Assay Detail
Binding
CHEMBL4425912
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Inhibition of ERK2 (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 | 7.72 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4565958 | — | — | 1 | 9.05 |
| CHEMBL4571067 | — | — | 1 | 9.03 |
| CHEMBL3409588 | — | — | 1 | 8.96 |
| CHEMBL4436718 | — | — | 1 | 8.74 |
| CHEMBL3544964 | RAVOXERTINIB | 2.0 | 1 | 8.51 |
| CHEMBL4435650 | — | — | 1 | 8.39 |
| CHEMBL4114404 | — | — | 1 | 8.23 |
| CHEMBL3675721 | — | — | 1 | 8.11 |
| CHEMBL4474917 | — | — | 1 | 8.00 |
| CHEMBL3675719 | — | — | 1 | 7.89 |
| CHEMBL4452981 | — | — | 1 | 7.80 |
| CHEMBL4459138 | — | — | 1 | 7.77 |
| CHEMBL4460988 | — | — | 1 | 7.64 |
| CHEMBL4592894 | — | — | 1 | 7.54 |
| CHEMBL4450215 | — | — | 1 | 7.43 |
| CHEMBL4434981 | — | — | 1 | 7.28 |
| CHEMBL4461076 | — | — | 1 | 7.05 |
| CHEMBL4527526 | — | — | 1 | 6.62 |
| CHEMBL4446409 | — | — | 1 | 6.54 |
| CHEMBL4463669 | — | — | 1 | 6.31 |
| CHEMBL4458128 | — | — | 1 | 5.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4565958 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4571067 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL3409588 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4436718 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3544964 | RAVOXERTINIB | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4435650 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4114404 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL3675721 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL4474917 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3675719 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4452981 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4459138 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4460988 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4592894 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4450215 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4434981 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4461076 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4527526 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4446409 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4463669 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4458128 | — | IC50 | = | 5650.0 | nM | 5.25 |