Target
Tyrosine-protein kinase BTK
Ligand
BDBM324368
Substrate
n/a
Meas. Tech.
BTK-POLYGAT-LS ASSAY
IC50
5.50±n/a nM
Citation
 Hopkins, BTMa, BPrince, RMarx, ILyssikatos, JPZheng, FPeterson, MPatience, 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:
BDBM324368
Synonyms:
5-(2-cyanopropan-2-yl)- N-(2-(2-hydroxyethyl)-8- (2-((1-methyl-1H- pyrazol-4- yl)amino)pyrimidin-4- yl)-2,3,4,5-tetrahydro- 1H-benzo[c]azepin-5-yl)- 1,3,4-oxadiazole-2- carboxamide | US10189829, Compound 64 | US10227341, Compound 64 | US10961237, Compound 64 | US11858926, Compound 64
Type:
Small organic molecule
Emp. Form.:
C27H30N10O3
Mol. Mass.:
542.5923
SMILES:
Cn1cc(Nc2nccc(n2)-c2ccc3C(CCN(CCO)Cc3c2)NC(=O)c2nnc(o2)C(C)(C)C#N)cn1
Structure:
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