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Target
Tyrosine-protein kinase BTK
Ligand
BDBM380440
Substrate
n/a
Meas. Tech.
Homogeneous Time-Resolved Fluorescence (HTRF)
IC50
<100.0±n/a nM
Citation
 Han, Y; Yu, R; Wang, Z; Liang, Z; Hu, Q; Zhu, L; Hu, Y; Sun, Y; Zhao, N; Peng, Y; Zhai, X; Luo, H; Xiao, D Inhibitors of bruton's tyrosine kinase US Patent  US9926299 Publication Date 3/27/2018 
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:
BDBM380440
Synonyms:
(R)-1-(1-acryloylpyrrolidin-3-yl)-5-amino-3-(3-methyl-4-(3-nitrophenoxy)phenyl)-1H-pyrazole-4-carboxamide | US9926299, 49
Type:
Small organic molecule
Emp. Form.:
C24H24N6O5
Mol. Mass.:
476.4846
SMILES:
Cc1cc(ccc1Oc1cccc(c1)[N+]([O-])=O)-c1nn([C@@H]2CCN(C2)C(=O)C=C)c(N)c1C(N)=O |r|
Structure:
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