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Target
Fibroblast growth factor receptor 4
Ligand
BDBM50465111
Substrate
n/a
Meas. Tech.
ChEMBL_2068061 (CHEMBL4723314)
IC50
2.2±n/a nM
Citation
 Fairhurst, RA; Knoepfel, T; Buschmann, N; Leblanc, C; Mah, R; Todorov, M; Nimsgern, P; Ripoche, S; Niklaus, M; Warin, N; Luu, VH; Madoerin, M; Wirth, J; Graus-Porta, D; Weiss, A; Kiffe, M; Wartmann, M; Kinyamu-Akunda, J; Sterker, D; Stamm, C; Adler, F; Buhles, A; Schadt, H; Couttet, P; Blank, J; Galuba, I; Trappe, J; Voshol, J; Ostermann, N; Zou, C; Berghausen, J; Del Rio Espinola, A; Jahnke, W; Furet, P Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. J Med Chem 63:12542-12573 (2020) [PubMed]  Article 
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:
BDBM50465111
Synonyms:
CHEMBL4279514
Type:
Small organic molecule
Emp. Form.:
C30H40N8O2
Mol. Mass.:
544.691
SMILES:
[H][C@@]12C[C@@]([H])(C=C1)[C@@H]([C@@H]2Nc1nc(Nc2ccc(cc2OCC(C)C)N2CCC(CC2)N(C)C)ncc1C#N)C(N)=O |r,c:5|
Structure:
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