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TargetPotassium voltage-gated channel subfamily H member 2
LigandBDBM50308562
Substrate/Competitorn/a
Meas. Tech.ChEMBL_613538
IC50 54±n/a nM
Citation Hughes, RORogier, DJJacobsen, EJWalker, JKMacinnes, ABond, BRZhang, LLYu, YZheng, YRumsey, JMWalgren, JLCurtiss, SWFobian, YMHeasley, SECubbage, JWMoon, JBBrown, DLAcker, BAMaddux, TMTollefson, MBMischke, BVOwen, DRFreskos, JNMolyneaux, JMBenson, AGBlevis-Bal, RM Design, synthesis, and biological evaluation of 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one, a potent, orally active, brain penetrant inhibitor of phosphodiesterase 5 (PDE5). J Med Chem53:2656-60 (2010) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Potassium voltage-gated channel subfamily H member 2
Name:Potassium voltage-gated channel subfamily H member 2
Synonyms:1,3-beta-glucan synthase component GLS2 | Eag-related protein 1 | Erg1 | Ether a-go-go related gene potassium channel (hERG) | Ether-a-go-go-related gene (HERG) | Ether-a-go-go-related gene potassium channel (hERG) | Ether-a-go-go-related gene potassium channel 1 | Ether-a-go-go-related gene potassium channel 1 (HERG) | Ether-a-go-go-related gene potassium channel 1 (hERG1) | Ether-a-go-go-related protein (hERG) | Ether-a-go-go-related protein 1 | Ether-a-go-go-related protein 1 (HERG) | Ether-a-go-go-related protein 1 (hERG) | H-ERG | HERG | Potassium voltage-gated channel subfamily H member 2 (hERG) | Transcriptional regulator ERG | Voltage-gated potassium channel subunit Kv11.1 | eag homolog | hERG Potassium Channel 1 | putative potassium channel subunit
Type:Multi-pass membrane protein
Mol. Mass.:126672.65
Organism:Homo sapiens (Human)
Description:Q12809
Residue:1159
Sequence:
MPVRRGHVAPQNTFLDTIIRKFEGQSRKFIIANARVENCAVIYCNDGFCELCGYSRAEVM
QRPCTCDFLHGPRTQRRAAAQIAQALLGAEERKVEIAFYRKDGSCFLCLVDVVPVKNEDG
AVIMFILNFEVVMEKDMVGSPAHDTNHRGPPTSWLAPGRAKTFRLKLPALLALTARESSV
RSGGAGGAGAPGAVVVDVDLTPAAPSSESLALDEVTAMDNHVAGLGPAEERRALVGPGSP
PRSAPGQLPSPRAHSLNPDASGSSCSLARTRSRESCASVRRASSADDIEAMRAGVLPPPP
RHASTGAMHPLRSGLLNSTSDSDLVRYRTISKIPQITLNFVDLKGDPFLASPTSDREIIA
PKIKERTHNVTEKVTQVLSLGADVLPEYKLQAPRIHRWTILHYSPFKAVWDWLILLLVIY
TAVFTPYSAAFLLKETEEGPPATECGYACQPLAVVDLIVDIMFIVDILINFRTTYVNANE
EVVSHPGRIAVHYFKGWFLIDMVAAIPFDLLIFGSGSEELIGLLKTARLLRLVRVARKLD
RYSEYGAAVLFLLMCTFALIAHWLACIWYAIGNMEQPHMDSRIGWLHNLGDQIGKPYNSS
GLGGPSIKDKYVTALYFTFSSLTSVGFGNVSPNTNSEKIFSICVMLIGSLMYASIFGNVS
AIIQRLYSGTARYHTQMLRVREFIRFHQIPNPLRQRLEEYFQHAWSYTNGIDMNAVLKGF
PECLQADICLHLNRSLLQHCKPFRGATKGCLRALAMKFKTTHAPPGDTLVHAGDLLTALY
FISRGSIEILRGDVVVAILGKNDIFGEPLNLYARPGKSNGDVRALTYCDLHKIHRDDLLE
VLDMYPEFSDHFWSSLEITFNLRDTNMIPGSPGSTELEGGFSRQRKRKLSFRRRTDKDTE
QPGEVSALGPGRAGAGPSSRGRPGGPWGESPSSGPSSPESSEDEGPGRSSSPLRLVPFSS
PRPPGEPPGGEPLMEDCEKSSDTCNPLSGAFSGVSNIFSFWGDSRGRQYQELPRCPAPTP
SLLNIPLSSPGRRPRGDVESRLDALQRQLNRLETRLSADMATVLQLLQRQMTLVPPAYSA
VTTPGPGPTSTSPLLPVSPLPTLTLDSLSQVSQFMACEELPPGAPELPQEGPTRRLSLPG
QLGALTSQPLHRHGSDPGS
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BDBM50308562
NameBDBM50308562
Synonyms:(+/-)-3-(4-((2S,3R)-3-hydroxybutan-2-yl)piperazin-1-yl)-1-(2-isopropoxyethyl)-7-(6-methoxypyridin-3-yl)pyrido[3,4-b]pyrazin-2(1H)-one | CHEMBL589069
TypeSmall organic molecule
Emp. Form.C26H36N6O4
Mol. Mass.496.6018
SMILESCCCOCCn1c2cc(ncc2nc(N2CCN(CC2)[C@@H](C)[C@@H](C)O)c1=O)-c1ccc(OC)nc1 |r|
Structure
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n/a