Reaction Details |
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Target | Tyrosine-protein kinase BTK |
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Ligand | BDBM165318 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1983359 (CHEMBL4616765) |
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IC50 | 16±n/a nM |
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Citation | Watterson, SH; Liu, Q; Beaudoin Bertrand, M; Batt, DG; Li, L; Pattoli, MA; Skala, S; Cheng, L; Obermeier, MT; Moore, R; Yang, Z; Vickery, R; Elzinga, PA; Discenza, L; D'Arienzo, C; Gillooly, KM; Taylor, TL; Pulicicchio, C; Zhang, Y; Heimrich, E; McIntyre, KW; Ruan, Q; Westhouse, RA; Catlett, IM; Zheng, N; Chaudhry, C; Dai, J; Galella, MA; Tebben, AJ; Pokross, M; Li, J; Zhao, R; Smith, D; Rampulla, R; Allentoff, A; Wallace, MA; Mathur, A; Salter-Cid, L; Macor, JE; Carter, PH; Fura, A; Burke, JR; Tino, JA Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK). J Med Chem62:3228-3250 (2019) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Tyrosine-protein kinase BTK |
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Name: | Tyrosine-protein kinase BTK |
Synonyms: | AGMX1 | ATK | Agammaglobulinaemia tyrosine kinase | Agammaglobulinemia tyrosine kinase | B cell progenitor kinase | B-cell progenitor kinase | BPK | BTK | BTK_HUMAN | Bruton tyrosine kinase | Tyrosine Kinase BTK | Tyrosine-protein kinase (BTK) | Tyrosine-protein kinase BTK (BTK) |
Type: | Enzyme |
Mol. Mass.: | 76289.95 |
Organism: | Homo sapiens (Human) |
Description: | Q06187 |
Residue: | 659 |
Sequence: | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEK
ITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEEL
RKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSS
HRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDE
YFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGK
EGGFIVRDSSKAGKYTVSVFAKSTGDPQGVIRHYVVCSTPQSQYYLAEKHLFSTIPELIN
YHQHNSAGLISRLKYPVSQQNKNAPSTAGLGYGSWEIDPKDLTFLKELGTGQFGVVKYGK
WRGQYDVAIKMIKEGSMSEDEFIEEAKVMMNLSHEKLVQLYGVCTKQRPIFIITEYMANG
CLLNYLREMRHRFQTQQLLEMCKDVCEAMEYLESKQFLHRDLAARNCLVNDQGVVKVSDF
GLSRYVLDDEYTSSVGSKFPVRWSPPEVLMYSKFSSKSDIWAFGVLMWEIYSLGKMPYER
FTNSETAEHIAQGLRLYRPHLASEKVYTIMYSCWHEKADERPTFKILLSNILDVMDEES
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BDBM165318 |
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n/a |
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Name | BDBM165318 |
Synonyms: | US10604504, Example 114 | US11623921, Example 114 | US9688629, 114 | US9802915, Example 114 | US9920031, Example 114 |
Type | Small organic molecule |
Emp. Form. | C19H22N4O2 |
Mol. Mass. | 338.4036 |
SMILES | Cc1[nH]c2c(ccc(NC3CCN(CC3)C(=O)C#C)c2c1C)C(N)=O |
Structure |
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