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Assay Detail

CHEMBL841209

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Binding
Inhibition of p56 Lck tyrosine kinase catalytic domain at 1 mM ATP
5
Total Activities
5
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

Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I.
Arnold LD, Calderwood DJ, Dixon RW, Johnston DN, Kamens JS, Munschauer R, Rafferty P, Ratnofsky SE.
Bioorg Med Chem Lett (2000) 10 : 2167 -2170
PubMed 11012021 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.15 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL69827 1 6.50
CHEMBL69129 1 6.26
CHEMBL47940 1 5.97
CHEMBL419082 1 5.88
CHEMBL69638 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL69827 IC50 = 317.0 nM 6.50
CHEMBL69129 IC50 = 544.0 nM 6.26
CHEMBL47940 IC50 = 1070.0 nM 5.97
CHEMBL419082 IC50 = 1320.0 nM 5.88
CHEMBL69638 IC50 > 10000.0 nM -