Reaction Details |
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Target | Tyrosine-protein kinase Lck |
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Ligand | BDBM17738 |
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Substrate/Competitor | biotinylated gastrin substrate |
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Meas. Tech. | HTRF Kinase Inhibition Assay |
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pH | 7.5±n/a |
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Temperature | 295.15±n/a K |
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IC50 | 1±n/a nM |
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Citation | Martin, MW; Newcomb, J; Nunes, JJ; McGowan, DC; Armistead, DM; Boucher, C; Buchanan, JL; Buckner, W; Chai, L; Elbaum, D; Epstein, LF; Faust, T; Flynn, S; Gallant, P; Gore, A; Gu, Y; Hsieh, F; Huang, X; Lee, JH; Metz, D; Middleton, S; Mohn, D; Morgenstern, K; Morrison, MJ; Novak, PM; Oliveira-dos-Santos, A; Powers, D; Rose, P; Schneider, S; Sell, S; Tudor, Y; Turci, SM; Welcher, AA; White, RD; Zack, D; Zhao, H; Zhu, L; Zhu, X; Ghiron, C; Amouzegh, P; Ermann, M; Jenkins, J; Johnston, D; Napier, S; Power, E Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity. J Med Chem49:4981-91 (2006) [PubMed] Article |
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More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
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Tyrosine-protein kinase Lck |
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Name: | Tyrosine-protein kinase Lck |
Synonyms: | 2.7.10.2 | LCK | LCK_HUMAN | LSK | Leukocyte C-terminal Src kinase | Lymphocyte cell-specific protein-tyrosine kinase | Lymphocyte-specific protein tyrosine kinase | P56-LCK | Protein YT16 | Proto-oncogene Lck | Proto-oncogene tyrosine-protein kinase LCK | Src/Lck kinase | T cell-specific protein-tyrosine kinase |
Type: | n/a |
Mol. Mass.: | 57987.83 |
Organism: | Homo sapiens (Human) |
Description: | P06239 |
Residue: | 509 |
Sequence: | MGCGCSSHPEDDWMENIDVCENCHYPIVPLDGKGTLLIRNGSEVRDPLVTYEGSNPPASP
LQDNLVIALHSYEPSHDGDLGFEKGEQLRILEQSGEWWKAQSLTTGQEGFIPFNFVAKAN
SLEPEPWFFKNLSRKDAERQLLAPGNTHGSFLIRESESTAGSFSLSVRDFDQNQGEVVKH
YKIRNLDNGGFYISPRITFPGLHELVRHYTNASDGLCTRLSRPCQTQKPQKPWWEDEWEV
PRETLKLVERLGAGQFGEVWMGYYNGHTKVAVKSLKQGSMSPDAFLAEANLMKQLQHQRL
VRLYAVVTQEPIYIITEYMENGSLVDFLKTPSGIKLTINKLLDMAAQIAEGMAFIEERNY
IHRDLRAANILVSDTLSCKIADFGLARLIEDNEYTAREGAKFPIKWTAPEAINYGTFTIK
SDVWSFGILLTEIVTHGRIPYPGMTNPEVIQNLERGYRMVRPDNCPEELYQLMRLCWKER
PEDRPTFDYLRSVLEDFFTATEGQYQPQP
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BDBM17738 |
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biotinylated gastrin substrate |
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Name: | biotinylated gastrin substrate |
Synonyms: | n/a |
Type: | Peptide |
Mol. Mass.: | 2100.22 |
Organism: | n/a |
Description: | n/a |
Residue: | 17 |
Sequence: | |