Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 1
Ligand
BDBM287044
Substrate
n/a
Meas. Tech.
Enzymatic Activity Assay
IC50
3.90±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:
BDBM287044
Synonyms:
8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-((2-isopropoxyethyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one | US10294223, Cpd No. 46 | US11078199, Cpd 46 | US9567334, Example 46 | US9815834, Compound 46
Type:
Small organic molecule
Emp. Form.:
C30H38Cl2N6O5
Mol. Mass.:
633.566
SMILES:
COc1cc(OC)c(Cl)c(c1Cl)-c1cc2cnc(NCCOC(C)C)nc2n(CCCN2CCN(CC2)C(=O)C=C)c1=O |(3.33,8.47,;4.67,7.7,;4.67,6.16,;6,5.39,;6,3.85,;7.34,3.08,;8.67,3.85,;4.67,3.08,;4.67,1.54,;3.33,3.85,;3.33,5.39,;2,6.16,;2,3.08,;.67,3.85,;-.67,3.08,;-2,3.85,;-3.33,3.08,;-3.33,1.54,;-4.67,.77,;-4.67,-.77,;-6,-1.54,;-6,-3.08,;-7.34,-3.85,;-7.34,-5.39,;-8.67,-3.08,;-2,.77,;-.67,1.54,;.67,.77,;.67,-.77,;2,-1.54,;2,-3.08,;3.33,-3.85,;3.33,-5.39,;4.67,-6.16,;6,-5.39,;6,-3.85,;4.67,-3.08,;7.34,-6.16,;8.67,-5.39,;7.34,-7.7,;8.67,-8.47,;2,1.54,;3.33,.77,)|
Structure:
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