Assay Detail
Binding
CHEMBL645826
Review assay metadata, readout intent, target linkage, and publication context from the same page.
concentration required to reduce AGT activity to 50% of control rate in intact HT-29 human colorectal carcinoma cells.
8
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HT-29 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Methylated-DNA--protein-cysteine methyltransferase (CHEMBL2864) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Resistance-modifying agents. 8. Inhibition of O(6)-alkylguanine-DNA alkyltransferase by O(6)-alkenyl-, O(6)-cycloalkenyl-, and O(6)-(2-oxoalkyl)guanines and potentiation of temozolomide cytotoxicity in vitro by O(6)-(1-cyclopentenylmethyl)guanine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 4.40 | 4.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL270483 | — | — | 2 | 4.94 |
| CHEMBL334050 | — | — | 2 | 4.43 |
| CHEMBL337713 | — | — | 2 | 4.03 |
| CHEMBL272689 | — | — | 2 | 4.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL270483 | — | IC50 | = | 11500.0 | nM | 4.94 |
| CHEMBL270483 | — | IC50 | = | 11900.0 | nM | 4.92 |
| CHEMBL334050 | — | IC50 | = | 37500.0 | nM | 4.43 |
| CHEMBL334050 | — | IC50 | = | 39600.0 | nM | 4.40 |
| CHEMBL337713 | — | IC50 | = | 94500.0 | nM | 4.03 |
| CHEMBL337713 | — | IC50 | = | 93200.0 | nM | 4.03 |
| CHEMBL272689 | — | IC50 | = | 95000.0 | nM | 4.02 |
| CHEMBL272689 | — | IC50 | = | 119000.0 | nM | - |