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TargetDual specificity mitogen-activated protein kinase kinase 1
LigandBDBM50391802
Substrate/Competitorn/a
Meas. Tech.ChEMBL_850079
IC50 0.9±n/a nM
Citation Rice, KDAay, NAnand, NKBlazey, CMBowles, OJBussenius, JCostanzo, SCurtis, JKDefina, SCDubenko, LEngst, SJoshi, AAKennedy, ARKim, AIKoltun, ESLougheed, JCManalo, JCMartini, JFNuss, JMPeto, CJTsang, THYu, PJohnston, S Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973). ACS Med Chem Lett3:416-421 (2012) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Dual specificity mitogen-activated protein kinase kinase 1
Name:Dual specificity mitogen-activated protein kinase kinase 1/Mitogen-activated protein kinase 1/RAF proto-oncogene serine/threonine-protein kinase
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 MEK1/2 | ERK activator kinase 1 | MAP kinase kinase 1 | MAPK/ERK kinase 1 | MAPK/ERK kinase 1 (MEK1) | MEK-1 | Mitogen-activated protein kinase 1 (MEK1)
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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BDBM50391802
NameBDBM50391802
Synonyms:(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl)(3-hydroxy-3-(piperidin-2-yl)azetidin-1-yl)methanone | CHEMBL2146883 | COBIMETINIB FUMARATE | Cotellic | GDC-0973 | XL518 | cobimetinib
TypeSmall organic molecule
Emp. Form.C21H21F3IN3O2
Mol. Mass.531.31
SMILESOC1(CN(C1)C(=O)c1ccc(F)c(F)c1Nc1ccc(I)cc1F)[C@@H]1CCCCN1 |r|
Structure
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n/a