Assay Detail
Binding
CHEMBL4425911
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Inhibition of ERK1 (unknown origin)
21
Total Activities
21
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 |
Publication
Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.40 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3409588 | — | — | 1 | 8.57 |
| CHEMBL4565958 | — | — | 1 | 8.42 |
| CHEMBL4571067 | — | — | 1 | 8.41 |
| CHEMBL4436718 | — | — | 1 | 8.30 |
| CHEMBL3544964 | RAVOXERTINIB | 2.0 | 1 | 8.21 |
| CHEMBL4435650 | — | — | 1 | 8.10 |
| CHEMBL4114404 | — | — | 1 | 7.89 |
| CHEMBL3675721 | — | — | 1 | 7.75 |
| CHEMBL4474917 | — | — | 1 | 7.72 |
| CHEMBL3675719 | — | — | 1 | 7.70 |
| CHEMBL4452981 | — | — | 1 | 7.58 |
| CHEMBL4459138 | — | — | 1 | 7.57 |
| CHEMBL4460988 | — | — | 1 | 7.37 |
| CHEMBL4592894 | — | — | 1 | 7.21 |
| CHEMBL4434981 | — | — | 1 | 7.13 |
| CHEMBL4450215 | — | — | 1 | 7.07 |
| CHEMBL4461076 | — | — | 1 | 6.82 |
| CHEMBL4527526 | — | — | 1 | 6.29 |
| CHEMBL4446409 | — | — | 1 | 6.26 |
| CHEMBL4463669 | — | — | 1 | 5.97 |
| CHEMBL4458128 | — | — | 1 | 5.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3409588 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4565958 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4571067 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4436718 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3544964 | RAVOXERTINIB | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4435650 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL4114404 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3675721 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4474917 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3675719 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4452981 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4459138 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4460988 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4592894 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4434981 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4450215 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL4461076 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4527526 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL4446409 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4463669 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL4458128 | — | IC50 | = | 9610.0 | nM | 5.02 |