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Target
Tyrosine-protein kinase BTK
Ligand
BDBM278940
Substrate
n/a
Meas. Tech.
Btk Enzyme Activity Assay
IC50
0.180±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:
BDBM278940
Synonyms:
4-{8-amino-3- [(6R,8aS)-6-methyl-3- oxohexahydro[1,3] oxazolo[3,4-a] pyridin-6-yl] imidazo[1,5-a] pyrazin-1-yl}-N-(4- cyclopropylpyridin- 2-yl)-3- fluorobenzamide | US10040805, Example 10
Type:
Small organic molecule
Emp. Form.:
C29H28FN7O3
Mol. Mass.:
541.5761
SMILES:
C[C@]1(CC[C@H]2COC(=O)N2C1)c1nc(-c2ccc(cc2F)C(=O)Nc2cc(ccn2)C2CC2)c2c(N)nccn12 |r|
Structure:
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