Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 1
Ligand
BDBM287519
Substrate
n/a
Meas. Tech.
Enzymatic Activity Assay
IC50
3.60±n/a nM
Citation
 Verner, E; Brameld, KA Quinolone derivatives as fibroblast growth factor receptor inhibitors US Patent  US9815834 Publication Date 11/14/2017 
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:
BDBM287519
Synonyms:
8-(2-((1-acryloylazetidin-3-yl)oxy)ethyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-((3-(4-ethylpiperazin-1-yl)propyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one | US10294223, Cpd No. 91 | US11078199, Cpd 91 | US9567334, Example 91 | US9815834, Compound 91
Type:
Small organic molecule
Emp. Form.:
C32H41Cl2N7O5
Mol. Mass.:
674.618
SMILES:
CCN1CCN(CCCNc2ncc3cc(-c4c(Cl)c(OC)cc(OC)c4Cl)c(=O)n(CCOC4CN(C4)C(=O)C=C)c3n2)CC1 |(-10.28,-8.09,;-10.28,-6.55,;-8.95,-5.78,;-8.95,-4.24,;-7.61,-3.47,;-6.28,-4.24,;-4.94,-3.47,;-4.94,-1.93,;-3.61,-1.16,;-3.61,.38,;-2.28,1.15,;-2.28,2.69,;-.94,3.46,;.39,2.69,;1.72,3.46,;3.06,2.69,;4.39,3.46,;4.39,5,;3.06,5.77,;5.73,5.78,;5.73,7.32,;7.06,8.09,;7.06,5,;7.06,3.46,;8.39,2.69,;9.73,3.46,;5.73,2.69,;5.73,1.15,;3.06,1.15,;4.39,.38,;1.72,.38,;1.72,-1.16,;3.06,-1.93,;3.06,-3.47,;4.39,-4.24,;4.79,-5.72,;6.28,-5.32,;5.88,-3.84,;7.61,-6.09,;7.61,-7.63,;8.95,-5.32,;10.28,-6.09,;.39,1.15,;-.94,.38,;-6.28,-5.78,;-7.61,-6.55,)|
Structure:
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