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Assay Detail

CHEMBL841199

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

Binding
Inhibition of human p56 Lck tyrosine kinase (lck64-509)
12
Total Activities
12
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 diverse N-7 substituents as potent inhibitors of Lck.
Calderwood DJ, Johnston DN, Munschauer R, Rafferty P.
Bioorg Med Chem Lett (2002) 12 : 1683 -1686
PubMed 12039590 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.90 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL47203 1 7.82
CHEMBL48554 1 7.38
CHEMBL296534 1 7.34
CHEMBL44942 1 7.09
CHEMBL47940 1 7.00
CHEMBL296103 1 6.92
CHEMBL297359 1 6.89
CHEMBL47202 1 6.77
CHEMBL45177 1 6.62
CHEMBL297278 1 6.62
CHEMBL431342 1 6.28
CHEMBL416444 1 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL47203 IC50 = 15.0 nM 7.82
CHEMBL48554 IC50 = 42.0 nM 7.38
CHEMBL296534 IC50 = 46.0 nM 7.34
CHEMBL44942 IC50 = 82.0 nM 7.09
CHEMBL47940 IC50 = 100.0 nM 7.00
CHEMBL296103 IC50 = 120.0 nM 6.92
CHEMBL297359 IC50 = 130.0 nM 6.89
CHEMBL47202 IC50 = 170.0 nM 6.77
CHEMBL45177 IC50 = 240.0 nM 6.62
CHEMBL297278 IC50 = 240.0 nM 6.62
CHEMBL431342 IC50 = 520.0 nM 6.28
CHEMBL416444 IC50 = 890.0 nM 6.05