| Reaction Details |
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 | Report a problem with these data |
| Target | Mitogen-activated protein kinase kinase kinase kinase 4 |
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| Ligand | BDBM50585632 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_2163563 (CHEMBL5048424) |
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| IC50 | 1422±n/a nM |
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| Citation |  Zhang, L; Moccia, M; Briggs, DC; Bharate, JB; Lakkaniga, NR; Knowles, P; Yan, W; Tran, P; Kharbanda, A; Wang, X; Leung, YK; Frett, B; Santoro, M; McDonald, NQ; Carlomagno, F; Li, HY Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose. J Med Chem65:1536-1551 (2022) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Mitogen-activated protein kinase kinase kinase kinase 4 |
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| Name: | Mitogen-activated protein kinase kinase kinase kinase 4 |
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| Synonyms: | HGK | HPK/GCK-like kinase HGK | KIAA0687 | M4K4_HUMAN | MAP4K4 | MAP4K4 (HGK) | MAPK/ERK kinase kinase kinase 4 | MEK kinase kinase 4 | MEKKK 4 | Mitogen-activated protein kinase kinase kinase kinase 4 (MAP4K4) | NIK | Nck-interacting kinase |
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| Type: | Serine/threonine-protein kinase |
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| Mol. Mass.: | 142114.73 |
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| Organism: | Homo sapiens (Human) |
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| Description: | O95819 |
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| Residue: | 1239 |
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| Sequence: | MANDSPAKSLVDIDLSSLRDPAGIFELVEVVGNGTYGQVYKGRHVKTGQLAAIKVMDVTE
DEEEEIKLEINMLKKYSHHRNIATYYGAFIKKSPPGHDDQLWLVMEFCGAGSITDLVKNT
KGNTLKEDWIAYISREILRGLAHLHIHHVIHRDIKGQNVLLTENAEVKLVDFGVSAQLDR
TVGRRNTFIGTPYWMAPEVIACDENPDATYDYRSDLWSCGITAIEMAEGAPPLCDMHPMR
ALFLIPRNPPPRLKSKKWSKKFFSFIEGCLVKNYMQRPSTEQLLKHPFIRDQPNERQVRI
QLKDHIDRTRKKRGEKDETEYEYSGSEEEEEEVPEQEGEPSSIVNVPGESTLRRDFLRLQ
QENKERSEALRRQQLLQEQQLREQEEYKRQLLAERQKRIEQQKEQRRRLEEQQRREREAR
RQQEREQRRREQEEKRRLEELERRRKEEEERRRAEEEKRRVEREQEYIRRQLEEEQRHLE
VLQQQLLQEQAMLLECRWREMEEHRQAERLQRQLQQEQAYLLSLQHDHRRPHPQHSQQPP
PPQQERSKPSFHAPEPKAHYEPADRAREVEDRFRKTNHSSPEAQSKQTGRVLEPPVPSRS
ESFSNGNSESVHPALQRPAEPQVPVRTTSRSPVLSRRDSPLQGSGQQNSQAGQRNSTSIE
PRLLWERVEKLVPRPGSGSSSGSSNSGSQPGSHPGSQSGSGERFRVRSSSKSEGSPSQRL
ENAVKKPEDKKEVFRPLKPADLTALAKELRAVEDVRPPHKVTDYSSSSEESGTTDEEDDD
VEQEGADESTSGPEDTRAASSLNLSNGETESVKTMIVHDDVESEPAMTPSKEGTLIVRQT
QSASSTLQKHKSSSSFTPFIDPRLLQISPSSGTTVTSVVGFSCDGMRPEAIRQDPTRKGS
VVNVNPTNTRPQSDTPEIRKYKKRFNSEILCAALWGVNLLVGTESGLMLLDRSGQGKVYP
LINRRRFQQMDVLEGLNVLVTISGKKDKLRVYYLSWLRNKILHNDPEVEKKQGWTTVGDL
EGCVHYKVVKYERIKFLVIALKSSVEVYAWAPKPYHKFMAFKSFGELVHKPLLVDLTVEE
GQRLKVIYGSCAGFHAVDVDSGSVYDIYLPTHIQCSIKPHAIIILPNTDGMELLVCYEDE
GVYVNTYGRITKDVVLQWGEMPTSVAYIRSNQTMGWGEKAIEIRSVETGHLDGVFMHKRA
QRLKFLCERNDKVFFASVRSGGSSQVYFMTLGRTSLLSW
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| BDBM50585632 |
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| n/a |
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| Name | BDBM50585632 |
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| Synonyms: | CHEMBL5070593 |
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| Type | Small organic molecule |
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| Emp. Form. | C27H30FN9O |
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| Mol. Mass. | 515.5852 |
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| SMILES | CN1CCN(CC1)c1cc(Nc2cc(C)n[nH]2)nc(Nc2ccc(CC(=O)Nc3cccc(F)c3)cc2)n1 |
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| Structure | 
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