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Target
Potassium voltage-gated channel subfamily H member 2
Ligand
BDBM264266
Substrate
n/a
Meas. Tech.
hERG Activity Assay
IC50
<10±n/a nM
Citation
 O Dowd, CR; Rountree, JS; Burkamp, F; Wilkinson, AJ Substituted pyrido[4,3-d]pyrimidines as Wee-1 inhibitors US Patent  US9714244 Publication Date 7/25/2017 
Target
Name:
Potassium voltage-gated channel subfamily H member 2
Synonyms:
1,3-beta-glucan synthase component GLS2 | Cytochrome P450 3A4 | ERG | ERG1 | Eag-related protein 1 | 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) | H-ERG | HERG | KCNH2 | KCNH2_HUMAN | 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:
MPVRRGHVAPQNTFLDTIIRKFEGQSRKFIIANARVENCAVIYCNDGFCELCGYSRAEVMQRPCTCDFLHGPRTQRRAAAQIAQALLGAEERKVEIAFYRKDGSCFLCLVDVVPVKNEDGAVIMFILNFEVVMEKDMVGSPAHDTNHRGPPTSWLAPGRAKTFRLKLPALLALTARESSVRSGGAGGAGAPGAVVVDVDLTPAAPSSESLALDEVTAMDNHVAGLGPAEERRALVGPGSPPRSAPGQLPSPRAHSLNPDASGSSCSLARTRSRESCASVRRASSADDIEAMRAGVLPPPPRHASTGAMHPLRSGLLNSTSDSDLVRYRTISKIPQITLNFVDLKGDPFLASPTSDREIIAPKIKERTHNVTEKVTQVLSLGADVLPEYKLQAPRIHRWTILHYSPFKAVWDWLILLLVIYTAVFTPYSAAFLLKETEEGPPATECGYACQPLAVVDLIVDIMFIVDILINFRTTYVNANEEVVSHPGRIAVHYFKGWFLIDMVAAIPFDLLIFGSGSEELIGLLKTARLLRLVRVARKLDRYSEYGAAVLFLLMCTFALIAHWLACIWYAIGNMEQPHMDSRIGWLHNLGDQIGKPYNSSGLGGPSIKDKYVTALYFTFSSLTSVGFGNVSPNTNSEKIFSICVMLIGSLMYASIFGNVSAIIQRLYSGTARYHTQMLRVREFIRFHQIPNPLRQRLEEYFQHAWSYTNGIDMNAVLKGFPECLQADICLHLNRSLLQHCKPFRGATKGCLRALAMKFKTTHAPPGDTLVHAGDLLTALYFISRGSIEILRGDVVVAILGKNDIFGEPLNLYARPGKSNGDVRALTYCDLHKIHRDDLLEVLDMYPEFSDHFWSSLEITFNLRDTNMIPGSPGSTELEGGFSRQRKRKLSFRRRTDKDTEQPGEVSALGPGRAGAGPSSRGRPGGPWGESPSSGPSSPESSEDEGPGRSSSPLRLVPFSSPRPPGEPPGGEPLMEDCEKSSDTCNPLSGAFSGVSNIFSFWGDSRGRQYQELPRCPAPTPSLLNIPLSSPGRRPRGDVESRLDALQRQLNRLETRLSADMATVLQLLQRQMTLVPPAYSAVTTPGPGPTSTSPLLPVSPLPTLTLDSLSQVSQFMACEELPPGAPELPQEGPTRRLSLPGQLGALTSQPLHRHGSDPGS
  
Inhibitor
Name:
BDBM264266
Synonyms:
6-(2,6-Dichlorophenyl)-2-((3-((methylamino)methyl)-4-morpholinophenyl)amino)pyrido[4,3-d]pyrimidin-5(6H)-one | US9714244, 20
Type:
Small organic molecule
Emp. Form.:
C25H24Cl2N6O2
Mol. Mass.:
511.403
SMILES:
CNCc1cc(Nc2ncc3c(ccn(-c4c(Cl)cccc4Cl)c3=O)n2)ccc1N1CCOCC1 |(-8,-3.85,;-6.67,-3.08,;-6.67,-1.54,;-5.33,-.77,;-4,-1.54,;-2.67,-.77,;-1.33,-1.54,;,-.77,;,.77,;1.33,1.54,;2.67,.77,;2.67,-.77,;4,-1.54,;5.33,-.77,;5.33,.77,;6.67,1.54,;6.67,3.08,;5.33,3.85,;8,3.85,;9.34,3.08,;9.34,1.54,;8,.77,;8,-.77,;4,1.54,;4,3.08,;1.33,-1.54,;-2.67,.77,;-4,1.54,;-5.33,.77,;-6.67,1.54,;-8,.77,;-9.34,1.54,;-9.34,3.08,;-8,3.85,;-6.67,3.08,)|
Structure:
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