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Target
Tyrosine-protein kinase BTK [C481S]
Ligand
BDBM50175583
Substrate
n/a
Meas. Tech.
In Vitro Inhibitory Activity Against BTK(wt)/BTK(C481S) (Determination of IC50 Value)
IC50
815±n/a nM
Citation
 Chen, R Substituted imidazo[1,5-a]pyrazines as Bruton's tyrosine kinase inhibitors US Patent  US11420975 Publication Date 8/23/2022 
Target
Name:
Tyrosine-protein kinase BTK [C481S]
Synonyms:
AGMX1 | ATK | BPK | BTK | BTK C481S | BTK_HUMAN | Tyrosine-protein kinase BTK (C481S) | Tyrosine-protein kinase BTK C481S
Type:
Enzyme Catalytic Domain
Mol. Mass.:
76273.88
Organism:
Homo sapiens (Human)
Description:
Q06187[C481S]
Residue:
659
Sequence:
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVFAKSTGDPQGVIRHYVVCSTPQSQYYLAEKHLFSTIPELINYHQHNSAGLISRLKYPVSQQNKNAPSTAGLGYGSWEIDPKDLTFLKELGTGQFGVVKYGKWRGQYDVAIKMIKEGSMSEDEFIEEAKVMMNLSHEKLVQLYGVCTKQRPIFIITEYMANGSLLNYLREMRHRFQTQQLLEMCKDVCEAMEYLESKQFLHRDLAARNCLVNDQGVVKVSDFGLSRYVLDDEYTSSVGSKFPVRWSPPEVLMYSKFSSKSDIWAFGVLMWEIYSLGKMPYERFTNSETAEHIAQGLRLYRPHLASEKVYTIMYSCWHEKADERPTFKILLSNILDVMDEES
  
Inhibitor
Name:
BDBM50175583
Synonyms:
ACP-196 | Acalabrutinib | US10239883, Example 6 | US10793576, Example ACP-196 | US10919899, ACP-196 | US10934296, Example 6 | US11420975, Acalabrutinlb | US9758524, Example 6
Type:
Small organic molecule
Emp. Form.:
C26H23N7O2
Mol. Mass.:
465.5065
SMILES:
[H][C@]1(CCCN1C(=O)C#CC)c1nc(-c2ccc(cc2)C(=O)Nc2ccccn2)c2c(N)nccn12 |r|
Structure:
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