Assay Detail
Binding
CHEMBL5107176
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Inhibition of SOS1 in human DLD-1 cells assessed as reduction in ERK phosphorylation incubated for 1 hr by fluorescence assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | DLD-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Orally Bioavailable SOS1 Inhibitors for Suppressing KRAS-Driven Carcinoma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.50 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5171547 | — | — | 1 | 8.00 |
| CHEMBL5184087 | — | — | 1 | 7.96 |
| CHEMBL5184590 | — | — | 1 | 7.89 |
| CHEMBL5201901 | — | — | 1 | 7.89 |
| CHEMBL5196432 | — | — | 1 | 7.80 |
| CHEMBL5209105 | — | — | 1 | 7.72 |
| CHEMBL5195849 | — | — | 1 | 7.54 |
| CHEMBL5201816 | — | — | 1 | 7.52 |
| CHEMBL5185398 | — | — | 1 | 7.47 |
| CHEMBL5203150 | — | — | 1 | 7.47 |
| CHEMBL5183723 | — | — | 1 | 7.40 |
| CHEMBL5170314 | — | — | 1 | 7.31 |
| CHEMBL5185573 | — | — | 1 | 7.29 |
| CHEMBL5193498 | — | — | 1 | 7.28 |
| CHEMBL5208418 | — | — | 1 | 7.16 |
| CHEMBL5183879 | — | — | 1 | 7.12 |
| CHEMBL5191638 | — | — | 1 | 7.11 |
| CHEMBL5181797 | — | — | 1 | 7.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5171547 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5184087 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5184590 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5201901 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5196432 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5209105 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5195849 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5201816 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5185398 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5203150 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5183723 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5170314 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5185573 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL5193498 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5208418 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5183879 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL5191638 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL5181797 | — | IC50 | = | 88.0 | nM | 7.06 |