Assay Detail
Binding
CHEMBL5737962
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Biological Activity Assay 2: NCI-H358 lung adenocarcinoma cells may be used to measure MCT4 activity in cells with high native levels of MCT4 and low levels of MCT1 and are known to those with skill in the art. Preparation of BCECF-loaded cells and lactate transport activity may be determined as described for Assay 1.
69
Total Activities
23
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Heterocyclic inhibitors of MCT4
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.42 | 7.66 |
| kon | 23 | - | - |
| k_off | 23 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5868830 | — | — | 3 | 7.66 |
| CHEMBL6061357 | — | — | 3 | 7.60 |
| CHEMBL5764687 | — | — | 3 | 7.48 |
| CHEMBL5741292 | — | — | 3 | 7.36 |
| CHEMBL5757699 | — | — | 3 | 7.31 |
| CHEMBL5772596 | — | — | 3 | 7.27 |
| CHEMBL5830820 | — | — | 3 | 7.22 |
| CHEMBL5918774 | — | — | 3 | 7.20 |
| CHEMBL5803742 | — | — | 3 | 7.09 |
| CHEMBL5994824 | — | — | 3 | 6.85 |
| CHEMBL5826532 | — | — | 3 | 6.80 |
| CHEMBL5920914 | — | — | 3 | 6.62 |
| CHEMBL5754446 | — | — | 3 | 6.47 |
| CHEMBL5935723 | — | — | 3 | 6.36 |
| CHEMBL5792951 | — | — | 3 | 6.34 |
| CHEMBL5957110 | — | — | 3 | 6.19 |
| CHEMBL5874865 | — | — | 3 | 6.07 |
| CHEMBL5911168 | — | — | 3 | 5.68 |
| CHEMBL5765868 | — | — | 3 | 5.38 |
| CHEMBL6052282 | — | — | 3 | 5.34 |
| CHEMBL5985401 | — | — | 3 | 4.66 |
| CHEMBL5790820 | — | — | 3 | 4.41 |
| CHEMBL5995179 | — | — | 3 | 4.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5868830 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL6061357 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5764687 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5741292 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5757699 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5772596 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL5830820 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5918774 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL5803742 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL5994824 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5826532 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5920914 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5754446 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL5935723 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL5792951 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL5957110 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL5874865 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL5911168 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL5765868 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL6052282 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL5985401 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL5790820 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL5995179 | — | IC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL5765868 | — | k_off | = | - | s-1 | - |
| CHEMBL5995179 | — | kon | = | - | — | - |
| CHEMBL5826532 | — | kon | = | - | — | - |
| CHEMBL5826532 | — | k_off | = | - | s-1 | - |
| CHEMBL5985401 | — | kon | = | - | — | - |
| CHEMBL5792951 | — | k_off | = | - | s-1 | - |
| CHEMBL5994824 | — | kon | = | - | — | - |
| CHEMBL5994824 | — | k_off | = | - | s-1 | - |
| CHEMBL5920914 | — | kon | = | - | — | - |
| CHEMBL5920914 | — | k_off | = | - | s-1 | - |
| CHEMBL5830820 | — | kon | = | - | — | - |
| CHEMBL5830820 | — | k_off | = | - | s-1 | - |
| CHEMBL5772596 | — | kon | = | - | — | - |
| CHEMBL5995179 | — | k_off | = | - | s-1 | - |
| CHEMBL5765868 | — | kon | = | - | — | - |
| CHEMBL5874865 | — | k_off | = | - | s-1 | - |
| CHEMBL5874865 | — | kon | = | - | — | - |
| CHEMBL5790820 | — | kon | = | - | — | - |
| CHEMBL5757699 | — | kon | = | - | — | - |
| CHEMBL5957110 | — | k_off | = | - | s-1 | - |
| CHEMBL5790820 | — | k_off | = | - | s-1 | - |
| CHEMBL5957110 | — | kon | = | - | — | - |
| CHEMBL5911168 | — | kon | = | - | — | - |
| CHEMBL5935723 | — | k_off | = | - | s-1 | - |
| CHEMBL5911168 | — | k_off | = | - | s-1 | - |
| CHEMBL5935723 | — | kon | = | - | — | - |
| CHEMBL5985401 | — | k_off | = | - | s-1 | - |