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TargetMitogen-activated protein kinase 1
LigandBDBM50505988
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1824520 (CHEMBL4324284)
IC50<0.300000±n/a nM
Citation Ward, RAAnderton, MJBethel, PBreed, JCook, CDavies, EJDobson, ADong, ZFairley, GFarrington, PFeron, LFlemington, VGibbons, FDGraham, MAGreenwood, RHanson, LHopcroft, PHowells, RHudson, JJames, MJones, CDJones, CRLi, YLamont, SLewis, RLindsay, NMcCabe, JMcGuire, TRawlins, PRoberts, KSandin, LSimpson, ISwallow, STang, JTomkinson, GTonge, MWang, ZZhai, B Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC). J Med Chem62:11004-11018 (2019) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Mitogen-activated protein kinase 1
Name:Mitogen-activated protein kinase 1
Synonyms:ERK2 | ERT1 | Extracellular signal-regulated kinase 2 | Extracellular signal-regulated kinase 2 (ERK-2) | Extracellular signal-regulated kinase 2 (ERK2) | MAP Kinase 2/ERK2 | MAPK 2 | MAPK1 | MK01_HUMAN | Mitogen activated kinase 1 (ERK-2) | Mitogen-activated protein kinase 1 (ERK-2) | Mitogen-activated protein kinase 1 (ERK2) | Mitogen-activated protein kinase 2 | PRKM1 | PRKM2 | p42-MAPK
Type:Ser/Thr Protein Kinase
Mol. Mass.:41392.76
Organism:Homo sapiens (Human)
Description:P28482
Residue:360
Sequence:
MAAAAAAGAGPEMVRGQVFDVGPRYTNLSYIGEGAYGMVCSAYDNVNKVRVAIKKISPFE
HQTYCQRTLREIKILLRFRHENIIGINDIIRAPTIEQMKDVYIVQDLMETDLYKLLKTQH
LSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLLNTTCDLKICDFGLARVADPDHDH
TGFLTEYVATRWYRAPEIMLNSKGYTKSIDIWSVGCILAEMLSNRPIFPGKHYLDQLNHI
LGILGSPSQEDLNCIINLKARNYLLSLPHKNKVPWNRLFPNADSKALDLLDKMLTFNPHK
RIEVEQALAHPYLEQYYDPSDEPIAEAPFKFDMELDDLPKEKLKELIFEETARFQPGYRS
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BDBM50505988
n/a
NameBDBM50505988
Synonyms:CHEMBL4482864
TypeSmall organic molecule
Emp. Form.C24H24F2N8O2
Mol. Mass.494.4966
SMILESCOC[C@H]1Cn2cc(nc2C(=O)N1Cc1ccc(F)c(F)c1)-c1nc(Nc2ccnn2C)ncc1C |r|
Structure
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