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Target
Serine/threonine-protein kinase TBK1
Ligand
BDBM5446
Substrate
n/a
Meas. Tech.
KinEASE-STK Assay
IC50
2.20e+3± 4.8e+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:
BDBM5446
Synonyms:
CHEMBL553 | ERLOTINIB HYDROCHLORIDE | Erlotinib | Erotinib | N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine Monohydrochloride | N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine | OSI-774 | Tarceva | US10189853, erlotinib | US10507209, Compound Erlotinib | US11524945, Compound Erlotinib | US9409845, Table 1, Compound 22: erlotinib | US9730934, Erlotinib | WO2022090481, Example erlotinib | cid_176870
Type:
Small organic molecule
Emp. Form.:
C22H23N3O4
Mol. Mass.:
393.4357
SMILES:
COCCOc1cc2ncnc(Nc3cccc(c3)C#C)c2cc1OCCOC
Structure:
Search PDB for entries with ligand similarity: