Reaction Details |
| Report a problem with these data |
Target | Dual specificity mitogen-activated protein kinase kinase 1/RAF proto-oncogene serine/threonine-protein kinase |
---|
Ligand | BDBM50095229 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_100226 (CHEMBL710955) |
---|
IC50 | 28±n/a nM |
---|
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] |
---|
More Info.: | Get all data from this article, Assay Method |
---|
|
Dual specificity mitogen-activated protein kinase kinase 1/RAF proto-oncogene serine/threonine-protein kinase |
---|
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
|
|
|
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
|
|
|
BDBM50095229 |
---|
n/a |
---|
Name | BDBM50095229 |
Synonyms: | 7-(3-Morpholin-4-yl-propoxy)-4-(4-phenoxy-phenylamino)-quinoline-3-carbonitrile | CHEMBL94965 |
Type | Small organic molecule |
Emp. Form. | C29H28N4O3 |
Mol. Mass. | 480.5576 |
SMILES | N#Cc1cnc2cc(OCCCN3CCOCC3)ccc2c1Nc1ccc(Oc2ccccc2)cc1 |
Structure |
|