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Target
Tyrosine-protein kinase BTK [C481S]
Ligand
BDBM568357
Substrate
n/a
Meas. Tech.
In Vitro Inhibitory Activity Against BTK(wt)/BTK(C481S) (Determination of IC50 Value)
IC50
<0.1±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:
BDBM568357
Synonyms:
US11420975, Compound A-10-10
Type:
Small organic molecule
Emp. Form.:
C32H33F3N8O3
Mol. Mass.:
634.6514
SMILES:
Nc1nccn2c(nc(-c3ccc(cc3)C(=O)Nc3cc(ccn3)C(F)(F)F)c12)C12CCC(CC1)(C2)NC(=O)CN1CCOCC1
Structure:
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