Reaction Details |
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Target | Mitogen-activated protein kinase 3 |
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Ligand | BDBM120095 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1922955 (CHEMBL4425911) |
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IC50 | 6.1±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 3 |
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Name: | Mitogen-activated protein kinase 3 |
Synonyms: | ERK1 | ERK1/ERK2 | Extracellular signal-regulated kinase 1 | Extracellular signal-regulated kinase 1 (ERK1) | MAP kinase ERK1 | MAPK3 | MAPK3/MAPK7 | MK03_HUMAN | Mitogen-activated protein kinase | Mitogen-activated protein kinase 3 | PRKM3 |
Type: | Protein |
Mol. Mass.: | 43136.58 |
Organism: | Homo sapiens (Human) |
Description: | curated by PDB 4QTB |
Residue: | 379 |
Sequence: | MAAAAAQGGGGGEPRRTEGVGPGVPGEVEMVKGQPFDVGPRYTQLQYIGEGAYGMVSSAY
DHVRKTRVAIKKISPFEHQTYCQRTLREIQILLRFRHENVIGIRDILRASTLEAMRDVYI
VQDLMETDLYKLLKSQQLSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLINTTCDL
KICDFGLARIADPEHDHTGFLTEYVATRWYRAPEIMLNSKGYTKSIDIWSVGCILAEMLS
NRPIFPGKHYLDQLNHILGILGSPSQEDLNCIINMKARNYLQSLPSKTKVAWAKLFPKSD
SKALDLLDRMLTFNPNKRITVEEALAHPYLEQYYDPTDEPVAEEPFTFAMELDDLPKERL
KELIFQETARFQPGVLEAP
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BDBM120095 |
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n/a |
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Name | BDBM120095 |
Synonyms: | US10525036, Example GDC-0994 | US10934304, Example GDC-0994 | US8697715, 39 | US9259470, 39 |
Type | Small organic molecule |
Emp. Form. | C21H18ClFN6O2 |
Mol. Mass. | 440.858 |
SMILES | Cn1nccc1Nc1nccc(n1)-c1ccn([C@H](CO)c2ccc(Cl)c(F)c2)c(=O)c1 |r| |
Structure |
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