Reaction Details |
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Target | Tyrosine-protein kinase BTK |
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Ligand | BDBM50134366 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1544942 (CHEMBL3748501) |
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IC50 | 4.0±n/a nM |
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Citation | Young, WB; Barbosa, J; Blomgren, P; Bremer, MC; Crawford, JJ; Dambach, D; Eigenbrot, C; Gallion, S; Johnson, AR; Kropf, JE; Lee, SH; Liu, L; Lubach, JW; Macaluso, J; Maciejewski, P; Mitchell, SA; Ortwine, DF; Di Paolo, J; Reif, K; Scheerens, H; Schmitt, A; Wang, X; Wong, H; Xiong, JM; Xu, J; Yu, C; Zhao, Z; Currie, KS Discovery of highly potent and selective Bruton's tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability. Bioorg Med Chem Lett26:575-9 (2016) [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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BDBM50134366 |
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n/a |
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Name | BDBM50134366 |
Synonyms: | CHEMBL3746115 |
Type | Small organic molecule |
Emp. Form. | C27H25N7O2S |
Mol. Mass. | 511.598 |
SMILES | CN1CCn2nc(Nc3cc(n[nH]c3=O)-c3cccc(NC(=O)c4cc5ccccc5s4)c3C)cc2C1 |
Structure |
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