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TargetTyrosine-protein kinase Lck
LigandBDBM50374617
Substrate/Competitorn/a
Meas. Tech.ChEMBL_469608 (CHEMBL934187)
IC50 12±n/a nM
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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Tyrosine-protein kinase Lck
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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BDBM50374617
n/a
NameBDBM50374617
Synonyms:CHEMBL405430
TypeSmall organic molecule
Emp. Form.C35H38N8O3
Mol. Mass.618.728
SMILESCOc1cc(Nc2ncc3c(n2)n2c4ccccc4nc2n(-c2c(C)cccc2C)c3=O)ccc1OCCCN1CCN(C)CC1 |(-3.89,-6.67,;-5.23,-7.43,;-5.23,-8.97,;-3.9,-9.74,;-3.91,-11.29,;-2.58,-12.06,;-1.25,-11.29,;-1.24,-9.74,;.08,-8.97,;1.42,-9.74,;1.42,-11.28,;.08,-12.06,;2.76,-12.05,;3.08,-13.56,;2.17,-14.79,;2.79,-16.2,;4.32,-16.36,;5.22,-15.13,;4.6,-13.73,;5.24,-12.32,;4.09,-11.29,;4.1,-9.74,;5.43,-8.97,;5.43,-7.44,;4.09,-6.67,;6.75,-6.67,;8.1,-7.44,;8.09,-8.98,;6.76,-9.75,;6.75,-11.29,;2.76,-8.96,;2.76,-7.42,;-5.23,-12.05,;-6.57,-11.29,;-6.57,-9.74,;-7.9,-8.97,;-9.24,-9.74,;-10.57,-8.97,;-10.57,-7.43,;-9.24,-6.66,;-7.9,-7.44,;-6.57,-6.68,;-6.56,-5.14,;-5.23,-4.37,;-7.9,-4.36,;-9.24,-5.13,)|
Structure
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