Reaction Details |
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Target | Tyrosine-protein kinase Lck |
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Ligand | BDBM50374628 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_469608 (CHEMBL934187) |
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IC50 | 6±n/a nM |
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Citation | Martin, MW; Newcomb, J; Nunes, JJ; Boucher, C; Chai, L; Epstein, LF; Faust, T; Flores, S; Gallant, P; Gore, A; Gu, Y; Hsieh, F; Huang, X; Kim, JL; Middleton, S; Morgenstern, K; Oliveira-dos-Santos, A; Patel, VF; Powers, D; Rose, P; Tudor, Y; Turci, SM; Welcher, AA; Zack, D; Zhao, H; Zhu, L; Zhu, X; Ghiron, C; Ermann, M; Johnston, D; Saluste, CG Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity. J Med Chem51:1637-48 (2008) [PubMed] Article |
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More Info.: | Get all data from this article, 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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BDBM50374628 |
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n/a |
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Name | BDBM50374628 |
Synonyms: | CHEMBL271131 |
Type | Small organic molecule |
Emp. Form. | C25H23N7O3 |
Mol. Mass. | 469.4952 |
SMILES | COc1cc(Nc2ncnc(n2)-n2c(Nc3ccccc3)nc3ccccc23)cc(OC)c1OC |
Structure |
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