Assay Detail
Binding
CHEMBL3425232
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PFKFB3 in human A549 cells assessed as decrease in lactate secretion after 4 hrs
32
Total Activities
32
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 | 32 | 4.97 | 5.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3422674 | — | — | 1 | 5.66 |
| CHEMBL3422651 | — | — | 1 | 5.24 |
| CHEMBL3422675 | — | — | 1 | 5.16 |
| CHEMBL3422673 | — | — | 1 | 5.06 |
| CHEMBL3421731 | — | — | 1 | 5.01 |
| CHEMBL3422664 | — | — | 1 | 4.92 |
| CHEMBL3422658 | — | — | 1 | 4.90 |
| CHEMBL3421733 | — | — | 1 | 4.86 |
| CHEMBL3421734 | — | — | 1 | 4.85 |
| CHEMBL3422677 | — | — | 1 | 4.81 |
| CHEMBL3422657 | — | — | 1 | 4.79 |
| CHEMBL3422667 | — | — | 1 | 4.71 |
| CHEMBL3421735 | — | — | 1 | 4.61 |
| CHEMBL3422659 | — | — | 1 | - |
| CHEMBL3422661 | — | — | 1 | - |
| CHEMBL3422662 | — | — | 1 | - |
| CHEMBL3422663 | — | — | 1 | - |
| CHEMBL3422665 | — | — | 1 | - |
| CHEMBL3422666 | — | — | 1 | - |
| CHEMBL3422668 | — | — | 1 | - |
| CHEMBL3422669 | — | — | 1 | - |
| CHEMBL3422654 | — | — | 1 | - |
| CHEMBL3422671 | — | — | 1 | - |
| CHEMBL3422672 | — | — | 1 | - |
| CHEMBL3421736 | — | — | 1 | - |
| CHEMBL3422676 | — | — | 1 | - |
| CHEMBL3422679 | — | — | 1 | - |
| CHEMBL3422680 | — | — | 1 | - |
| CHEMBL3422670 | — | — | 1 | - |
| CHEMBL3421732 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3422674 | — | IC50 | = | 2180.0 | nM | 5.66 |
| CHEMBL3422651 | — | IC50 | = | 5770.0 | nM | 5.24 |
| CHEMBL3422675 | — | IC50 | = | 6950.0 | nM | 5.16 |
| CHEMBL3422673 | — | IC50 | = | 8710.0 | nM | 5.06 |
| CHEMBL3421731 | — | IC50 | = | 9710.0 | nM | 5.01 |
| CHEMBL3422664 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL3422658 | — | IC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL3421733 | — | IC50 | = | 13700.0 | nM | 4.86 |
| CHEMBL3421734 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL3422677 | — | IC50 | = | 15400.0 | nM | 4.81 |
| CHEMBL3422657 | — | IC50 | = | 16400.0 | nM | 4.79 |
| CHEMBL3422667 | — | IC50 | = | 19600.0 | nM | 4.71 |
| CHEMBL3421735 | — | IC50 | = | 24700.0 | nM | 4.61 |
| CHEMBL3422653 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3422652 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3422659 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3422661 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3422662 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3422663 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3422665 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3422666 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3422668 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3422669 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3422654 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3422671 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3422672 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3421736 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3422676 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3422679 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3422680 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3422670 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3421732 | — | IC50 | > | 30000.0 | nM | - |