| 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 | BDBM392323 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_2047203 (CHEMBL4701902) |
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| IC50 | >30000±n/a nM |
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| Citation |  LaMarche, MJ; Acker, M; Argintaru, A; Bauer, D; Boisclair, J; Chan, H; Chen, CH; Chen, YN; Chen, Z; Deng, Z; Dore, M; Dunstan, D; Fan, J; Fekkes, P; Firestone, B; Fodor, M; Garcia-Fortanet, J; Fortin, PD; Fridrich, C; Giraldes, J; Glick, M; Grunenfelder, D; Hao, HX; Hentemann, M; Ho, S; Jouk, A; Kang, ZB; Karki, R; Kato, M; Keen, N; Koenig, R; LaBonte, LR; Larrow, J; Liu, G; Liu, S; Majumdar, D; Mathieu, S; Meyer, MJ; Mohseni, M; Ntaganda, R; Palermo, M; Perez, L; Pu, M; Ramsey, T; Reilly, J; Sarver, P; Sellers, WR; Sendzik, M; Shultz, MD; Slisz, J; Slocum, K; Smith, T; Spence, S; Stams, T; Straub, C; Tamez, V; Toure, BB; Towler, C; Wang, P; Wang, H; Williams, SL; Yang, F; Yu, B; Zhang, JH; Zhu, S Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer. J Med Chem63:13578-13594 (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 |
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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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| BDBM392323 |
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| n/a |
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| Name | BDBM392323 |
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| Synonyms: | 3-((2-amino-3-chloropyridin-4-yl)thio)-6-(4-(aminomethyl)-4-methylpiperidin-1-yl)pyrazin-2-amine | US10301278, Example 42 |
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| Type | Small organic molecule |
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| Emp. Form. | C16H22ClN7S |
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| Mol. Mass. | 379.911 |
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| SMILES | CC1(CN)CCN(CC1)c1cnc(Sc2ccnc(N)c2Cl)c(N)n1 |
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| Structure | 
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