Assay Detail
Binding
CHEMBL2444904
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Inhibition of MCT4-mediated [14C]-lactate uptake in human SiHa cells in lactate-containing medium assessed as remaining lactate concentration in culture medium after 24 hrs by liquid scintillation counting
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SiHa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and pharmacological evaluation of carboxycoumarins as a new antitumor treatment targeting lactate transport in cancer cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.76 | 7.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2442509 | — | — | 1 | 7.23 |
| CHEMBL2442512 | — | — | 1 | 6.14 |
| CHEMBL1303766 | — | — | 1 | 6.07 |
| CHEMBL2442515 | — | — | 1 | 5.90 |
| CHEMBL2442510 | — | — | 1 | 5.85 |
| CHEMBL2442513 | — | — | 1 | 5.72 |
| CHEMBL1830821 | — | — | 1 | 5.64 |
| CHEMBL2442514 | — | — | 1 | 5.62 |
| CHEMBL2442508 | — | — | 1 | 5.10 |
| CHEMBL76602 | alpha-CYANO-4-HYDROXYCINNAMIC ACID | — | 1 | 4.36 |
| CHEMBL2442511 | — | — | 1 | - |
| CHEMBL2442516 | — | — | 1 | - |
| CHEMBL2442517 | — | — | 1 | - |
| CHEMBL2442503 | — | — | 1 | - |
| CHEMBL2442504 | — | — | 1 | - |
| CHEMBL2442505 | — | — | 1 | - |
| CHEMBL2442506 | — | — | 1 | - |
| CHEMBL2442507 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2442509 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL2442512 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL1303766 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL2442515 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL2442510 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2442513 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL1830821 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL2442514 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL2442508 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL76602 | alpha-CYANO-4-HYDROXYCINNAMIC ACID | IC50 | = | 43500.0 | nM | 4.36 |
| CHEMBL2442511 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2442516 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2442517 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2442503 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2442504 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2442505 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2442506 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2442507 | — | IC50 | > | 30000.0 | nM | - |