Reaction Details Report a problem with these data
Target
Fibroblast growth factor receptor 4
Ligand
BDBM101058
Substrate
n/a
Meas. Tech.
Omnia Assay Protocol for Potency Assessment Against FGFR 4 Enzyme
IC50
<500±n/a nM
Citation
 D Agostino, LA; Sjin, RT; Niu, D; McDonald, JJ; Zhu, Z; Liu, H; Mazdiyasni, H; Petter, RC; Singh, J; Barrague, M; Gross, A; Munson, M; Harvey, D; Scholte, A; Maniar, S Substituted pyrido[2,3-d]pyrimidines as inhibitors of protein kinases US Patent  US10618902 Publication Date 4/14/2020 
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:
BDBM101058
Synonyms:
US10189794, Compound I-242 | US10618902, Compound I-242 | US10774052, Compound I-242 | US9695132, I-242
Type:
Small organic molecule
Emp. Form.:
C26H23Cl2N5O5
Mol. Mass.:
556.397
SMILES:
COc1ccc(Nc2ncc3cc(-c4c(Cl)c(OC)cc(OC)c4Cl)c(=O)n(C)c3n2)c(NC(=O)C=C)c1 |(-5.37,-7.38,;-4.04,-6.61,;-4.04,-5.07,;-2.7,-4.3,;-2.7,-2.76,;-4.04,-1.99,;-4.04,-.45,;-2.7,.32,;-2.7,1.86,;-1.37,2.63,;-.04,1.86,;1.3,2.63,;2.63,1.86,;3.97,2.63,;5.3,1.86,;5.3,.32,;6.63,2.63,;7.97,1.86,;9.3,2.63,;6.63,4.17,;5.3,4.94,;5.3,6.48,;6.63,7.25,;3.97,4.17,;2.63,4.94,;2.63,.32,;3.97,-.45,;1.3,-.45,;1.3,-1.99,;-.04,.32,;-1.37,-.45,;-5.37,-2.76,;-6.7,-1.99,;-8.04,-2.76,;-8.04,-4.3,;-9.37,-1.99,;-10.7,-2.76,;-5.37,-4.3,)|
Structure:
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