Reaction Details | |||
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Target | Tyrosine-protein kinase Lyn | ||
Ligand | BDBM286984 | ||
Substrate/Competitor | n/a | ||
Meas. Tech. | ChEMBL_1664163 (CHEMBL4013844) | ||
IC50 | 631±n/a nM | ||
Citation | Brameld, KA; Owens, TD; Verner, E; Venetsanakos, E; Bradshaw, JM; Phan, VT; Tam, D; Leung, K; Shu, J; LaStant, J; Loughhead, DG; Ton, T; Karr, DE; Gerritsen, ME; Goldstein, DM; Funk, JO Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors. J Med Chem60:6516-6527 (2017) [PubMed] Article | ||
More Info.: | Get all data from this article, Assay Method | ||
Tyrosine-protein kinase Lyn | |||
Name: | Tyrosine-protein kinase Lyn | ||
Synonyms: | JTK8 | LYN | LYN_HUMAN | Lck/Yes-related novel protein tyrosine kinase | Tyrosine-protein kinase Lyn (LYN) | V-yes-1 Yamaguchi sarcoma viral related oncogene homolog | p53Lyn | p56Lyn | ||
Type: | Protein | ||
Mol. Mass.: | 58575.92 | ||
Organism: | Homo sapiens (Human) | ||
Description: | P07948 | ||
Residue: | 512 | ||
Sequence: |
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BDBM286984 | |||
n/a | |||
Name | BDBM286984 | ||
Synonyms: | 8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one | US10294223, Cpd No. 6 | US11078199, Cpd 6 | US9567334, Example 6 | US9815834, Compound 6 | ||
Type | Small organic molecule | ||
Emp. Form. | C26H30Cl2N6O4 | ||
Mol. Mass. | 561.46 | ||
SMILES | CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCCN3CCN(CC3)C(=O)C=C)c2n1 |(-6.67,-.77,;-6.67,.77,;-5.33,1.54,;-5.33,3.08,;-4,3.85,;-2.67,3.08,;-1.33,3.85,;,3.08,;1.33,3.85,;1.33,5.39,;,6.16,;2.67,6.16,;2.67,7.7,;1.33,8.47,;4,5.39,;4,3.85,;5.33,3.08,;6.67,3.85,;2.67,3.08,;2.67,1.54,;,1.54,;1.33,.77,;-1.33,.77,;-1.33,-.77,;,-1.54,;,-3.08,;1.33,-3.85,;1.33,-5.39,;2.67,-6.16,;4,-5.39,;4,-3.85,;2.67,-3.08,;5.33,-6.16,;6.67,-5.39,;5.33,-7.7,;6.67,-8.47,;-2.67,1.54,;-4,.77,)| | ||
Structure |