Target
Mitogen-activated protein kinase 1
Ligand
BDBM50265971
Substrate
n/a
Meas. Tech.
ChEMBL_1700375 (CHEMBL4051357)
IC50
<0.300000±n/a nM
Citation
 Ward, RABethel, PCook, CDavies, EDebreczeni, JEFairley, GFeron, LFlemington, VGraham, MAGreenwood, RGriffin, NHanson, LHopcroft, PHoward, TDHudson, JJames, MJones, CDJones, CRLamont, SLewis, RLindsay, NRoberts, KSimpson, ISt-Gallay, SSwallow, STang, JTonge, MWang, ZZhai, B Structure-Guided Discovery of Potent and Selective Inhibitors of ERK1/2 from a Modestly Active and Promiscuous Chemical Start Point. J Med Chem 60:3438-3450 (2017) [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:
BDBM50265971
Synonyms:
CHEMBL4087393
Type:
Small organic molecule
Emp. Form.:
C20H25N7O2
Mol. Mass.:
395.4582
SMILES:
COCCN1[C@@H](C)Cc2[nH]c(cc2C1=O)-c1nc(Nc2ccnn2C)ncc1C |r|
Structure:
Search PDB for entries with ligand similarity: