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Target
Tyrosine-protein kinase BTK
Ligand
BDBM374597
Substrate
n/a
Meas. Tech.
25P Btk Enzyme Activity Assay
IC50
0.150±n/a nM
Citation
Siu, T; Altman, MD; Andresen, BM; Liu, J; Kozlowski, J; Boga, SB; Yu, Y; Anand, R; Cai, J; Wang, D; Liu, S Indazole and azaindazole Btk inhibitors US Patent US10246457 Publication Date 4/2/2019
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:
BDBM374597
Synonyms:
2-[3-{3-amino-7-[1-(1-methylethyl)-1H-pyrazol-4-yl]-1H-indazol-5-yl}-2-(hydroxymethyl)phenyl]-6-tert-butyl-8-fluorophthalazin-1(2H)-one | US10246457, Example 6
Type:
Small organic molecule
Emp. Form.:
C32H32FN7O2
Mol. Mass.:
565.6406
SMILES:
CC(C)n1cc(cn1)-c1cc(cc2c(N)n[nH]c12)-c1cccc(c1CO)-n1ncc2cc(cc(F)c2c1=O)C(C)(C)C