Assay Detail
Binding
CHEMBL5226037
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 6His-tagged SOS1 (unknown origin) mediated GST-tagged KRAS G12D activation preincubated for 15 mins followed by KRAS G12D addition and measured after 30 mins by HTRF assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, Synthesis, and Bioevaluation of Pyrido[2,3-<i>d</i>]pyrimidin-7-ones as Potent SOS1 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.84 | 7.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5275216 | — | — | 1 | 7.17 |
| CHEMBL5280533 | — | — | 1 | 7.15 |
| CHEMBL4519023 | — | — | 1 | 7.14 |
| CHEMBL5290547 | — | — | 1 | 7.14 |
| CHEMBL5286601 | — | — | 1 | 7.13 |
| CHEMBL5269963 | — | — | 1 | 7.11 |
| CHEMBL5284292 | — | — | 1 | 7.07 |
| CHEMBL5266985 | — | — | 1 | 7.06 |
| CHEMBL5267612 | — | — | 1 | 7.04 |
| CHEMBL5280431 | — | — | 1 | 7.03 |
| CHEMBL5275839 | — | — | 1 | 7.03 |
| CHEMBL5274267 | — | — | 1 | 7.02 |
| CHEMBL5279147 | — | — | 1 | 6.87 |
| CHEMBL5266146 | — | — | 1 | 6.86 |
| CHEMBL5282775 | — | — | 1 | 6.77 |
| CHEMBL5279160 | — | — | 1 | 6.65 |
| CHEMBL5287813 | — | — | 1 | 6.33 |
| CHEMBL5281607 | — | — | 1 | 6.16 |
| CHEMBL5271901 | — | — | 1 | 6.10 |
| CHEMBL5275170 | — | — | 1 | 6.06 |
| CHEMBL5288876 | — | — | 1 | - |
| CHEMBL5270449 | — | — | 1 | - |
| CHEMBL5288585 | — | — | 1 | - |
| CHEMBL5290546 | — | — | 1 | - |
| CHEMBL5270088 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5275216 | — | IC50 | = | 67.4 | nM | 7.17 |
| CHEMBL5280533 | — | IC50 | = | 70.5 | nM | 7.15 |
| CHEMBL4519023 | — | IC50 | = | 71.8 | nM | 7.14 |
| CHEMBL5290547 | — | IC50 | = | 72.1 | nM | 7.14 |
| CHEMBL5286601 | — | IC50 | = | 73.4 | nM | 7.13 |
| CHEMBL5269963 | — | IC50 | = | 77.5 | nM | 7.11 |
| CHEMBL5284292 | — | IC50 | = | 85.6 | nM | 7.07 |
| CHEMBL5266985 | — | IC50 | = | 87.8 | nM | 7.06 |
| CHEMBL5267612 | — | IC50 | = | 90.8 | nM | 7.04 |
| CHEMBL5280431 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL5275839 | — | IC50 | = | 92.8 | nM | 7.03 |
| CHEMBL5274267 | — | IC50 | = | 95.4 | nM | 7.02 |
| CHEMBL5279147 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL5266146 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL5282775 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL5279160 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL5287813 | — | IC50 | = | 463.0 | nM | 6.33 |
| CHEMBL5281607 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL5271901 | — | IC50 | = | 801.0 | nM | 6.10 |
| CHEMBL5275170 | — | IC50 | = | 869.0 | nM | 6.06 |
| CHEMBL5288876 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5270449 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5288585 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5290546 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5270088 | — | IC50 | > | 5000.0 | nM | - |