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Assay Detail

CHEMBL765997

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

Binding
Tested in vitro for the inhibition of protein-tyrosine kinase p56lck using angiotensin I (1.2 mM) and [gamma-32P]-ATP (50 pM)
19
Total Activities
19
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

Synthesis and protein-tyrosine kinase inhibitory activity of polyhydroxylated stilbene analogues of piceatannol.
Thakkar K, Geahlen RL, Cushman M.
J Med Chem (1993) 36 : 2950 -2955
PubMed 8411012 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 4.47 4.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL101659 1 4.80
CHEMBL99852 1 4.77
CHEMBL329033 1 4.72
CHEMBL441643 1 4.44
CHEMBL103464 1 4.24
CHEMBL69863 PICEATANNOL 1 4.18
CHEMBL99801 1 4.13
CHEMBL100577 1 -
CHEMBL101078 1 -
CHEMBL101337 1 -
CHEMBL100016 1 -
CHEMBL100650 1 -
CHEMBL101506 PINOSYLVIN 1 -
CHEMBL100687 1 -
CHEMBL165 RESVERATROL 3.0 1 -
CHEMBL100553 1 -
CHEMBL100922 (E)-3,4-STILBENDIOL 1 -
CHEMBL327955 1 -
CHEMBL329520 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL101659 IC50 = 16000.0 nM 4.80
CHEMBL99852 IC50 = 17000.0 nM 4.77
CHEMBL329033 IC50 = 19000.0 nM 4.72
CHEMBL441643 IC50 = 36000.0 nM 4.44
CHEMBL103464 IC50 = 58000.0 nM 4.24
CHEMBL69863 PICEATANNOL IC50 = 66000.0 nM 4.18
CHEMBL99801 IC50 = 74000.0 nM 4.13
CHEMBL100577 IC50 > 2030000.0 nM -
CHEMBL101078 IC50 = 487000.0 nM -
CHEMBL101337 IC50 > 2030000.0 nM -
CHEMBL100016 IC50 = 234000.0 nM -
CHEMBL100650 IC50 > 2030000.0 nM -
CHEMBL101506 PINOSYLVIN IC50 = 193000.0 nM -
CHEMBL100687 IC50 > 2030000.0 nM -
CHEMBL165 RESVERATROL IC50 = 112000.0 nM -
CHEMBL100553 IC50 > 2030000.0 nM -
CHEMBL100922 (E)-3,4-STILBENDIOL IC50 = 203000.0 nM -
CHEMBL327955 IC50 > 2030000.0 nM -
CHEMBL329520 IC50 = 1560000.0 nM -