Ki Summary

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Target

Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha

Ligand

BDBM50300952

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_597960 (CHEMBL1042745)

IC50

15±n/a nM

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

More Info.:

Get all data from this article, Assay Method

Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha

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

BDBM50300952

n/a

Name

BDBM50300952

Synonyms:

3-(trans-4-hydroxycyclohexylamino)-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[2,3-b]pyrazin-2(1H)-one | CHEMBL566820

Type

Small organic molecule

Emp. Form.

C24H31N5O4

Mol. Mass.

453.534

SMILES

CCCOCCn1c2cc(cnc2nc(N[C@H]2CC[C@H](O)CC2)c1=O)-c1ccc(OC)nc1 |r,wU:16.16,wD:19.20,(3.98,.08,;2.65,-.69,;2.65,-2.23,;1.32,-3,;1.32,-4.54,;-.02,-5.31,;-.02,-6.85,;1.31,-7.63,;2.64,-6.86,;3.96,-7.62,;3.97,-9.17,;2.64,-9.93,;1.31,-9.17,;-.02,-9.93,;-1.36,-9.16,;-2.7,-9.93,;-4.03,-9.15,;-5.37,-9.93,;-6.7,-9.15,;-6.69,-7.6,;-8.02,-6.82,;-5.35,-6.84,;-4.03,-7.62,;-1.35,-7.63,;-2.68,-6.86,;5.29,-6.85,;6.63,-7.62,;7.96,-6.84,;7.95,-5.3,;9.28,-4.53,;10.62,-5.29,;6.61,-4.54,;5.28,-5.31,)|

Structure