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TargetMitogen-activated protein kinase 1
LigandBDBM418007
Substrate/Competitorn/a
Meas. Tech.ChEMBL_2121006 (CHEMBL4830153)
IC50 2.7±n/a nM
Citation Heightman, TDBerdini, VBevan, LBuck, IMCarr, MGCourtin, ACoyle, JEDay, JEHEast, CFazal, LGriffiths-Jones, CMHoward, SKucia-Tran, JMartins, VMuench, SMunck, JMNorton, DO'Reilly, MPalmer, NPathuri, PPeakman, TMReader, MRees, DCRich, SJShah, AWallis, NGWalton, HWilsher, NEWoolford, AJCooke, MCousin, DOnions, SShannon, JWatts, JMurray, CW Discovery of ASTX029, A Clinical Candidate Which Modulates the Phosphorylation and Catalytic Activity of ERK1/2. J Med Chem64:12286-12303 (2021) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Mitogen-activated protein kinase 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:
BDBM418007
n/a
NameBDBM418007
Synonyms:US10457669, Example 1083 | US10457669, Example 685 | US11001575, Example 685
TypeSmall organic molecule
Emp. Form.C29H31ClFN5O5
Mol. Mass.584.038
SMILESCOc1cc(F)cc(c1)[C@@H](CO)NC(=O)[C@@H](C)N1Cc2ccc(cc2C1=O)-c1nc(NC2CCOCC2)ncc1Cl |r|
Structure
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