Reaction Details |
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Target | Tyrosine-protein kinase BTK |
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Ligand | BDBM50519156 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1873903 (CHEMBL4375192) |
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IC50 | 0.200000±n/a nM |
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Citation | Caldwell, RD; Qiu, H; Askew, BC; Bender, AT; Brugger, N; Camps, M; Dhanabal, M; Dutt, V; Eichhorn, T; Gardberg, AS; Goutopoulos, A; Grenningloh, R; Head, J; Healey, B; Hodous, BL; Huck, BR; Johnson, TL; Jones, C; Jones, RC; Mochalkin, I; Morandi, F; Nguyen, N; Meyring, M; Potnick, JR; Santos, DC; Schmidt, R; Sherer, B; Shutes, A; Urbahns, K; Follis, AV; Wegener, AA; Zimmerli, SC; Liu-Bujalski, L Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases. J Med Chem62:7643-7655 (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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BDBM50519156 |
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n/a |
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Name | BDBM50519156 |
Synonyms: | CHEMBL4466205 |
Type | Small organic molecule |
Emp. Form. | C27H25N3O2 |
Mol. Mass. | 423.5063 |
SMILES | C=CC(=O)N1CCC[C@H](C1)n1nc(-c2ccc(Oc3ccccc3)cc2)c2ccccc12 |r| |
Structure |
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