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Target
Tyrosine-protein kinase BTK
Ligand
BDBM278934
Substrate
n/a
Meas. Tech.
Btk Enzyme Activity Assay
IC50
2.50±n/a nM
Citation
 Liu, J; Kozlowski, JA; Gao, X; Guiadeen, DG; Liu, S; Wang, 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:
BDBM278934
Synonyms:
4-{8-amino-3- [(7S,9aR)-7-methyl-2- (1-methylethyl)-4- oxooctahydro-2H- pyrido[1,2-a]pyrazin-7- yl]imidazo[1,5-a] pyrazin-1-yl}-3- ethoxy-N-[1-methyl-5- (trifluoromethyl)- 1H-pyrazol-3- yl]benzamide | US10040805, Example 4
Type:
Small organic molecule
Emp. Form.:
C32H38F3N9O3
Mol. Mass.:
653.6978
SMILES:
CCOc1cc(ccc1-c1nc(n2ccnc(N)c12)[C@@]1(C)CC[C@@H]2CN(CC(=O)N2C1)C(C)C)C(=O)Nc1cc(n(C)n1)C(F)(F)F |r|
Structure:
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