Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 4
Ligand
BDBM438569
Substrate
n/a
Meas. Tech.
ChEMBL_2075295 (CHEMBL4730829)
IC50
6.0±n/a nM
Citation
 Liu, H; Niu, D; Tham Sjin, RT; Dubrovskiy, A; Zhu, Z; McDonald, JJ; Fahnoe, K; Wang, Z; Munson, M; Scholte, A; Barrague, M; Fitzgerald, M; Liu, J; Kothe, M; Sun, F; Murtie, J; Ge, J; Rocnik, J; Harvey, D; Ospina, B; Perron, K; Zheng, G; Shehu, E; D'Agostino, LA Discovery of Selective, Covalent FGFR4 Inhibitors with Antitumor Activity in Models of Hepatocellular Carcinoma. ACS Med Chem Lett 11:1899-1904 (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:
Human
Description:
P22455
Residue:
802
Sequence:
MRLLLALLGVLLSVPGPPVLSLEASEEVELEPCLAPSLEQQEQELTVALGQPVRLCCGRAERGGHWYKEGSRLAPAGRVRGWRGRLEIASFLPEDAGRYLCLARGSMIVLQNLTLITGDSLTSSNDDEDPKSHRDPSNRHSYPQQAPYWTHPQRMEKKLHAVPAGNTVKFRCPAAGNPTPTIRWLKDGQAFHGENRIGGIRLRHQHWSLVMESVVPSDRGTYTCLVENAVGSIRYNYLLDVLERSPHRPILQAGLPANTTAVVGSDVELLCKVYSDAQPHIQWLKHIVINGSSFGADGFPYVQVLKTADINSSEVEVLYLRNVSAEDAGEYTCLAGNSIGLSYQSAWLTVLPEEDPTWTAAAPEARYTDIILYASGSLALAVLLLLAGLYRGQALHGRHPRPPATVQKLSRFPLARQFSLESGSSGKSSSSLVRGVRLSSSGPALLAGLVSLDLPLDPLWEFPRDRLVLGKPLGEGCFGQVVRAEAFGMDPARPDQASTVAVKMLKDNASDKDLADLVSEMEVMKLIGRHKNIINLLGVCTQEGPLYVIVECAAKGNLREFLRARRPPGPDLSPDGPRSSEGPLSFPVLVSCAYQVARGMQYLESRKCIHRDLAARNVLVTEDNVMKIADFGLARGVHHIDYYKKTSNGRLPVKWMAPEALFDRVYTHQSDVWSFGILLWEIFTLGGSPYPGIPVEELFSLLREGHRMDRPPHCPPELYGLMRECWHAAPSQRPTFKQLVEALDKVLLAVSEEYLDLRLTFGPYSPSGGDASSTCSSSDSVFSHDPLPLGSSSFPFGSGVQT
  
Inhibitor
Name:
BDBM438569
Synonyms:
US10618902, Compound I-250
Type:
Small organic molecule
Emp. Form.:
C22H23Cl2N5O6S
Mol. Mass.:
556.419
SMILES:
COc1cc(OC)c(Cl)c(c1Cl)-c1cc2cnc(N[C@@H]3COC[C@@H]3NS(=O)(=O)C=C)nc2n(C)c1=O |r,wU:19.19,23.25,(7.98,5.76,;6.65,4.99,;6.65,3.45,;7.98,2.68,;7.98,1.14,;9.32,.37,;9.32,-1.27,;6.65,.37,;6.65,-1.17,;5.31,1.14,;5.31,2.68,;3.98,3.45,;3.98,.37,;2.65,1.14,;1.31,.37,;-.02,1.14,;-1.35,.37,;-1.35,-1.17,;-2.69,-1.94,;-4.02,-1.17,;-4.18,.36,;-5.69,.68,;-6.46,-.65,;-5.43,-1.8,;-5.75,-3.3,;-7.21,-3.78,;-8.36,-2.75,;-8.68,-4.25,;-7.53,-5.28,;-9,-5.76,;-.02,-1.94,;1.31,-1.17,;2.65,-1.94,;2.65,-3.48,;3.98,-1.17,;5.31,-1.94,)|
Structure:
Search PDB for entries with ligand similarity: