Assay Detail
Binding
CHEMBL5736013
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TBDAlphaScreen Binding Assay: Compounds are diluted to a final start concentration of 100 μM and are tested in duplicate. Assay-ready plates (ARPs) are generated using an Access Labcyte Workstation with a Labcyte Echo 550 or 555 accoustic dispenser. For compound a start concentration of 100 μM, 150 nL of compound solution is transferred per well in 11 concentrations in duplicate with serial 1:5 dilutions.The assay is run using a fully automated robotic system in a darkened room below 100 Lux. 10 μL of KRAS SOS1 GDP mix is added into columns 1-24 to the 150 nL of compound solution (final dilution in the assay 1:100, final DMSO concentration 1%).After a 30 minute incubation time 5 μL of bead mix is added into columns 1-23. Plates are kept at room temperature in a darkened incubator. After a further 60 minute incubation, the signal is measured using a PerkinElmer Envision HTS Multilabel Reader using the AlphaScreen specifications from PerkinElmer.
450
Total Activities
149
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Benzylamino substituted pyridopyrimidinones and derivatives as SOS1 inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 150 | 8.11 | 9.00 |
| kon | 150 | - | - |
| k_off | 150 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6009434 | — | — | 3 | 9.00 |
| CHEMBL6000292 | — | — | 3 | 9.00 |
| CHEMBL5907163 | — | — | 3 | 8.70 |
| CHEMBL6052669 | — | — | 3 | 8.70 |
| CHEMBL5943007 | — | — | 3 | 8.70 |
| CHEMBL5745704 | — | — | 3 | 8.70 |
| CHEMBL5846727 | — | — | 3 | 8.70 |
| CHEMBL5781021 | — | — | 3 | 8.70 |
| CHEMBL5966878 | — | — | 3 | 8.70 |
| CHEMBL5962826 | — | — | 3 | 8.70 |
| CHEMBL5914084 | — | — | 3 | 8.70 |
| CHEMBL5884848 | — | — | 3 | 8.70 |
| CHEMBL5889849 | — | — | 3 | 8.70 |
| CHEMBL5905465 | — | — | 3 | 8.70 |
| CHEMBL5861561 | — | — | 3 | 8.52 |
| CHEMBL5954448 | — | — | 3 | 8.52 |
| CHEMBL5785306 | — | — | 3 | 8.52 |
| CHEMBL5935155 | — | — | 3 | 8.52 |
| CHEMBL5921060 | — | — | 3 | 8.52 |
| CHEMBL5911313 | — | — | 3 | 8.52 |
| CHEMBL6010852 | — | — | 3 | 8.52 |
| CHEMBL5842335 | — | — | 3 | 8.52 |
| CHEMBL5809336 | — | — | 3 | 8.40 |
| CHEMBL5996000 | — | — | 3 | 8.40 |
| CHEMBL5895016 | — | — | 3 | 8.40 |
| CHEMBL6050475 | — | — | 3 | 8.40 |
| CHEMBL5774260 | — | — | 3 | 8.40 |
| CHEMBL6042806 | — | — | 3 | 8.40 |
| CHEMBL5788088 | — | — | 3 | 8.40 |
| CHEMBL5962781 | — | — | 3 | 8.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6000292 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL6009434 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5884848 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL6052669 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5966878 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5962826 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5914084 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5781021 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5907163 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5846727 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5745704 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5943007 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5905465 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5889849 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5861561 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5935155 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5785306 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL6010852 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5921060 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5911313 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5954448 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5842335 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL6044436 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5885018 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5760466 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5785130 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5851040 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5941695 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL6042806 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5774260 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5788088 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5962781 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5784521 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5895016 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5809336 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5996000 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5970898 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL6050475 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5808866 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5813811 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL6036140 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5779861 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5802092 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5988943 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5878137 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5828192 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5950832 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5897531 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5865315 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5857676 | — | IC50 | = | 5.0 | nM | 8.30 |