Reaction Details |
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Target | Tau-tubulin kinase 1 |
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Ligand | BDBM50609159 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2276686 |
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IC50 | 2.7±n/a nM |
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Citation | Halkina, T; Henderson, JL; Lin, EY; Himmelbauer, MK; Jones, JH; Nevalainen, M; Feng, J; King, K; Rooney, M; Johnson, JL; Marcotte, DJ; Chodaparambil, JV; Kumar, PR; Patterson, TA; Murugan, P; Schuman, E; Wong, L; Hesson, T; Lamore, S; Bao, C; Calhoun, M; Certo, H; Amaral, B; Dillon, GM; Gilfillan, R; de Turiso, FG Discovery of Potent and Brain-Penetrant Tau Tubulin Kinase 1 (TTBK1) Inhibitors that Lower Tau Phosphorylation In Vivo. J Med Chem64:6358-6380 (2021) [PubMed] |
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More Info.: | Get all data from this article, Assay Method |
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Tau-tubulin kinase 1 |
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Name: | Tau-tubulin kinase 1 |
Synonyms: | BDTK | BDTK | Brain-derived tau kinase | KIAA1855 | TTBK1 | TTBK1_HUMAN | Tau-tubulin kinase 1 |
Type: | PROTEIN |
Mol. Mass.: | 142714.76 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_104387 |
Residue: | 1321 |
Sequence: | MQCLAAALKDETNMSGGGEQADILPANYVVKDRWKVLKKIGGGGFGEIYEAMDLLTRENV
ALKVESAQQPKQVLKMEVAVLKKLQGKDHVCRFIGCGRNEKFNYVVMQLQGRNLADLRRS
QPRGTFTLSTTLRLGKQILESIEAIHSVGFLHRDIKPSNFAMGRLPSTYRKCYMLDFGLA
RQYTNTTGDVRPPRNVAGFRGTVRYASVNAHKNREMGRHDDLWSLFYMLVEFAVGQLPWR
KIKDKEQVGMIKEKYEHRMLLKHMPSEFHLFLDHIASLDYFTKPDYQLIMSVFENSMKER
GIAENEAFDWEKAGTDALLSTSTSTPPQQNTRQTAAMFGVVNVTPVPGDLLRENTEDVLQ
GEHLSDQENAPPILPGRPSEGLGPSPHLVPHPGGPEAEVWEETDVNRNKLRINIGKSPCV
EEEQSRGMGVPSSPVRAPPDSPTTPVRSLRYRRVNSPESERLSTADGRVELPERRSRMDL
PGSPSRQACSSQPAQMLSVDTGHADRQASGRMDVSASVEQEALSNAFRSVPLAEEEDFDS
KEWVIIDKETELKDFPPGAEPSTSGTTDEEPEELRPLPEEGEERRRLGAEPTVRPRGRSM
QALAEEDLQHLPPQPLPPQLSQGDGRSETSQPPTPGSPSHSPLHSGPRPRRRESDPTGPQ
RQVFSVAPPFEVNGLPRAVPLSLPYQDFKRDLSDYRERARLLNRVRRVGFSHMLLTTPQV
PLAPVQPQANGKEEEEEEEEDEEEEEEDEEEEEEEEEEEEEEEEEEEEEEEAAAAVALGE
VLGPRSGSSSEGSERSTDRSQEGAPSTLLADDQKESRGRASMADGDLEPEEGSKTLVLVS
PGDMKKSPVTAELAPDPDLGTLAALTPQHERPQPTGSQLDVSEPGTLSSVLKSEPKPPGP
GAGLGAGTVTTGVGGVAVTSSPFTKVERTFVHIAEKTHLNVMSSGGQALRSEEFSAGGEL
GLELASDGGAVEEGARAPLENGLALSGLNGAEIEGSALSGAPRETPSEMATNSLPNGPAL
ADGPAPVSPLEPSPEKVATISPRRHAMPGSRPRSRIPVLLSEEDTGSEPSGSLSAKERWS
KRARPQQDLARLVMEKRQGRLLLRLASGASSSSSEEQRRASETLSGTGSEEDTPASEPAA
ALPRKSGRAAATRSRIPRPIGLRMPMPVAAQQPASRSHGAAPALDTAITSRLQLQTPPGS
ATAADLRPKQPPGRGLGPGRAQAGARPPAPRSPRLPASTSAARNASASPRSQSLSRRESP
SPSHQARPGVPPPRGVPPARAQPDGTPSPGGSKKGPRGKLQAQRATTKGRAGGAEGRAGA
R
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BDBM50609159 |
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n/a |
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Name | BDBM50609159 |
Synonyms: | CHEMBL5280210 |
Type | Small organic molecule |
Emp. Form. | C18H19N5O2 |
Mol. Mass. | 337.3758 |
SMILES | CC[C@](C)(O)C#Cc1cc2n(ccc2cn1)-c1cc(OC)nc(N)n1 |r| |
Structure |
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