Assay Detail
Binding
CHEMBL645820
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Inhibition of AGT activity to 50% of control rate in HT-29 cell extract
24
Total Activities
24
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 | Expert |
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 | 24 | 5.69 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL337677 | — | — | 1 | 8.52 |
| CHEMBL407874 | 6-O-BENZYLGUANINE | 3.0 | 1 | 6.75 |
| CHEMBL405259 | — | — | 1 | 6.41 |
| CHEMBL439608 | — | — | 1 | 6.26 |
| CHEMBL429409 | — | — | 1 | 5.80 |
| CHEMBL272182 | — | — | 1 | 5.58 |
| CHEMBL325053 | — | — | 1 | 5.07 |
| CHEMBL270982 | — | — | 1 | 4.80 |
| CHEMBL270483 | — | — | 1 | 4.70 |
| CHEMBL407876 | — | — | 1 | 4.60 |
| CHEMBL334050 | — | — | 1 | 4.11 |
| CHEMBL405197 | — | — | 1 | - |
| CHEMBL272689 | — | — | 1 | - |
| CHEMBL130392 | — | — | 1 | - |
| CHEMBL270945 | — | — | 1 | - |
| CHEMBL272397 | — | — | 1 | - |
| CHEMBL446625 | — | — | 1 | - |
| CHEMBL338451 | — | — | 1 | - |
| CHEMBL406495 | — | — | 1 | - |
| CHEMBL270946 | — | — | 1 | - |
| CHEMBL406419 | — | — | 1 | - |
| CHEMBL337713 | — | — | 1 | - |
| CHEMBL405533 | — | — | 1 | - |
| CHEMBL226395 | METHYLGUANINE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL337677 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL407874 | 6-O-BENZYLGUANINE | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL405259 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL439608 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL429409 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL272182 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL325053 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL270982 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL270483 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL407876 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL334050 | — | IC50 | = | 77000.0 | nM | 4.11 |
| CHEMBL405197 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL272689 | — | IC50 | = | 192000.0 | nM | - |
| CHEMBL130392 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL270945 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL272397 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL446625 | — | IC50 | = | 548000.0 | nM | - |
| CHEMBL338451 | — | IC50 | = | 554000.0 | nM | - |
| CHEMBL406495 | — | IC50 | = | 1006000.0 | nM | - |
| CHEMBL270946 | — | IC50 | = | 493000.0 | nM | - |
| CHEMBL406419 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL337713 | — | IC50 | = | 151000.0 | nM | - |
| CHEMBL405533 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL226395 | METHYLGUANINE | IC50 | = | 428000.0 | nM | - |