| Reaction Details |
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 | Report a problem with these data |
| Target | Potassium voltage-gated channel subfamily H member 2 |
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| Ligand | BDBM50029668 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1436969 (CHEMBL3389028) |
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| IC50 | 16200±n/a nM |
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| Citation |  Finlay, MR; Anderton, M; Ashton, S; Ballard, P; Bethel, PA; Box, MR; Bradbury, RH; Brown, SJ; Butterworth, S; Campbell, A; Chorley, C; Colclough, N; Cross, DA; Currie, GS; Grist, M; Hassall, L; Hill, GB; James, D; James, M; Kemmitt, P; Klinowska, T; Lamont, G; Lamont, SG; Martin, N; McFarland, HL; Mellor, MJ; Orme, JP; Perkins, D; Perkins, P; Richmond, G; Smith, P; Ward, RA; Waring, MJ; Whittaker, D; Wells, S; Wrigley, GL Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. J Med Chem57:8249-67 (2014) [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 |
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| 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 |
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| Type: | Multi-pass membrane protein |
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| Mol. Mass.: | 126672.65 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q12809 |
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| Residue: | 1159 |
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| 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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| BDBM50029668 |
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| n/a |
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| Name | BDBM50029668 |
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| Synonyms: | AZD-9291 | Osimertinib | US10085983, Compound AZD-9291 | US10227342, Example 24 | US11111233, Example AZD9291 | US11896597, Compound AZD9291 | US20230322822, Compound AZD9291 | US9890168, Compound AZD-9291 | WO2022090481, Example osimertinib |
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| Type | Small organic molecule |
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| Emp. Form. | C28H33N7O2 |
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| Mol. Mass. | 499.6073 |
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| SMILES | COc1cc(N(C)CCN(C)C)c(NC(=O)C=C)cc1Nc1nccc(n1)-c1cn(C)c2ccccc12 |
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| Structure | 
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