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Target
Tyrosine-protein kinase BTK
Ligand
BDBM374599
Substrate
n/a
Meas. Tech.
25P Btk Enzyme Activity Assay
IC50
268±n/a nM
Citation
 Siu, T; Altman, MD; Andresen, BM; Liu, J; Kozlowski, J; Boga, SB; Yu, Y; Anand, R; Cai, J; Wang, D; Liu, S Indazole and azaindazole Btk inhibitors US Patent  US10246457 Publication Date 4/2/2019 
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:
BDBM374599
Synonyms:
3-amino-5-[3-({[2-fluoro-4-(2,2,2-trifluoro-1,1-dimethylethyl)phenyl]carbonyl}amino)-2-methylphenyl]-1H-indazole-7-carboxamide | US10246457, Example 8
Type:
Small organic molecule
Emp. Form.:
C26H23F4N5O2
Mol. Mass.:
513.4867
SMILES:
Cc1c(NC(=O)c2ccc(cc2F)C(C)(C)C(F)(F)F)cccc1-c1cc(C(N)=O)c2[nH]nc(N)c2c1
Structure:
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