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TargetMitogen-activated protein kinase; ERK1/ERK2
LigandBDBM50396073
Substrate/Competitorn/a
Meas. Tech.ChEMBL_772881
IC50 16±n/a nM
Citation Liddle JAtkinson FLBarker MDCarter PSCurtis NRDavis RPDouault CDickson MCElwes DGarton NSGray MHayhow TGHobbs CIJones ELeach SLeavens KLewis HDMcCleary SNeu MPatel VKPreston AGRamirez-Molina CShipley TJSkone PASmithers NSomers DOWalker ALWatson RJWeingarten GG Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. Bioorg Med Chem Lett 21:6188-94 (2011) [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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BDBM50396073
n/a
NameBDBM50396073
Synonyms:CHEMBL1235110
TypeSmall organic molecule
Emp. Form.C18H24N6O
Mol. Mass.340.4228
SMILESCc1cccc(Nc2nc(N[C@@H]3CCCC[C@@H]3N)ncc2C(N)=O)c1 |r|
Structure
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