Assay Detail
Binding
CHEMBL3395586
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Inhibition of human DLK transfected in HEK293 cells assessed as JNK phosphorylation after 5.5 hrs by Hoechst-33342 staining-based assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Mitogen-activated protein kinase kinase kinase 12 (CHEMBL1908389) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.64 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3393333 | — | — | 1 | 7.52 |
| CHEMBL3393334 | — | — | 1 | 7.24 |
| CHEMBL3393340 | — | — | 1 | 7.21 |
| CHEMBL3393337 | — | — | 1 | 7.19 |
| CHEMBL3393327 | — | — | 1 | 7.16 |
| CHEMBL3393329 | — | — | 1 | 7.16 |
| CHEMBL3393330 | — | — | 1 | 7.10 |
| CHEMBL3393320 | — | — | 1 | 6.96 |
| CHEMBL3393332 | — | — | 1 | 6.90 |
| CHEMBL3393336 | — | — | 1 | 6.85 |
| CHEMBL3393331 | — | — | 1 | 6.71 |
| CHEMBL3393339 | — | — | 1 | 6.67 |
| CHEMBL3393312 | — | — | 1 | 6.64 |
| CHEMBL3393335 | — | — | 1 | 6.63 |
| CHEMBL3393324 | — | — | 1 | 6.52 |
| CHEMBL3393322 | — | — | 1 | 6.39 |
| CHEMBL3393321 | — | — | 1 | 6.39 |
| CHEMBL3393323 | — | — | 1 | 6.36 |
| CHEMBL3393315 | — | — | 1 | 6.31 |
| CHEMBL3393308 | — | — | 1 | 6.19 |
| CHEMBL3393310 | — | — | 1 | 6.12 |
| CHEMBL3393318 | — | — | 1 | 6.00 |
| CHEMBL3393317 | — | — | 1 | 6.00 |
| CHEMBL3393314 | — | — | 1 | 5.89 |
| CHEMBL3393338 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3393333 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3393334 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3393340 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL3393337 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL3393327 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL3393329 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3393330 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL3393320 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL3393332 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL3393336 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL3393331 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL3393339 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL3393312 | — | IC50 | = | 229.0 | nM | 6.64 |
| CHEMBL3393335 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL3393324 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3393322 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL3393321 | — | IC50 | = | 408.0 | nM | 6.39 |
| CHEMBL3393323 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL3393315 | — | IC50 | = | 486.0 | nM | 6.31 |
| CHEMBL3393308 | — | IC50 | = | 641.0 | nM | 6.19 |
| CHEMBL3393310 | — | IC50 | = | 767.0 | nM | 6.12 |
| CHEMBL3393318 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3393317 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3393314 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3393338 | — | IC50 | = | 1600.0 | nM | 5.80 |