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Target
Tyrosine-protein kinase BTK
Ligand
BDBM267873
Substrate
n/a
Meas. Tech.
ChEMBL_1706714 (CHEMBL4057947)
IC50
0.100000±n/a nM
Citation
 Boga, SB; Alhassan, AB; Liu, J; Guiadeen, D; Krikorian, A; Gao, X; Wang, J; Yu, Y; Anand, R; Liu, S; Yang, C; Wu, H; Cai, J; Zhu, H; Desai, J; Maloney, K; Gao, YD; Fischmann, TO; Presland, J; Mansueto, M; Xu, Z; Leccese, E; Knemeyer, I; Garlisi, CG; Bays, N; Stivers, P; Brandish, PE; Hicks, A; Cooper, A; Kim, RM; Kozlowski, JA Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis. Bioorg Med Chem Lett 27:3939-3943 (2017) [PubMed]  Article 
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:
BDBM267873
Synonyms:
4-(8-amino-3-{(3R)-1-[(3-methyloxetan-3-yl)carbonyl]piperidin-3-yl}imidazo[1,5-a]pyrazin-1-yl)-N-(4-chloropyridin-2-yl)-3-fluorobenzamide | US9718828, Example, 486
Type:
Small organic molecule
Emp. Form.:
C26H23F4N7O2
Mol. Mass.:
541.5001
SMILES:
CC(=O)N1CCC[C@H](C1)c1nc(-c2ccc(cc2F)C(=O)Nc2cc(ccn2)C(F)(F)F)c2c(N)nccn12 |r|
Structure:
Search PDB for entries with ligand similarity: