Target
Mitogen-activated protein kinase 1
Ligand
BDBM365144
Substrate
n/a
Meas. Tech.
Enzymatic Assay
IC50
0.655±n/a nM
Citation
 Kolesnikov, ADo, S Serine/threonine kinase inhibitors US Patent  US9867833 Publication Date 1/16/2018 
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:
BDBM365144
Synonyms:
6-methyl-4-(2-((1-methyl-1H- pyrazol-5- yl)amino)pyrimidin-4-yl)-9- (2,2,2-trifluoroethyl)-8,9- dihydro-1,2,2a1,6- tetraazabenzo[cd]azulen- 7(6H)-one | US10278975, Compound I-71S | US11376260, Example I-71S | US9867833, Compound I-71(R)
Type:
Small organic molecule
Emp. Form.:
C20H18F3N9O
Mol. Mass.:
457.4118
SMILES:
CN1c2cc(cc3nnc([C@H](CC(F)(F)F)CC1=O)n23)-c1ccnc(Nc2ccnn2C)n1 |r|
Structure:
Search PDB for entries with ligand similarity: