Assay Detail
Binding
CHEMBL5617873
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Allosteric inhibition of N-terminal His-tagged human recombinant SHP2 extracted from Escherichia coli using DiFMUP as substrate preincubated with compound for 60 mins followed by substrate addition and measured after 30 mins by fluorescence based microplate reader analysis
44
Total Activities
44
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
Discovery of novel substituted pyridine carboxamide derivatives as potent allosteric SHP2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 44 | 7.66 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5618343 | — | — | 1 | 9.89 |
| CHEMBL5618733 | — | — | 1 | 9.89 |
| CHEMBL5619476 | — | — | 1 | 9.77 |
| CHEMBL5619863 | — | — | 1 | 9.23 |
| CHEMBL5619365 | — | — | 1 | 9.22 |
| CHEMBL5619074 | — | — | 1 | 8.99 |
| CHEMBL5619866 | — | — | 1 | 8.97 |
| CHEMBL5618566 | — | — | 1 | 8.77 |
| CHEMBL5620154 | — | — | 1 | 8.73 |
| CHEMBL5619937 | — | — | 1 | 8.19 |
| CHEMBL5618608 | — | — | 1 | 8.18 |
| CHEMBL5619118 | — | — | 1 | 7.95 |
| CHEMBL4650521 | BATOPROTAFIB | 2.0 | 1 | 7.70 |
| CHEMBL5619482 | — | — | 1 | 7.53 |
| CHEMBL5619265 | — | — | 1 | 7.52 |
| CHEMBL5618322 | — | — | 1 | 7.49 |
| CHEMBL5619941 | — | — | 1 | 7.44 |
| CHEMBL5619774 | — | — | 1 | 7.40 |
| CHEMBL5620322 | — | — | 1 | 7.30 |
| CHEMBL5618116 | — | — | 1 | 7.29 |
| CHEMBL5619759 | — | — | 1 | 7.28 |
| CHEMBL5620194 | — | — | 1 | 7.17 |
| CHEMBL5618941 | — | — | 1 | 7.11 |
| CHEMBL5618632 | — | — | 1 | 7.05 |
| CHEMBL5618351 | — | — | 1 | 7.05 |
| CHEMBL5618981 | — | — | 1 | 6.95 |
| CHEMBL5620018 | — | — | 1 | 6.93 |
| CHEMBL5619709 | — | — | 1 | 6.89 |
| CHEMBL5620236 | — | — | 1 | 6.83 |
| CHEMBL5619832 | — | — | 1 | 6.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5618343 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL5618733 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL5619476 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL5619863 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL5619365 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5619074 | — | IC50 | = | 1.03 | nM | 8.99 |
| CHEMBL5619866 | — | IC50 | = | 1.08 | nM | 8.97 |
| CHEMBL5618566 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5620154 | — | IC50 | = | 1.87 | nM | 8.73 |
| CHEMBL5619937 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL5618608 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL5619118 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL4650521 | BATOPROTAFIB | IC50 | = | 20.1 | nM | 7.70 |
| CHEMBL5619482 | — | IC50 | = | 29.4 | nM | 7.53 |
| CHEMBL5619265 | — | IC50 | = | 30.1 | nM | 7.52 |
| CHEMBL5618322 | — | IC50 | = | 32.3 | nM | 7.49 |
| CHEMBL5619941 | — | IC50 | = | 36.2 | nM | 7.44 |
| CHEMBL5619774 | — | IC50 | = | 39.6 | nM | 7.40 |
| CHEMBL5620322 | — | IC50 | = | 49.8 | nM | 7.30 |
| CHEMBL5618116 | — | IC50 | = | 51.9 | nM | 7.29 |
| CHEMBL5619759 | — | IC50 | = | 52.8 | nM | 7.28 |
| CHEMBL5620194 | — | IC50 | = | 67.8 | nM | 7.17 |
| CHEMBL5618941 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL5618351 | — | IC50 | = | 89.1 | nM | 7.05 |
| CHEMBL5618632 | — | IC50 | = | 88.6 | nM | 7.05 |
| CHEMBL5618981 | — | IC50 | = | 113.1 | nM | 6.95 |
| CHEMBL5620018 | — | IC50 | = | 118.6 | nM | 6.93 |
| CHEMBL5619709 | — | IC50 | = | 127.9 | nM | 6.89 |
| CHEMBL5620236 | — | IC50 | = | 146.8 | nM | 6.83 |
| CHEMBL5619832 | — | IC50 | = | 173.8 | nM | 6.76 |
| CHEMBL5619179 | — | IC50 | = | 174.5 | nM | 6.76 |
| CHEMBL5619285 | — | IC50 | = | 217.6 | nM | 6.66 |
| CHEMBL5619949 | — | IC50 | = | 219.3 | nM | 6.66 |
| CHEMBL5618829 | — | IC50 | = | 296.3 | nM | 6.53 |
| CHEMBL5620279 | — | IC50 | = | 332.2 | nM | 6.48 |
| CHEMBL5619377 | — | IC50 | = | 364.8 | nM | 6.44 |
| CHEMBL5618125 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL5618370 | — | IC50 | - | — | - | |
| CHEMBL5618614 | — | IC50 | - | — | - | |
| CHEMBL5618947 | — | IC50 | - | — | - | |
| CHEMBL5618993 | — | IC50 | - | — | - | |
| CHEMBL5618658 | — | IC50 | - | — | - | |
| CHEMBL5618236 | — | IC50 | - | — | - | |
| CHEMBL5619628 | — | IC50 | - | — | - |