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TargetO43924/P16499/P18545/P35913/P51160/Q13956
LigandBDBM50193586
Substrate/Competitorn/a
Meas. Tech.ChEMBL_387456 (CHEMBL870381)
IC50 62±n/a nM
Citation Giovannoni, MP; Vergelli, C; Biancalani, C; Cesari, N; Graziano, A; Biagini, P; Gracia, J; Gavaldà, A; Dal Piaz, V Novel pyrazolopyrimidopyridazinones with potent and selective phosphodiesterase 5 (PDE5) inhibitory activity as potential agents for treatment of erectile dysfunction. J Med Chem49:5363-71 (2006) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
O43924/P16499/P18545/P35913/P51160/Q13956
Name:O43924/P16499/P18545/P35913/P51160/Q13956
Synonyms:Phosphodiesterase 6
Type:n/a
Mol. Mass.:n/a
Description:ASSAY_ID of ChEMBL is 387456
Components:This complex has 6 components.
Component 1
Name:Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma
Synonyms:CNRG_HUMAN | GMP-PDE gamma | PDE6G | PDEG
Type:PROTEIN
Mol. Mass.:9648.05
Organism:Homo sapiens (Human)
Description:ChEMBL_105761
Residue:87
Sequence:
MNLEPPKAEFRSATRVAGGPVTPRKGPPKFKQRQTRQFKSKPPKKGVQGFGDDIPGMEGL
GTDITVICPWEAFNHLELHELAQYGII
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Component 2
Name:Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit delta
Synonyms:3',5'-cyclic phosphodiesterase | GMP-PDE delta | PDE6D | PDE6D_HUMAN | PDED | Protein p17 | Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit delta
Type:PROTEIN
Mol. Mass.:17418.30
Organism:Homo sapiens (Human)
Description:ChEMBL_105761
Residue:150
Sequence:
MSAKDERAREILRGFKLNWMNLRDAETGKILWQGTEDLSVPGVEHEARVPKKILKCKAVS
RELNFSSTEQMEKFRLEQKVYFKGQCLEEWFFEFGFVIPNSTNTWQSLIEAAPESQMMPA
SVLTGNVIIETKFFDDDLLVSTSRVRLFYV
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Component 3
Name:Cone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha'
Synonyms:3',5'-cyclic phosphodiesterase | PDE6C | PDE6C_HUMAN | PDEA2 | Phosphodiesterase 6C | Phosphodiesterase 6C (PDE6C)
Type:Protein
Mol. Mass.:99132.02
Organism:Homo sapiens (Human)
Description:P51160
Residue:858
Sequence:
MGEINQVAVEKYLEENPQFAKEYFDRKLRVEVLGEIFKNSQVPVQSSMSFSELTQVEESA
LCLELLWTVQEEGGTPEQGVHRALQRLAHLLQADRCSMFLCRSRNGIPEVASRLLDVTPT
SKFEDNLVGPDKEVVFPLDIGIVGWAAHTKKTHNVPDVKKNSHFSDFMDKQTGYVTKNLL
ATPIVVGKEVLAVIMAVNKVNASEFSKQDEEVFSKYLNFVSIILRLHHTSYMYNIESRRS
QILMWSANKVFEELTDVERQFHKALYTVRSYLNCERYSIGLLDMTKEKEFYDEWPIKLGE
VEPYKGPKTPDGREVNFYKIIDYILHGKEEIKVIPTPPADHWTLISGLPTYVAENGFICN
MMNAPADEYFTFQKGPVDETGWVIKNVLSLPIVNKKEDIVGVATFYNRKDGKPFDEHDEY
ITETLTQFLGWSLLNTDTYDKMNKLENRKDIAQEMLMNQTKATPEEIKSILKFQEKLNVD
VIDDCEEKQLVAILKEDLPDPRSAELYEFRFSDFPLTEHGLIKCGIRLFFEINVVEKFKV
PVEVLTRWMYTVRKGYRAVTYHNWRHGFNVGQTMFTLLMTGRLKKYYTDLEAFAMLAAAF
CHDIDHRGTNNLYQMKSTSPLARLHGSSILERHHLEYSKTLLQDESLNIFQNLNKRQFET
VIHLFEVAIIATDLALYFKKRTMFQKIVDACEQMQTEEEAIKYVTVDPTKKEIIMAMMMT
ACDLSAITKPWEVQSQVALMVANEFWEQGDLERTVLQQQPIPMMDRNKRDELPKLQVGFI
DFVCTFVYKEFSRFHKEITPMLSGLQNNRVEWKSLADEYDAKMKVIEEEAKKQEGGAEKA
AEDSGGGDDKKSKTCLML
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Component 4
Name:Retinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma
