Reaction Details |
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Target | Tyrosine-protein kinase Lck |
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Ligand | BDBM50341345 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_742455 (CHEMBL1769103) |
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Kd | 1800±n/a nM |
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Citation | Goldstein, DM; Soth, M; Gabriel, T; Dewdney, N; Kuglstatter, A; Arzeno, H; Chen, J; Bingenheimer, W; Dalrymple, SA; Dunn, J; Farrell, R; Frauchiger, S; La Fargue, J; Ghate, M; Graves, B; Hill, RJ; Li, F; Litman, R; Loe, B; McIntosh, J; McWeeney, D; Papp, E; Park, J; Reese, HF; Roberts, RT; Rotstein, D; San Pablo, B; Sarma, K; Stahl, M; Sung, ML; Suttman, RT; Sjogren, EB; Tan, Y; Trejo, A; Welch, M; Weller, P; Wong, BR; Zecic, H Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors J Med Chem54:2255-65 (2011) [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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BDBM50341345 |
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n/a |
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Name | BDBM50341345 |
Synonyms: | 6-(2-Chlorophenyl)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one | CHEMBL1766490 |
Type | Small organic molecule |
Emp. Form. | C19H19ClN4O2 |
Mol. Mass. | 370.833 |
SMILES | Cn1c2nc(NC3CCOCC3)ncc2cc(-c2ccccc2Cl)c1=O |
Structure |
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