Assay Detail
Binding
CHEMBL751006
Review assay metadata, readout intent, target linkage, and publication context from the same page.
O6-Alkylguanine-DNA Alkyltransferase-Inactivating Activity (Concentration of inactivator required to produce 50% reduction in ATPase activity)
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Methylated-DNA--protein-cysteine methyltransferase (CHEMBL2864) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Inactivation of O6-alkylguanine-DNA alkyltransferase. 1. Novel O6-(hetarylmethyl)guanines having basic rings in the side chain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.73 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL146769 | — | — | 1 | 8.30 |
| CHEMBL151579 | — | — | 1 | 7.75 |
| CHEMBL345550 | — | — | 1 | 7.48 |
| CHEMBL151495 | — | — | 1 | 7.40 |
| CHEMBL407874 | 6-O-BENZYLGUANINE | 3.0 | 1 | 7.40 |
| CHEMBL150324 | — | — | 1 | 7.16 |
| CHEMBL146768 | — | — | 1 | 7.10 |
| CHEMBL146734 | — | — | 1 | 6.89 |
| CHEMBL151785 | — | — | 1 | 6.70 |
| CHEMBL150918 | — | — | 1 | 6.64 |
| CHEMBL151552 | — | — | 1 | 6.60 |
| CHEMBL150427 | — | — | 1 | 6.46 |
| CHEMBL342497 | — | — | 1 | 6.37 |
| CHEMBL151784 | — | — | 1 | 5.85 |
| CHEMBL147472 | — | — | 1 | 5.07 |
| CHEMBL146977 | — | — | 1 | 4.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL146769 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL151579 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL345550 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL151495 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL407874 | 6-O-BENZYLGUANINE | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL150324 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL146768 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL146734 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL151785 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL150918 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL151552 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL150427 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL342497 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL151784 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL147472 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL146977 | — | IC50 | = | 35000.0 | nM | 4.46 |