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TargetMitogen-activated protein kinase 3
LigandBDBM120095
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1922955 (CHEMBL4425911)
IC50 6.1±n/a nM
Citation Blake, JFBurkard, MChan, JChen, HChou, KJDiaz, DDudley, DAGaudino, JJGould, SEGrina, JHunsaker, TLiu, LMartinson, MMoreno, DMueller, LOrr, CPacheco, PQin, ARasor, KRen, LRobarge, KShahidi-Latham, SStults, JSullivan, FWang, WYin, JZhou, ABelvin, MMerchant, MMoffat, JSchwarz, JB Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development. J Med Chem59:5650-60 (2016) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Mitogen-activated protein kinase 3
Name:Mitogen-activated protein kinase 3
Synonyms:ERK1 | ERK1/ERK2 | Extracellular signal-regulated kinase 1 | Extracellular signal-regulated kinase 1 (ERK1) | MAP kinase ERK1 | MAPK3 | MAPK3/MAPK7 | MK03_HUMAN | Mitogen-activated protein kinase | Mitogen-activated protein kinase 3 | PRKM3
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:
BDBM120095
n/a
NameBDBM120095
Synonyms:US10525036, Example GDC-0994 | US10934304, Example GDC-0994 | US8697715, 39 | US9259470, 39
TypeSmall organic molecule
Emp. Form.C21H18ClFN6O2
Mol. Mass.440.858
SMILESCn1nccc1Nc1nccc(n1)-c1ccn([C@H](CO)c2ccc(Cl)c(F)c2)c(=O)c1 |r|
Structure
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