Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 1
Ligand
BDBM287517
Substrate
n/a
Meas. Tech.
FGFR Family Enzymatic Activity Assay
IC50
1.40±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:
BDBM287517
Synonyms:
(S)-8-((1-(1-acryloylazetidin-3-yl)pyrrolidin-2-yl)methyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one | US10294223, Cpd No. 113 | US11078199, Cpd 113 | US9567334, Example 113 | US9815834, Compound 113
Type:
Small organic molecule
Emp. Form.:
C27H30Cl2N6O4
Mol. Mass.:
573.471
SMILES:
CNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(C[C@@H]3CCCN3C3CN(C3)C(=O)C=C)c2n1 |r,wU:24.24,(-6.67,-.86,;-6.67,.68,;-5.33,1.45,;-5.33,2.99,;-4,3.76,;-2.67,2.99,;-1.33,3.76,;,2.99,;1.33,3.76,;1.33,5.3,;,6.07,;2.67,6.07,;2.67,7.61,;4,8.38,;4,5.3,;4,3.76,;5.33,2.99,;6.67,3.76,;2.67,2.99,;2.67,1.45,;,1.45,;1.33,.68,;-1.33,.68,;-1.33,-.86,;-2.67,-1.63,;-4.13,-1.16,;-5.04,-2.4,;-4.13,-3.65,;-2.67,-3.17,;-1.58,-4.26,;-1.58,-5.8,;-.04,-5.8,;-.04,-4.26,;1.05,-6.89,;.65,-8.38,;2.54,-6.49,;3.63,-7.58,;-2.67,1.45,;-4,.68,)|
Structure:
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