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Target
Tyrosine-protein kinase BTK
Ligand
BDBM17744
Substrate
n/a
Meas. Tech.
HTRF Kinase Inhibition Assay
IC50
100±n/a nM
Citation
 Martin, MW; Newcomb, J; Nunes, JJ; McGowan, DC; Armistead, DM; Boucher, C; Buchanan, JL; Buckner, W; Chai, L; Elbaum, D; Epstein, LF; Faust, T; Flynn, S; Gallant, P; Gore, A; Gu, Y; Hsieh, F; Huang, X; Lee, JH; Metz, D; Middleton, S; Mohn, D; Morgenstern, K; Morrison, MJ; Novak, PM; Oliveira-dos-Santos, A; Powers, D; Rose, P; Schneider, S; Sell, S; Tudor, Y; Turci, SM; Welcher, AA; White, RD; Zack, D; Zhao, H; Zhu, L; Zhu, X; Ghiron, C; Amouzegh, P; Ermann, M; Jenkins, J; Johnston, D; Napier, S; Power, E Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity. J Med Chem 49:4981-91 (2006) [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:
BDBM17744
Synonyms:
2,6-dimethylphenyl N-[2-({3,5-dimethoxy-4-[3-(4-methylpiperazin-1-yl)propoxy]phenyl}amino)pyrimidin-4-yl]-N-(2,4-dimethoxyphenyl)carbamate | 2-aminopyrimidine carbamate, 43
Type:
Small organic molecule
Emp. Form.:
C37H46N6O7
Mol. Mass.:
686.7971
SMILES:
COc1ccc(N(C(=O)Oc2c(C)cccc2C)c2ccnc(Nc3cc(OC)c(OCCCN4CCN(C)CC4)c(OC)c3)n2)c(OC)c1
Structure:
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