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Target
Tyrosine-protein kinase BTK
Ligand
BDBM480424
Substrate
n/a
Meas. Tech.
In Vitro Kinase Assay
IC50
<1.000±n/a nM
Citation
 Hopkins, BT; Ma, B; Prince, R; Marx, I; Schulz, J; Nevalainen, M; Dechantsreiter, M Inhibiting agents for Bruton's tyrosine kinase US Patent  US10899753 Publication Date 1/26/2021 
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:
BDBM480424
Synonyms:
(R)-2-(tert-butyl)-N-(1-fluoro-2-(4-((1-methyl-1H-pyrazol-3-yl)amino)-1,3,5-triazin-2-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-5-yl)oxazole-4-carboxamide | US10899753, Example 112
Type:
Small organic molecule
Emp. Form.:
C26H29FN8O2
Mol. Mass.:
504.5593
SMILES:
Cn1ccc(Nc2ncnc(n2)-c2ccc3[C@@H](CCCCc3c2F)NC(=O)c2coc(n2)C(C)(C)C)n1 |r|
Structure:
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