Target
Tyrosine-protein kinase BTK
Ligand
BDBM359050
Substrate
n/a
Meas. Tech.
Btk Enzyme Activity Assay
IC50
1.40±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:
BDBM359050
Synonyms:
(1R,6R,8aS)-6-[8- amino-1-(4-{(1R)-1-[3- (difluoromethyl)phenyl]-1- hydroxyethyl}phenyl) imidazo[1,5-a]pyrazin- 3-yl]-1- (trifluoromethyl) hexahydroindolizin-3(2H)- one | US10214546, Example 182 | US10214546, Example 184
Type:
Small organic molecule
Emp. Form.:
C30H28F5N5O2
Mol. Mass.:
585.5676
SMILES:
C[C@@](O)(c1ccc(cc1)-c1nc([C@@H]2CC[C@H]3C(CC(=O)N3C2)C(F)(F)F)n2ccnc(N)c12)c1cccc(c1)C(F)F |r|
Structure:
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