Assay Detail
Binding
CHEMBL5683282
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal 6His-tagged human ERK5 expressed in baculovirus infected Sf21 cells co-expressing HA-tagged human MEK5-DD using ARKKRRHPSGPPTA peptide as substrate incubated for 20 mins in presence of [gamma-32P]-ATP by radiochemical assay
22
Total Activities
22
Compounds Tested
1
Activity Types
2
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| 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 |
|---|---|---|---|
| IC50 | 22 | 6.43 | 7.18 |
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 |
|---|---|---|---|---|
| CHEMBL1673051 | — | — | 1 | 7.18 |
| CHEMBL5687018 | — | — | 1 | 7.09 |
| CHEMBL1673039 | — | — | 1 | 7.06 |
| CHEMBL1673052 | — | — | 1 | 7.01 |
| CHEMBL1673043 | — | — | 1 | 6.94 |
| CHEMBL5686992 | — | — | 1 | 6.85 |
| CHEMBL1673053 | — | — | 1 | 6.84 |
| CHEMBL2381340 | — | — | 1 | 6.79 |
| CHEMBL1673047 | — | — | 1 | 6.77 |
| CHEMBL2381339 | — | — | 1 | 6.70 |
| CHEMBL1673041 | — | — | 1 | 6.63 |
| CHEMBL1673040 | — | — | 1 | 6.53 |
| CHEMBL1673048 | — | — | 1 | 6.47 |
| CHEMBL1673046 | — | — | 1 | 6.44 |
| CHEMBL5686989 | — | — | 1 | 6.06 |
| CHEMBL1673057 | — | — | 1 | 5.95 |
| CHEMBL5687005 | — | — | 1 | 5.90 |
| CHEMBL1672987 | — | — | 1 | 5.84 |
| CHEMBL4632948 | — | — | 1 | 5.82 |
| CHEMBL5687010 | — | — | 1 | 5.76 |
| CHEMBL5687020 | — | — | 1 | 5.61 |
| CHEMBL1673056 | — | — | 1 | 5.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1673051 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL5687018 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL1673039 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL1673052 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL1673043 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL5686992 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1673053 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL2381340 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL1673047 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL2381339 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL1673041 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL1673040 | — | IC50 | = | 297.0 | nM | 6.53 |
| CHEMBL1673048 | — | IC50 | = | 338.0 | nM | 6.47 |
| CHEMBL1673046 | — | IC50 | = | 364.0 | nM | 6.44 |
| CHEMBL5686989 | — | IC50 | = | 873.0 | nM | 6.06 |
| CHEMBL1673057 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL5687005 | — | IC50 | = | 1253.0 | nM | 5.90 |
| CHEMBL1672987 | — | IC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL4632948 | — | IC50 | = | 1530.0 | nM | 5.82 |
| CHEMBL5687010 | — | IC50 | = | 1724.0 | nM | 5.76 |
| CHEMBL5687020 | — | IC50 | = | 2460.0 | nM | 5.61 |
| CHEMBL1673056 | — | IC50 | = | 5090.0 | nM | 5.29 |