Reaction Details |
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Target | Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha |
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Ligand | BDBM50300989 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_597960 (CHEMBL1042745) |
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IC50 | 15±n/a nM |
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Citation | Hughes, RO; Walker, JK; Rogier, DJ; Heasley, SE; Blevis-Bal, RM; Benson, AG; Jacobsen, EJ; Cubbage, JW; Fobian, YM; Owen, DR; Freskos, JN; Molyneaux, JM; Brown, DL; Acker, BA; Maddux, TM; Tollefson, MB; Moon, JB; Mischke, BV; Rumsey, JM; Zheng, Y; MacInnes, A; Bond, BR; Yu, Y Optimization of the aminopyridopyrazinones class of PDE5 inhibitors: discovery of 3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one. Bioorg Med Chem Lett19:5209-13 (2009) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha |
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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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BDBM50300989 |
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n/a |
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Name | BDBM50300989 |
Synonyms: | (S)-3-(2-hydroxypropylamino)-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one | CHEMBL566367 |
Type | Small organic molecule |
Emp. Form. | C21H27N5O4 |
Mol. Mass. | 413.4702 |
SMILES | CCCOCCn1c2cc(ncc2nc(NC[C@H](C)O)c1=O)-c1ccc(OC)nc1 |r| |
Structure |
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