Target
Fibroblast growth factor receptor 1
Ligand
BDBM287536
Substrate
n/a
Meas. Tech.
Enzymatic Activity Assay
IC50
1.20±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:
BDBM287536
Synonyms:
1-(3-(4-acryloylpiperazin-1-yl)propyl)-3-(2,6-dichloro-3,5-dimethoxyphenyl)-7-(methylamino)-1,6-naphthyridin-2(1H)-one | US11078199, Cpd 142 | US9567334, Example 142
Type:
Small organic molecule
Emp. Form.:
C27H31Cl2N5O4
Mol. Mass.:
560.472
SMILES:
CNc1cc2n(CCCN3CCN(CC3)C(=O)C=C)c(=O)c(cc2cn1)-c1c(Cl)c(OC)cc(OC)c1Cl |(-7.34,-1.16,;-7.34,.38,;-6,1.15,;-4.67,.38,;-3.33,1.15,;-2,.38,;-2,-1.16,;-.67,-1.93,;-.67,-3.47,;.67,-4.24,;.67,-5.78,;2,-6.55,;3.33,-5.78,;3.33,-4.24,;2,-3.46,;4.67,-6.55,;4.67,-8.09,;6,-5.78,;7.34,-6.55,;-.67,1.15,;.67,.38,;-.67,2.69,;-2,3.46,;-3.33,2.69,;-4.67,3.46,;-6,2.69,;.67,3.46,;.67,5,;-.67,5.77,;2,5.78,;2,7.32,;3.33,8.09,;3.33,5,;3.33,3.46,;4.67,2.69,;6,3.46,;2,2.69,;2,1.15,)|
Structure:
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