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Target
Tyrosine-protein kinase BTK
Ligand
BDBM377753
Substrate
n/a
Meas. Tech.
Human BTK LanthaScreen Assay
IC50
1.60±n/a nM
Citation
 Springer, JR; Devadas, B; Garland, DJ; Grapperhaus, ML; Han, S; Hockerman, SL; Hughes, RO; Saiah, E; Schnute, ME; Selness, SR; Walker, DP; Wan, Z; Xing, L; Zapf, CW; Schmidt, MA Bruton's tyrosine kinase inhibitors US Patent  US10266513 Publication Date 4/23/2019 
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:
BDBM377753
Synonyms:
5-amino-1-(1-cyanopiperidin-3-yl)- 3-{4-[4-fluoro-2- methoxyphenoxy]phenyl}-1H- pyrazole-4-carboxamide | US10266513, Example 47 | US10815213, Example 47
Type:
Small organic molecule
Emp. Form.:
C23H23FN6O3
Mol. Mass.:
450.4655
SMILES:
COc1cc(F)ccc1Oc1ccc(cc1)-c1nn(C2CCCN(C2)C#N)c(N)c1C(N)=O
Structure:
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