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Target
Serine/threonine-protein kinase TBK1
Ligand
BDBM153728
Substrate
n/a
Meas. Tech.
KinEASE-STK Assay
IC50
7.3e+2± 3.0e+2 nM
Citation
 Richters, A; Basu, D; Engel, J; Ercanoglu, MS; Balke-Want, H; Tesch, R; Thomas, RK; Rauh, D Identification and further development of potent TBK1 inhibitors. ACS Chem Biol 10:289-98 (2015) [PubMed]  Article 
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:
BDBM153728
Synonyms:
2-(4-Aminophenoxy)-N-(5-methyl-1H-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)pyrimidin-4-amine (15k)
Type:
Small organic molecule
Emp. Form.:
C19H24N8O
Mol. Mass.:
380.4469
SMILES:
CN1CCN(CC1)c1cc(Nc2cc(C)[nH]n2)nc(Oc2ccc(N)cc2)n1
Structure:
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