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Assay Detail

CHEMBL2013769

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

Binding
Inhibition of Chk1
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Serine/threonine-protein kinase Chk1 (CHEMBL4630)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of triazolones as checkpoint kinase 1 inhibitors.
Oza V, Ashwell S, Brassil P, Breed J, Ezhuthachan J, Deng C, Grondine M, Horn C, Liu D, Lyne P, Newcombe N, Pass M, Read J, Su M, Toader D, Yu D, Yu Y, Zabludoff S.
Bioorg Med Chem Lett (2012) 22 : 2330 -2337
PubMed 22342147 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 52 7.35 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1223526 1 10.00
CHEMBL2012879 1 8.52
CHEMBL2012859 1 8.40
CHEMBL2012858 1 8.30
CHEMBL2012857 1 8.22
CHEMBL487273 1 8.15
CHEMBL2012852 1 8.05
CHEMBL2012877 1 8.00
CHEMBL1223456 1 8.00
CHEMBL2012856 1 8.00
CHEMBL2012863 1 8.00
CHEMBL2012878 1 8.00
CHEMBL2012853 1 7.70
CHEMBL1223524 1 7.70
CHEMBL2012882 1 7.70
CHEMBL2012881 1 7.70
CHEMBL2012880 1 7.70
CHEMBL2012860 1 7.70
CHEMBL2012850 1 7.70
CHEMBL2012842 1 7.70
CHEMBL2012841 1 7.70
CHEMBL2012883 1 7.52
CHEMBL2012872 1 7.52
CHEMBL2012870 1 7.52
CHEMBL2012861 1 7.52
CHEMBL2012848 1 7.52
CHEMBL2012865 1 7.52
CHEMBL2012847 1 7.40
CHEMBL2012855 1 7.40
CHEMBL2012862 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1223526 IC50 = 0.1 nM 10.00
CHEMBL2012879 IC50 = 3.0 nM 8.52
CHEMBL2012859 IC50 = 4.0 nM 8.40
CHEMBL2012858 IC50 = 5.0 nM 8.30
CHEMBL2012857 IC50 = 6.0 nM 8.22
CHEMBL487273 IC50 = 7.0 nM 8.15
CHEMBL2012852 IC50 = 9.0 nM 8.05
CHEMBL2012877 IC50 = 10.0 nM 8.00
CHEMBL1223456 IC50 = 10.0 nM 8.00
CHEMBL2012856 IC50 = 10.0 nM 8.00
CHEMBL2012863 IC50 = 10.0 nM 8.00
CHEMBL2012878 IC50 = 10.0 nM 8.00
CHEMBL2012841 IC50 = 20.0 nM 7.70
CHEMBL1223524 IC50 = 20.0 nM 7.70
CHEMBL2012882 IC50 = 20.0 nM 7.70
CHEMBL2012881 IC50 = 20.0 nM 7.70
CHEMBL2012880 IC50 = 20.0 nM 7.70
CHEMBL2012860 IC50 = 20.0 nM 7.70
CHEMBL2012853 IC50 = 20.0 nM 7.70
CHEMBL2012850 IC50 = 20.0 nM 7.70
CHEMBL2012842 IC50 = 20.0 nM 7.70
CHEMBL2012865 IC50 = 30.0 nM 7.52
CHEMBL2012848 IC50 = 30.0 nM 7.52
CHEMBL2012861 IC50 = 30.0 nM 7.52
CHEMBL2012872 IC50 = 30.0 nM 7.52
CHEMBL2012883 IC50 = 30.0 nM 7.52
CHEMBL2012870 IC50 = 30.0 nM 7.52
CHEMBL2012847 IC50 = 40.0 nM 7.40
CHEMBL2012855 IC50 = 40.0 nM 7.40
CHEMBL2012862 IC50 = 40.0 nM 7.40
CHEMBL2012868 IC50 = 40.0 nM 7.40
CHEMBL2012884 IC50 = 50.0 nM 7.30
CHEMBL2012871 IC50 = 90.0 nM 7.05
CHEMBL2012874 IC50 = 90.0 nM 7.05
CHEMBL2012866 IC50 = 100.0 nM 7.00
CHEMBL2012843 IC50 = 110.0 nM 6.96
CHEMBL2012864 IC50 = 130.0 nM 6.89
CHEMBL452021 IC50 = 150.0 nM 6.82
CHEMBL2012839 IC50 = 160.0 nM 6.80
CHEMBL2012875 IC50 = 210.0 nM 6.68
CHEMBL2012873 IC50 = 240.0 nM 6.62
CHEMBL2012854 IC50 = 300.0 nM 6.52
CHEMBL2012867 IC50 = 300.0 nM 6.52
CHEMBL2012876 IC50 = 400.0 nM 6.40
CHEMBL2012840 IC50 = 420.0 nM 6.38
CHEMBL2012844 IC50 = 440.0 nM 6.36
CHEMBL2012845 IC50 = 440.0 nM 6.36
CHEMBL2012846 IC50 = 560.0 nM 6.25
CHEMBL2012851 IC50 = 600.0 nM 6.22
CHEMBL487274 IC50 = 800.0 nM 6.10