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Assay Detail

CHEMBL934544

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Binding
Inhibition of Lyn by luminescence based kinase assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase Lyn (CHEMBL3905)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

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-pyrrolidin-1-yl)-ethoxy]-phenyl}-amine).
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.
Drug Metab Dispos (2007) 35 : 929 -936
PubMed 17371799 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.99 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL256101 1 8.38
CHEMBL230686 1 7.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL256101 Ki = 4.19 nM 8.38
CHEMBL230686 Ki = 25.9 nM 7.59