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Target
Tyrosine-protein kinase Lyn
Ligand
BDBM50198782
Substrate
n/a
Meas. Tech.
ChEMBL_478597 (CHEMBL934544)
Ki
25.9±n/a nM
Citation
 Hu, SX; Soll, R; Yee, S; Lohse, DL; Kousba, A; Zeng, B; Yu, X; McPherson, A; Renick, J; Cao, J; Tabak, A; Hood, J; Doukas, J; Noronha, G; Martin, M Metabolism and pharmacokinetics of a novel Src kinase inhibitor TG100435 ([7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine) and its active N-oxide metabolite TG100855 ([7-(2,6-dichloro-phenyl)-5-methylbenzo[1,2,4]triazin-3-yl]-{4-[2-(1-oxy-pyrr Drug Metab Dispos 35:929-36 (2007) [PubMed]  Article 
Target
Name:
Tyrosine-protein kinase Lyn
Synonyms:
JTK8 | LYN | LYN_HUMAN | Lck/Yes-related novel protein tyrosine kinase | Tyrosine-protein kinase Lyn (LYN) | V-yes-1 Yamaguchi sarcoma viral related oncogene homolog | p53Lyn | p56Lyn
Type:
Protein
Mol. Mass.:
58575.92
Organism:
Homo sapiens (Human)
Description:
P07948
Residue:
512
Sequence:
MGCIKSKGKDSLSDDGVDLKTQPVRNTERTIYVRDPTSNKQQRPVPESQLLPGQRFQTKDPEEQGDIVVALYPYDGIHPDDLSFKKGEKMKVLEEHGEWWKAKSLLTKKEGFIPSNYVAKLNTLETEEWFFKDITRKDAERQLLAPGNSAGAFLIRESETLKGSFSLSVRDFDPVHGDVIKHYKIRSLDNGGYYISPRITFPCISDMIKHYQKQADGLCRRLEKACISPKPQKPWDKDAWEIPRESIKLVKRLGAGQFGEVWMGYYNNSTKVAVKTLKPGTMSVQAFLEEANLMKTLQHDKLVRLYAVVTREEPIYIITEYMAKGSLLDFLKSDEGGKVLLPKLIDFSAQIAEGMAYIERKNYIHRDLRAANVLVSESLMCKIADFGLARVIEDNEYTAREGAKFPIKWTAPEAINFGCFTIKSDVWSFGILLYEIVTYGKIPYPGRTNADVMTALSQGYRMPRVENCPDELYDIMKMCWKEKAEERPTFDYLQSVLDDFYTATEGQYQQQP
  
Inhibitor
Name:
BDBM50198782
Synonyms:
([7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine) | 7-(2,6-dichlorophenyl)-5-methyl-N-(4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)benzo[e][1,2,4]triazin-3-amine | 7-(2,6-dichlorophenyl)-5-methyl-N-[4-(2-pyrrolidin-1-ylethoxy)-phenyl]-1,2,4-benzotriazin-3-amine | CHEMBL230686 | TG-100435 | US8481536, 367 | US8481536, 575
Type:
Small organic molecule
Emp. Form.:
C26H25Cl2N5O
Mol. Mass.:
494.416
SMILES:
Cc1cc(cc2nnc(Nc3ccc(OCCN4CCCC4)cc3)nc12)-c1c(Cl)cccc1Cl
Structure:
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