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TargetP04972/P11541/P16586/P22571/P23439/Q95142
LigandBDBM50166821
Substrate/Competitorn/a
Meas. Tech.ChEMBL_305227 (CHEMBL831646)
IC50 275±n/a nM
Citation Xia, GLi, JPeng, ALai, SZhang, SShen, JLiu, ZChen, XJi, R Synthesis and phosphodiesterase 5 inhibitory activity of novel pyrido[1,2-e]purin-4(3H)-one derivatives. Bioorg Med Chem Lett15:2790-4 (2005) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
P04972/P11541/P16586/P22571/P23439/Q95142
Name:P04972/P11541/P16586/P22571/P23439/Q95142
Synonyms:Phosphodiesterase 6
Type:n/a
Mol. Mass.:n/a
Description:ASSAY_ID of ChEMBL is 155381
Components:This complex has 6 components.
Component 1
Name:Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma
Synonyms:CNRG_BOVIN | GMP-PDE gamma | PDE6G | PDEG
Type:PROTEIN
Mol. Mass.:9674.16
Organism:Bos taurus
Description:ChEMBL_104859
Residue:87
Sequence:
MNLEPPKAEIRSATRVMGGPVTPRKGPPKFKQRQTRQFKSKPPKKGVQGFGDDIPGMEGL
GTDITVICPWEAFNHLELHELAQYGII
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Component 2
Name:Cone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha'
Synonyms:PDE V-C1 | PDE6C | PDE6C_BOVIN | PDEA2 | cGMP phosphodiesterase 6C
Type:PROTEIN
Mol. Mass.:98783.85
Organism:Bos taurus
Description:ChEMBL_104859
Residue:855
Sequence:
MGEISQETVEKYLEANPQFAKEYFNRKLQVEVPSGGAQAPASASFPGRTLAEEAALYLEL
LEVLLEEAGSVELAAHRALQRLAQLLQADRCSMFLCRARNGTPEVASKLLDVTPTSKFED
NLVVPDREAVFPLDVGIVGWVAHTKKTFNVPDVKKNSHFSDFMDKQTGYVTRNLLATPIV
MGKEVLAVFMAVNKVDASEFSKQDEEVFSKYLSFVSIILKLHHTNYLYNIESRRSQILMW
SANKVFEELTDVERQFHKALYTVRTYLNCERYSIGLLDMTKEKEFYDEWPVKLGEVEPYK
GPKTPDGREVIFYKIIDYILHGKEEIKVIPTPPMDHWTLISGLPTYVAENGFICNMLNAP
ADEYFTFQKGPVDETGWVIKNVLSLPIVNKKEDIVGVATFYNRKDGKPFDEYDEHIAETL
TQFLGWSLLNTDTYEKMNKLENRKDIAQEMLMNHTKATPDEIKSILKFKEKLNIDVIEDC
EEKQLVTILKEDLPDPRTADLYEFRFRHLPITEHELIKCGLRLFFEINVVEKFKVPVEVL
TRWMYTVRKGYRAVTYHNWRHGFNVGQTMFTLLMTGRLKKYYTDLEAFAMLAAAFCHDID
HRGTNNLYQMKSTSPLARLHGSSILERHHLEYSKTLLQDESLNIFQNLNKRQYETVIHLF
EVAIIATDLALYFKKRTMFQKIVDACEKMETEEEAIKYVTIDPTKKEIIMAMMMTACDLS
AITKPWEVQSQVALLVANEFWEQGDLERTVLQQQPIPMMDRNKKDELPKLQVGFIDFVCT
FVYKEFSRFHKEITPMLNGLQNNRVEWKSLADEYDEKMKVIEEMKKQEEGNTTEKAVEDS
GGGGDDKKSKTCLML
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Component 3
Name:Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha
Synonyms:PDE6A | PDE6A_BOVIN | PDEA | Phosphodiesterase 6 | Phosphodiesterase 6A
Type:Enzyme
Mol. Mass.:99320.22
Organism:Bos taurus (Bovine)
Description:P11541
Residue:859
Sequence:
MGEVTAEEVEKFLDSNVSFAKQYYNLRYRAKVISDLLGPREAAVDFSNYHALNSVEESEI
IFDLLRDFQDNLQAEKCVFNVMKKLCFLLQADRMSLFMYRARNGIAELATRLFNVHKDAV
LEECLVAPDSEIVFPLDMGVVGHVALSKKIVNVPNTEEDEHFCDFVDTLTEYQTKNILAS
PIMNGKDVVAIIMVVNKVDGPHFTENDEEILLKYLNFANLIMKVFHLSYLHNCETRRGQI
LLWSGSKVFEELTDIERQFHKALYTVRAFLNCDRYSVGLLDMTKQKEFFDVWPVLMGEAP
PYAGPRTPDGREINFYKVIDYILHGKEDIKVIPNPPPDHWALVSGLPTYVAQNGLICNIM
