Reaction Details |
| Report a problem with these data |
Target | O43924/P16499/P18545/P35913/P51160/Q13956 |
---|
Ligand | BDBM14777 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_304857 (CHEMBL828416) |
---|
IC50 | 2000±n/a nM |
---|
Citation | Manallack, DT; Hughes, RA; Thompson, PE The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases. J Med Chem48:3449-62 (2005) [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
|
|
|
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
|
|
|
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
|
|
|
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
|
|
|
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
|
|
|
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
|
|
|
BDBM14777 |
---|
n/a |
---|
Name | BDBM14777 |
Synonyms: | (2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,17-triazatetracyclo[8.7.0.0^{3,8}.0^{11,16}]heptadeca-1(10),11(16),12,14-tetraene-4,7-dione | (6R,12aR)-6-(1,3-benzodioxol-5-yl)-2-methyl-2,3,6,7,12,12a-hexahydropyrazino[1,2,1,6]pyrido[3,4-b]indole-1,4-dione | CHEMBL779 | Cialis | GF 196960 | Tadalafil |
Type | Small organic molecule |
Emp. Form. | C22H19N3O4 |
Mol. Mass. | 389.404 |
SMILES | [H][C@]12Cc3c([nH]c4ccccc34)[C@H](N1C(=O)CN(C)C2=O)c1ccc2OCOc2c1 |r| |
Structure |
|