| Reaction Details |
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 | Report a problem with these data |
| Target | Tyrosine-protein kinase Yes |
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| Ligand | BDBM267790 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_2061799 (CHEMBL4717052) |
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| IC50 | 21±n/a nM |
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| Citation |  Liu, J; Guiadeen, D; Krikorian, A; Gao, X; Wang, J; Boga, SB; Alhassan, AB; Yu, Y; Vaccaro, H; Liu, S; Yang, C; Wu, H; Cooper, A; de Man, J; Kaptein, A; Maloney, K; Hornak, V; Gao, YD; Fischmann, TO; Raaijmakers, H; Vu-Pham, D; Presland, J; Mansueto, M; Xu, Z; Leccese, E; Zhang-Hoover, J; Knemeyer, I; Garlisi, CG; Bays, N; Stivers, P; Brandish, PE; Hicks, A; Kim, R; Kozlowski, JA Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis. ACS Med Chem Lett7:198-203 (2016) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Tyrosine-protein kinase Yes |
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| Name: | Tyrosine-protein kinase Yes |
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| Synonyms: | Proto-oncogene c-Yes | VHL/Tyrosine-protein kinase Yes | YES | YES1 | YES_HUMAN | p61-yes |
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| Type: | Protein |
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| Mol. Mass.: | 60801.54 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P07947 |
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| Residue: | 543 |
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| Sequence: | MGCIKSKENKSPAIKYRPENTPEPVSTSVSHYGAEPTTVSPCPSSSAKGTAVNFSSLSMT
PFGGSSGVTPFGGASSSFSVVPSSYPAGLTGGVTIFVALYDYEARTTEDLSFKKGERFQI
INNTEGDWWEARSIATGKNGYIPSNYVAPADSIQAEEWYFGKMGRKDAERLLLNPGNQRG
IFLVRESETTKGAYSLSIRDWDEIRGDNVKHYKIRKLDNGGYYITTRAQFDTLQKLVKHY
TEHADGLCHKLTTVCPTVKPQTQGLAKDAWEIPRESLRLEVKLGQGCFGEVWMGTWNGTT
KVAIKTLKPGTMMPEAFLQEAQIMKKLRHDKLVPLYAVVSEEPIYIVTEFMSKGSLLDFL
KEGDGKYLKLPQLVDMAAQIADGMAYIERMNYIHRDLRAANILVGENLVCKIADFGLARL
IEDNEYTARQGAKFPIKWTAPEAALYGRFTIKSDVWSFGILQTELVTKGRVPYPGMVNRE
VLEQVERGYRMPCPQGCPESLHELMNLCWKKDPDERPTFEYIQSFLEDYFTATEPQYQPG
ENL
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| BDBM267790 |
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| n/a |
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| Name | BDBM267790 |
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| Synonyms: | 4-(8-amino-3-{(3R,6S)-6-methyl-1-[(3-methyloxetan-3-yl)carbonyl]piperidin-3-yl}imidazo[1,5-a]pyrazin-1-yl)-3-fluoro-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide | US9718828, Example, 396 |
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| Type | Small organic molecule |
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| Emp. Form. | C29H27F4N7O2 |
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| Mol. Mass. | 581.564 |
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| SMILES | C[C@H]1CC[C@H](CN1C(=O)C1CC1)c1nc(-c2ccc(cc2F)C(=O)Nc2cc(ccn2)C(F)(F)F)c2c(N)nccn12 |r| |
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| Structure | 
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