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Target
Serine/threonine-protein kinase TBK1
Ligand
BDBM397739
Substrate
n/a
Meas. Tech.
Inhibition Assay
IC50
20.0±n/a nM
Citation
Bigi, S; Keung, W; Swann, S; Vu, PH; Woodhead, SJ; Gangloff, AR Heteroarylamide inhibitors of TBK1 US Patent US9994547 Publication Date 6/12/2018
More Info.:
Target
Name:
Serine/threonine-protein kinase TBK1
Synonyms:
NAK | NF-kappa-B-activating kinase | Protein cereblon/Serine/threonine-protein kinase TBK1 | T2K | TANK-binding kinase 1 (TBK-1) | TANK-binding kinase 1 (TBK1) | TBK1 | TBK1_HUMAN
Type:
protein
Mol. Mass.:
83645.20
Organism:
Homo sapiens (Human)
Description:
Q9UHD2
Residue:
729
Sequence:
MQSTSNHLWLLSDILGQGATANVFRGRHKKTGDLFAIKVFNNISFLRPVDVQMREFEVLKKLNHKNIVKLFAIEEETTTRHKVLIMEFCPCGSLYTVLEEPSNAYGLPESEFLIVLRDVVGGMNHLRENGIVHRDIKPGNIMRVIGEDGQSVYKLTDFGAARELEDDEQFVSLYGTEEYLHPDMYERAVLRKDHQKKYGATVDLWSIGVTFYHAATGSLPFRPFEGPRRNKEVMYKIITGKPSGAISGVQKAENGPIDWSGDMPVSCSLSRGLQVLLTPVLANILEADQEKCWGFDQFFAETSDILHRMVIHVFSLQQMTAHKIYIHSYNTATIFHELVYKQTKIISSNQELIYEGRRLVLEPGRLAQHFPKTTEENPIFVVSREPLNTIGLIYEKISLPKVHPRYDLDGDASMAKAITGVVCYACRIASTLLLYQELMRKGIRWLIELIKDDYNETVHKKTEVVITLDFCIRNIEKTVKVYEKLMKINLEAAELGEISDIHTKLLRLSSSQGTIETSLQDIDSRLSPGGSLADAWAHQEGTHPKDRNVEKLQVLLNCMTEIYYQFKKDKAERRLAYNEEQIHKFDKQKLYYHATKAMTHFTDECVKKYEAFLNKSEEWIRKMLHLRKQLLSLTNQCFDIEEEVSKYQEYTNELQETLPQKMFTASSGIKHTMTPIYPSSNTLVEMTLGMKKLKEEMEGVVKELAENNHILERFGSLTMDGGLRNVDCL
Inhibitor
Name:
BDBM397739
Synonyms:
(1R,2S)-N-(5-(6-cyano-5-(((S)-1-(dimethylamino)-1-oxopropan-2-yl)amino)pyridin-3-yl)pyrazin-2-yl)-2-methylcyclopropanecarboxamide | US9994547, Example 108
Type:
Small organic molecule
Emp. Form.:
C20H23N7O2
Mol. Mass.:
393.4423
SMILES:
C[C@H](Nc1cc(cnc1C#N)-c1cnc(NC(=O)[C@@H]2C[C@@H]2C)cn1)C(=O)N(C)C |r|