Reaction Details |
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Target | Potassium voltage-gated channel subfamily H member 2 |
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Ligand | BDBM50559108 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2067975 (CHEMBL4723228) |
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IC50 | 18000±n/a nM |
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Citation | Fairhurst, RA; Knoepfel, T; Buschmann, N; Leblanc, C; Mah, R; Todorov, M; Nimsgern, P; Ripoche, S; Niklaus, M; Warin, N; Luu, VH; Madoerin, M; Wirth, J; Graus-Porta, D; Weiss, A; Kiffe, M; Wartmann, M; Kinyamu-Akunda, J; Sterker, D; Stamm, C; Adler, F; Buhles, A; Schadt, H; Couttet, P; Blank, J; Galuba, I; Trappe, J; Voshol, J; Ostermann, N; Zou, C; Berghausen, J; Del Rio Espinola, A; Jahnke, W; Furet, P Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. J Med Chem63:12542-12573 (2020) [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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BDBM50559108 |
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n/a |
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Name | BDBM50559108 |
Synonyms: | CHEMBL4745615 |
Type | Small organic molecule |
Emp. Form. | C26H31N7O5 |
Mol. Mass. | 521.5682 |
SMILES | COCCOc1cc(NC(=O)N2CCCc3cc(CN4CC[C@H](N(C)C)C4=O)c(C=O)nc23)ncc1C#N |r| |
Structure |
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