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Target
Tyrosine-protein kinase BTK
Ligand
BDBM263560
Substrate
n/a
Meas. Tech.
TR-FRET (Time Resolved FRET) Assay
pH
7.15±n/a
IC50
3.20±0 nM
Comments
extracted
Citation
 Lopez-Tapia, FJ; Kong, N; So, S; Lou, Y; Dominique, R Inhibitors of bruton's tyrosine kinase US Patent  US9556150 Publication Date 1/31/2017 
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:
BDBM263560
Synonyms:
2-{5-amino-1-[2-chloro-4-(3- cyano-2-fluoro-phenoxy)- phenyl]-1h-pyrazole-4- carbonyl}-1h-indole-5- carboxylic acid | US9556150, i-48
Type:
Small organic molecule
Emp. Form.:
C26H15ClFN5O4
Mol. Mass.:
515.88
SMILES:
Nc1c(cnn1-c1ccc(Oc2cccc(C#N)c2F)cc1Cl)C(=O)c1cc2cc(ccc2[nH]1)C(O)=O
Structure:
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