Reaction Details |
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Target | Dual specificity mitogen-activated protein kinase kinase 1 [K97R] |
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Ligand | BDBM200387 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Radioactive Binding Assay |
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IC50 | 16.0±n/a nM |
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Citation | Bock, MG; Moebitz, H; Panigrahi, SK; Poddutoori, R; Samajdar, S Compounds and compositions as inhibitors of MEK US Patent US9629836 Publication Date 4/25/2017 |
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More Info.: | Get all data from this article, Assay Method |
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Dual specificity mitogen-activated protein kinase kinase 1 [K97R] |
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Name: | Dual specificity mitogen-activated protein kinase kinase 1 [K97R] |
Synonyms: | Dual specificity mitogen-activated protein kinase kinase 1 (MEK1)(K97R) | MAP2K1 | MEK1 | MEK1 (K97R) | MP2K1_HUMAN | PRKMK1 |
Type: | n/a |
Mol. Mass.: | 43467.04 |
Organism: | Homo sapiens (Human) |
Description: | Biotinylated full length MEK1 with an inactivating K97R ATP binding site mutation. |
Residue: | 393 |
Sequence: | MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKV
GELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARRLIHLEIKPAIRNQIIRELQVLHE
CNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYL
REKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHY
SVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSY
GMDSRPPMAIFELLDYIVNEPPPKLPSGVFSLEFQDFVNKCLIKNPAERADLKQLMVHAF
IKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV
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BDBM200387 |
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n/a |
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Name | BDBM200387 |
Synonyms: | US10011599, Example 15 | US9227969, 15 | US9629836, 15 |
Type | Small organic molecule |
Emp. Form. | C29H28ClFN6O2 |
Mol. Mass. | 547.023 |
SMILES | Cc1ccnc(Oc2ccc(c(Cl)c2)-c2cc3c4n(cnc4cnc3cc2F)C2(C)CCN(CCO)CC2)n1 |
Structure |
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