Assay Detail
Binding
CHEMBL751007
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O6-Alkylguanine-DNA Alkyltransferase-Inactivating Activity in Raji cells (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 |
| Cell Type | Raji |
| 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 | 6.69 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL146769 | — | — | 1 | 8.00 |
| CHEMBL151579 | — | — | 1 | 7.52 |
| CHEMBL151495 | — | — | 1 | 7.30 |
| CHEMBL345550 | — | — | 1 | 7.22 |
| CHEMBL150324 | — | — | 1 | 7.16 |
| CHEMBL150918 | — | — | 1 | 7.05 |
| CHEMBL407874 | 6-O-BENZYLGUANINE | 3.0 | 1 | 7.00 |
| CHEMBL146768 | — | — | 1 | 6.92 |
| CHEMBL151785 | — | — | 1 | 6.92 |
| CHEMBL151552 | — | — | 1 | 6.70 |
| CHEMBL146734 | — | — | 1 | 6.70 |
| CHEMBL150427 | — | — | 1 | 6.66 |
| CHEMBL342497 | — | — | 1 | 6.66 |
| CHEMBL151784 | — | — | 1 | 5.27 |
| CHEMBL146977 | — | — | 1 | 5.22 |
| CHEMBL147472 | — | — | 1 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL146769 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL151579 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL151495 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL345550 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL150324 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL150918 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL407874 | 6-O-BENZYLGUANINE | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL146768 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL151785 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL151552 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL146734 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL150427 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL342497 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL151784 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL146977 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL147472 | — | IC50 | = | 21000.0 | nM | 4.68 |