Synonyms:CNCG_HUMAN | GMP-PDE gamma | PDE6H
Type:PROTEIN
Mol. Mass.:9078.33
Organism:Homo sapiens (Human)
Description:ChEMBL_105761
Residue:83
Sequence:
MSDNTTLPAPASNQGPTTPRKGPPKFKQRQTRQFKSKPPKKGVKGFGDDIPGMEGLGTDI
TVICPWEAFSHLELHELAQFGII
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Component 5
Name:Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha
Synonyms:PDE6A | PDE6A_HUMAN | PDEA | Rod cGMP-specific 3',5'-cyclic phosphodiesterase alpha
Type:PROTEIN
Mol. Mass.:99531.10
Organism:Homo sapiens (Human)
Description:ChEMBL_1347866
Residue:860
Sequence:
MGEVTAEEVEKFLDSNIGFAKQYYNLHYRAKLISDLLGAKEAAVDFSNYHSPSSMEESEI
IFDLLRDFQENLQTEKCIFNVMKKLCFLLQADRMSLFMYRTRNGIAELATRLFNVHKDAV
LEDCLVMPDQEIVFPLDMGIVGHVAHSKKIANVPNTEEDEHFCDFVDILTEYKTKNILAS
PIMNGKDVVAIIMAVNKVDGSHFTKRDEEILLKYLNFANLIMKVYHLSYLHNCETRRGQI
LLWSGSKVFEELTDIERQFHKALYTVRAFLNCDRYSVGLLDMTKQKEFFDVWPVLMGEVP
PYSGPRTPDGREINFYKVIDYILHGKEDIKVIPNPPPDHWALVSGLPAYVAQNGLICNIM
NAPAEDFFAFQKEPLDESGWMIKNVLSMPIVNKKEEIVGVATFYNRKDGKPFDEMDETLM
ESLTQFLGWSVLNPDTYESMNKLENRKDIFQDIVKYHVKCDNEEIQKILKTREVYGKEPW
ECEEEELAEILQAELPDADKYEINKFHFSDLPLTELELVKCGIQMYYELKVVDKFHIPQE
ALVRFMYSLSKGYRKITYHNWRHGFNVGQTMFSLLVTGKLKRYFTDLEALAMVTAAFCHD
IDHRGTNNLYQMKSQNPLAKLHGSSILERHHLEFGKTLLRDESLNIFQNLNRRQHEHAIH
MMDIAIIATDLALYFKKRTMFQKIVDQSKTYESEQEWTQYMMLEQTRKEIVMAMMMTACD
LSAITKPWEVQSQVALLVAAEFWEQGDLERTVLQQNPIPMMDRNKADELPKLQVGFIDFV
CTFVYKEFSRFHEEITPMLDGITNNRKEWKALADEYDAKMKVQEEKKQKQQSAKSAAAGN
QPGGNPSPGGATTSKSCCIQ
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Component 6
Name:Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit beta
Synonyms:GMP-PDE beta | PDE6B | PDE6B_HUMAN | PDEB
Type:PROTEIN
Mol. Mass.:98308.48
Organism:Homo sapiens (Human)
Description:ChEMBL_105761
Residue:854
Sequence:
MSLSEEQARSFLDQNPDFARQYFGKKLSPENVAAACEDGCPPDCDSLRDLCQVEESTALL
ELVQDMQESINMERVVFKVLRRLCTLLQADRCSLFMYRQRNGVAELATRLFSVQPDSVLE
DCLVPPDSEIVFPLDIGVVGHVAQTKKMVNVEDVAECPHFSSFADELTDYKTKNMLATPI
MNGKDVVAVIMAVNKLNGPFFTSEDEDVFLKYLNFATLYLKIYHLSYLHNCETRRGQVLL
WSANKVFEELTDIERQFHKAFYTVRAYLNCERYSVGLLDMTKEKEFFDVWSVLMGESQPY
SGPRTPDGREIVFYKVIDYVLHGKEEIKVIPTPSADHWALASGLPSYVAESGFICNIMNA
SADEMFKFQEGALDDSGWLIKNVLSMPIVNKKEEIVGVATFYNRKDGKPFDEQDEVLMES
LTQFLGWSVMNTDTYDKMNKLENRKDIAQDMVLYHVKCDRDEIQLILPTRARLGKEPADC
DEDELGEILKEELPGPTTFDIYEFHFSDLECTELDLVKCGIQMYYELGVVRKFQIPQEVL
VRFLFSISKGYRRITYHNWRHGFNVAQTMFTLLMTGKLKSYYTDLEAFAMVTAGLCHDID
HRGTNNLYQMKSQNPLAKLHGSSILERHHLEFGKFLLSEETLNIYQNLNRRQHEHVIHLM
DIAIIATDLALYFKKRAMFQKIVDESKNYQDKKSWVEYLSLETTRKEIVMAMMMTACDLS
AITKPWEVQSKVALLVAAEFWEQGDLERTVLDQQPIPMMDRNKAAELPKLQVGFIDFVCT
FVYKEFSRFHEEILPMFDRLQNNRKEWKALADEYEAKVKALEEKEEEERVAAKKVGTEIC
NGGPAPKSSTCCIL
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BDBM50193586
n/a
NameBDBM50193586
Synonyms:7-benzyl-4-isopropyl-9-methyl-2-phenyl-7H-3,3a,5,7,8-pentaaza-cyclopenta[a]naphthalen-6-one | CHEMBL213060
TypeSmall organic molecule
Emp. Form.C25H23N5O
Mol. Mass.409.483
SMILESCC(C)c1nc2c(c(C)nn(Cc3ccccc3)c2=O)c2cc(nn12)-c1ccccc1
Structure
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