Reaction Details |
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Target | Tyrosine-protein kinase ITK/TSK [357-620,Y512E] |
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Ligand | BDBM213219 |
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Substrate/Competitor | n/a |
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Meas. Tech. | LanthaScreen Kinase Binding Assay |
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IC50 | 13±0 nM |
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Citation | Harling, JD; Deakin, AM; Campos, S; Grimley, R; Chaudry, L; Nye, C; Polyakova, O; Bessant, CM; Barton, N; Somers, D; Barrett, J; Graves, RH; Hanns, L; Kerr, WJ; Solari, 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 |
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More Info.: | Get all data from this article, Assay Method |
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Tyrosine-protein kinase ITK/TSK [357-620,Y512E] |
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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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BDBM213219 |
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n/a |
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Name | BDBM213219 |
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) |
Type | Small organic molecule |
Emp. Form. | C23H27N7O2S |
Mol. Mass. | 465.571 |
SMILES | C=CC(=O)N1CC[C@@H](C1)Nc1cc(CN2CCOCC2)cc(Nc2nc3cccnc3s2)n1 |r| |
Structure |
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