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Assay Detail

CHEMBL942096

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

Binding
Inhibition of Chk2 kinase
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Serine/threonine-protein kinase Chk2 (CHEMBL2527)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of novel, selective and potent Chk2 inhibitors.
Larson G, Yan S, Chen H, Rong F, Hong Z, Wu JZ.
Bioorg Med Chem Lett (2007) 17 : 172 -175
PubMed 17035018 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 5.73 7.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL250230 1 7.06
CHEMBL251256 1 6.85
CHEMBL398561 1 6.66
CHEMBL399237 1 6.52
CHEMBL251284 1 6.51
CHEMBL253115 1 6.38
CHEMBL253116 1 6.34
CHEMBL249251 1 6.34
CHEMBL400772 1 6.33
CHEMBL401105 1 6.05
CHEMBL253324 1 6.00
CHEMBL253542 1 5.92
CHEMBL253541 1 5.75
CHEMBL398759 1 5.64
CHEMBL249253 1 5.30
CHEMBL249252 1 5.10
CHEMBL399151 1 4.96
CHEMBL398758 1 4.96
CHEMBL438150 1 4.77
CHEMBL249255 1 4.72
CHEMBL251629 1 4.72
CHEMBL251628 1 4.43
CHEMBL251471 1 4.40
CHEMBL398760 1 -
CHEMBL251473 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL250230 IC50 = 87.0 nM 7.06
CHEMBL251256 IC50 = 140.0 nM 6.85
CHEMBL398561 IC50 = 220.0 nM 6.66
CHEMBL399237 IC50 = 300.0 nM 6.52
CHEMBL251284 IC50 = 310.0 nM 6.51
CHEMBL253115 IC50 = 420.0 nM 6.38
CHEMBL253116 IC50 = 460.0 nM 6.34
CHEMBL249251 IC50 = 460.0 nM 6.34
CHEMBL400772 IC50 = 470.0 nM 6.33
CHEMBL401105 IC50 = 900.0 nM 6.05
CHEMBL253324 IC50 = 1000.0 nM 6.00
CHEMBL253542 IC50 = 1200.0 nM 5.92
CHEMBL253541 IC50 = 1800.0 nM 5.75
CHEMBL398759 IC50 = 2300.0 nM 5.64
CHEMBL249253 IC50 = 5000.0 nM 5.30
CHEMBL249252 IC50 = 8000.0 nM 5.10
CHEMBL399151 IC50 = 11000.0 nM 4.96
CHEMBL398758 IC50 = 11000.0 nM 4.96
CHEMBL438150 IC50 = 17000.0 nM 4.77
CHEMBL249255 IC50 = 19000.0 nM 4.72
CHEMBL251629 IC50 = 19000.0 nM 4.72
CHEMBL251628 IC50 = 37000.0 nM 4.43
CHEMBL251471 IC50 = 40000.0 nM 4.40
CHEMBL398760 IC50 > 40000.0 nM -
CHEMBL251473 IC50 > 40000.0 nM -