Assay Detail
Binding
CHEMBL3631402
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Inhibition of Xct in human CCF-STTG1 cells assessed as glutamate release after 2 hrs by fluorometry
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CCF-STTG1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Incorporation of metabolically stable ketones into a small molecule probe to increase potency and water solubility.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.34 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3629669 | — | — | 1 | 8.40 |
| CHEMBL3629579 | — | — | 1 | 8.00 |
| CHEMBL3629668 | — | — | 1 | 8.00 |
| CHEMBL3629578 | — | — | 1 | 7.70 |
| CHEMBL3629576 | — | — | 1 | 7.52 |
| CHEMBL3629671 | — | — | 1 | 7.52 |
| CHEMBL3629577 | — | — | 1 | 7.40 |
| CHEMBL3629575 | — | — | 1 | 7.22 |
| CHEMBL3629670 | — | — | 1 | 7.00 |
| CHEMBL401989 | ERASTIN | — | 1 | 6.70 |
| CHEMBL3629580 | — | — | 1 | 6.52 |
| CHEMBL3629574 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3629669 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3629579 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3629668 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3629578 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3629576 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3629671 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3629577 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3629575 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3629670 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL401989 | ERASTIN | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3629580 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3629574 | — | IC50 | = | 800.0 | nM | 6.10 |