Target
Fibroblast growth factor receptor 3
Ligand
BDBM262077
Substrate
n/a
Meas. Tech.
FGFR Enzymatic Assay (pre-incubated for 10 minutes)
IC50
<10±n/a nM
Citation
 Sokolsky, AWu, LYao, W Bicyclic heterocycles as FGFR4 inhibitors US Patent  US10251892 Publication Date 4/9/2019
Target
Name:
Fibroblast growth factor receptor 3
Synonyms:
CD_antigen: CD333 | FGFR-3 | FGFR3 | FGFR3_HUMAN | Fibroblast growth factor receptor | Fibroblast growth factor receptor 3 (FGFR3) | JTK4
Type:
Protein
Mol. Mass.:
87699.57
Organism:
Homo sapiens (Human)
Description:
P22607
Residue:
806
Sequence:
MGAPACALALCVAVAIVAGASSESLGTEQRVVGRAAEVPGPEPGQQEQLVFGSGDAVELSCPPPGGGPMGPTVWVKDGTGLVPSERVLVGPQRLQVLNASHEDSGAYSCRQRLTQRVLCHFSVRVTDAPSSGDDEDGEDEAEDTGVDTGAPYWTRPERMDKKLLAVPAANTVRFRCPAAGNPTPSISWLKNGREFRGEHRIGGIKLRHQQWSLVMESVVPSDRGNYTCVVENKFGSIRQTYTLDVLERSPHRPILQAGLPANQTAVLGSDVEFHCKVYSDAQPHIQWLKHVEVNGSKVGPDGTPYVTVLKTAGANTTDKELEVLSLHNVTFEDAGEYTCLAGNSIGFSHHSAWLVVLPAEEELVEADEAGSVYAGILSYGVGFFLFILVVAAVTLCRLRSPPKKGLGSPTVHKISRFPLKRQVSLESNASMSSNTPLVRIARLSSGEGPTLANVSELELPADPKWELSRARLTLGKPLGEGCFGQVVMAEAIGIDKDRAAKPVTVAVKMLKDDATDKDLSDLVSEMEMMKMIGKHKNIINLLGACTQGGPLYVLVEYAAKGNLREFLRARRPPGLDYSFDTCKPPEEQLTFKDLVSCAYQVARGMEYLASQKCIHRDLAARNVLVTEDNVMKIADFGLARDVHNLDYYKKTTNGRLPVKWMAPEALFDRVYTHQSDVWSFGVLLWEIFTLGGSPYPGIPVEELFKLLKEGHRMDKPANCTHDLYMIMRECWHAAPSQRPTFKQLVEDLDRVLTVTSTDEYLDLSAPFEQYSPGGQDTPSSSSSGDDSVFAHDLLPPAPPSSGGSRT
  
Inhibitor
Name:
BDBM262077
Synonyms:
1-((1-(cyclopropylmethyl)-1H-pyrazol-4-yl)methyl)-3-(2,6-difluoro-3,5-dimethoxyphenyl)-7-(1,3-dimethyl-1H-pyrazol-4-yl)-3,4-dihydropyrido[4,3-d]pyrimidin-2(1H)-one | US10251892, Example 126 | US11173162, Example 126 | US9708318, 126
Type:
Small organic molecule
Emp. Form.:
C28H29F2N7O3
Mol. Mass.:
549.5718
SMILES:
COc1cc(OC)c(F)c(N2Cc3cnc(cc3N(Cc3cnn(CC4CC4)c3)C2=O)-c2cn(C)nc2C)c1F
Structure:
Search PDB for entries with ligand similarity: