Assay Detail
Binding
CHEMBL3425231
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Inhibition of PFKFB3 in human A549 cells assessed as reduction of fructose-1,6-bisphosphate formation after 4 hrs by MS/MS analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A549 |
| 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
Structure-Based Design of Potent and Selective Inhibitors of the Metabolic Kinase PFKFB3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.13 | 7.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3422678 | — | — | 1 | 7.17 |
| CHEMBL3422674 | — | — | 1 | 6.85 |
| CHEMBL3422676 | — | — | 1 | 6.55 |
| CHEMBL3422677 | — | — | 1 | 6.53 |
| CHEMBL3422651 | — | — | 1 | 6.46 |
| CHEMBL3422672 | — | — | 1 | 6.20 |
| CHEMBL3421731 | — | — | 1 | 6.01 |
| CHEMBL3422664 | — | — | 1 | 5.52 |
| CHEMBL3422671 | — | — | 1 | 5.13 |
| CHEMBL3422670 | — | — | 1 | 4.85 |
| CHEMBL3422652 | — | — | 1 | - |
| CHEMBL3422657 | — | — | 1 | - |
| CHEMBL3422658 | — | — | 1 | - |
| CHEMBL3422659 | — | — | 1 | - |
| CHEMBL3422679 | — | — | 1 | - |
| CHEMBL3422680 | — | — | 1 | - |
| CHEMBL3421733 | — | — | 1 | - |
| CHEMBL3421735 | — | — | 1 | - |
| CHEMBL3422654 | — | — | 1 | - |
| CHEMBL3421736 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3422678 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3422674 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3422676 | — | IC50 | = | 281.0 | nM | 6.55 |
| CHEMBL3422677 | — | IC50 | = | 297.0 | nM | 6.53 |
| CHEMBL3422651 | — | IC50 | = | 343.0 | nM | 6.46 |
| CHEMBL3422672 | — | IC50 | = | 633.0 | nM | 6.20 |
| CHEMBL3421731 | — | IC50 | = | 979.0 | nM | 6.01 |
| CHEMBL3422664 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL3422671 | — | IC50 | = | 7480.0 | nM | 5.13 |
| CHEMBL3422670 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL3422652 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3422657 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3422658 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3422659 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3422679 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3422680 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3421733 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3421735 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3422654 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3421736 | — | IC50 | > | 30000.0 | nM | - |