Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetMitogen-activated protein kinase 1/3
LigandBDBM50419258
Substrate/Competitorn/a
Meas. Tech.ChEMBL_772881 (CHEMBL1838284)
IC50 79±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 Lett21:6188-94 (2011) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Mitogen-activated protein kinase 1/3
Name:Mitogen-activated protein kinase 1/3
Synonyms:Mitogen-activated protein kinase; ERK1/ERK2 | 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 | 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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
Component 2
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:
BDBM50419258
n/a
NameBDBM50419258
Synonyms:CHEMBL1835070
TypeSmall organic molecule
Emp. Form.C18H24N6O
Mol. Mass.340.4228
SMILESCc1ccc(Nc2nc(N[C@@H]3CCCC[C@@H]3N)ncc2C(N)=O)cc1 |r|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: