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Target
Tyrosine-protein kinase BTK
Ligand
BDBM441040
Substrate
n/a
Meas. Tech.
Inhibition TR-FRET (Time Resolved FRET) Assay
IC50
3200±n/a nM
Citation
 Frattini, S; Bakker, R; Giovannini, R; Fossati, G; Hamprecht, D; Lingard, I; Pautsch, A; Wellenzohn, B Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors US Patent  US10640486 Publication Date 5/5/2020 
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:
BDBM441040
Synonyms:
1-[4-(3-Oxo-tetrahydro-imidazo[5,1-c][1,4]oxazin-2-yl)-benzyl]-1H-[1,2,3]triazole-4-carboxylic acid (2-amino-4-methyl-6,7-dihydro-5H-[1]pyrindin-5-yl)-amide | US10640486, Example 87
Type:
Small organic molecule
Emp. Form.:
C25H28N8O3
Mol. Mass.:
488.5416
SMILES:
Cc1cc(N)nc2CCC(NC(=O)c3cn(Cc4ccc(cc4)N4CC5COCCN5C4=O)nn3)c12
Structure:
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