Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 1
Ligand
BDBM287158
Substrate
n/a
Meas. Tech.
Enzymatic Activity Assay
IC50
1.30±n/a nM
Citation
 Verner, E; Brameld, KA Quinolone derivatives as fibroblast growth factor receptor inhibitors US Patent  US11078199 Publication Date 8/3/2021 
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:
BDBM287158
Synonyms:
8-(2-((1-acryloylazetidin-3-yl)oxy)ethyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(((1r,4r)-4-hydroxycyclohexyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one | US10294223, Cpd No. 109 | US11078199, Cpd 109 | US9567334, Example 109 | US9815834, Compound 109
Type:
Small organic molecule
Emp. Form.:
C29H33Cl2N5O6
Mol. Mass.:
618.508
SMILES:
COc1cc(OC)c(Cl)c(c1Cl)-c1cc2cnc(N[C@H]3CC[C@H](O)CC3)nc2n(CCOC2CN(C2)C(=O)C=C)c1=O |r,wU:19.19,wD:22.23,(4.39,7.86,;3.06,7.09,;3.06,5.55,;4.39,4.78,;4.39,3.24,;5.73,2.47,;7.06,3.24,;3.06,2.47,;3.06,.93,;1.72,3.24,;1.72,4.78,;.39,5.55,;.39,2.47,;-.94,3.24,;-2.28,2.47,;-3.61,3.24,;-4.94,2.47,;-4.94,.93,;-6.28,.16,;-6.28,-1.38,;-4.94,-2.15,;-4.94,-3.69,;-6.28,-4.46,;-6.28,-6,;-7.61,-3.69,;-7.61,-2.15,;-3.61,.16,;-2.28,.93,;-.94,.16,;-.94,-1.38,;.39,-2.15,;.39,-3.69,;1.72,-4.46,;2.12,-5.95,;3.61,-5.55,;3.21,-4.06,;4.94,-6.32,;4.94,-7.86,;6.28,-5.55,;7.61,-6.32,;.39,.93,;1.72,.16,)|
Structure:
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