Assay Detail
Binding
CHEMBL4414022
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of SHP2 in human KYSE520 cells assessed as reduction in ERK phosphorylation after 2 hrs by SureFire p-ERK assay
15
Total Activities
15
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 | 15 | 7.39 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4581388 | — | — | 1 | 8.40 |
| CHEMBL4537504 | — | — | 1 | 8.30 |
| CHEMBL4546378 | — | — | 1 | 8.30 |
| CHEMBL4578698 | — | — | 1 | 8.00 |
| CHEMBL4476848 | — | — | 1 | 7.75 |
| CHEMBL4442335 | — | — | 1 | 7.55 |
| CHEMBL4533113 | — | — | 1 | 7.31 |
| CHEMBL4531137 | — | — | 1 | 7.02 |
| CHEMBL4060033 | — | — | 1 | 6.60 |
| CHEMBL4469071 | — | — | 1 | 6.13 |
| CHEMBL4447768 | — | — | 1 | 5.97 |
| CHEMBL4468062 | — | — | 1 | - |
| CHEMBL4546245 | — | — | 1 | - |
| CHEMBL4523033 | — | — | 1 | - |
| CHEMBL4440701 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4581388 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4537504 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4546378 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4578698 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4476848 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4442335 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4533113 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4531137 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL4060033 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4469071 | — | IC50 | = | 746.0 | nM | 6.13 |
| CHEMBL4447768 | — | IC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL4468062 | — | IC50 | - | — | - | |
| CHEMBL4546245 | — | IC50 | - | — | - | |
| CHEMBL4523033 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL4440701 | — | IC50 | - | — | - |