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TargetTyrosine-protein kinase ITK/TSK [357-620,Y512E]
LigandBDBM213219
Substrate/Competitorn/a
Meas. Tech.LanthaScreen Kinase Binding Assay
IC50 2.0e+2±0 nM
Citation Harling, JDDeakin, AMCampos, SGrimley, RChaudry, LNye, CPolyakova, OBessant, CMBarton, NSomers, DBarrett, JGraves, RHHanns, LKerr, WJSolari, R Discovery of novel irreversible inhibitors of interleukin (IL)-2-inducible tyrosine kinase (Itk) by targeting cysteine 442 in the ATP pocket. J Biol Chem288:28195-206 (2013) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Tyrosine-protein kinase ITK/TSK [357-620,Y512E]
Name:Tyrosine-protein kinase ITK/TSK [357-620,Y512E]
Synonyms:EMT | ITK | ITK_HUMAN | Interlukin-2-inducible tyrosine kinase (Itk) | LYK
Type:Enzyme
Mol. Mass.:30027.99
Organism:Homo sapiens (Human)
Description:Human Itk truncation (357-620 aa) with Y512E mutation
Residue:264
Sequence:
VIDPSELTFVQEIGSGQFGLVHLGYWLNKDKVAIKTIREGAMSEEDFIEEAEVMMKLSHP
KLVQLYGVCLEQAPICLVFEFMEHGCLSDYLRTQRGLFAAETLLGMCLDVCEGMAYLEEA
CVIHRDLAARNCLVGENQVIKVSDFGMTRFVLDDQETSSTGTKFPVKWASPEVFSFSRYS
SKSDVWSFGVLMWEVFSEGKIPYENRSNSEVVEDISTGFRLYKPRLASTHVYQIMNHCWK
ERPEDRPAFSRLLRQLAEIAESGL
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  Blast E-value cutoff:
BDBM213219
n/a
NameBDBM213219
Synonyms:(S)-1-(3-((4-(Morpholinomethyl)-6-(thiazolo[5,4-b]pyridin-2-ylamino)pyridin-2-yl)amino)pyrrolidin-1-yl)propan-1-one (15) | N-[(3S)-1-Acryloyl-3-pyrrolidinyl]-4-(4-morpholinylmethyl)-N'-[1,3]thiazolo[5,4-b]pyridin-2-yl-2,6-pyridinediamine (8)
TypeSmall organic molecule
Emp. Form.C23H27N7O2S
Mol. Mass.465.571
SMILESC=CC(=O)N1CC[C@@H](C1)Nc1cc(CN2CCOCC2)cc(Nc2nc3cccnc3s2)n1 |r|
Structure
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