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Target
Potassium voltage-gated channel subfamily H member 2
Ligand
BDBM50005548
Substrate
n/a
Meas. Tech.
ChEMBL_939922 (CHEMBL2327304)
IC50
>27000±n/a nM
Citation
Brown, DG; Bernstein, PR; Wu, Y; Urbanek, RA; Becker, CW; Throner, SR; Dembofsky, BT; Steelman, GB; Lazor, LA; Scott, CW; Wood, MW; Wesolowski, SS; Nugiel, DA; Koch, S; Yu, J; Pivonka, DE; Li, S; Thompson, C; Zacco, A; Elmore, CS; Schroeder, P; Liu, J; Hurley, CA; Ward, S; Hunt, HJ; Williams, K; McLaughlin, J; Hoesch, V; Sydserff, S; Maier, D; Aharony, D Azepines and piperidines with dual norepinephrine dopamine uptake inhibition and antidepressant activity. ACS Med Chem Lett 4:46-51 (2013) [PubMed] Article
More Info.:
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:
BDBM50005548
Synonyms:
(+)-2-Methyl-4-phenyl-1,2,3,4-tetrahydro-isoquinolin-8-ylamine | (+/-)-2-Methyl-4-phenyl-1,2,3,4-tetrahydro-isoquinolin-8-ylamine | (-)-2-Methyl-4-phenyl-1,2,3,4-tetrahydro-isoquinolin-8-ylamine | (Nomifensine) 2-Methyl-4-phenyl-1,2,3,4-tetrahydro-isoquinolin-8-ylamine | 2-Methyl-4-phenyl-1,2,3,4-tetrahydro-isoquinolin-8-ylamine | 2-Methyl-4-phenyl-1,2,3,4-tetrahydro-isoquinolin-8-ylamine (Nomifensine) | 2-Methyl-4-phenyl-1,2,3,4-tetrahydro-isoquinolin-8-ylamine(Nomifensine) | 2-methyl-4-phenyl-1,2,3,4-tetrahydroisoquinolin-8-amine | CHEMBL273575 | NOMIFENSINE | NOMIFENSINE2-Methyl-4-phenyl-1,2,3,4-tetrahydro-isoquinolin-8-ylamine
Type:
Small organic molecule
Emp. Form.:
C16H18N2
Mol. Mass.:
238.3275
SMILES:
CN1CC(c2ccccc2)c2cccc(N)c2C1