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Target
Tyrosine-protein kinase BTK [C481S]
Ligand
BDBM412841
Substrate
n/a
Meas. Tech.
BTKC481S Binding Affinity
IC50
<10±n/a nM
Citation
 Guisot, N Pyrazolopyrimidine derivatives as BTK inhibitors for the treatment of cancer US Patent  US10399989 Publication Date 9/3/2019 
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:
BDBM412841
Synonyms:
N-[[4-[4-amino-1-[(1R,4R)-4-fluorocyclopent-2-en-1-yl]pyrazolo[3,4-d]pyrimidin-3-yl]phenyl]methyl]-2-methoxy-benzamide | US10399989, Example 54 | US10611766, Example 54
Type:
Small organic molecule
Emp. Form.:
C25H23FN6O2
Mol. Mass.:
458.4875
SMILES:
COc1ccccc1C(=O)NCc1ccc(cc1)-c1nn([C@@H]2C[C@@H](F)C=C2)c2ncnc(N)c12 |r,c:27|
Structure:
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