Reaction Details |
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Target | Dual specificity mitogen-activated protein kinase kinase 1/RAF proto-oncogene serine/threonine-protein kinase |
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Ligand | BDBM50095232 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_100226 (CHEMBL710955) |
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IC50 | 2.4±n/a nM |
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Citation | Zhang, N; Wu, B; Powell, D; Wissner, A; Floyd, MB; Kovacs, ED; Toral-Barza, L; Kohler, C Synthesis and structure-activity relationships of 3-cyano-4-(phenoxyanilino)quinolines as MEK (MAPKK) inhibitors. Bioorg Med Chem Lett10:2825-8 (2000) [PubMed] |
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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/RAF proto-oncogene serine/threonine-protein kinase |
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Name: | Dual specificity mitogen-activated protein kinase kinase 1/RAF proto-oncogene serine/threonine-protein kinase |
Synonyms: | Serine/threonine-protein kinase RAF and Dual specificity mitogen-activated protein kinase kinase 1 (Raf/MEK) |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of ChEMBL is 100226 |
Components: | This complex has 2 components. |
Component 1 |
Name: | RAF proto-oncogene serine/threonine-protein kinase |
Synonyms: | C-Raf Protein Kinase | Proto-oncogene c-RAF (RAF1) | RAF | RAF proto-oncogene
serine/threonine-protein kinase (C-Raf) | RAF1 | RAF1_HUMAN | Raf-1 | Serine/threonine-protein kinase
RAF | Serine/threonine-protein kinase C-Raf | cRaf |
Type: | Serine/threonine-protein kinase |
Mol. Mass.: | 73082.52 |
Organism: | Homo sapiens (Human) |
Description: | P04049 |
Residue: | 648 |
Sequence: | MEHIQGAWKTISNGFGFKDAVFDGSSCISPTIVQQFGYQRRASDDGKLTDPSKTSNTIRV
FLPNKQRTVVNVRNGMSLHDCLMKALKVRGLQPECCAVFRLLHEHKGKKARLDWNTDAAS
LIGEELQVDFLDHVPLTTHNFARKTFLKLAFCDICQKFLLNGFRCQTCGYKFHEHCSTKV
PTMCVDWSNIRQLLLFPNSTIGDSGVPALPSLTMRRMRESVSRMPVSSQHRYSTPHAFTF
NTSSPSSEGSLSQRQRSTSTPNVHMVSTTLPVDSRMIEDAIRSHSESASPSALSSSPNNL
SPTGWSQPKTPVPAQRERAPVSGTQEKNKIRPRGQRDSSYYWEIEASEVMLSTRIGSGSF
GTVYKGKWHGDVAVKILKVVDPTPEQFQAFRNEVAVLRKTRHVNILLFMGYMTKDNLAIV
TQWCEGSSLYKHLHVQETKFQMFQLIDIARQTAQGMDYLHAKNIIHRDMKSNNIFLHEGL
TVKIGDFGLATVKSRWSGSQQVEQPTGSVLWMAPEVIRMQDNNPFSFQSDVYSYGIVLYE
LMTGELPYSHINNRDQIIFMVGRGYASPDLSKLYKNCPKAMKRLVADCVKKVKEERPLFP
QILSSIELLQHSLPKINRSASEPSLHRAAHTEDINACTLTTSPRLPVF
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Component 2 |
Name: | Dual specificity mitogen-activated protein kinase kinase 1 |
Synonyms: | Dual specificity mitogen-activated protein kinase (MEK) | Dual specificity mitogen-activated protein kinase kinase 1 (MEK) | Dual specificity mitogen-activated protein kinase kinase 1 (MEK1) | Dual specificity mitogen-activated protein kinase kinase 1/Mitogen-activated protein kinase 1/RAF proto-oncogene serine/threonine-protein kinase | Dual specificity mitogen-activated protein kinase kinase MEK1/2 | ERK activator kinase 1 | MAP kinase kinase 1 | MAP2K1 | MAPK/ERK kinase 1 | MAPK/ERK kinase 1 (MEK1) | MEK-1 | MEK1 | MP2K1_HUMAN | Mitogen-activated protein kinase 1 (MEK1) | PRKMK1 | VHL-MAP2K1/MAP2K2 |
Type: | Other Protein Type |
Mol. Mass.: | 43439.03 |
Organism: | Homo sapiens (Human) |
Description: | Full-length human MEK-1 was generated by PCR and purified as a fusion protein from Escherichia coli lysates. |
Residue: | 393 |
Sequence: | MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKV
GELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHE
CNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYL
REKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHY
SVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSY
GMDSRPPMAIFELLDYIVNEPPPKLPSGVFSLEFQDFVNKCLIKNPAERADLKQLMVHAF
IKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV
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BDBM50095232 |
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n/a |
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Name | BDBM50095232 |
Synonyms: | 6-Methoxy-7-(3-morpholin-4-yl-propoxy)-4-(4-phenoxy-phenylamino)-quinoline-3-carbonitrile | CHEMBL414139 |
Type | Small organic molecule |
Emp. Form. | C30H30N4O4 |
Mol. Mass. | 510.5836 |
SMILES | COc1cc2c(Nc3ccc(Oc4ccccc4)cc3)c(cnc2cc1OCCCN1CCOCC1)C#N |
Structure |
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