Assay Detail
Binding
CHEMBL5317827
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MCT1 transport activity in human A549 cells using 3-BP as substrate assessed as reduction in intracellular 3-BP level by measuring increase in cell viability incubated for 72 hrs by MTT assay
17
Total Activities
17
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 |
Publication
Indole Derivatives as New Structural Class of Potent and Antiproliferative Inhibitors of Monocarboxylate Transporter 1 (MCT1; SLC16A1).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.81 | 7.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5435709 | — | — | 1 | 7.09 |
| CHEMBL5419493 | — | — | 1 | 7.08 |
| CHEMBL76602 | alpha-CYANO-4-HYDROXYCINNAMIC ACID | — | 1 | 7.06 |
| CHEMBL5401494 | — | — | 1 | 6.98 |
| CHEMBL5405329 | — | — | 1 | 6.98 |
| CHEMBL5409450 | — | — | 1 | 6.96 |
| CHEMBL5433941 | — | — | 1 | 6.96 |
| CHEMBL5394985 | — | — | 1 | 6.96 |
| CHEMBL5440350 | — | — | 1 | 6.95 |
| CHEMBL5421503 | — | — | 1 | 6.87 |
| CHEMBL5427293 | — | — | 1 | 6.71 |
| CHEMBL5397576 | — | — | 1 | 6.71 |
| CHEMBL5431419 | — | — | 1 | 6.70 |
| CHEMBL5439235 | — | — | 1 | 6.67 |
| CHEMBL5402273 | — | — | 1 | 6.54 |
| CHEMBL5402599 | — | — | 1 | 6.50 |
| CHEMBL5427387 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5435709 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL5419493 | — | IC50 | = | 82.3 | nM | 7.08 |
| CHEMBL76602 | alpha-CYANO-4-HYDROXYCINNAMIC ACID | IC50 | = | 87.2 | nM | 7.06 |
| CHEMBL5401494 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL5405329 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL5409450 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL5433941 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL5394985 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL5440350 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL5421503 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL5427293 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL5397576 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL5431419 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL5439235 | — | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL5402273 | — | IC50 | = | 287.0 | nM | 6.54 |
| CHEMBL5402599 | — | IC50 | = | 314.0 | nM | 6.50 |
| CHEMBL5427387 | — | IC50 | = | 793.0 | nM | 6.10 |