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Target
Potassium voltage-gated channel subfamily H member 2
Ligand
BDBM264259
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:
BDBM264259
Synonyms:
6-(2,6-Dichlorophenyl)-2-((3-methoxy-4-(piperazin-1-yl)phenyl)amino)pyrido[4,3-d]pyrimidin-5(6H)-one, HCl | US9714244, 13
Type:
Small organic molecule
Emp. Form.:
C24H22Cl2N6O2
Mol. Mass.:
497.376
SMILES:
COc1cc(Nc2ncc3c(ccn(-c4c(Cl)cccc4Cl)c3=O)n2)ccc1N1CCNCC1 |(-2.67,2.7,;-4,1.93,;-4,.38,;-2.67,-.38,;-2.67,-1.93,;-1.33,-2.69,;,-1.93,;,-.38,;1.33,.38,;2.67,-.38,;2.67,-1.93,;4,-2.69,;5.33,-1.93,;5.33,-.38,;6.67,.38,;6.67,1.93,;5.33,2.69,;8,2.69,;9.34,1.93,;9.34,.38,;8,-.38,;8,-1.93,;4,.38,;4,1.93,;1.33,-2.69,;-4,-2.69,;-5.33,-1.93,;-5.33,-.38,;-6.67,.38,;-8,-.38,;-9.34,.38,;-9.34,1.93,;-8,2.69,;-6.67,1.93,)|
Structure:
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