NAPSEDFFAFQKEPLDESGWMIKNVLSMPIVNKKEEIVGVATFYNRKDGKPFDEMDETLM
ESLTQFLGWSVLNPDTYELMNKLENRKDIFQDMVKYHVKCDNEEIQTILKTREVYGKEPW
ECEEEELAEILQGELPDADKYEINKFHFSDLPLTELELVKCGIQMYYELKVVDKFHIPQE
ALVRFMYSLSKGYRRITYHNWRHGFNVGQTMFSLLVTGKLKRYFTDLEALAMVTAAFCHD
IDHRGTNNLYQMKSQNPLAKLHGSSILERHHLEFGKTLLRDESLNIFQNLNRRQHEHAIH
MMDIAIIATDLALYFKKRTMFQKIVDQSKTYETQQEWTQYMMLDQTRKEIVMAMMMTACD
LSAITKPWEVQSKVALLVAAEFWEQGDLERTVLQQNPIPMMDRNKADELPKLQVGFIDFV
CTFVYKEFSRFHEEITPMLDGITNNRKEWKALADEYETKMKGLEEEKQKQQAANQAAAGS
QHGGKQPGGGPASKSCCVQ
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Component 4
Name:Retinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma
Synonyms:CNCG_BOVIN | GMP-PDE gamma | PDE6H
Type:PROTEIN
Mol. Mass.:9106.39
Organism:Bos taurus
Description:ChEMBL_104859
Residue:83
Sequence:
MSDNTVLAPPTSNQGPTTPRKGPPKFKQRQTRQFKSKPPKKGVKGFGDDIPGMEGLGTDI
TVICPWEAFSHLELHELAQFGII
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Component 5
Name:Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit delta
Synonyms:GMP-PDE delta | PDE6D | PDE6D_BOVIN
Type:PROTEIN
Mol. Mass.:17388.28
Organism:Bos taurus
Description:ChEMBL_104859
Residue:150
Sequence:
MSAKDERAREILRGFKLNWMNLRDAETGKILWQGTEDLSVPGVEHEARVPKKILKCKAVS
RELNFSSAEQMEKFRLEQKVYFKGQCLEEWFFEFGFVIPNSTNTWQSLIEAAPESQMMPA
SVLTGNVIIETKFFDDDLLVSTSRVRLFYV
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Component 6
Name:Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit beta
Synonyms:GMP-PDE beta | PDE6B | PDE6B_BOVIN | PDEB
Type:PROTEIN
Mol. Mass.:98307.54
Organism:Bos taurus
Description:ChEMBL_104859
Residue:853
Sequence:
MSLSEGQVHRFLDQNPGFADQYFGRKLSPEDVANACEDGCPEGCTSFRELCQVEESAALF
ELVQDMQENVNMERVVFKILRRLCSILHADRCSLFMYRQRNGVAELATRLFSVQPDSVLE
DCLVPPDSEIVFPLDIGVVGHVAQTKKMVNVQDVMECPHFSSFADELTDYVTRNILATPI
MNGKDVVAVIMAVNKLDGPCFTSEDEDVFLKYLNFGTLNLKIYHLSYLHNCETRRGQVLL
WSANKVFEELTDIERQFHKAFYTVRAYLNCDRYSVGLLDMTKEKEFFDVWPVLMGEAQAY
SGPRTPDGREILFYKVIDYILHGKEDIKVIPSPPADHWALASGLPTYVAESGFICNIMNA
PADEMFNFQEGPLDDSGWIVKNVLSMPIVNKKEEIVGVATFYNRKDGKPFDEQDEVLMES
LTQFLGWSVLNTDTYDKMNKLENRKDIAQDMVLYHVRCDREEIQLILPTRERLGKEPADC
EEDELGKILKEVLPGPAKFDIYEFHFSDLECTELELVKCGIQMYYELGVVRKFQIPQEVL
VRFLFSVSKGYRRITYHNWRHGFNVAQTMFTLLMTGKLKSYYTDLEAFAMVTAGLCHDID
HRGTNNLYQMKSQNPLAKLHGSSILERHHLEFGKFLLSEETLNIYQNLNRRQHEHVIHLM
DIAIIATDLALYFKKRTMFQKIVDESKNYEDRKSWVEYLSLETTRKEIVMAMMMTACDLS
AITKPWEVQSKVALLVAAEFWEQGDLERTVLDQQPIPMMDRNKAAELPKLQVGFIDFVCT
FVYKEFSRFHEEILPMFDRLQNNRKEWKALADEYEAKVKALEEDQKKETTAKKVGTEICN
GGPAPRSSTCRIL
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BDBM50166821
n/a
NameBDBM50166821
Synonyms:3-[2-Ethoxy-5-(4-isopropyl-piperazine-1-sulfonyl)-phenyl]-5-methyl-2H-2,4,4b,9-tetraaza-fluoren-1-one | CHEMBL196142
TypeSmall organic molecule
Emp. Form.C25H30N6O4S
Mol. Mass.510.608
SMILESCCOc1ccc(cc1-c1nc2c(nc3cccc(C)n23)c(=O)[nH]1)S(=O)(=O)N1CCN(CC1)C(C)C
Structure
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