Reaction Details Report a problem with these data
Target
Tyrosine-protein kinase BTK
Ligand
BDBM209866
Substrate
n/a
Meas. Tech.
TR-FRET Competition Assay
pH
7.5±n/a
Ki
62.3±0.0 nM
Comments
extracted
Citation
 Telliez, JB; Dowty, ME; Wang, L; Jussif, J; Lin, T; Li, L; Moy, E; Balbo, P; Li, W; Zhao, Y; Crouse, K; Dickinson, C; Symanowicz, P; Hegen, M; Banker, ME; Vincent, F; Unwalla, R; Liang, S; Gilbert, AM; Brown, MF; Hayward, M; Montgomery, J; Yang, X; Bauman, J; Trujillo, JI; Casimiro-Garcia, A; Vajdos, FF; Leung, L; Geoghegan, KF; Quazi, A; Xuan, D; Jones, L; Hett, E; Wright, K; Clark, JD; Thorarensen, A Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition. ACS Chem Biol 11:3442-3451 (2016) [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:
BDBM209866
Synonyms:
PF-06651600 | US11111242, Example 5 | US20230348487, Example PF-06651600 | US9617258, Example 5
Type:
Small organic molecule
Emp. Form.:
C15H19N5O
Mol. Mass.:
285.3443
SMILES:
C[C@H]1CC[C@H](CN1C(=O)C=C)Nc1ncnc2[nH]ccc12 |r|
Structure:
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