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Target
Mitogen-activated protein kinase 1
Ligand
BDBM244099
Substrate
n/a
Meas. Tech.
Activated ERK2 Kinase Assay
pH
7.5±n/a
IC50
114±n/a nM
Comments
extracted
Citation
 Dillon, MP; Lindvall, M; Poon, D; Ramurthy, S; Rauniyar, V; Shafer, C; Subramanian, S; Tanner, HR Substituted pyrrolo[3,4-d]pyrimidines as kinase inhibitors US Patent  US9546173 Publication Date 1/17/2017 
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:
BDBM244099
Synonyms:
2-(((1r,4s)-4-cyanocyclohexyl)amino)-n-((s)-2-hydroxy-1-phenylethyl)-5,5-dimethyl-5h-pyrrolo[3,4-d]pyrimidine-6(7h)-carboxamide | US9546173, cmpd 81
Type:
Small organic molecule
Emp. Form.:
C24H30N6O2
Mol. Mass.:
434.534
SMILES:
CC1(C)N(Cc2nc(N[C@H]3CC[C@@H](CC3)C#N)ncc12)C(=O)N[C@H](CO)c1ccccc1 |r,wU:9.8,wD:23.25,12.15,(-1.29,5.91,;-.52,4.58,;.25,5.91,;.39,3.33,;-.52,2.08,;-1.98,2.56,;-3.32,1.79,;-4.65,2.56,;-5.98,1.79,;-5.98,.25,;-4.65,-.52,;-4.65,-2.06,;-5.98,-2.89,;-7.32,-2.06,;-7.32,-.52,;-5.98,-4.43,;-5.98,-5.97,;-4.65,4.1,;-3.32,4.87,;-1.98,4.1,;1.93,3.33,;2.7,4.66,;2.7,2,;4.24,2,;5.01,3.33,;6.55,3.33,;5.01,.66,;4.24,-.67,;5.01,-2,;6.55,-2,;7.32,-.67,;6.55,.66,)|
Structure:
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