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Assay Detail

CHEMBL841200

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

Binding
Inhibition of p56 Lck tyrosine kinase in Jurkat cells where p56lck autophosphorylation is inhibited.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Jurkat
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

The preparation and sar of 4-(anilino), 4-(phenoxy), and 4-(thiophenoxy)-quinazolines: Inhibitors of p56lck and EGF-R tyrosine kinase activity
Myers MR, Setzer NN, Spada A, Zulli AL, Hsu CJ, Zilberstein A, Johnson SE, Hook LE, Jacoski MV
Bioorg Med Chem Lett (1997) 7 : 417 -420
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.66 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL406845 1 8.40
CHEMBL306380 1 8.30
CHEMBL212948 DAMNACANTHAL 1 7.77
CHEMBL555201 1 5.52
CHEMBL335400 1 5.30
CHEMBL541586 1 5.00
CHEMBL544833 1 5.00
CHEMBL542729 1 5.00
CHEMBL542733 1 5.00
CHEMBL539552 1 5.00
CHEMBL545541 1 4.70
CHEMBL555797 1 4.30
CHEMBL538528 1 4.30
CHEMBL544836 1 -
CHEMBL542237 1 -
CHEMBL545767 1 -
CHEMBL555844 1 -
CHEMBL132605 1 -
CHEMBL543429 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL406845 IC50 = 4.0 nM 8.40
CHEMBL306380 IC50 = 5.0 nM 8.30
CHEMBL212948 DAMNACANTHAL IC50 = 17.0 nM 7.77
CHEMBL555201 IC50 = 3000.0 nM 5.52
CHEMBL335400 IC50 = 5000.0 nM 5.30
CHEMBL541586 IC50 = 10000.0 nM 5.00
CHEMBL544833 IC50 = 10000.0 nM 5.00
CHEMBL542729 IC50 = 10000.0 nM 5.00
CHEMBL542733 IC50 = 10000.0 nM 5.00
CHEMBL539552 IC50 = 10000.0 nM 5.00
CHEMBL545541 IC50 = 20000.0 nM 4.70
CHEMBL555797 IC50 = 50000.0 nM 4.30
CHEMBL538528 IC50 = 50000.0 nM 4.30
CHEMBL544836 IC50 > 100000.0 nM -
CHEMBL542237 IC50 > 100000.0 nM -
CHEMBL545767 IC50 > 50000.0 nM -
CHEMBL555844 IC50 > 100000.0 nM -
CHEMBL132605 IC50 > 50000.0 nM -
CHEMBL543429 IC50 > 100000.0 nM -