Assay Detail
Binding
CHEMBL4324285
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MEK U911-activated ERK2 (unknown origin) using ERKtide as substrate preincubated for 20 mins followed by substrate addition in presence of 1 mM ATP after 10 mins by rapidfire mass spectrometry analysis
8
Total Activities
8
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 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 | 8 | 9.33 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4470113 | — | — | 1 | 9.89 |
| CHEMBL4440109 | — | — | 1 | 9.49 |
| CHEMBL4452853 | — | — | 1 | 9.47 |
| CHEMBL4587118 | — | — | 1 | 9.46 |
| CHEMBL4071576 | — | — | 1 | 9.30 |
| CHEMBL4551714 | — | — | 1 | 9.22 |
| CHEMBL4482864 | TIZATERKIB | 1.0 | 1 | 9.18 |
| CHEMBL4458562 | — | — | 1 | 8.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4470113 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL4440109 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL4452853 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL4587118 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL4071576 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4551714 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4482864 | TIZATERKIB | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL4458562 | — | IC50 | = | 2.6 | nM | 8.59 |