Reaction Details |
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Target | Serine/threonine-protein kinase TBK1 |
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Ligand | BDBM10100 |
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Substrate/Competitor | n/a |
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Meas. Tech. | KinEASE-STK Assay |
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IC50 | 526± 43 nM |
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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 Biol10:289-98 (2015) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Serine/threonine-protein kinase TBK1 |
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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: | MQSTSNHLWLLSDILGQGATANVFRGRHKKTGDLFAIKVFNNISFLRPVDVQMREFEVLK
KLNHKNIVKLFAIEEETTTRHKVLIMEFCPCGSLYTVLEEPSNAYGLPESEFLIVLRDVV
GGMNHLRENGIVHRDIKPGNIMRVIGEDGQSVYKLTDFGAARELEDDEQFVSLYGTEEYL
HPDMYERAVLRKDHQKKYGATVDLWSIGVTFYHAATGSLPFRPFEGPRRNKEVMYKIITG
KPSGAISGVQKAENGPIDWSGDMPVSCSLSRGLQVLLTPVLANILEADQEKCWGFDQFFA
ETSDILHRMVIHVFSLQQMTAHKIYIHSYNTATIFHELVYKQTKIISSNQELIYEGRRLV
LEPGRLAQHFPKTTEENPIFVVSREPLNTIGLIYEKISLPKVHPRYDLDGDASMAKAITG
VVCYACRIASTLLLYQELMRKGIRWLIELIKDDYNETVHKKTEVVITLDFCIRNIEKTVK
VYEKLMKINLEAAELGEISDIHTKLLRLSSSQGTIETSLQDIDSRLSPGGSLADAWAHQE
GTHPKDRNVEKLQVLLNCMTEIYYQFKKDKAERRLAYNEEQIHKFDKQKLYYHATKAMTH
FTDECVKKYEAFLNKSEEWIRKMLHLRKQLLSLTNQCFDIEEEVSKYQEYTNELQETLPQ
KMFTASSGIKHTMTPIYPSSNTLVEMTLGMKKLKEEMEGVVKELAENNHILERFGSLTMD
GGLRNVDCL
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BDBM10100 |
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n/a |
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Name | BDBM10100 |
Synonyms: | (3Z)-5-fluoro-4-[(3S)-4-hydroxy-3-(methylamino)but-1-yn-1-yl]-3-[(3-methoxy-1H-pyrrol-2-yl)methylidene]-2,3-dihydro-1H-indol-2-one | 4-alkynyl oxindole 7f | ROCHE screening, 73 |
Type | Small organic molecule |
Emp. Form. | C19H18FN3O3 |
Mol. Mass. | 355.3629 |
SMILES | CN[C@H](CO)C#Cc1c2\C(=C\c3[nH]ccc3OC)C(=O)Nc2ccc1F |r| |
Structure |
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