Reaction Details |
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Target | Tyrosine-protein kinase Lyn |
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Ligand | BDBM50151366 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_305891 (CHEMBL832906) |
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IC50 | >0.500000±n/a nM |
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Citation | Chen, P; Doweyko, AM; Norris, D; Gu, HH; Spergel, SH; Das, J; Moquin, RV; Lin, J; Wityak, J; Iwanowicz, EJ; McIntyre, KW; Shuster, DJ; Behnia, K; Chong, S; de Fex, H; Pang, S; Pitt, S; Shen, DR; Thrall, S; Stanley, P; Kocy, OR; Witmer, MR; Kanner, SB; Schieven, GL; Barrish, JC Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity. J Med Chem47:4517-29 (2004) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Tyrosine-protein kinase Lyn |
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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: | MGCIKSKGKDSLSDDGVDLKTQPVRNTERTIYVRDPTSNKQQRPVPESQLLPGQRFQTKD
PEEQGDIVVALYPYDGIHPDDLSFKKGEKMKVLEEHGEWWKAKSLLTKKEGFIPSNYVAK
LNTLETEEWFFKDITRKDAERQLLAPGNSAGAFLIRESETLKGSFSLSVRDFDPVHGDVI
KHYKIRSLDNGGYYISPRITFPCISDMIKHYQKQADGLCRRLEKACISPKPQKPWDKDAW
EIPRESIKLVKRLGAGQFGEVWMGYYNNSTKVAVKTLKPGTMSVQAFLEEANLMKTLQHD
KLVRLYAVVTREEPIYIITEYMAKGSLLDFLKSDEGGKVLLPKLIDFSAQIAEGMAYIER
KNYIHRDLRAANVLVSESLMCKIADFGLARVIEDNEYTAREGAKFPIKWTAPEAINFGCF
TIKSDVWSFGILLYEIVTYGKIPYPGRTNADVMTALSQGYRMPRVENCPDELYDIMKMCW
KEKAEERPTFDYLQSVLDDFYTATEGQYQQQP
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BDBM50151366 |
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n/a |
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Name | BDBM50151366 |
Synonyms: | (2-Chloro-6-methyl-phenyl)-[8-((S)-3-methyl-piperazin-1-yl)-2,5,9,9b-tetraaza-cyclopenta[a]naphthalen-4-yl]-amine | BMS-279700 | CHEMBL189338 |
Type | Small organic molecule |
Emp. Form. | C21H22ClN7 |
Mol. Mass. | 407.899 |
SMILES | C[C@H]1CN(CCN1)c1ccc2nc(Nc3c(C)cccc3Cl)c3cncn3c2n1 |
Structure |
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