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Target
Mitogen-activated protein kinase 1
Ligand
BDBM50532351
Substrate
n/a
Meas. Tech.
ChEMBL_1922956 (CHEMBL4425912)
IC50
0.900000±n/a nM
Citation
 Blake, JF; Burkard, M; Chan, J; Chen, H; Chou, KJ; Diaz, D; Dudley, DA; Gaudino, JJ; Gould, SE; Grina, J; Hunsaker, T; Liu, L; Martinson, M; Moreno, D; Mueller, L; Orr, C; Pacheco, P; Qin, A; Rasor, K; Ren, L; Robarge, K; Shahidi-Latham, S; Stults, J; Sullivan, F; Wang, W; Yin, J; Zhou, A; Belvin, M; Merchant, M; Moffat, J; Schwarz, JB Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development. J Med Chem 59:5650-60 (2016) [PubMed]  Article 
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:
BDBM50532351
Synonyms:
CHEMBL4565958
Type:
Small organic molecule
Emp. Form.:
C21H18ClFN6O2
Mol. Mass.:
440.858
SMILES:
Cc1n[nH]cc1Nc1nccc(n1)-c1ccn([C@H](CO)c2ccc(Cl)c(F)c2)c(=O)c1 |r|
Structure:
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