Target
Tyrosine-protein kinase BTK
Ligand
BDBM324346
Substrate
n/a
Meas. Tech.
In Vitro BTK Kinase Assay
IC50
505±n/a nM
Citation
 Hopkins, BTMa, BPrince, RMarx, ILyssikatos, JP Inhibiting agents for bruton's tyrosine kinase US Patent  US10227341 Publication Date 3/12/2019 
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:
BDBM324346
Synonyms:
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)-5- (1-methylcyclopropyl)- 1,3,4-oxadiazole-2- carboxamide | US10189829, Compound 125 | US10227341, Compound 125 | US10961237, Compound 125 | US11858926, Compound 125
Type:
Small organic molecule
Emp. Form.:
C27H31N9O3
Mol. Mass.:
529.5935
SMILES:
Cn1cc(Nc2nccc(n2)-c2ccc3C(CCN(CCO)Cc3c2)NC(=O)c2nnc(o2)C2(C)CC2)cn1
Structure:
Search PDB for entries with ligand similarity: