Assay Detail
Binding
CHEMBL1003946
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Inhibition of GST-fused human MLK3
8
Total Activities
8
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 11 (CHEMBL2708) ↗| 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 | 8 | 6.78 | 7.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL460989 | — | — | 1 | 7.26 |
| CHEMBL290352 | CEP-1347 | 3.0 | 1 | 7.19 |
| CHEMBL460990 | — | — | 1 | 7.19 |
| CHEMBL517117 | — | — | 1 | 7.06 |
| CHEMBL492258 | — | — | 1 | 6.80 |
| CHEMBL492257 | — | — | 1 | 6.56 |
| CHEMBL375085 | — | — | 1 | 6.14 |
| CHEMBL510795 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL460989 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL290352 | CEP-1347 | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL460990 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL517117 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL492258 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL492257 | — | IC50 | = | 274.0 | nM | 6.56 |
| CHEMBL375085 | — | IC50 | = | 724.0 | nM | 6.14 |
| CHEMBL510795 | — | IC50 | = | 1000.0 | nM | 6.00 |