Target
Tyrosine-protein kinase BTK
Ligand
BDBM358992
Substrate
n/a
Meas. Tech.
Btk Enzyme Activity Assay
IC50
1.20±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:
BDBM358992
Synonyms:
(6R,8aS)-6-[8-amino-5- chloro-1-(4-{(1R)-1- hydroxy-1-[3-(2,2,2- trifluoro-1,1- dimethylethyl)phenyl] ethyl}phenyl)imidazo[1, 5-a]pyrazin-3- yl]hexahydroindolizin- 3(2H)-one | US10214546, Example 124
Type:
Small organic molecule
Emp. Form.:
C32H33ClF3N5O2
Mol. Mass.:
612.085
SMILES:
CC(C)(c1cccc(c1)[C@](C)(O)c1ccc(cc1)-c1nc([C@@H]2CC[C@H]3CCC(=O)N3C2)n2c(Cl)cnc(N)c12)C(F)(F)F |r|
Structure:
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