Assay Detail
Binding
CHEMBL5365321
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Inhibition of ERK1/2 phosphorylation in human PANC-1 cells incubated for 3 hrs
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PANC-1 |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Mitogen-activated protein kinase; ERK1/ERK2 (CHEMBL1907606) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
Targeting KRAS<sup>G12D</sup> Mutations: Discovery of Small Molecule Inhibitors for the Potential Treatment of Intractable Cancers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 8.31 | 9.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5439556 | — | — | 1 | 9.12 |
| CHEMBL5396786 | — | — | 1 | 8.70 |
| CHEMBL4858364 | MRTX-1133 | 1.0 | 1 | 8.64 |
| CHEMBL5430105 | — | — | 1 | 8.30 |
| CHEMBL5422015 | — | — | 1 | 8.15 |
| CHEMBL5437386 | — | — | 1 | 8.05 |
| CHEMBL5436095 | — | — | 1 | 8.00 |
| CHEMBL5430644 | — | — | 1 | 7.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5439556 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL5396786 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4858364 | MRTX-1133 | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5430105 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5422015 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5437386 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5436095 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5430644 | — | IC50 | = | 33.0 | nM | 7.48 |