Target
Tyrosine-protein kinase BTK
Ligand
BDBM358941
Substrate
n/a
Meas. Tech.
Btk Enzyme Activity Assay
IC50
0.410±n/a nM
Citation
 Liu, JKozlowski, JABoga, SBGao, XGuiadeen, DGCai, JLiu, SWang, DWu, HYang, 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:
BDBM358941
Synonyms:
(6R,8aS)-6-[8-amino-1- (4-{hydroxy[3- (trifluoromethyl)phenyl] methyl}phenyl)imidazo [1,5-a]pyrazin-3- yl]hexahydroindolizin- 3(2H)-one | US10214546, Example 72 | US10214546, Example 73
Type:
Small organic molecule
Emp. Form.:
C28H26F3N5O2
Mol. Mass.:
521.5335
SMILES:
Nc1nccn2c(nc(-c3ccc(cc3)C(O)c3cccc(c3)C(F)(F)F)c12)[C@@H]1CC[C@H]2CCC(=O)N2C1 |r|
Structure:
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