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TargetTyrosine-protein kinase ITK/TSK [357-620,Y512E]
LigandBDBM213215
Substrate/Competitorn/a
Meas. Tech.LanthaScreen Kinase Binding Assay
IC50 3.2e+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:
BDBM213215
n/a
NameBDBM213215
Synonyms:N-(cis-2-{[4-(4-Morpholinylmethyl)-6-([1,3]thiazolo[5,4-b]pyridin-2-ylamino)-2-pyrimidinyl]amino}cyclohexyl)-2-propenamide (4)
TypeSmall organic molecule
Emp. Form.C24H30N8O2S
Mol. Mass.494.612
SMILESC=CC(=O)N[C@H]1CCCC[C@H]1Nc1nc(CN2CCOCC2)cc(Nc2nc3cccnc3s2)n1 |r|
Structure
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