Assay Detail
Binding
CHEMBL4712039
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant SHP2 (262 to 532 amino acids) (unknown origin) incubated for 1 hr using 10 uM DiFMUP by 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
From Pyrazolones to Azaindoles: Evolution of Active-Site SHP2 Inhibitors Based on Scaffold Hopping and Bioisosteric Replacement.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.13 | 7.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4750435 | — | — | 1 | 7.51 |
| CHEMBL1765357 | — | — | 1 | 7.22 |
| CHEMBL4763014 | — | — | 1 | 7.19 |
| CHEMBL4781443 | — | — | 1 | 7.12 |
| CHEMBL4742016 | — | — | 1 | 6.92 |
| CHEMBL4755222 | — | — | 1 | 6.89 |
| CHEMBL4741433 | — | — | 1 | 6.85 |
| CHEMBL4747136 | — | — | 1 | 6.62 |
| CHEMBL4783825 | — | — | 1 | 6.41 |
| CHEMBL4795725 | — | — | 1 | 6.39 |
| CHEMBL501993 | — | — | 1 | 6.39 |
| CHEMBL4749307 | — | — | 1 | 6.39 |
| CHEMBL4753055 | — | — | 1 | 5.96 |
| CHEMBL4752755 | — | — | 1 | 5.92 |
| CHEMBL4743897 | — | — | 1 | 5.82 |
| CHEMBL4760652 | — | — | 1 | 5.80 |
| CHEMBL4788228 | — | — | 1 | 5.70 |
| CHEMBL4776595 | — | — | 1 | 5.70 |
| CHEMBL4786030 | — | — | 1 | 5.64 |
| CHEMBL1232829 | — | — | 1 | 5.51 |
| CHEMBL4785204 | — | — | 1 | 5.50 |
| CHEMBL4786693 | — | — | 1 | 5.47 |
| CHEMBL4750922 | — | — | 1 | 5.17 |
| CHEMBL4762054 | — | — | 1 | 5.17 |
| CHEMBL4750590 | — | — | 1 | 5.12 |
| CHEMBL590043 | — | — | 1 | 4.92 |
| CHEMBL4762351 | — | — | 1 | - |
| CHEMBL4785466 | — | — | 1 | - |
| CHEMBL4764690 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4750435 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1765357 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4763014 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4781443 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4742016 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4755222 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4741433 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4747136 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4783825 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4795725 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL501993 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4749307 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4753055 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4752755 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4743897 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4760652 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4788228 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4776595 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4786030 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL1232829 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4785204 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4786693 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4750922 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL4762054 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL4750590 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL590043 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4762351 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4785466 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4764690 | — | IC50 | > | 10000.0 | nM | - |