Assay Detail
Functional
CHEMBL960988
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human HCT116 cells after 72 hrs by luminescence-based cell viability assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HCT-116 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.25 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1794070 | GSK-579289A | — | 1 | 7.96 |
| CHEMBL1615278 | — | — | 1 | 7.92 |
| CHEMBL1964265 | — | — | 1 | 7.89 |
| CHEMBL1964263 | — | — | 1 | 7.82 |
| CHEMBL1964264 | — | — | 1 | 7.77 |
| CHEMBL222419 | GSK-237701A | — | 1 | 7.60 |
| CHEMBL1794068 | GSK-326090A | — | 1 | 7.52 |
| CHEMBL1964261 | — | — | 1 | 7.50 |
| CHEMBL1794069 | GSK-571989A | — | 1 | 7.47 |
| CHEMBL1964262 | — | — | 1 | 7.35 |
| CHEMBL1794067 | GSK-978744A | — | 1 | 7.14 |
| CHEMBL493326 | GSK-317314A | — | 1 | 6.49 |
| CHEMBL522709 | GSK-317315A | — | 1 | 6.32 |
| CHEMBL521806 | GSK-237700A | — | 1 | 6.00 |
| CHEMBL514162 | GW852849X | — | 1 | 5.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1794070 | GSK-579289A | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1615278 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1964265 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1964263 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1964264 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL222419 | GSK-237701A | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1794068 | GSK-326090A | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1964261 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1794069 | GSK-571989A | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1964262 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL1794067 | GSK-978744A | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL493326 | GSK-317314A | IC50 | = | 321.0 | nM | 6.49 |
| CHEMBL522709 | GSK-317315A | IC50 | = | 476.0 | nM | 6.32 |
| CHEMBL521806 | GSK-237700A | IC50 | = | 994.0 | nM | 6.00 |
| CHEMBL514162 | GW852849X | IC50 | = | 1140.0 | nM | 5.94 |