Target
Fibroblast growth factor receptor 4
Ligand
BDBM249394
Substrate
FGFR1 substrate peptide
Meas. Tech.
Kinase HotSpot Assay
pH
7.5±n/a
Temperature
298.15±n/a K
IC50
201±n/a nM
Comments
extracted
Citation
 Reynolds, DHao, MWang, JPrajapati, SSatoh, TSelvaraj, A Pyrimidine FGFR4 inhibitors US Patent  US9434697 Publication Date 9/6/2016 
Target
Name:
Fibroblast growth factor receptor 4
Synonyms:
CD_antigen: CD334 FGFR4 | FGFR-4 | FGFR4 | FGFR4_HUMAN | Fibroblast growth factor receptor | Fibroblast growth factor receptor 4 (FGFR4) | JK2 | JTK2 | TKF
Type:
Protein
Mol. Mass.:
87957.45
Organism:
Homo sapiens (Human)
Description:
P22455
Residue:
802
Sequence:
MRLLLALLGVLLSVPGPPVLSLEASEEVELEPCLAPSLEQQEQELTVALGQPVRLCCGRAERGGHWYKEGSRLAPAGRVRGWRGRLEIASFLPEDAGRYLCLARGSMIVLQNLTLITGDSLTSSNDDEDPKSHRDPSNRHSYPQQAPYWTHPQRMEKKLHAVPAGNTVKFRCPAAGNPTPTIRWLKDGQAFHGENRIGGIRLRHQHWSLVMESVVPSDRGTYTCLVENAVGSIRYNYLLDVLERSPHRPILQAGLPANTTAVVGSDVELLCKVYSDAQPHIQWLKHIVINGSSFGADGFPYVQVLKTADINSSEVEVLYLRNVSAEDAGEYTCLAGNSIGLSYQSAWLTVLPEEDPTWTAAAPEARYTDIILYASGSLALAVLLLLAGLYRGQALHGRHPRPPATVQKLSRFPLARQFSLESGSSGKSSSSLVRGVRLSSSGPALLAGLVSLDLPLDPLWEFPRDRLVLGKPLGEGCFGQVVRAEAFGMDPARPDQASTVAVKMLKDNASDKDLADLVSEMEVMKLIGRHKNIINLLGVCTQEGPLYVIVECAAKGNLREFLRARRPPGPDLSPDGPRSSEGPLSFPVLVSCAYQVARGMQYLESRKCIHRDLAARNVLVTEDNVMKIADFGLARGVHHIDYYKKTSNGRLPVKWMAPEALFDRVYTHQSDVWSFGILLWEIFTLGGSPYPGIPVEELFSLLREGHRMDRPPHCPPELYGLMRECWHAAPSQRPTFKQLVEALDKVLLAVSEEYLDLRLTFGPYSPSGGDASSTCSSSDSVFSHDPLPLGSSSFPFGSGVQT
  
Inhibitor
Name:
BDBM249394
Synonyms:
US10537571, Compound 105 | US10912774, Compound 105 | US9434697, 105 | US9730931, Compound 105
Type:
Small organic molecule
Emp. Form.:
C23H23ClN6O4
Mol. Mass.:
482.92
SMILES:
COc1cc(NC(=O)N(C)c2cc(Nc3ccccc3NC(=O)C=C)ncn2)c(Cl)c(OC)c1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
FGFR1 substrate peptide
Synonyms:
n/a
Type:
Protein
Mol. Mass.:
1596.80
Organism:
Artificial Organism
Description:
SEQ ID NO:1
Residue:
14
Sequence:
KKKSPGEYVNIEFG