Assay Detail
Binding
CHEMBL4237203
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Activation of SOS1 in human HeLa cells assessed as increase in RAS-GTP levels after 30 mins by pull-down assay
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Quinazolines That Activate SOS1-Mediated Nucleotide Exchange on RAS.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 42 | 5.23 | 5.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4239886 | — | — | 1 | 5.96 |
| CHEMBL4243567 | — | — | 1 | 5.75 |
| CHEMBL4248160 | — | — | 1 | 5.70 |
| CHEMBL4241069 | — | — | 1 | 5.60 |
| CHEMBL4247794 | — | — | 1 | 5.60 |
| CHEMBL4238147 | — | — | 1 | 5.57 |
| CHEMBL4243577 | — | — | 1 | 5.52 |
| CHEMBL4239768 | — | — | 1 | 5.38 |
| CHEMBL4237333 | — | — | 1 | 5.21 |
| CHEMBL4245081 | — | — | 1 | 5.19 |
| CHEMBL4243999 | — | — | 1 | 5.18 |
| CHEMBL4237885 | — | — | 1 | 5.15 |
| CHEMBL4250348 | — | — | 1 | 5.11 |
| CHEMBL1198227 | — | — | 1 | 5.01 |
| CHEMBL4245906 | — | — | 1 | 4.88 |
| CHEMBL4242567 | — | — | 1 | 4.79 |
| CHEMBL1197658 | — | — | 1 | 4.79 |
| CHEMBL4237599 | — | — | 1 | 4.66 |
| CHEMBL4242100 | — | — | 1 | 4.36 |
| CHEMBL4249825 | — | — | 1 | - |
| CHEMBL4246533 | — | — | 1 | - |
| CHEMBL4239782 | — | — | 1 | - |
| CHEMBL4250799 | — | — | 1 | - |
| CHEMBL4244009 | — | — | 1 | - |
| CHEMBL4249474 | — | — | 1 | - |
| CHEMBL4244333 | — | — | 1 | - |
| CHEMBL4247355 | — | — | 1 | - |
| CHEMBL4249331 | — | — | 1 | - |
| CHEMBL4246362 | — | — | 1 | - |
| CHEMBL4238401 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4239886 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4243567 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4248160 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4241069 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4247794 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4238147 | — | EC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4243577 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4239768 | — | EC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL4237333 | — | EC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL4245081 | — | EC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL4243999 | — | EC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL4237885 | — | EC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL4250348 | — | EC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL1198227 | — | EC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL4245906 | — | EC50 | = | 13100.0 | nM | 4.88 |
| CHEMBL4242567 | — | EC50 | = | 16300.0 | nM | 4.79 |
| CHEMBL1197658 | — | EC50 | = | 16400.0 | nM | 4.79 |
| CHEMBL4237599 | — | EC50 | = | 21900.0 | nM | 4.66 |
| CHEMBL4242100 | — | EC50 | = | 44200.0 | nM | 4.36 |
| CHEMBL1616690 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4247895 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4248355 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL579127 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL379386 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL533658 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4241603 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4237445 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4251375 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4247087 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4250158 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4249702 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4238401 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4246362 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4249331 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4247355 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4244333 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4249474 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4244009 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4250799 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4239782 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4246533 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4249825 | — | EC50 | > | 100000.0 | nM | - |