| Reaction Details |
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 | Report a problem with these data |
| Target | Tyrosine-protein kinase ITK/TSK [357-620,Y512E] |
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| Ligand | BDBM213223 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | LanthaScreen Kinase Binding Assay |
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| IC50 | 7.9±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] |
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| Synonyms: | EMT | ITK | ITK_HUMAN | Interlukin-2-inducible tyrosine kinase (Itk) | LYK |
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| Type: | Enzyme |
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| Mol. Mass.: | 30027.99 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Human Itk truncation (357-620 aa) with Y512E mutation |
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| Residue: | 264 |
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| Sequence: | VIDPSELTFVQEIGSGQFGLVHLGYWLNKDKVAIKTIREGAMSEEDFIEEAEVMMKLSHP
KLVQLYGVCLEQAPICLVFEFMEHGCLSDYLRTQRGLFAAETLLGMCLDVCEGMAYLEEA
CVIHRDLAARNCLVGENQVIKVSDFGMTRFVLDDQETSSTGTKFPVKWASPEVFSFSRYS
SKSDVWSFGVLMWEVFSEGKIPYENRSNSEVVEDISTGFRLYKPRLASTHVYQIMNHCWK
ERPEDRPAFSRLLRQLAEIAESGL
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| BDBM213223 |
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| n/a |
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| Name | BDBM213223 |
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| Synonyms: | 1-((S)-3-((4-((((R)-3,3-Dimethylbutan-2-yl)amino)methyl)-6-(thiazolo[5,4-b]pyridin-2-ylamino)pyridin-2-yl)amino)pyrrolidin-1-yl)prop-2-en-1-one (13) |
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| Type | Small organic molecule |
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| Emp. Form. | C25H33N7OS |
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| Mol. Mass. | 479.641 |
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| SMILES | C[C@@H](NCc1cc(N[C@H]2CCN(C2)C(=O)C=C)nc(Nc2nc3cccnc3s2)c1)C(C)(C)C |r| |
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| Structure | 
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