Assay Detail
Binding
CHEMBL1000436
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-fused human MLK1 expressed in CHO cells assessed as MKK4 phosphorylation
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Mitogen-activated protein kinase kinase kinase 9 (CHEMBL2872) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.94 | 7.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL460990 | — | — | 1 | 7.48 |
| CHEMBL290352 | CEP-1347 | 3.0 | 1 | 7.14 |
| CHEMBL460989 | — | — | 1 | 6.90 |
| CHEMBL492258 | — | — | 1 | 6.71 |
| CHEMBL517743 | — | — | 1 | 6.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL460990 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL290352 | CEP-1347 | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL460989 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL492258 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL517743 | — | IC50 | = | 345.0 | nM | 6.46 |