Target
Tyrosine-protein kinase BTK [386-659]
Ligand
BDBM467843
Substrate
n/a
Meas. Tech.
Kinase Lanthascreen Binding Assay
IC50
10.0±n/a nM
Citation
 Arora, NBacani, GMBarbay, JKBembenek, SDCai, MChen, WDeckhut, CPEdwards, JPGhosh, BHao, BKreutter, KDLi, GTichenor, MSVenable, JDWei, JWiener, JJWu, YZhu, YZhang, FZhang, ZXiao, K Inhibitors of Bruton's tyrosine kinase and methods of their use US Patent  US10822348 Publication Date 11/3/2020 
Target
Name:
Tyrosine-protein kinase BTK [386-659]
Synonyms:
AGMX1 | ATK | BPK | BTK | BTK_HUMAN | Tyrosine-protein kinase BTK (386-659)
Type:
Enzyme Catalytic Domain
Mol. Mass.:
31815.18
Organism:
Homo sapiens (Human)
Description:
aa 386-659
Residue:
274
Sequence:
STAGLGYGSWEIDPKDLTFLKELGTGQFGVVKYGKWRGQYDVAIKMIKEGSMSEDEFIEEAKVMMNLSHEKLVQLYGVCTKQRPIFIITEYMANGCLLNYLREMRHRFQTQQLLEMCKDVCEAMEYLESKQFLHRDLAARNCLVNDQGVVKVSDFGLSRYVLDDEYTSSVGSKFPVRWSPPEVLMYSKFSSKSDIWAFGVLMWEIYSLGKMPYERFTNSETAEHIAQGLRLYRPHLASEKVYTIMYSCWHEKADERPTFKILLSNILDVMDEES
  
Inhibitor
Name:
BDBM467843
Synonyms:
(R)-N-(1-Acryloylpiperidin-3-yl)-5-(2'-methyl-[1,1'-biphenyl]-3-yl)- 4-oxo-4,5-dihydro-3H-1-thia-3,5,8-triazaacenaphthylene-2- carboxamide; | US10800792, Example 504 | US10822348, Example 504
Type:
Small organic molecule
Emp. Form.:
C30H27N5O3S
Mol. Mass.:
537.632
SMILES:
Cc1ccccc1-c1cccc(c1)-n1c2ccnc3sc(C(=O)N[C@@H]4CCCN(C4)C(=O)C=C)c([nH]c1=O)c23 |r|
Structure:
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