Assay Detail
Binding
CHEMBL4324286
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ERK1/2 in human A375 cells assessed as inhibition of ERK phosphorylation after 2 hrs
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Mitogen-activated protein kinase; ERK1/ERK2 (CHEMBL1907606) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.85 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4482864 | TIZATERKIB | 1.0 | 1 | 8.77 |
| CHEMBL3590107 | — | — | 1 | 8.60 |
| CHEMBL4440109 | — | — | 1 | 8.47 |
| CHEMBL4452853 | — | — | 1 | 8.33 |
| CHEMBL4458562 | — | — | 1 | 8.04 |
| CHEMBL4071576 | — | — | 1 | 7.92 |
| CHEMBL4551714 | — | — | 1 | 7.52 |
| CHEMBL3544964 | RAVOXERTINIB | 2.0 | 1 | 7.51 |
| CHEMBL3590106 | ULIXERTINIB | 2.0 | 1 | 5.51 |
| CHEMBL4470113 | — | — | 1 | - |
| CHEMBL4587118 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4482864 | TIZATERKIB | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3590107 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4440109 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4452853 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL4458562 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL4071576 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4551714 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3544964 | RAVOXERTINIB | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3590106 | ULIXERTINIB | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4470113 | — | IC50 | > | 14000.0 | nM | - |
| CHEMBL4587118 | — | IC50 | - | — | - |