. | 464.4873 |
SMILES | CCc1nn(CCOCC(F)(F)F)c2c(Nc3cc(C)ccn3)nc(nc12)N1CCNCC1 |
Structure |
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