Assay Detail
Binding
CHEMBL1003945
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Inhibition of GST-fused human MLK1
9
Total Activities
9
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 |
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 | 9 | 7.02 | 7.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL460990 | — | — | 1 | 7.58 |
| CHEMBL290352 | CEP-1347 | 3.0 | 1 | 7.42 |
| CHEMBL517743 | — | — | 1 | 7.31 |
| CHEMBL492258 | — | — | 1 | 7.18 |
| CHEMBL517117 | — | — | 1 | 7.00 |
| CHEMBL460989 | — | — | 1 | 6.99 |
| CHEMBL492257 | — | — | 1 | 6.73 |
| CHEMBL375085 | — | — | 1 | 5.96 |
| CHEMBL459308 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL460990 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL290352 | CEP-1347 | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL517743 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL492258 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL517117 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL460989 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL492257 | — | IC50 | = | 188.0 | nM | 6.73 |
| CHEMBL375085 | — | IC50 | = | 1106.0 | nM | 5.96 |
| CHEMBL459308 | — | IC50 | - | — | - |