Assay Detail
Binding
CHEMBL3106983
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant GST-tagged PFKFB3 expressed in Escherichia coli BL21(DE3) using fructose 6-phosphate as substrate preincubated for 30 mins before substrate addition measured after 60 mins by kinase-glo assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (CHEMBL2331053) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Targeting the Warburg Effect in cancer; relationships for 2-arylpyridazinones as inhibitors of the key glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 5.12 | 6.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3105838 | — | — | 1 | 6.31 |
| CHEMBL3105833 | — | — | 1 | 5.58 |
| CHEMBL3105830 | — | — | 1 | 5.47 |
| CHEMBL3105828 | — | — | 1 | 5.16 |
| CHEMBL3105839 | — | — | 1 | 5.13 |
| CHEMBL3105826 | — | — | 1 | 5.08 |
| CHEMBL3105832 | — | — | 1 | 5.06 |
| CHEMBL3105827 | — | — | 1 | 5.04 |
| CHEMBL3105829 | — | — | 1 | 5.02 |
| CHEMBL3105834 | — | — | 1 | 4.96 |
| CHEMBL3105845 | — | — | 1 | 4.89 |
| CHEMBL3105844 | — | — | 1 | 4.58 |
| CHEMBL3105825 | — | — | 1 | 4.26 |
| CHEMBL3105835 | — | — | 1 | - |
| CHEMBL3105836 | — | — | 1 | - |
| CHEMBL1463854 | — | — | 1 | - |
| CHEMBL3105840 | — | — | 1 | - |
| CHEMBL3105841 | — | — | 1 | - |
| CHEMBL3105842 | — | — | 1 | - |
| CHEMBL3105843 | — | — | 1 | - |
| CHEMBL3105846 | — | — | 1 | - |
| CHEMBL3105847 | — | — | 1 | - |
| CHEMBL3105831 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3105838 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL3105833 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3105830 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL3105828 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL3105839 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL3105826 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL3105832 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL3105827 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL3105829 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL3105834 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL3105845 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL3105844 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL3105825 | — | IC50 | = | 55000.0 | nM | 4.26 |
| CHEMBL3105835 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL3105836 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL1463854 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3105840 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL3105841 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3105842 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3105843 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3105846 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL3105847 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3105831 | — | IC50 | > | 10000000.0 | nM | - |