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Assay Detail

CHEMBL842020

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

Binding
Inhibition of p56 Lck tyrosine kinase, in presence of 1 mM ATP
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 22 6.40 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL69068 1 8.52
CHEMBL307982 1 7.96
CHEMBL47940 1 7.80
CHEMBL302481 1 7.52
CHEMBL68888 1 7.16
CHEMBL302281 1 7.12
CHEMBL66716 1 7.12
CHEMBL302279 1 6.54
CHEMBL68430 1 6.42
CHEMBL71722 1 6.34
CHEMBL71541 1 6.28
CHEMBL67268 1 6.20
CHEMBL70034 1 6.12
CHEMBL304113 1 6.10
CHEMBL303195 1 6.00
CHEMBL305748 1 5.97
CHEMBL68773 1 5.88
CHEMBL66102 1 5.68
CHEMBL68082 1 5.51
CHEMBL71985 1 5.26
CHEMBL67211 1 4.80
CHEMBL67598 1 4.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL69068 IC50 = 3.0 nM 8.52
CHEMBL307982 IC50 = 11.0 nM 7.96
CHEMBL47940 IC50 = 16.0 nM 7.80
CHEMBL302481 IC50 = 30.0 nM 7.52
CHEMBL68888 IC50 = 69.0 nM 7.16
CHEMBL302281 IC50 = 75.0 nM 7.12
CHEMBL66716 IC50 = 75.0 nM 7.12
CHEMBL302279 IC50 = 290.0 nM 6.54
CHEMBL68430 IC50 = 380.0 nM 6.42
CHEMBL71722 IC50 = 459.0 nM 6.34
CHEMBL71541 IC50 = 529.0 nM 6.28
CHEMBL67268 IC50 = 633.0 nM 6.20
CHEMBL70034 IC50 = 751.0 nM 6.12
CHEMBL304113 IC50 = 790.0 nM 6.10
CHEMBL303195 IC50 = 1010.0 nM 6.00
CHEMBL305748 IC50 = 1060.0 nM 5.97
CHEMBL68773 IC50 = 1310.0 nM 5.88
CHEMBL66102 IC50 = 2110.0 nM 5.68
CHEMBL68082 IC50 = 3090.0 nM 5.51
CHEMBL71985 IC50 = 5550.0 nM 5.26
CHEMBL67211 IC50 = 15800.0 nM 4.80
CHEMBL67598 IC50 = 26200.0 nM 4.58