Target
Interleukin-1 receptor-associated kinase 4
Ligand
BDBM278880
Substrate
n/a
Meas. Tech.
IRAK4 Kinase Assay
pH
7.2±n/a
IC50
21.0±n/a nM
Comments
extracted
Citation
 Lim, JAltman, MDGibeau, CR Thienopyrazine inhibitors of IRAK4 activity US Patent  US10040802 Publication Date 8/7/2018 
Target
Name:
Interleukin-1 receptor-associated kinase 4
Synonyms:
IRAK-4 | IRAK4 | IRAK4_HUMAN | Interleukin-1 receptor-associated kinase 4 (IRAK-4) | Interleukin-1 receptor-associated kinase 4 (IRAK4) | Renal carcinoma antigen NY-REN-64
Type:
Protein
Mol. Mass.:
51519.08
Organism:
Homo sapiens (Human)
Description:
Q9NWZ3
Residue:
460
Sequence:
MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLDEAFTAKISDFGLARASEKFAQTVMTSRIVGTTAYMAPEALRGEITPKSDIYSFGVVLLEIITGLPAVDEHREPQLLLDIKEEIEDEEKTIEDYIDKKMNDADSTSVEAMYSVASQCLHEKKNKRPDIKKVQQLLQEMTAS
  
Inhibitor
Name:
BDBM278880
Synonyms:
2-[(1S,4S)- or (1R,4R)- 2,5-diazabicyclo [2.2.2]oct-2-yl]-N- [4-(difluoromethyl) thiophen-3-yl] thieno[2,3-b] pyrazine-7- carboxamide trifluoroacetate | US10040802, Example 59
Type:
Small organic molecule
Emp. Form.:
C20H18F5N5O3S2
Mol. Mass.:
535.511
SMILES:
OC(=O)C(F)(F)F.FC(F)c1cscc1NC(=O)c1csc2ncc(nc12)N1C[C@H]2CC[C@@H]1CN2 |r|
Structure:
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