Assay Detail
Binding
CHEMBL5238191
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of SOS1/KRAS G13D mutant protein-protein interaction in human DLD-1 cells assessed as ERK1/2 phosphorylation measured after 1 hr by homogeneous time-resolved fluorescence (HTRF) method
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | DLD-1 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design and Structural Optimization of Orally Bioavailable SOS1 Inhibitors for the Treatment of KRAS-Driven Carcinoma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 51 | 7.52 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5274240 | — | — | 1 | 9.05 |
| CHEMBL5285694 | — | — | 1 | 8.85 |
| CHEMBL5267448 | — | — | 1 | 8.77 |
| CHEMBL5290978 | — | — | 1 | 8.62 |
| CHEMBL5274435 | — | — | 1 | 8.54 |
| CHEMBL5283813 | — | — | 1 | 8.33 |
| CHEMBL5274631 | — | — | 1 | 8.30 |
| CHEMBL5275185 | — | — | 1 | 8.22 |
| CHEMBL5274075 | — | — | 1 | 8.10 |
| CHEMBL5291466 | — | — | 1 | 8.05 |
| CHEMBL5284732 | — | — | 1 | 8.02 |
| CHEMBL5275813 | — | — | 1 | 8.01 |
| CHEMBL5269752 | — | — | 1 | 8.00 |
| CHEMBL5266753 | — | — | 1 | 8.00 |
| CHEMBL5289720 | — | — | 1 | 7.96 |
| CHEMBL5184590 | — | — | 1 | 7.85 |
| CHEMBL5279781 | — | — | 1 | 7.82 |
| CHEMBL5277035 | — | — | 1 | 7.80 |
| CHEMBL5288800 | — | — | 1 | 7.75 |
| CHEMBL5281957 | — | — | 1 | 7.72 |
| CHEMBL5271862 | — | — | 1 | 7.68 |
| CHEMBL5274284 | — | — | 1 | 7.66 |
| CHEMBL5269832 | — | — | 1 | 7.66 |
| CHEMBL5281653 | — | — | 1 | 7.60 |
| CHEMBL5268043 | — | — | 1 | 7.60 |
| CHEMBL5276625 | — | — | 1 | 7.58 |
| CHEMBL4519023 | — | — | 1 | 7.51 |
| CHEMBL5266717 | — | — | 1 | 7.50 |
| CHEMBL5276698 | — | — | 1 | 7.42 |
| CHEMBL5268844 | — | — | 1 | 7.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5274240 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5285694 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5267448 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5290978 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5274435 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5283813 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL5274631 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5275185 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5274075 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5291466 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5284732 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL5275813 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL5269752 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5266753 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5289720 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5184590 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5279781 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5277035 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5288800 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5281957 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5271862 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5274284 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5269832 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5281653 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5268043 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5276625 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4519023 | — | IC50 | = | 30.7 | nM | 7.51 |
| CHEMBL5266717 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5276698 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5268844 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5272348 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5283652 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5274802 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5287122 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL5284268 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL5286250 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL5277097 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL5281525 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL5278120 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL5268192 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL5280314 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL5273306 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL5277716 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL5279412 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL5271433 | — | IC50 | = | 295.0 | nM | 6.53 |
| CHEMBL5276246 | — | IC50 | = | 367.0 | nM | 6.43 |
| CHEMBL5271195 | — | IC50 | = | 376.0 | nM | 6.42 |
| CHEMBL5281209 | — | IC50 | = | 691.0 | nM | 6.16 |
| CHEMBL5267923 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL5273838 | — | IC50 | = | 780.0 | nM | 6.11 |