Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 1
Ligand
BDBM287525
Substrate
n/a
Meas. Tech.
Caliper-Based Kinase Assay
Temperature
298.15±n/a K
IC50
11.9±n/a nM
Comments
extracted
Citation
 Verner, E; Brameld, KA Quinolone derivatives as fibroblast growth factor receptor inhibitors US Patent  US9567334 Publication Date 2/14/2017 
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:
BDBM287525
Synonyms:
8-(2-((1-acryloylazetidin-3-yl)oxy)ethyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-((2-(pyrrolidin-1-yl)ethyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one | US10294223, Cpd No. 93 | US11078199, Cpd 93 | US9567334, Example 93
Type:
Small organic molecule
Emp. Form.:
C29H34Cl2N6O5
Mol. Mass.:
617.523
SMILES:
COc1cc(OC)c(Cl)c(c1Cl)-c1cc2cnc(NCCN3CCCC3)nc2n(CCOC2CN(C2)C(=O)C=C)c1=O |(5.01,7.86,;3.68,7.09,;3.68,5.55,;5.01,4.78,;5.01,3.24,;6.35,2.47,;7.68,3.24,;3.68,2.47,;3.68,.93,;2.35,3.24,;2.35,4.78,;1.01,5.55,;1.01,2.47,;-.32,3.24,;-1.65,2.47,;-2.99,3.24,;-4.32,2.47,;-4.32,.93,;-5.65,.16,;-5.65,-1.38,;-6.99,-2.15,;-6.99,-3.69,;-8.23,-4.6,;-7.76,-6.06,;-6.22,-6.06,;-5.74,-4.6,;-2.99,.16,;-1.65,.93,;-.32,.16,;-.32,-1.38,;1.01,-2.15,;1.01,-3.69,;2.35,-4.46,;2.75,-5.95,;4.23,-5.55,;3.83,-4.06,;5.57,-6.32,;5.57,-7.86,;6.9,-5.55,;8.23,-6.32,;1.01,.93,;2.35,.16,)|
Structure:
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