Assay Detail
Binding
CHEMBL4414023
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human 6His-tagged SHP2 (1 to 525 residues) expressed in Escherichia coli BL21 Star (DE3) using DiFMUP as surrogate substrate as preincubated for 30 to 60 mins followed by substrate addition and measured after 30 mins bpV-based fluorescence assay
16
Total Activities
16
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
6-Amino-3-methylpyrimidinones as Potent, Selective, and Orally Efficacious SHP2 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.19 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4546378 | — | — | 1 | 8.30 |
| CHEMBL4533113 | — | — | 1 | 7.92 |
| CHEMBL4578698 | — | — | 1 | 7.85 |
| CHEMBL4537504 | — | — | 1 | 7.75 |
| CHEMBL4581388 | — | — | 1 | 7.66 |
| CHEMBL4476848 | — | — | 1 | 7.64 |
| CHEMBL4531137 | — | — | 1 | 7.58 |
| CHEMBL4447768 | — | — | 1 | 7.51 |
| CHEMBL4442335 | — | — | 1 | 7.32 |
| CHEMBL4469071 | — | — | 1 | 7.17 |
| CHEMBL4060033 | — | — | 1 | 7.15 |
| CHEMBL4440701 | — | — | 1 | 6.98 |
| CHEMBL4468062 | — | — | 1 | 6.75 |
| CHEMBL4523033 | — | — | 1 | 6.74 |
| CHEMBL4546245 | — | — | 1 | 6.37 |
| CHEMBL4514244 | — | — | 1 | 4.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4546378 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4533113 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4578698 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4537504 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4581388 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4476848 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4531137 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4447768 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4442335 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4469071 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4060033 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4440701 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL4468062 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL4523033 | — | IC50 | = | 181.0 | nM | 6.74 |
| CHEMBL4546245 | — | IC50 | = | 429.0 | nM | 6.37 |
| CHEMBL4514244 | — | IC50 | = | 46000.0 | nM | 4.34 |