Reaction Details
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Tyrosine-protein kinase BTK
Ligand
BDBM267593
Substrate
n/a
Meas. Tech.
Btk Enzyme Activity Assay A
pH
7.2±n/a
Temperature
298.15±n/a K
EC50
<10.00±n/a nM
Comments
extracted
Citation
De Man, AP; Sterrenburg, J; Raaijmakers, HC; Kaptein, A; Oubrie, AA; Rewinkel, JB; Jans, CG; Wijkmans, JC; Barf, TA; Cooper, AB; Kim, RM; Boga, SB; Zhu, HY; Gao, X; Yao, X; Anand, R; Wu, H; Liu, S; Yang, C; Alhassan, A; Wang, J; Yu, Y; Liu, J; Vaccaro, HM BTK Inhibitors US Patent US9718828 Publication Date 8/1/2017 More Info.:
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:
BDBM267593
Synonyms:
4-(8-amino-3-((trans)-6-methyl-1-(tetrahydrofuran-2-carbonyl)piperidin-3-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(4-(trifluoromethyl)pyridin-2-yl)benzamide | US9718828, Example, 186
Type:
Small organic molecule
Emp. Form.:
C28H29F3N8O2
Mol. Mass.:
566.5775
SMILES:
CCNC(=O)N1C[C@@H](CC[C@H]1C)c1nc(-c2ccc(cc2)C(=O)Nc2cc(ccn2)C(F)(F)F)c2c(N)nccn12 |r|
Structure:
