Target
Mitogen-activated protein kinase 1
Ligand
BDBM50573872
Substrate
n/a
Meas. Tech.
ChEMBL_2121006 (CHEMBL4830153)
IC50
2.6±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 Chem 64:12286-12303 (2021) [PubMed]  Article 
Target
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:
MAAAAAAGAGPEMVRGQVFDVGPRYTNLSYIGEGAYGMVCSAYDNVNKVRVAIKKISPFEHQTYCQRTLREIKILLRFRHENIIGINDIIRAPTIEQMKDVYIVQDLMETDLYKLLKTQHLSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLLNTTCDLKICDFGLARVADPDHDHTGFLTEYVATRWYRAPEIMLNSKGYTKSIDIWSVGCILAEMLSNRPIFPGKHYLDQLNHILGILGSPSQEDLNCIINLKARNYLLSLPHKNKVPWNRLFPNADSKALDLLDKMLTFNPHKRIEVEQALAHPYLEQYYDPSDEPIAEAPFKFDMELDDLPKEKLKELIFEETARFQPGYRS
  
Inhibitor
Name:
BDBM50573872
Synonyms:
CHEMBL4868536
Type:
Small organic molecule
Emp. Form.:
C29H30ClN5O4
Mol. Mass.:
548.033
SMILES:
OC[C@@]1(CCc2ccccc12)NC(=O)CN1Cc2ccc(cc2C1=O)-c1nc(NC2CCOCC2)ncc1Cl |r|
Structure:
Search PDB for entries with ligand similarity: