Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 1
Ligand
BDBM286987
Substrate
n/a
Meas. Tech.
FGFR Family Enzymatic Activity Assay
IC50
0.100±n/a nM
Citation
 Verner, E; Brameld, KA Quinolone derivatives as fibroblast growth factor receptor inhibitors US Patent  US10294223 Publication Date 5/21/2019 
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:
BDBM286987
Synonyms:
8-(3-(4-acryloylpiperazin-1-yl)propyl)-2-((cyclopropylmethyl)amino)-6-(2,6-dichloro-3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one | US10294223, Cpd No. 7 | US11078199, Cpd 7 | US9567334, Example 7 | US9815834, Compound 7
Type:
Small organic molecule
Emp. Form.:
C29H34Cl2N6O4
Mol. Mass.:
601.524
SMILES:
COc1cc(OC)c(Cl)c(c1Cl)-c1cc2cnc(NCC3CC3)nc2n(CCCN2CCN(CC2)C(=O)C=C)c1=O |(2.77,8.47,;4.1,7.7,;4.1,6.16,;5.44,5.39,;5.44,3.85,;6.77,3.08,;8.11,3.85,;4.1,3.08,;4.1,1.54,;2.77,3.85,;2.77,5.39,;1.44,6.16,;1.44,3.08,;.1,3.85,;-1.23,3.08,;-2.56,3.85,;-3.9,3.08,;-3.9,1.54,;-5.23,.77,;-5.23,-.77,;-6.57,-1.54,;-8.11,-1.54,;-7.34,-2.87,;-2.56,.77,;-1.23,1.54,;.1,.77,;.1,-.77,;1.44,-1.54,;1.44,-3.08,;2.77,-3.85,;2.77,-5.39,;4.1,-6.16,;5.44,-5.39,;5.44,-3.85,;4.1,-3.08,;6.77,-6.16,;8.11,-5.39,;6.77,-7.7,;8.11,-8.47,;1.44,1.54,;2.77,.77,)|
Structure:
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