Assay Detail
Functional
CHEMBL2013770
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of camptothecin-induced cell cycle arrest in human HT-29 cells assessed as abrogation at G2/M checkpoint measuring phosphohistone-H3 level treated with compound 2 hrs after camptothecin-challenge
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HT-29 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Synthesis and evaluation of triazolones as checkpoint kinase 1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 49 | 5.89 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2012861 | — | — | 1 | 7.70 |
| CHEMBL487273 | — | — | 1 | 7.70 |
| CHEMBL2012856 | — | — | 1 | 7.10 |
| CHEMBL2012862 | — | — | 1 | 6.68 |
| CHEMBL2012863 | — | — | 1 | 6.62 |
| CHEMBL2012881 | — | — | 1 | 6.62 |
| CHEMBL2012859 | — | — | 1 | 6.42 |
| CHEMBL1223526 | — | — | 1 | 6.29 |
| CHEMBL2012850 | — | — | 1 | 6.24 |
| CHEMBL2012858 | — | — | 1 | 6.20 |
| CHEMBL2012848 | — | — | 1 | 6.12 |
| CHEMBL2012847 | — | — | 1 | 6.07 |
| CHEMBL2012872 | — | — | 1 | 6.05 |
| CHEMBL2012870 | — | — | 1 | 6.02 |
| CHEMBL2012866 | — | — | 1 | 6.01 |
| CHEMBL2012842 | — | — | 1 | 6.00 |
| CHEMBL2012864 | — | — | 1 | 5.96 |
| CHEMBL2012878 | — | — | 1 | 5.96 |
| CHEMBL2012879 | — | — | 1 | 5.96 |
| CHEMBL2012855 | — | — | 1 | 5.89 |
| CHEMBL2012865 | — | — | 1 | 5.70 |
| CHEMBL2012882 | — | — | 1 | 5.70 |
| CHEMBL1223524 | — | — | 1 | 5.70 |
| CHEMBL2012860 | — | — | 1 | 5.68 |
| CHEMBL2012877 | — | — | 1 | 5.66 |
| CHEMBL2012841 | — | — | 1 | 5.48 |
| CHEMBL2012868 | — | — | 1 | 5.48 |
| CHEMBL2012874 | — | — | 1 | 5.48 |
| CHEMBL2012869 | — | — | 1 | 5.46 |
| CHEMBL2012871 | — | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2012861 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL487273 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2012856 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2012862 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL2012863 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2012881 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2012859 | — | EC50 | = | 380.0 | nM | 6.42 |
| CHEMBL1223526 | — | EC50 | = | 510.0 | nM | 6.29 |
| CHEMBL2012850 | — | EC50 | = | 580.0 | nM | 6.24 |
| CHEMBL2012858 | — | EC50 | = | 630.0 | nM | 6.20 |
| CHEMBL2012848 | — | EC50 | = | 750.0 | nM | 6.12 |
| CHEMBL2012847 | — | EC50 | = | 850.0 | nM | 6.07 |
| CHEMBL2012872 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL2012870 | — | EC50 | = | 960.0 | nM | 6.02 |
| CHEMBL2012866 | — | EC50 | = | 970.0 | nM | 6.01 |
| CHEMBL2012842 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2012864 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2012878 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2012879 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2012855 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2012865 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2012882 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL1223524 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2012860 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL2012877 | — | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL2012868 | — | EC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL2012874 | — | EC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL2012841 | — | EC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL2012869 | — | EC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL2012871 | — | EC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL2012883 | — | EC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL2012873 | — | EC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL2012875 | — | EC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL2012867 | — | EC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL2012880 | — | EC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL2012884 | — | EC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL2012876 | — | EC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL2012854 | — | EC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL1223456 | — | EC50 | - | — | - | |
| CHEMBL2012839 | — | EC50 | > | 13000.0 | nM | - |
| CHEMBL2012840 | — | EC50 | > | 13000.0 | nM | - |
| CHEMBL2012843 | — | EC50 | > | 13000.0 | nM | - |
| CHEMBL2012844 | — | EC50 | > | 13000.0 | nM | - |
| CHEMBL2012845 | — | EC50 | > | 13000.0 | nM | - |
| CHEMBL2012846 | — | EC50 | > | 13000.0 | nM | - |
| CHEMBL2012849 | — | EC50 | > | 13000.0 | nM | - |
| CHEMBL2012851 | — | EC50 | > | 13000.0 | nM | - |
| CHEMBL2012852 | — | EC50 | > | 13000.0 | nM | - |
| CHEMBL2012853 | — | EC50 | > | 13000.0 | nM | - |