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TargetMitogen-activated protein kinase; ERK1/ERK2
LigandBDBM50126732
Substrate/Competitorn/a
Meas. Tech.ChEMBL_124147
IC50>30000±n/a nM
Citation Goldberg DRButz TCardozo MGEckner RJHammach AHuang JJakes SKapadia SKashem MLukas SMorwick TMPanzenbeck MPatel UPav SPeet GWPeterson JDProkopowicz ASSnow RJSellati RTakahashi HTan JTschantz MAWang XJWang YWolak JXiong PMoss N Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase. J Med Chem 46:1337-49 (2003) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Mitogen-activated protein kinase; ERK1/ERK2
Name:Mitogen-activated protein kinase; ERK1/ERK2
Synonyms:pERK1/2 | t-ERK1/2
Type:n/a
Mol. Mass.:n/a
Description:ASSAY_ID of ChEMBL is 124147
Components:This complex has 2 components.
Component 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 | Mitogen activated kinase 1 (ERK-2) | Mitogen-activated protein kinase 1 (ERK-2) | Mitogen-activated protein kinase 1 (ERK2) | Mitogen-activated protein kinase 2 | 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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Component 2
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
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BDBM50126732
n/a
NameBDBM50126732
Synonyms:2-(2,6-Dichloro-phenylamino)-7-(3-diethylamino-propenyl)-1,6-dimethyl-1,8-dihydro-imidazo[4,5-h]isoquinolin-9-one | CHEMBL281957
TypeSmall organic molecule
Emp. Form.C25H27Cl2N5O
Mol. Mass.484.421
SMILESCCN(CC)CC=Cc1[nH]c(=O)c2c3n(C)c(Nc4c(Cl)cccc4Cl)nc3ccc2c1C |w:6.5|
Structure
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