Assay Detail
Binding
CHEMBL5683281
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Inhibition of EGF-stimulated ERK5 autophosphorylation in human HeLa cells preincubated with compound for 1 hrs followed by EGF stimulation for 17 mins by SDS-PAGE analysis
22
Total Activities
22
Compounds Tested
1
Activity Types
2
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 22 | 6.34 | 7.10 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| EFO_ID | EFO_ID | - | — | MONDO:0004992 |
| EFO_TERM | EFO_TERM | - | — | cancer |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5687018 | — | — | 1 | 7.10 |
| CHEMBL2381340 | — | — | 1 | 7.05 |
| CHEMBL1673043 | — | — | 1 | 6.80 |
| CHEMBL1673039 | — | — | 1 | 6.72 |
| CHEMBL1673053 | — | — | 1 | 6.70 |
| CHEMBL1673051 | — | — | 1 | 6.70 |
| CHEMBL1673052 | — | — | 1 | 6.64 |
| CHEMBL1673040 | — | — | 1 | 6.62 |
| CHEMBL5686992 | — | — | 1 | 6.62 |
| CHEMBL1673046 | — | — | 1 | 6.62 |
| CHEMBL1673041 | — | — | 1 | 6.58 |
| CHEMBL2381339 | — | — | 1 | 6.58 |
| CHEMBL1673047 | — | — | 1 | 6.51 |
| CHEMBL1673048 | — | — | 1 | 6.50 |
| CHEMBL1673057 | — | — | 1 | 5.91 |
| CHEMBL5686989 | — | — | 1 | 5.88 |
| CHEMBL5687020 | — | — | 1 | 5.51 |
| CHEMBL5687005 | — | — | 1 | 5.39 |
| CHEMBL5687010 | — | — | 1 | 5.33 |
| CHEMBL1673056 | — | — | 1 | 4.94 |
| CHEMBL4632948 | — | — | 1 | - |
| CHEMBL1672987 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5687018 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2381340 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1673043 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1673039 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL1673053 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1673051 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1673052 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL1673040 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5686992 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL1673046 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL1673041 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL2381339 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL1673047 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL1673048 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL1673057 | — | EC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL5686989 | — | EC50 | = | 1320.0 | nM | 5.88 |
| CHEMBL5687020 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL5687005 | — | EC50 | = | 4110.0 | nM | 5.39 |
| CHEMBL5687010 | — | EC50 | = | 4680.0 | nM | 5.33 |
| CHEMBL1673056 | — | EC50 | = | 11380.0 | nM | 4.94 |
| CHEMBL4632948 | — | EC50 | > | 500.0 | nM | - |
| CHEMBL1672987 | — | EC50 | > | 1000.0 | nM | - |