Target
Mitogen-activated protein kinase 1
Ligand
BDBM365158
Substrate
n/a
Meas. Tech.
Enzymatic Assay
IC50
4.61±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:
BDBM365158
Synonyms:
4-(9-((5-chloropyridin-3- yl)oxy)-8,9-dihydro-7H-6- oxa-1,2,2a1- triazabenzo[cd]azulen-4-yl)- N-(1-methyl-1H-pyrazol-5- yl)pyridin-2-amine | US10517878, Compound I-78 | US10842799, I-78 | US9867833, Compound I-78(S)
Type:
Small organic molecule
Emp. Form.:
C23H19ClN8O2
Mol. Mass.:
474.902
SMILES:
Cn1nccc1Nc1cc(ccn1)-c1cc2OCCC(Oc3cncc(Cl)c3)c3nnc(c1)n23
Structure:
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