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Assay Detail

CHEMBL842024

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

Binding
Inhibitory activity against p56 Lck tyrosine kinase at a concentration of 5 uM ATP.
28
Total Activities
28
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

Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck II.
Burchat AF, Calderwood DJ, Hirst GC, Holman NJ, Johnston DN, Munschauer R, Rafferty P, Tometzki GB.
Bioorg Med Chem Lett (2000) 10 : 2171 -2174
PubMed 11012022 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 7.37 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL302281 1 8.70
CHEMBL68888 1 8.40
CHEMBL303195 1 8.30
CHEMBL66102 1 8.22
CHEMBL67268 1 8.10
CHEMBL68430 1 7.96
CHEMBL302279 1 7.77
CHEMBL305748 1 7.70
CHEMBL67598 1 7.52
CHEMBL66716 1 7.52
CHEMBL71985 1 7.40
CHEMBL68773 1 6.88
CHEMBL68082 1 6.84
CHEMBL69868 1 6.58
CHEMBL69544 1 6.51
CHEMBL67560 1 6.33
CHEMBL67211 1 6.03
CHEMBL68663 1 5.83
CHEMBL70034 1 -
CHEMBL307982 1 -
CHEMBL69068 1 -
CHEMBL304113 1 -
CHEMBL47940 1 -
CHEMBL71722 1 -
CHEMBL433097 1 -
CHEMBL69649 1 -
CHEMBL302481 1 -
CHEMBL71541 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL302281 IC50 = 2.0 nM 8.70
CHEMBL68888 IC50 = 4.0 nM 8.40
CHEMBL303195 IC50 = 5.0 nM 8.30
CHEMBL66102 IC50 = 6.0 nM 8.22
CHEMBL67268 IC50 = 8.0 nM 8.10
CHEMBL68430 IC50 = 11.0 nM 7.96
CHEMBL302279 IC50 = 17.0 nM 7.77
CHEMBL305748 IC50 = 20.0 nM 7.70
CHEMBL67598 IC50 = 30.0 nM 7.52
CHEMBL66716 IC50 = 30.0 nM 7.52
CHEMBL71985 IC50 = 40.0 nM 7.40
CHEMBL68773 IC50 = 131.0 nM 6.88
CHEMBL68082 IC50 = 144.0 nM 6.84
CHEMBL69868 IC50 = 260.0 nM 6.58
CHEMBL69544 IC50 = 310.0 nM 6.51
CHEMBL67560 IC50 = 470.0 nM 6.33
CHEMBL67211 IC50 = 942.0 nM 6.03
CHEMBL68663 IC50 = 1490.0 nM 5.83
CHEMBL70034 IC50 < 3.0 nM -
CHEMBL307982 IC50 < 1.0 nM -
CHEMBL69068 IC50 < 3.0 nM -
CHEMBL304113 IC50 < 3.0 nM -
CHEMBL47940 IC50 < 1.0 nM -
CHEMBL71722 IC50 < 3.0 nM -
CHEMBL433097 IC50 < 3.0 nM -
CHEMBL69649 IC50 < 1.0 nM -
CHEMBL302481 IC50 < 1.0 nM -
CHEMBL71541 IC50 < 3.0 nM -