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Target
Mitogen-activated protein kinase 1 [8-360]
Ligand
BDBM192356
Substrate
n/a
Meas. Tech.
Enzymatic Assay
pH
7.3±n/a
IC50
1.6±n/a nM
Comments
extracted
Citation
 Blake, JF; Chen, H; Chicarelli, MJ; Demeese, J; Garrey, RF; Gaudino, J; Gazzard, L; Kaus, RJ; Kintz, S; Mohr, PJ; Moreno, DA; Schwarz, J; Siedem, CS; Wallace, EM Substituted quinazolines as serine/threonine kinase inhibitors US Patent  US9187462 Publication Date 11/17/2015 
Target
Name:
Mitogen-activated protein kinase 1 [8-360]
Synonyms:
ERK2 | Human ERK-2 | MAPK1 | MK01_HUMAN | Mitogen Activated Kinase 1 | Mitogen-activated protein kinase 1 (ERK-2) | Mitogen-activated protein kinase 1 (aa 8-360) | PRKM1 | PRKM2
Type:
n/a
Mol. Mass.:
40835.09
Organism:
Homo sapiens (Human)
Description:
P28482 aa 8-360
Residue:
353
Sequence:
GAGPEMVRGQVFDVGPRYTNLSYIGEGAYGMVCSAYDNVNKVRVAIKKISPFEHQTYCQRTLREIKILLRFRHENIIGINDIIRAPTIEQMKDVYIVQDLMETDLYKLLKTQHLSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLLNTTCDLKICDFGLARVADPDHDHTGFLTEYVATRWYRAPEIMLNSKGYTKSIDIWSVGCILAEMLSNRPIFPGKHYLDQLNHILGILGSPSQEDLNCIINLKARNYLLSLPHKNKVPWNRLFPNADSKALDLLDKMLTFNPHKRIEVEQALAHPYLEQYYDPSDEPIAEAPFKFDMELDDLPKEKLKELIFEETARFQPGYRS
  
Inhibitor
Name:
BDBM192356
Synonyms:
US9187462, I-36
Type:
Small organic molecule
Emp. Form.:
C25H26ClF2N5O2
Mol. Mass.:
501.956
SMILES:
Fc1ccc(cc1Cl)[C@H](NC(=O)c1ccc2cnc(NC3CCOCC3)nc2c1)[C@]1(F)CCNC1 |r|
Structure:
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