Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 1
Ligand
BDBM287030
Substrate
n/a
Meas. Tech.
Caliper-Based Kinase Assay
Temperature
298.15±n/a K
IC50
1.30±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:
BDBM287030
Synonyms:
8-(2-((1-acryloylazetidin-3-yl)oxy)ethyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-((2-morpholinoethyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one | US10294223, Cpd No. 70 | US11078199, Cpd 70 | US9567334, Example 70 | US9815834, Compound 70
Type:
Small organic molecule
Emp. Form.:
C29H34Cl2N6O6
Mol. Mass.:
633.523
SMILES:
COc1cc(OC)c(Cl)c(c1Cl)-c1cc2cnc(NCCN3CCOCC3)nc2n(CCOC2CN(C2)C(=O)C=C)c1=O |(2.39,7.86,;3.72,7.09,;3.72,5.55,;5.06,4.78,;5.06,3.24,;6.39,2.47,;7.73,3.24,;3.72,2.47,;3.72,.93,;2.39,3.24,;2.39,4.78,;1.06,5.55,;1.06,2.47,;-.28,3.24,;-1.61,2.47,;-2.94,3.24,;-4.28,2.47,;-4.28,.93,;-5.61,.16,;-5.61,-1.38,;-6.94,-2.15,;-6.94,-3.69,;-8.28,-4.46,;-8.28,-6,;-6.94,-6.77,;-5.61,-6,;-5.61,-4.46,;-2.94,.16,;-1.61,.93,;-.28,.16,;-.28,-1.38,;1.06,-2.15,;1.06,-3.69,;2.39,-4.46,;2.79,-5.95,;4.28,-5.55,;3.88,-4.06,;5.61,-6.32,;5.61,-7.86,;6.94,-5.55,;8.28,-6.32,;1.06,.93,;2.39,.16,)|
Structure:
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