Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 1
Ligand
BDBM287526
Substrate
n/a
Meas. Tech.
Enzymatic Activity Assay
IC50
1.000±n/a nM
Citation
 Verner, E; Brameld, KA Quinolone derivatives as fibroblast growth factor receptor inhibitors US Patent  US9815834 Publication Date 11/14/2017 
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:
BDBM287526
Synonyms:
(R)-8-(2-((1-acryloylazetidin-3-yl)(methyl)amino)ethyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-((1-methoxypropan-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one | US10294223, Cpd No. 116 | US11078199, Cpd 116 | US9567334, Example 116 | US9815834, Compound 116
Type:
Small organic molecule
Emp. Form.:
C28H34Cl2N6O5
Mol. Mass.:
605.513
SMILES:
COC[C@@H](C)Nc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)c(=O)n(CCN(C)C3CN(C3)C(=O)C=C)c2n1 |r,wD:3.3,(-8.28,-4.46,;-6.94,-3.69,;-6.94,-2.15,;-5.61,-1.38,;-4.28,-2.15,;-5.61,.16,;-4.28,.93,;-4.28,2.47,;-2.94,3.24,;-1.61,2.47,;-.28,3.24,;1.06,2.47,;2.39,3.24,;2.39,4.78,;1.06,5.55,;3.72,5.55,;3.72,7.09,;5.06,7.86,;5.06,4.78,;5.06,3.24,;6.39,2.47,;7.73,3.24,;3.72,2.47,;3.72,.93,;1.06,.93,;2.39,.16,;-.28,.16,;-.28,-1.38,;1.06,-2.15,;1.06,-3.69,;-.28,-4.46,;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,;-1.61,.93,;-2.94,.16,)|
Structure:
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