Reaction Details |
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Target | Mitogen-activated protein kinase 1 |
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Ligand | BDBM50505988 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1824520 (CHEMBL4324284) |
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IC50 | <0.300000±n/a nM |
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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 Chem62:11004-11018 (2019) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Mitogen-activated protein kinase 1 |
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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: | MAAAAAAGAGPEMVRGQVFDVGPRYTNLSYIGEGAYGMVCSAYDNVNKVRVAIKKISPFE
HQTYCQRTLREIKILLRFRHENIIGINDIIRAPTIEQMKDVYIVQDLMETDLYKLLKTQH
LSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLLNTTCDLKICDFGLARVADPDHDH
TGFLTEYVATRWYRAPEIMLNSKGYTKSIDIWSVGCILAEMLSNRPIFPGKHYLDQLNHI
LGILGSPSQEDLNCIINLKARNYLLSLPHKNKVPWNRLFPNADSKALDLLDKMLTFNPHK
RIEVEQALAHPYLEQYYDPSDEPIAEAPFKFDMELDDLPKEKLKELIFEETARFQPGYRS
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BDBM50505988 |
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n/a |
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Name | BDBM50505988 |
Synonyms: | CHEMBL4482864 |
Type | Small organic molecule |
Emp. Form. | C24H24F2N8O2 |
Mol. Mass. | 494.4966 |
SMILES | COC[C@H]1Cn2cc(nc2C(=O)N1Cc1ccc(F)c(F)c1)-c1nc(Nc2ccnn2C)ncc1C |r| |
Structure |
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