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TargetDual specificity mitogen-activated protein kinase kinase 1
LigandBDBM50336316
Substrate/Competitorn/a
Meas. Tech.ChEMBL_471139 (CHEMBL938202)
IC50>10000±n/a nM
Citation Mulvihill, MJJi, QSCoate, HRCooke, ADong, HFeng, LForeman, KRosenfeld-Franklin, MHonda, AMak, GMulvihill, KMNigro, AIO'Connor, MPirrit, CSteinig, AGSiu, KStolz, KMSun, YTavares, PAYao, YGibson, NW Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors. Bioorg Med Chem16:1359-75 (2008) [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
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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BDBM50336316
n/a
NameBDBM50336316
Synonyms:CHEMBL410659 | cis-3-(3-(azetidin-1-ylmethyl)cyclobutyl)-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-8-amine | cis-3-(3-azetidin-1-ylmethylcyclobutyl)-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-8-ylamine
TypeSmall organic molecule
Emp. Form.C29H28N6
Mol. Mass.460.5728
SMILESNc1nccn2c(nc(-c3ccc4ccc(nc4c3)-c3ccccc3)c12)[C@@H]1C[C@H](CN2CCC2)C1 |wU:26.30,28.33,(7.04,-25.52,;7.05,-27.06,;5.72,-27.83,;5.72,-29.37,;7.05,-30.15,;8.39,-29.37,;9.86,-29.85,;10.77,-28.6,;9.86,-27.34,;10.64,-26.02,;9.88,-24.69,;10.64,-23.36,;12.19,-23.36,;12.96,-22.02,;14.5,-22.04,;15.28,-23.37,;14.5,-24.71,;12.96,-24.7,;12.18,-26.03,;16.82,-23.38,;17.59,-24.72,;19.13,-24.72,;19.9,-23.38,;19.12,-22.05,;17.59,-22.05,;8.39,-27.82,;10.34,-31.32,;9.65,-32.69,;11.02,-33.38,;11.5,-34.85,;10.47,-35.99,;8.93,-36.07,;9.01,-37.61,;10.55,-37.53,;11.72,-32.01,)|
Structure
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