Target
Fibroblast growth factor receptor 4
Ligand
BDBM291255
Substrate
n/a
Meas. Tech.
Enzymatic Assay
pH
7.5±n/a
IC50
<10±n/a nM
Comments
extracted
Citation
 Lu, LWu, LShen, BYao, W Bicyclic heterocycles as FGFR4 inhibitors US Patent  US9580423 Publication Date 2/28/2017 
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:
BDBM291255
Synonyms:
N-(5-(2'-(2,6-difluoro-3,5- dimethoxyphenyl)-3'-oxo-2',3'- dihydro-1'H-spiro[cyclopropane- 1,4'-[2,7]naphthyridine]-6'-yl)-1- ((1-methyl-1H-1,2,4-triazol-3- yl)methyl)-1H-pyrazol-4- yl)acrylamide | US10016438, Example 23 | US9580423, Example 23 | US9801889, Example 23
Type:
Small organic molecule
Emp. Form.:
C28H26F2N8O4
Mol. Mass.:
576.554
SMILES:
COc1cc(OC)c(F)c(N2Cc3cnc(cc3C3(CC3)C2=O)-c2c(NC(=O)C=C)cnn2Cc2ncn(C)n2)c1F
Structure:
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