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Assay Detail

CHEMBL870977

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of Lck in presence of 0.5 uM ATP by HTRF kinase assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Tyrosine-protein kinase Lck (CHEMBL258)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity.
Martin MW, Newcomb J, Nunes JJ, McGowan DC, Armistead DM, Boucher C, Buchanan JL, Buckner W, Chai L, Elbaum D, Epstein LF, Faust T, Flynn S, Gallant P, Gore A, Gu Y, Hsieh F, Huang X, Lee JH, Metz D, Middleton S, Mohn D, Morgenstern K, Morrison MJ, Novak PM, Oliveira-dos-Santos A, Powers D, Rose P, Schneider S, Sell S, Tudor Y, Turci SM, Welcher AA, White RD, Zack D, Zhao H, Zhu L, Zhu X, Ghiron C, Amouzegh P, Ermann M, Jenkins J, Johnston D, Napier S, Power E.
J Med Chem (2006) 49 : 4981 -4991
PubMed 16884310 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 8.71 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL386760 1 9.22
CHEMBL385898 1 9.00
CHEMBL211460 1 9.00
CHEMBL263769 1 9.00
CHEMBL442485 1 9.00
CHEMBL215289 1 9.00
CHEMBL215730 1 9.00
CHEMBL211845 1 9.00
CHEMBL212721 1 9.00
CHEMBL214775 1 9.00
CHEMBL212668 1 9.00
CHEMBL212143 1 9.00
CHEMBL264803 1 9.00
CHEMBL379733 1 9.00
CHEMBL379080 1 9.00
CHEMBL215411 1 8.70
CHEMBL213100 1 8.70
CHEMBL377481 1 8.00
CHEMBL215847 1 7.92
CHEMBL209908 1 7.89
CHEMBL427047 1 7.85
CHEMBL215726 1 7.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL386760 IC50 = 0.6 nM 9.22
CHEMBL385898 IC50 = 1.0 nM 9.00
CHEMBL211460 IC50 = 1.0 nM 9.00
CHEMBL263769 IC50 = 1.0 nM 9.00
CHEMBL442485 IC50 = 1.0 nM 9.00
CHEMBL215289 IC50 = 1.0 nM 9.00
CHEMBL215730 IC50 = 1.0 nM 9.00
CHEMBL211845 IC50 = 1.0 nM 9.00
CHEMBL212721 IC50 = 1.0 nM 9.00
CHEMBL214775 IC50 = 1.0 nM 9.00
CHEMBL212668 IC50 = 1.0 nM 9.00
CHEMBL212143 IC50 = 1.0 nM 9.00
CHEMBL264803 IC50 = 1.0 nM 9.00
CHEMBL379733 IC50 = 1.0 nM 9.00
CHEMBL379080 IC50 = 1.0 nM 9.00
CHEMBL215411 IC50 = 2.0 nM 8.70
CHEMBL213100 IC50 = 2.0 nM 8.70
CHEMBL377481 IC50 = 10.0 nM 8.00
CHEMBL215847 IC50 = 12.0 nM 7.92
CHEMBL209908 IC50 = 13.0 nM 7.89
CHEMBL427047 IC50 = 14.0 nM 7.85
CHEMBL215726 IC50 = 49.0 nM 7.31