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TargetTyrosine-protein kinase BTK
LigandBDBM165319
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1983359 (CHEMBL4616765)
IC50 18±n/a nM
Citation Watterson, SHLiu, QBeaudoin Bertrand, MBatt, DGLi, LPattoli, MASkala, SCheng, LObermeier, MTMoore, RYang, ZVickery, RElzinga, PADiscenza, LD'Arienzo, CGillooly, KMTaylor, TLPulicicchio, CZhang, YHeimrich, EMcIntyre, KWRuan, QWesthouse, RACatlett, IMZheng, NChaudhry, CDai, JGalella, MATebben, AJPokross, MLi, JZhao, RSmith, DRampulla, RAllentoff, AWallace, MAMathur, ASalter-Cid, LMacor, JECarter, PHFura, ABurke, JRTino, JA Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK). J Med Chem62:3228-3250 (2019) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Tyrosine-protein kinase BTK
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:
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEK
ITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEEL
RKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSS
HRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDE
YFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGK
EGGFIVRDSSKAGKYTVSVFAKSTGDPQGVIRHYVVCSTPQSQYYLAEKHLFSTIPELIN
YHQHNSAGLISRLKYPVSQQNKNAPSTAGLGYGSWEIDPKDLTFLKELGTGQFGVVKYGK
WRGQYDVAIKMIKEGSMSEDEFIEEAKVMMNLSHEKLVQLYGVCTKQRPIFIITEYMANG
CLLNYLREMRHRFQTQQLLEMCKDVCEAMEYLESKQFLHRDLAARNCLVNDQGVVKVSDF
GLSRYVLDDEYTSSVGSKFPVRWSPPEVLMYSKFSSKSDIWAFGVLMWEIYSLGKMPYER
FTNSETAEHIAQGLRLYRPHLASEKVYTIMYSCWHEKADERPTFKILLSNILDVMDEES
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM165319
n/a
NameBDBM165319
Synonyms:US10604504, Example 115 | US11623921, Example 115 | US9688629, 115 | US9802915, Example 115 | US9920031, Example 115
TypeSmall organic molecule
Emp. Form.C19H22N4O2
Mol. Mass.338.4036
SMILESCc1[nH]c2c(ccc(N3CCC[C@@H](C3)NC(=O)C#C)c2c1C)C(N)=O |r|
Structure
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