Assay Detail
Binding
CHEMBL4425914
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Inhibition of ERK in PMA-stimulated human HepG2 cells assessed as inhibition of p90RSK serine-380 phosphorylation
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 0 — Uncurated / Unknown |
| 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 | 6.65 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4571067 | — | — | 1 | 8.10 |
| CHEMBL3544964 | RAVOXERTINIB | 2.0 | 1 | 7.92 |
| CHEMBL4436718 | — | — | 1 | 7.47 |
| CHEMBL4565958 | — | — | 1 | 7.42 |
| CHEMBL4435650 | — | — | 1 | 7.36 |
| CHEMBL3409588 | — | — | 1 | 7.31 |
| CHEMBL4114404 | — | — | 1 | 7.19 |
| CHEMBL3675721 | — | — | 1 | 7.00 |
| CHEMBL4474917 | — | — | 1 | 6.90 |
| CHEMBL3675719 | — | — | 1 | 6.89 |
| CHEMBL4459138 | — | — | 1 | 6.88 |
| CHEMBL4460988 | — | — | 1 | 6.64 |
| CHEMBL4452981 | — | — | 1 | 6.61 |
| CHEMBL4450215 | — | — | 1 | 6.53 |
| CHEMBL4592894 | — | — | 1 | 6.28 |
| CHEMBL4434981 | — | — | 1 | 6.20 |
| CHEMBL4461076 | — | — | 1 | 5.60 |
| CHEMBL4446409 | — | — | 1 | 5.46 |
| CHEMBL4458128 | — | — | 1 | 5.30 |
| CHEMBL4463669 | — | — | 1 | 5.30 |
| CHEMBL4527526 | — | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4571067 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3544964 | RAVOXERTINIB | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4436718 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4565958 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4435650 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3409588 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4114404 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL3675721 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4474917 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL3675719 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL4459138 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL4460988 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4452981 | — | IC50 | = | 247.0 | nM | 6.61 |
| CHEMBL4450215 | — | IC50 | = | 298.0 | nM | 6.53 |
| CHEMBL4592894 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL4434981 | — | IC50 | = | 635.0 | nM | 6.20 |
| CHEMBL4461076 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4446409 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL4458128 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4463669 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4527526 | — | IC50 | = | 5000.0 | nM | 5.30 |