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Assay Detail

CHEMBL701411

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Binding
Inhibition of human lck kinase.
13
Total Activities
13
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

Pyrazolo[3,4-d]pyrimidines containing an extended 3-substituent as potent inhibitors of Lck -- a selectivity insight.
Burchat AF, Calderwood DJ, Friedman MM, Hirst GC, Li B, Rafferty P, Ritter K, Skinner BS.
Bioorg Med Chem Lett (2002) 12 : 1687 -1690
PubMed 12039591 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.22 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL47787 1 8.40
CHEMBL43773 1 8.00
CHEMBL416091 1 7.72
CHEMBL295601 1 7.55
CHEMBL295528 1 7.51
CHEMBL46785 1 7.40
CHEMBL45683 1 7.30
CHEMBL417006 1 7.04
CHEMBL297363 1 7.03
CHEMBL45693 1 6.96
CHEMBL46176 1 6.78
CHEMBL45651 1 6.68
CHEMBL402673 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL47787 IC50 = 4.0 nM 8.40
CHEMBL43773 IC50 = 10.0 nM 8.00
CHEMBL416091 IC50 = 19.0 nM 7.72
CHEMBL295601 IC50 = 28.0 nM 7.55
CHEMBL295528 IC50 = 31.0 nM 7.51
CHEMBL46785 IC50 = 40.0 nM 7.40
CHEMBL45683 IC50 = 50.0 nM 7.30
CHEMBL417006 IC50 = 92.0 nM 7.04
CHEMBL297363 IC50 = 93.0 nM 7.03
CHEMBL45693 IC50 = 110.0 nM 6.96
CHEMBL46176 IC50 = 167.0 nM 6.78
CHEMBL45651 IC50 = 209.0 nM 6.68
CHEMBL402673 IC50 = 3120.0 nM 5.51