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Target
Mitogen-activated protein kinase 1
Ligand
BDBM50505994
Substrate
n/a
Meas. Tech.
ChEMBL_1824520 (CHEMBL4324284)
IC50
<0.300000±n/a nM
Citation
 Ward, RA; Anderton, MJ; Bethel, P; Breed, J; Cook, C; Davies, EJ; Dobson, A; Dong, Z; Fairley, G; Farrington, P; Feron, L; Flemington, V; Gibbons, FD; Graham, MA; Greenwood, R; Hanson, L; Hopcroft, P; Howells, R; Hudson, J; James, M; Jones, CD; Jones, CR; Li, Y; Lamont, S; Lewis, R; Lindsay, N; McCabe, J; McGuire, T; Rawlins, P; Roberts, K; Sandin, L; Simpson, I; Swallow, S; Tang, J; Tomkinson, G; Tonge, M; Wang, Z; Zhai, B Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC). J Med Chem 62:11004-11018 (2019) [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:
BDBM50505994
Synonyms:
CHEMBL4440109
Type:
Small organic molecule
Emp. Form.:
C23H22F2N8O
Mol. Mass.:
464.4706
SMILES:
C[C@H]1Cn2cc(nc2C(=O)N1Cc1ccc(F)c(F)c1)-c1nc(Nc2ccnn2C)ncc1C |r|
Structure:
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