Reaction Details |
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Target | Mitogen-activated protein kinase 1 |
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Ligand | BDBM50532352 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1922956 (CHEMBL4425912) |
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IC50 | 16±n/a nM |
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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 Chem59:5650-60 (2016) [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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BDBM50532352 |
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n/a |
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Name | BDBM50532352 |
Synonyms: | CHEMBL4452981 |
Type | Small organic molecule |
Emp. Form. | C22H20ClFN6O2 |
Mol. Mass. | 454.885 |
SMILES | CCn1nccc1Nc1nccc(n1)-c1ccn([C@H](CO)c2ccc(Cl)c(F)c2)c(=O)c1 |r| |
Structure |
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