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TargetTyrosine-protein kinase Lck
LigandBDBM50341345
Substrate/Competitorn/a
Meas. Tech.ChEMBL_742455 (CHEMBL1769103)
Kd 1800±n/a nM
Citation Goldstein, DMSoth, MGabriel, TDewdney, NKuglstatter, AArzeno, HChen, JBingenheimer, WDalrymple, SADunn, JFarrell, RFrauchiger, SLa Fargue, JGhate, MGraves, BHill, RJLi, FLitman, RLoe, BMcIntosh, JMcWeeney, DPapp, EPark, JReese, HFRoberts, RTRotstein, DSan Pablo, BSarma, KStahl, MSung, MLSuttman, RTSjogren, EBTan, YTrejo, AWelch, MWeller, PWong, BRZecic, 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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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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BDBM50341345
n/a
NameBDBM50341345
Synonyms:6-(2-Chlorophenyl)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one | CHEMBL1766490
TypeSmall organic molecule
Emp. Form.C19H19ClN4O2
Mol. Mass.370.833
SMILESCn1c2nc(NC3CCOCC3)ncc2cc(-c2ccccc2Cl)c1=O
Structure
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