Target
Mitogen-activated protein kinase 1
Ligand
BDBM365049
Substrate
n/a
Meas. Tech.
Enzymatic Assay
IC50
<0.020±n/a nM
Citation
 Kolesnikov, ADo, S Serine/threonine kinase inhibitors US Patent  US10842799 Publication Date 11/24/2020 
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:
BDBM365049
Synonyms:
4-(3-benzyl-3,4-dihydro-5- thia-1,2,2a1- triazaacenaphthylen-7-yl)-N- (1-methyl-1H-pyrazol-5- yl)pyrimidin-2-amine | US10517878, Compound I-16 | US10842799, I-16 | US9867833, Compound I-16(S)
Type:
Small organic molecule
Emp. Form.:
C23H20N8S
Mol. Mass.:
440.524
SMILES:
Cn1nccc1Nc1nccc(n1)-c1cc2SCC(Cc3ccccc3)c3nnc(c1)n23
Structure:
Search PDB for entries with ligand similarity: