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Target
Tyrosine-protein kinase BTK
Ligand
BDBM263565
Substrate
n/a
Meas. Tech.
TR-FRET (Time Resolved FRET) Assay
pH
7.15±n/a
IC50
1.70±0 nM
Comments
extracted
Citation
 Lopez-Tapia, FJ; Kong, N; So, S; Lou, Y; Dominique, R Inhibitors of bruton's tyrosine kinase US Patent  US9556150 Publication Date 1/31/2017 
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:
BDBM263565
Synonyms:
2-(4-{5-amino-4-[5-(3- dimethylamino-pyrrolidine-1- carbonyl)-1h-indole-2-carbonyl]- pyrazol-1yl}-3-chloro-phenoxy)- n,n-dimethyl-benzamide acetic acid salt | US9556150, i-53
Type:
Small organic molecule
Emp. Form.:
C33H32ClN7O4
Mol. Mass.:
626.105
SMILES:
CNC1CCN(C1)C(=O)c1ccc2[nH]c(cc2c1)C(=O)c1cnn(c1N)-c1ccc(Oc2ccccc2C(=O)N(C)C)cc1Cl
Structure:
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