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| Reaction Details | |||
|---|---|---|---|
 | Report a problem with these data | ||
| Target | Vascular endothelial growth factor receptor 2 | ||
| Ligand | BDBM286984 | ||
| Substrate/Competitor | n/a | ||
| Meas. Tech. | ChEMBL_1664139 (CHEMBL4013820) | ||
| IC50 | 705±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 | ||
| Vascular endothelial growth factor receptor 2 | |||
| Name: | Vascular endothelial growth factor receptor 2 | ||
| Synonyms: | CD_antigen=CD309 | FLK1 | Fetal liver kinase 1 (FLK-1) | Flk-1/KDR | KDR | Kinase Insert Domain Receptor | Protein-tyrosine kinase receptor Flk-1 | VEGFR kinase (KDR) | VEGFR-2 | VEGFR-2 (KDR) | VEGFR2 | VGFR2_HUMAN | Vascular Endothelial Growth Factor Receptor Kinase 2 | Vascular endothelial growth factor receptor (VEGFR-2) | Vascular endothelial growth factor receptor 2 (KDR) | Vascular endothelial growth factor receptor 2 (VEGFR-2) | Vascular endothelial growth factor receptor 2 (VEGFR2) | Vascular endothelial growth factor receptor 2 precursor (VEGFR-2) | Vascular endothelial growth factor receptor-2 (VEGFR-2) | ||
| Type: | Receptor Tyrosine Kinase | ||
| Mol. Mass.: | 151510.97 | ||
| Organism: | Homo sapiens (Human) | ||
| Description: | P35968 | ||
| Residue: | 1356 | ||
| Sequence: |
| ||
| 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 | 
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