Assay Detail
Binding
CHEMBL4032893
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Allosteric inhibition of SHP2 E76A mutant (unknown origin) expressed in Escherichia coli BL21(DE3) using DIFMUP as substrate preincubated for 20 mins followed by substrate addition measured after 20 mins by phosphatase assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Allosteric Inhibitors of SHP2 with Therapeutic Potential for Cancer Treatment.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 5.40 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4060033 | — | — | 1 | 6.92 |
| CHEMBL4091173 | — | — | 1 | 6.15 |
| CHEMBL4097267 | — | — | 1 | 6.14 |
| CHEMBL4086829 | — | — | 1 | 5.97 |
| CHEMBL4076685 | — | — | 1 | 5.90 |
| CHEMBL4076593 | — | — | 1 | 5.86 |
| CHEMBL4081681 | — | — | 1 | 5.83 |
| CHEMBL4061410 | — | — | 1 | 5.83 |
| CHEMBL4092889 | — | — | 1 | 5.78 |
| CHEMBL4084959 | — | — | 1 | 5.75 |
| CHEMBL4066473 | — | — | 1 | 5.61 |
| CHEMBL4080745 | — | — | 1 | 5.59 |
| CHEMBL4059663 | — | — | 1 | 5.57 |
| CHEMBL4070077 | — | — | 1 | 5.55 |
| CHEMBL4088619 | — | — | 1 | 5.49 |
| CHEMBL4103648 | — | — | 1 | 5.48 |
| CHEMBL4087630 | — | — | 1 | 5.44 |
| CHEMBL4104973 | — | — | 1 | 5.27 |
| CHEMBL4099691 | — | — | 1 | 4.91 |
| CHEMBL4075896 | — | — | 1 | 4.85 |
| CHEMBL4088271 | — | — | 1 | 4.72 |
| CHEMBL4062053 | — | — | 1 | 4.69 |
| CHEMBL4104752 | — | — | 1 | 4.33 |
| CHEMBL4064584 | — | — | 1 | 4.29 |
| CHEMBL4082381 | — | — | 1 | 4.28 |
| CHEMBL4073557 | — | — | 1 | 4.28 |
| CHEMBL4066276 | — | — | 1 | - |
| CHEMBL4068493 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4060033 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4091173 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL4097267 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL4086829 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL4076685 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL4076593 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL4081681 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL4061410 | — | IC50 | = | 1490.0 | nM | 5.83 |
| CHEMBL4092889 | — | IC50 | = | 1650.0 | nM | 5.78 |
| CHEMBL4084959 | — | IC50 | = | 1760.0 | nM | 5.75 |
| CHEMBL4066473 | — | IC50 | = | 2460.0 | nM | 5.61 |
| CHEMBL4080745 | — | IC50 | = | 2550.0 | nM | 5.59 |
| CHEMBL4059663 | — | IC50 | = | 2680.0 | nM | 5.57 |
| CHEMBL4070077 | — | IC50 | = | 2810.0 | nM | 5.55 |
| CHEMBL4088619 | — | IC50 | = | 3270.0 | nM | 5.49 |
| CHEMBL4103648 | — | IC50 | = | 3280.0 | nM | 5.48 |
| CHEMBL4087630 | — | IC50 | = | 3620.0 | nM | 5.44 |
| CHEMBL4104973 | — | IC50 | = | 5320.0 | nM | 5.27 |
| CHEMBL4099691 | — | IC50 | = | 12320.0 | nM | 4.91 |
| CHEMBL4075896 | — | IC50 | = | 14200.0 | nM | 4.85 |
| CHEMBL4088271 | — | IC50 | = | 19070.0 | nM | 4.72 |
| CHEMBL4062053 | — | IC50 | = | 20300.0 | nM | 4.69 |
| CHEMBL4104752 | — | IC50 | = | 46500.0 | nM | 4.33 |
| CHEMBL4064584 | — | IC50 | = | 51700.0 | nM | 4.29 |
| CHEMBL4082381 | — | IC50 | = | 52830.0 | nM | 4.28 |
| CHEMBL4073557 | — | IC50 | = | 52300.0 | nM | 4.28 |
| CHEMBL4066276 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4068493 | — | IC50 | > | 100000.0 | nM | - |