Reaction Details | |||
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Target | Fibroblast growth factor receptor 1 | ||
Ligand | BDBM50238813 | ||
Substrate/Competitor | n/a | ||
Meas. Tech. | ChEBML_1664148 | ||
IC50 | 0.700000±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 | ||
Fibroblast growth factor receptor 1 | |||
Name: | Fibroblast growth factor receptor 1 | ||
Synonyms: | BFGFR | Basic fibroblast growth factor receptor 1 | Basic fibroblast growth factor receptor 1 (FGFR1) | CD_antigen=CD331 | CEK | FGFBR | FGFR-1 | FGFR-1 Tyrosine Kinase | FGFR-1, (FL) | FGFR1 | FGFR1_HUMAN | FLG | FLT2 | Fibroblast growth factor receptor (FGFR) | Fibroblast growth factor receptor 1 (FGFR-1) | Fibroblast growth factor receptor 1 (FGFR1) | Fms-like tyrosine kinase 2 | HBGFR | N-sam | VEGF-receptor 2 and Fibroblast growth factor receptor 1 | bFGF-R | c-fgr | ||
Type: | Receptor | ||
Mol. Mass.: | 91861.70 | ||
Organism: | Homo sapiens (Human) | ||
Description: | P11362 | ||
Residue: | 822 | ||
Sequence: |
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BDBM50238813 | |||
n/a | |||
Name | BDBM50238813 | ||
Synonyms: | CHEMBL4083740 | ||
Type | Small organic molecule | ||
Emp. Form. | C23H25Cl2N5O4 | ||
Mol. Mass. | 506.382 | ||
SMILES | CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCCCNC(=O)C=C)c2n1 |(28.89,-34.94,;28.89,-33.4,;30.23,-32.63,;30.23,-31.09,;31.56,-30.32,;32.89,-31.08,;34.23,-30.3,;35.57,-31.08,;36.9,-30.32,;36.9,-28.79,;35.56,-28.02,;38.23,-28.02,;38.23,-26.48,;39.56,-25.71,;39.57,-28.79,;39.56,-30.33,;40.9,-31.11,;42.23,-30.34,;38.23,-31.1,;38.22,-32.64,;35.56,-32.63,;36.89,-33.4,;34.22,-33.4,;34.22,-34.94,;35.55,-35.71,;35.54,-37.25,;36.88,-38.03,;36.87,-39.57,;38.2,-40.34,;39.54,-39.57,;38.2,-41.88,;39.53,-42.65,;32.89,-32.63,;31.56,-33.4,)| | ||
Structure |