Assay Detail
Binding
CHEMBL4612964
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ERK5 in human HeLa cells assessed as reduction in EGF-induced ERK5 autophosphorylation pretreated for 1 hr followed by EGF stimulation and measured after 17 mins by 32p kinase assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and Structure-Activity Relationships of DCLK1 Kinase Inhibitors Based on a 5,11-Dihydro-6<i>H</i>-benzo[<i>e</i>]pyrimido[5,4-<i>b</i>][1,4]diazepin-6-one Scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.39 | 7.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1673051 | — | — | 1 | 7.18 |
| CHEMBL4636072 | — | — | 1 | 7.10 |
| CHEMBL1673039 | — | — | 1 | 7.06 |
| CHEMBL1673052 | — | — | 1 | 7.01 |
| CHEMBL1673053 | — | — | 1 | 6.84 |
| CHEMBL4648947 | — | — | 1 | 6.65 |
| CHEMBL4636475 | — | — | 1 | 6.56 |
| CHEMBL1673048 | — | — | 1 | 6.50 |
| CHEMBL4643632 | — | — | 1 | 6.32 |
| CHEMBL1673057 | — | — | 1 | 5.94 |
| CHEMBL1672987 | — | — | 1 | 5.92 |
| CHEMBL4634326 | — | — | 1 | 5.92 |
| CHEMBL1673056 | — | — | 1 | 5.91 |
| CHEMBL1673054 | — | — | 1 | 5.51 |
| CHEMBL4639395 | — | — | 1 | 5.47 |
| CHEMBL4638880 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1673051 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4636072 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL1673039 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL1673052 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL1673053 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL4648947 | — | IC50 | = | 222.0 | nM | 6.65 |
| CHEMBL4636475 | — | IC50 | = | 276.0 | nM | 6.56 |
| CHEMBL1673048 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4643632 | — | IC50 | = | 482.0 | nM | 6.32 |
| CHEMBL1673057 | — | IC50 | = | 1138.0 | nM | 5.94 |
| CHEMBL1672987 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4634326 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1673056 | — | IC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL1673054 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4639395 | — | IC50 | = | 3350.0 | nM | 5.47 |
| CHEMBL4638880 | — | IC50 | > | 10000.0 | nM | - |