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TargetTyrosine-protein kinase Yes
LigandBDBM255256
Substrate/Competitorn/a
Meas. Tech.ChEMBL_2071898 (CHEMBL4727432)
IC50 12±n/a nM
Citation Liu, JGuiadeen, DKrikorian, AGao, XWang, JBabu Boga, SAlhassan, ABYu, WSelyutin, OYu, YAnand, RXu, JKelly, JDuffy, JLLiu, SYang, CWu, HCai, JBennett, CMaloney, KMTyagarajan, SGao, YDFischmann, TOPresland, JMansueto, MXu, ZLeccese, EZhang-Hoover, JKnemeyer, IGarlisi, CGStivers, PBrandish, PEHicks, AKim, RKozlowski, JA Potent, non-covalent reversible BTK inhibitors with 8-amino-imidazo[1,5-a]pyrazine core featuring 3-position bicyclic ring substitutes. Bioorg Med Chem Lett30:0 (2020) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Tyrosine-protein kinase Yes
Name:Tyrosine-protein kinase Yes
Synonyms:Proto-oncogene c-Yes | VHL/Tyrosine-protein kinase Yes | YES | YES1 | YES_HUMAN | p61-yes
Type:Protein
Mol. Mass.:60801.54
Organism:Homo sapiens (Human)
Description:P07947
Residue:543
Sequence:
MGCIKSKENKSPAIKYRPENTPEPVSTSVSHYGAEPTTVSPCPSSSAKGTAVNFSSLSMT
PFGGSSGVTPFGGASSSFSVVPSSYPAGLTGGVTIFVALYDYEARTTEDLSFKKGERFQI
INNTEGDWWEARSIATGKNGYIPSNYVAPADSIQAEEWYFGKMGRKDAERLLLNPGNQRG
IFLVRESETTKGAYSLSIRDWDEIRGDNVKHYKIRKLDNGGYYITTRAQFDTLQKLVKHY
TEHADGLCHKLTTVCPTVKPQTQGLAKDAWEIPRESLRLEVKLGQGCFGEVWMGTWNGTT
KVAIKTLKPGTMMPEAFLQEAQIMKKLRHDKLVPLYAVVSEEPIYIVTEFMSKGSLLDFL
KEGDGKYLKLPQLVDMAAQIADGMAYIERMNYIHRDLRAANILVGENLVCKIADFGLARL
IEDNEYTARQGAKFPIKWTAPEAALYGRFTIKSDVWSFGILQTELVTKGRVPYPGMVNRE
VLEQVERGYRMPCPQGCPESLHELMNLCWKKDPDERPTFEYIQSFLEDYFTATEPQYQPG
ENL
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM255256
n/a
NameBDBM255256
Synonyms:US9481682, 4
TypeSmall organic molecule
Emp. Form.C27H24F3N7O2
Mol. Mass.535.5204
SMILESNc1nccn2c(nc(-c3ccc(cc3)C(=O)Nc3cc(ccn3)C(F)(F)F)c12)[C@@H]1CC[C@H]2CCC(=O)N2C1 |r|
Structure
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