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TargetMitogen-activated protein kinase 3
LigandBDBM50347388
Substrate/Competitorn/a
Meas. Tech.ChEMBL_754584
IC50 3730±n/a nM
Citation Heathcote DAPatel HKroll SHHazel PPeriyasamy MAlikian MKanneganti SKJogalekar ASScheiper BBarbazanges MBlum ABrackow JSiwicka APace RDFuchter MJSnyder JPLiotta DCFreemont PSAboagye EOCoombes RCBarrett AGAli S A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. J Med Chem 53:8508-22 (2010) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Mitogen-activated protein kinase 3
Name:MAP kinase ERK1
Synonyms:ERK1 | ERK1/ERK2 | Extracellular signal-regulated kinase 1 | Extracellular signal-regulated kinase 1 (ERK1) | MAP kinase ERK1 | Mitogen-activated protein kinase
Type:Protein
Mol. Mass.:43136.58
Organism:Homo sapiens (Human)
Description:curated by PDB 4QTB
Residue:379
Sequence:
MAAAAAQGGGGGEPRRTEGVGPGVPGEVEMVKGQPFDVGPRYTQLQYIGEGAYGMVSSAY
DHVRKTRVAIKKISPFEHQTYCQRTLREIQILLRFRHENVIGIRDILRASTLEAMRDVYI
VQDLMETDLYKLLKSQQLSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLINTTCDL
KICDFGLARIADPEHDHTGFLTEYVATRWYRAPEIMLNSKGYTKSIDIWSVGCILAEMLS
NRPIFPGKHYLDQLNHILGILGSPSQEDLNCIINMKARNYLQSLPSKTKVAWAKLFPKSD
SKALDLLDRMLTFNPNKRITVEEALAHPYLEQYYDPTDEPVAEEPFTFAMELDDLPKERL
KELIFQETARFQPGVLEAP
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50347388
n/a
NameBDBM50347388
Synonyms:CHEMBL1234833
TypeSmall organic molecule
Emp. Form.C20H27N5O3
Mol. Mass.385.4601
SMILESCC(C)c1cnn2c(NCc3ccccc3)cc(N[C@@H](CO)[C@H](O)CO)nc12 |r|
Structure
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