Ki Summary

Reaction Details

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Target

P04972/P11541/P16586/P22571/P23439/Q95142

Ligand

BDBM14390

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_155382 (CHEMBL760835)

IC50

20±n/a nM

Citation

Kim, DK; Young Lee, J; Park, HJ; Minh Thai, K Synthesis and phosphodiesterase 5 inhibitory activity of new sildenafil analogues containing a phosphonate group in the 5(')-sulfonamide moiety of phenyl ring. Bioorg Med Chem Lett14:2099-103 (2004) [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:

Sequence:

MNLEPPKAEIRSATRVMGGPVTPRKGPPKFKQRQTRQFKSKPPKKGVQGFGDDIPGMEGL
GTDITVICPWEAFNHLELHELAQYGII

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

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

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:

Sequence:

MSDNTVLAPPTSNQGPTTPRKGPPKFKQRQTRQFKSKPPKKGVKGFGDDIPGMEGLGTDI
TVICPWEAFSHLELHELAQFGII

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

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

BDBM14390

n/a

Name

BDBM14390

Synonyms:

5-[2-ethoxy-5-(4-methyl-1-piperazinylsulfonyl)phenyl]-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one | 5-{2-ethoxy-5-[(4-methylpiperazine-1-)sulfonyl]phenyl}-1-methyl-3-propyl-1H,6H,7H-pyrazolo[4,3-d]pyrimidin-7-one | CHEMBL192 | SILDENAFIL CITRATE | Sildenafil | Sildenafil# | US11155558, Compound sildenafil | US11242347, Compound sildenafil | Viagra

Type

Small organic molecule

Emp. Form.

C22H30N6O4S

Mol. Mass.

474.576

SMILES

CCCc1nn(C)c2c1nc([nH]c2=O)-c1cc(ccc1OCC)S(=O)(=O)N1CCN(C)CC1

Structure