Target
Fibroblast growth factor receptor 1
Ligand
BDBM387926
Substrate
n/a
Meas. Tech.
Enzymatic Activity Assay
IC50
0.700±n/a nM
Citation
 Verner, EBrameld, KA Quinolone derivatives as fibroblast growth factor receptor inhibitors US Patent  US11078199 Publication Date 8/3/2021 
Target
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:
MWSWKCLLFWAVLVTATLCTARPSPTLPEQAQPWGAPVEVESFLVHPGDLLQLRCRLRDDVQSINWLRDGVQLAESNRTRITGEEVEVQDSVPADSGLYACVTSSPSGSDTTYFSVNVSDALPSSEDDDDDDDSSSEEKETDNTKPNRMPVAPYWTSPEKMEKKLHAVPAAKTVKFKCPSSGTPNPTLRWLKNGKEFKPDHRIGGYKVRYATWSIIMDSVVPSDKGNYTCIVENEYGSINHTYQLDVVERSPHRPILQAGLPANKTVALGSNVEFMCKVYSDPQPHIQWLKHIEVNGSKIGPDNLPYVQILKTAGVNTTDKEMEVLHLRNVSFEDAGEYTCLAGNSIGLSHHSAWLTVLEALEERPAVMTSPLYLEIIIYCTGAFLISCMVGSVIVYKMKSGTKKSDFHSQMAVHKLAKSIPLRRQVTVSADSSASMNSGVLLVRPSRLSSSGTPMLAGVSEYELPEDPRWELPRDRLVLGKPLGEGCFGQVVLAEAIGLDKDKPNRVTKVAVKMLKSDATEKDLSDLISEMEMMKMIGKHKNIINLLGACTQDGPLYVIVEYASKGNLREYLQARRPPGLEYCYNPSHNPEEQLSSKDLVSCAYQVARGMEYLASKKCIHRDLAARNVLVTEDNVMKIADFGLARDIHHIDYYKKTTNGRLPVKWMAPEALFDRIYTHQSDVWSFGVLLWEIFTLGGSPYPGVPVEELFKLLKEGHRMDKPSNCTNELYMMMRDCWHAVPSQRPTFKQLVEDLDRIVALTSNQEYLDLSMPLDQYSPSFPDTRSSTCSSGEDSVFSHEPLPEEPCLPRHPAQLANGGLKRR
  
Inhibitor
Name:
BDBM387926
Synonyms:
1-(2-((1-acryloylazetidin-3-yl)(2-methoxyethyl)amino)ethyl)-3-(2,6-dichloro-3,5-dimethoxyphenyl)-7-(methylamino)-1,6-naphthyridin-2(1H)-one | US10294223, Cpd No. 153 | US11078199, Cpd 153
Type:
Small organic molecule
Emp. Form.:
C28H33Cl2N5O5
Mol. Mass.:
590.498
SMILES:
CNc1cc2n(CCN(CCOC)C3CN(C3)C(=O)C=C)c(=O)c(cc2cn1)-c1c(Cl)c(OC)cc(OC)c1Cl |(-4,-5.71,;-2.67,-6.48,;-1.33,-5.71,;-1.33,-4.17,;,-3.4,;,-1.86,;-1.33,-1.09,;-2.67,-1.86,;-4,-1.09,;-5.33,-1.86,;-6.67,-1.09,;-8,-1.86,;-9.34,-1.09,;-4,.45,;-5.09,1.54,;-4,2.63,;-2.91,1.54,;-4,4.17,;-2.67,4.94,;-5.33,4.94,;-5.33,6.48,;1.33,-1.09,;1.33,.45,;2.67,-1.86,;2.67,-3.4,;1.33,-4.17,;1.33,-5.71,;,-6.48,;4,-1.09,;4,.45,;2.67,1.22,;5.33,1.22,;5.33,2.76,;6.67,3.53,;6.67,.45,;6.67,-1.09,;8,-1.86,;9.34,-1.09,;5.33,-1.86,;5.33,-3.4,)|
Structure:
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