Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 1
Ligand
BDBM287521
Substrate
n/a
Meas. Tech.
Caliper-Based Kinase Assay
Temperature
298.15±n/a K
IC50
2.10±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:
BDBM287521
Synonyms:
(S)¿N-(1-(2-(6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(ethylamino)-7-oxopyrido[2,3-d]-pyrimidin-8(7H)-yl)ethyl)piperidin-3-yl)acrylamide | US11078199, Cpd 137 | US9567334, Example 137
Type:
Small organic molecule
Emp. Form.:
C27H32Cl2N6O4
Mol. Mass.:
575.487
SMILES:
CCNc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCN3CCC[C@@H](C3)NC(=O)C=C)c2n1 |r,wU:30.33,(-7.34,-2.7,;-6,-1.93,;-6,-.39,;-4.67,.38,;-4.67,1.92,;-3.33,2.69,;-2,1.92,;-.67,2.69,;.67,1.92,;2,2.69,;2,4.23,;.67,5,;3.33,5.01,;3.33,6.55,;4.67,7.32,;4.67,4.23,;4.67,2.69,;6,1.92,;7.34,2.69,;3.33,1.92,;3.33,.38,;.67,.38,;2,-.39,;-.67,-.39,;-.67,-1.93,;.67,-2.7,;.67,-4.24,;-.67,-5.01,;-.67,-6.54,;.67,-7.31,;2,-6.54,;2,-5.01,;3.33,-7.32,;4.67,-6.55,;4.67,-5.01,;6,-7.32,;7.34,-6.55,;-2,.38,;-3.33,-.39,)|
Structure:
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