Reaction Details |
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Target | P04972/P11541/P16586/P22571/P23439/Q95142 |
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Ligand | BDBM50130020 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_155383 (CHEMBL760836) |
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IC50 | 4.4±n/a nM |
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Citation | Ukita, T; Nakamura, Y; Kubo, A; Yamamoto, Y; Moritani, Y; Saruta, K; Higashijima, T; Kotera, J; Fujishige, K; Takagi, M; Kikkawa, K; Omori, K 1,7- and 2,7-naphthyridine derivatives as potent and highly specific PDE5 inhibitors. Bioorg Med Chem Lett13:2341-5 (2003) [PubMed] |
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More Info.: | Get all data from this article, Assay Method |
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P04972/P11541/P16586/P22571/P23439/Q95142 |
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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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BDBM50130020 |
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n/a |
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Name | BDBM50130020 |
Synonyms: | 2-(2-Methyl-pyridin-4-ylmethyl)-1-oxo-8-(pyridin-2-ylmethoxy)-4-(3,4,5-trimethoxy-phenyl)-1,2-dihydro-[2,7]naphthyridine-3-carboxylic acid methyl ester | CHEMBL77795 |
Type | Small organic molecule |
Emp. Form. | C32H30N4O7 |
Mol. Mass. | 582.6032 |
SMILES | COC(=O)c1c(-c2cc(OC)c(OC)c(OC)c2)c2ccnc(OCc3ccccn3)c2c(=O)n1Cc1ccnc(C)c1 |
Structure |
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