Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 1
Ligand
BDBM387929
Substrate
n/a
Meas. Tech.
FGFR Family Enzymatic Activity Assay
IC50
1.70±n/a nM
Citation
 Verner, E; Brameld, KA Quinolone derivatives as fibroblast growth factor receptor inhibitors US Patent  US10294223 Publication Date 5/21/2019 
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:
BDBM387929
Synonyms:
1-(2-((1-acryloylpiperidin-4-yl)(methyl)amino)ethyl)-3-(2,6-dichloro-3,5-dimethoxyphenyl)-7-(ethylamino)-1,6-naphthyridin-2(1H)-one | US10294223, Cpd No. 157 | US11078199, Cpd 157
Type:
Small organic molecule
Emp. Form.:
C29H35Cl2N5O4
Mol. Mass.:
588.525
SMILES:
CCNc1cc2n(CCN(C)C3CCN(CC3)C(=O)C=C)c(=O)c(cc2cn1)-c1c(Cl)c(OC)cc(OC)c1Cl |(-8.67,-.38,;-7.34,-1.16,;-6,-.38,;-4.67,-1.16,;-3.33,-.38,;-2,-1.16,;-.67,-.38,;-.67,1.16,;.67,1.93,;.67,3.46,;-.67,4.23,;2,4.23,;3.33,3.46,;4.67,4.23,;4.67,5.78,;3.33,6.55,;2,5.78,;6,6.55,;6,8.08,;7.34,5.78,;8.67,6.55,;.67,-1.16,;2,-.38,;.67,-2.7,;-.67,-3.46,;-2,-2.7,;-3.33,-3.46,;-4.67,-2.7,;2,-3.46,;2,-5,;.67,-5.78,;3.33,-5.78,;3.33,-7.32,;4.67,-8.08,;4.67,-5,;4.67,-3.46,;6,-2.7,;7.34,-3.46,;3.33,-2.7,;3.33,-1.16,)|
Structure:
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