Target
Tyrosine-protein kinase BTK
Ligand
BDBM278949
Substrate
n/a
Meas. Tech.
Btk Enzyme Activity Assay
IC50
0.330±n/a nM
Citation
 Liu, JKozlowski, JAGao, XGuiadeen, DGLiu, SWang, D Substituted imidazo[1,5-a]pyrazines as Btk inhibitors US Patent  US10040805 Publication Date 8/7/2018 
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:
BDBM278949
Synonyms:
4-{8-amino-3- [(6R,8aS)-6-methyl-3- oxooctahydroindolizin- 6-yl]imidazo[1,5-a] pyrazin-1-yl}-3- methoxy-N-[4- (trifluoromethyl) pyridin-2-yl] benzamide | US10040805, Example 19
Type:
Small organic molecule
Emp. Form.:
C29H28F3N7O3
Mol. Mass.:
579.5729
SMILES:
COc1cc(ccc1-c1nc(n2ccnc(N)c12)[C@]1(C)CC[C@H]2CCC(=O)N2C1)C(=O)Nc1cc(ccn1)C(F)(F)F |r|
Structure:
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