Assay Detail
Binding
CHEMBL4701889
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Allosteric inhibition of 6x-histidine tagged human SHP2 (Met1-L525 residues) expressed in Escherichia coli BL21 Star (DE3) using IRS1_pY1172(dPEG8)pY122 incubated for 30 mins by fluorescence based DIFMUP assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Tyrosine-protein phosphatase non-receptor type 11 (CHEMBL3864) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.50 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4740294 | — | — | 1 | 8.15 |
| CHEMBL4763213 | — | — | 1 | 8.00 |
| CHEMBL4650521 | BATOPROTAFIB | 2.0 | 1 | 7.96 |
| CHEMBL4755819 | — | — | 1 | 7.92 |
| CHEMBL4747789 | — | — | 1 | 7.85 |
| CHEMBL4743002 | — | — | 1 | 7.77 |
| CHEMBL4789106 | — | — | 1 | 7.77 |
| CHEMBL4795635 | — | — | 1 | 7.66 |
| CHEMBL4784611 | — | — | 1 | 7.64 |
| CHEMBL4750422 | — | — | 1 | 7.54 |
| CHEMBL4762625 | — | — | 1 | 7.54 |
| CHEMBL4756767 | — | — | 1 | 7.17 |
| CHEMBL4746224 | — | — | 1 | 7.16 |
| CHEMBL4060033 | — | — | 1 | 7.16 |
| CHEMBL4754023 | — | — | 1 | 7.12 |
| CHEMBL4778151 | — | — | 1 | 6.78 |
| CHEMBL4445214 | — | — | 1 | 6.58 |
| CHEMBL4540461 | — | — | 1 | 6.52 |
| CHEMBL4453719 | — | — | 1 | 5.89 |
| CHEMBL4581173 | — | — | 1 | 5.24 |
| CHEMBL4585337 | — | — | 1 | 5.19 |
| CHEMBL4763856 | — | — | 1 | 5.00 |
| CHEMBL4473316 | — | — | 1 | 4.92 |
| CHEMBL4562377 | — | — | 1 | 4.66 |
| CHEMBL4514244 | — | — | 1 | 4.33 |
| CHEMBL4459456 | — | — | 1 | 4.27 |
| CHEMBL4797606 | — | — | 1 | 4.19 |
| CHEMBL4566119 | — | — | 1 | 4.00 |
| CHEMBL4558200 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4740294 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4763213 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4650521 | BATOPROTAFIB | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4755819 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4747789 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4743002 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4789106 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4795635 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4784611 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4750422 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4762625 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4756767 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4746224 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4060033 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4754023 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4778151 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL4445214 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4540461 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4453719 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4581173 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL4585337 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL4763856 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL4473316 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4562377 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL4514244 | — | IC50 | = | 47000.0 | nM | 4.33 |
| CHEMBL4459456 | — | IC50 | = | 54000.0 | nM | 4.27 |
| CHEMBL4797606 | — | IC50 | = | 64000.0 | nM | 4.19 |
| CHEMBL4566119 | — | IC50 | = | 99000.0 | nM | 4.00 |
| CHEMBL4558200 | — | IC50 | > | 100000.0 | nM | - |