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Assay Detail

CHEMBL842076

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

Binding
Inhibition of p56 Lck tyrosine kinase
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

The development of novel and selective p56lck tyrosine kinase inhibitors.
Bullington JL, Cameron JC, Davis JE, Dodd JH, Harris CA, Henry JR, Pellegrino-Gensey JL, Rupert KC, Siekierka JJ.
Bioorg Med Chem Lett (1998) 8 : 2489 -2494
PubMed 9873567 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.07 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL84807 1 7.50
CHEMBL84808 1 6.99
CHEMBL83721 1 6.96
CHEMBL82560 1 6.84
CHEMBL421341 1 6.51
CHEMBL81862 1 6.33
CHEMBL81793 1 6.22
CHEMBL312563 1 6.15
CHEMBL82404 1 6.13
CHEMBL311746 1 6.06
CHEMBL82345 1 6.00
CHEMBL83376 1 5.85
CHEMBL83161 1 5.82
CHEMBL79872 1 5.77
CHEMBL309230 1 5.77
CHEMBL69863 PICEATANNOL 1 5.30
CHEMBL86228 1 5.30
CHEMBL84338 1 5.30
CHEMBL309706 1 5.30
CHEMBL83598 1 5.30
CHEMBL79780 1 -
CHEMBL309991 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL84807 IC50 = 32.0 nM 7.50
CHEMBL84808 IC50 = 102.0 nM 6.99
CHEMBL83721 IC50 = 110.0 nM 6.96
CHEMBL82560 IC50 = 144.0 nM 6.84
CHEMBL421341 IC50 = 310.0 nM 6.51
CHEMBL81862 IC50 = 470.0 nM 6.33
CHEMBL81793 IC50 = 600.0 nM 6.22
CHEMBL312563 IC50 = 710.0 nM 6.15
CHEMBL82404 IC50 = 740.0 nM 6.13
CHEMBL311746 IC50 = 880.0 nM 6.06
CHEMBL82345 IC50 = 1000.0 nM 6.00
CHEMBL83376 IC50 = 1400.0 nM 5.85
CHEMBL83161 IC50 = 1500.0 nM 5.82
CHEMBL79872 IC50 = 1700.0 nM 5.77
CHEMBL309230 IC50 = 1700.0 nM 5.77
CHEMBL69863 PICEATANNOL IC50 = 5000.0 nM 5.30
CHEMBL86228 IC50 = 5000.0 nM 5.30
CHEMBL84338 IC50 = 5000.0 nM 5.30
CHEMBL309706 IC50 = 5000.0 nM 5.30
CHEMBL83598 IC50 = 5000.0 nM 5.30
CHEMBL79780 IC50 > 5000.0 nM -
CHEMBL309991 IC50 > 5000.0 nM -