Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 1
Ligand
BDBM287077
Substrate
n/a
Meas. Tech.
Enzymatic Activity Assay
IC50
2.60±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:
BDBM287077
Synonyms:
(S)-8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-((1-hydroxypropan-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one | US10294223, Cpd No. 83 | US11078199, Cpd 83 | US9567334, Example 83 | US9815834, Compound 83
Type:
Small organic molecule
Emp. Form.:
C28H34Cl2N6O5
Mol. Mass.:
605.513
SMILES:
COc1cc(OC)c(Cl)c(c1Cl)-c1cc2cnc(N[C@@H](C)CO)nc2n(CCCN2CCN(CC2)C(=O)C=C)c1=O |r,wU:19.20,(4,8.09,;2.67,7.31,;2.67,5.78,;4,5,;4,3.46,;5.33,2.69,;6.67,3.46,;2.67,2.69,;2.67,1.15,;1.33,3.46,;1.33,5,;,5.77,;,2.69,;-1.33,3.46,;-2.67,2.69,;-4,3.46,;-5.33,2.69,;-5.33,1.15,;-6.67,.38,;-6.67,-1.16,;-5.33,-1.93,;-8,-1.93,;-8,-3.47,;-4,.38,;-2.67,1.15,;-1.33,.38,;-1.33,-1.16,;,-1.93,;,-3.47,;1.33,-4.24,;1.33,-5.78,;2.67,-6.55,;4,-5.78,;4,-4.24,;2.67,-3.47,;5.33,-6.55,;5.33,-8.09,;6.67,-5.78,;8,-6.55,;,1.15,;1.33,.38,)|
Structure:
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