Reaction Details |
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Target | Potassium voltage-gated channel subfamily H member 2 |
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Ligand | BDBM154061 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1925813 (CHEMBL4428885) |
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Ki | 2000±n/a nM |
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Citation | DiMauro, EF; Altmann, S; Berry, LM; Bregman, H; Chakka, N; Chu-Moyer, M; Bojic, EF; Foti, RS; Fremeau, R; Gao, H; Gunaydin, H; Guzman-Perez, A; Hall, BE; Huang, H; Jarosh, M; Kornecook, T; Lee, J; Ligutti, J; Liu, D; Moyer, BD; Ortuno, D; Rose, PE; Schenkel, LB; Taborn, K; Wang, J; Wang, Y; Yu, V; Weiss, MM Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors. J Med Chem59:7818-39 (2016) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Potassium voltage-gated channel subfamily H member 2 |
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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: | MPVRRGHVAPQNTFLDTIIRKFEGQSRKFIIANARVENCAVIYCNDGFCELCGYSRAEVM
QRPCTCDFLHGPRTQRRAAAQIAQALLGAEERKVEIAFYRKDGSCFLCLVDVVPVKNEDG
AVIMFILNFEVVMEKDMVGSPAHDTNHRGPPTSWLAPGRAKTFRLKLPALLALTARESSV
RSGGAGGAGAPGAVVVDVDLTPAAPSSESLALDEVTAMDNHVAGLGPAEERRALVGPGSP
PRSAPGQLPSPRAHSLNPDASGSSCSLARTRSRESCASVRRASSADDIEAMRAGVLPPPP
RHASTGAMHPLRSGLLNSTSDSDLVRYRTISKIPQITLNFVDLKGDPFLASPTSDREIIA
PKIKERTHNVTEKVTQVLSLGADVLPEYKLQAPRIHRWTILHYSPFKAVWDWLILLLVIY
TAVFTPYSAAFLLKETEEGPPATECGYACQPLAVVDLIVDIMFIVDILINFRTTYVNANE
EVVSHPGRIAVHYFKGWFLIDMVAAIPFDLLIFGSGSEELIGLLKTARLLRLVRVARKLD
RYSEYGAAVLFLLMCTFALIAHWLACIWYAIGNMEQPHMDSRIGWLHNLGDQIGKPYNSS
GLGGPSIKDKYVTALYFTFSSLTSVGFGNVSPNTNSEKIFSICVMLIGSLMYASIFGNVS
AIIQRLYSGTARYHTQMLRVREFIRFHQIPNPLRQRLEEYFQHAWSYTNGIDMNAVLKGF
PECLQADICLHLNRSLLQHCKPFRGATKGCLRALAMKFKTTHAPPGDTLVHAGDLLTALY
FISRGSIEILRGDVVVAILGKNDIFGEPLNLYARPGKSNGDVRALTYCDLHKIHRDDLLE
VLDMYPEFSDHFWSSLEITFNLRDTNMIPGSPGSTELEGGFSRQRKRKLSFRRRTDKDTE
QPGEVSALGPGRAGAGPSSRGRPGGPWGESPSSGPSSPESSEDEGPGRSSSPLRLVPFSS
PRPPGEPPGGEPLMEDCEKSSDTCNPLSGAFSGVSNIFSFWGDSRGRQYQELPRCPAPTP
SLLNIPLSSPGRRPRGDVESRLDALQRQLNRLETRLSADMATVLQLLQRQMTLVPPAYSA
VTTPGPGPTSTSPLLPVSPLPTLTLDSLSQVSQFMACEELPPGAPELPQEGPTRRLSLPG
QLGALTSQPLHRHGSDPGS
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BDBM154061 |
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n/a |
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Name | BDBM154061 |
Synonyms: | US9012443, 57 |
Type | Small organic molecule |
Emp. Form. | C18H10ClF3N4O2S2 |
Mol. Mass. | 470.876 |
SMILES | FC(F)(F)c1ccc(cc1Cl)-c1nccc2cc(ccc12)S(=O)(=O)Nc1ncns1 |
Structure |
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