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Target
Tyrosine-protein kinase BTK
Ligand
BDBM359058
Substrate
n/a
Meas. Tech.
Btk Enzyme Activity Assay
IC50
1.20±n/a nM
Citation
 Liu, J; Kozlowski, JA; Boga, SB; Gao, X; Guiadeen, DG; Cai, J; Liu, S; Wang, D; Wu, H; Yang, C Btk inhibitors US Patent  US10214546 Publication Date 2/26/2019 
Target
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:
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVFAKSTGDPQGVIRHYVVCSTPQSQYYLAEKHLFSTIPELINYHQHNSAGLISRLKYPVSQQNKNAPSTAGLGYGSWEIDPKDLTFLKELGTGQFGVVKYGKWRGQYDVAIKMIKEGSMSEDEFIEEAKVMMNLSHEKLVQLYGVCTKQRPIFIITEYMANGCLLNYLREMRHRFQTQQLLEMCKDVCEAMEYLESKQFLHRDLAARNCLVNDQGVVKVSDFGLSRYVLDDEYTSSVGSKFPVRWSPPEVLMYSKFSSKSDIWAFGVLMWEIYSLGKMPYERFTNSETAEHIAQGLRLYRPHLASEKVYTIMYSCWHEKADERPTFKILLSNILDVMDEES
  
Inhibitor
Name:
BDBM359058
Synonyms:
(6R,8aS)-6-[8-amino-5- chloro-1-(2-fluoro-4- {1-hydroxy-1-[3- (trifluoromethyl)phenyl] ethyl}phenyl)imidazo [1,5-a]pyrazin-3- yl]hexahydroindolizin- 3(2H)-one | US10214546, Example 190 | US10214546, Example 193
Type:
Small organic molecule
Emp. Form.:
C29H26ClF4N5O2
Mol. Mass.:
587.996
SMILES:
CC(O)(c1cccc(c1)C(F)(F)F)c1ccc(-c2nc([C@@H]3CC[C@H]4CCC(=O)N4C3)n3c(Cl)cnc(N)c23)c(F)c1 |r|
Structure:
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