Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 1
Ligand
BDBM287537
Substrate
n/a
Meas. Tech.
Caliper-Based Kinase Assay
Temperature
298.15±n/a K
IC50
3.40±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:
BDBM287537
Synonyms:
8-(2-((1-acryloylazetidin-3-yl)oxy)ethyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-((3-(4-methylpiperazin-1-yl)propyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one | US10294223, Cpd No. 97 | US11078199, Cpd 97 | US9567334, Example 97
Type:
Small organic molecule
Emp. Form.:
C31H39Cl2N7O5
Mol. Mass.:
660.591
SMILES:
COc1cc(OC)c(Cl)c(c1Cl)-c1cc2cnc(NCCCN3CCN(C)CC3)nc2n(CCOC2CN(C2)C(=O)C=C)c1=O |(7.06,7.86,;5.73,7.09,;5.73,5.55,;7.06,4.78,;7.06,3.24,;8.39,2.47,;9.73,3.24,;5.73,2.47,;5.73,.93,;4.39,3.24,;4.39,4.78,;3.06,5.55,;3.06,2.47,;1.72,3.24,;.39,2.47,;-.94,3.24,;-2.28,2.47,;-2.28,.93,;-3.61,.16,;-3.61,-1.38,;-4.94,-2.15,;-4.94,-3.69,;-6.28,-4.46,;-7.61,-3.69,;-8.95,-4.46,;-8.95,-6,;-10.28,-6.77,;-7.61,-6.77,;-6.28,-6,;-.94,.16,;.39,.93,;1.72,.16,;1.72,-1.38,;3.06,-2.15,;3.06,-3.69,;4.39,-4.46,;4.79,-5.95,;6.28,-5.55,;5.88,-4.06,;7.61,-6.32,;7.61,-7.86,;8.95,-5.55,;10.28,-6.32,;3.06,.93,;4.39,.16,)|
Structure:
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