Target
Tyrosine-protein kinase BTK
Ligand
BDBM350138
Substrate
n/a
Meas. Tech.
Btk Enzyme Activity Assay
IC50
52.0±n/a nM
Citation
 Liu, JKozlowski, JAAndresen, BMBoga, SBGao, XGuiadeen, DGCai, JLiu, SWang, DWu, HYang, C Tertiary alcohol imidazopyrazine BTK inhibitors US Patent  US10208047 Publication Date 2/19/2019 
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:
BDBM350138
Synonyms:
4-[8-amino-1-(4-{(1R)-1- hydroxy-1-[3- (trifluoromethyl)phenyl] ethyl}phenyl)imidazo[1,5- a]pyrazin-3-yl]-2,5- dioxobicyclo[2.2.2]octane- 1-carboxylic acid | US10208047, Example 6
Type:
Small organic molecule
Emp. Form.:
C30H25F3N4O5
Mol. Mass.:
578.5385
SMILES:
C[C@@](O)(c1ccc(cc1)-c1nc(n2ccnc(N)c12)C12CCC(CC1=O)(C(O)=O)C(=O)C2)c1cccc(c1)C(F)(F)F |r|
Structure:
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