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Target
Tyrosine-protein kinase BTK
Ligand
BDBM324386
Substrate
n/a
Meas. Tech.
BTK-POLYGAT-LS ASSAY
IC50
5.50±n/a nM
Citation
 Hopkins, BT; Ma, B; Prince, R; Marx, I; Lyssikatos, JP; Zheng, F; Peterson, M; Patience, DB Inhibiting agents for Bruton's tyrosine kinase US Patent  US10189829 Publication Date 1/29/2019 
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:
BDBM324386
Synonyms:
5-(tert-butyl)-N- (8-(2-((1- methyl-1H-pyrazol-4- yl)amino)pyrimidin-4- yl)-2-(tetrahydrofuran-3- yl)-2,3,4,5-tetrahydro- 1H-benzo[c]azepin- 5-yl)- 1,3,4-thiadiazole-2- carboxamide | US10189829, Compound 131 | US10227341, Compound 131 | US10961237, Compound 131, | US11858926, Compound 131
Type:
Small organic molecule
Emp. Form.:
C29H35N9O2S
Mol. Mass.:
573.712
SMILES:
Cn1cc(Nc2nccc(n2)-c2ccc3C(CCN(Cc3c2)C2CCOC2)NC(=O)c2nnc(s2)C(C)(C)C)cn1
Structure:
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