Assay Detail
Binding
CHEMBL5732987
Review assay metadata, readout intent, target linkage, and publication context from the same page.
MCT4-Mediated Lactate Transport in MDA-MB-231 Breast Cancer Cells: MDA-MB-231 breast cancer 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. MCT4 activity may be assessed by monitoring the intracellular pH change that accompanies lactate/proton symport, using the pH-sensitive fluorescent dye 2′,7′-bis-(carboxyethyl)-5(6)-carboxyfluorescein (BCECF), in a manner similar to that previously reported for MCT1 and MCT4. The following is an exemplary procedure for assaying MCT4 activity of the compounds of Formula (I).
663
Total Activities
217
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 | 221 | 7.61 | 9.52 |
| kon | 221 | - | - |
| k_off | 221 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5268154 | — | — | 3 | 9.52 |
| CHEMBL5937220 | — | — | 3 | 9.52 |
| CHEMBL5556465 | — | — | 3 | 9.49 |
| CHEMBL5562055 | — | — | 3 | 9.46 |
| CHEMBL5789173 | — | — | 3 | 9.46 |
| CHEMBL5267318 | — | — | 3 | 9.44 |
| CHEMBL6012305 | — | — | 3 | 9.27 |
| CHEMBL5270910 | — | — | 3 | 9.24 |
| CHEMBL5560319 | — | — | 3 | 9.23 |
| CHEMBL5935003 | — | — | 3 | 9.23 |
| CHEMBL6010364 | — | — | 3 | 9.08 |
| CHEMBL6031816 | — | — | 3 | 9.00 |
| CHEMBL5956640 | — | — | 3 | 9.00 |
| CHEMBL5904074 | — | — | 3 | 8.96 |
| CHEMBL5904026 | — | — | 3 | 8.92 |
| CHEMBL5993465 | — | — | 3 | 8.89 |
| CHEMBL5958336 | — | — | 3 | 8.89 |
| CHEMBL6037396 | — | — | 3 | 8.85 |
| CHEMBL5804342 | — | — | 3 | 8.77 |
| CHEMBL5940699 | — | — | 3 | 8.72 |
| CHEMBL5759787 | — | — | 3 | 8.72 |
| CHEMBL5790479 | — | — | 3 | 8.72 |
| CHEMBL6054294 | — | — | 3 | 8.70 |
| CHEMBL5864334 | — | — | 3 | 8.68 |
| CHEMBL6006208 | — | — | 3 | 8.68 |
| CHEMBL5803571 | — | — | 3 | 8.66 |
| CHEMBL5811534 | — | — | 3 | 8.62 |
| CHEMBL6035770 | — | — | 3 | 8.62 |
| CHEMBL5833032 | — | — | 3 | 8.62 |
| CHEMBL6022434 | — | — | 3 | 8.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5937220 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5268154 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5556465 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL5562055 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL5789173 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL5267318 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL6012305 | — | IC50 | = | 0.54 | nM | 9.27 |
| CHEMBL5270910 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL5935003 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL5560319 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL6010364 | — | IC50 | = | 0.83 | nM | 9.08 |
| CHEMBL5956640 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL6031816 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5904074 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5904026 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5958336 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5993465 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL6037396 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5804342 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5940699 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5790479 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5759787 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL6054294 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL6006208 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5864334 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5803571 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL6035770 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5833032 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5811534 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL6022434 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5923718 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL6056725 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL6017525 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5982634 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5832566 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5996320 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5792832 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5916507 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5981118 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL5825779 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL5892585 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL5811771 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL5855607 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL5903728 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5871500 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL5740985 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL5902995 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL6022870 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5870870 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL6063241 | — | IC50 | = | 4.1 | nM | 8.39 |