Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 1
Ligand
BDBM287528
Substrate
n/a
Meas. Tech.
Enzymatic Activity Assay
IC50
1.20±n/a nM
Citation
 Verner, E; Brameld, 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:
BDBM287528
Synonyms:
8-(2-((1-acryloylazetidin-3-yl)oxy)ethyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-((2-(4-ethylpiperazin-1-yl)ethyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one | US10294223, Cpd No. 94 | US11078199, Cpd 94 | US9567334, Example 94 | US9815834, Compound 94
Type:
Small organic molecule
Emp. Form.:
C31H39Cl2N7O5
Mol. Mass.:
660.591
SMILES:
CCN1CCN(CCNc2ncc3cc(-c4c(Cl)c(OC)cc(OC)c4Cl)c(=O)n(CCOC4CN(C4)C(=O)C=C)c3n2)CC1 |(-5.61,-8.47,;-6.94,-7.7,;-6.94,-6.16,;-8.28,-5.39,;-8.28,-3.85,;-6.94,-3.08,;-6.94,-1.54,;-5.61,-.77,;-5.61,.77,;-4.28,1.54,;-4.28,3.08,;-2.94,3.85,;-1.61,3.08,;-.28,3.85,;1.06,3.08,;2.39,3.85,;2.39,5.39,;1.06,6.16,;3.72,6.16,;3.72,7.7,;5.06,8.47,;5.06,5.39,;5.06,3.85,;6.39,3.08,;7.73,3.85,;3.72,3.08,;3.72,1.54,;1.06,1.54,;2.39,.77,;-.28,.77,;-.28,-.77,;1.06,-1.54,;1.06,-3.08,;2.39,-3.85,;2.79,-5.34,;4.28,-4.94,;3.88,-3.45,;5.61,-5.71,;5.61,-7.25,;6.94,-4.94,;8.28,-5.71,;-1.61,1.54,;-2.94,.77,;-5.61,-3.85,;-5.61,-5.39,)|
Structure:
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