Assay Detail
Binding
CHEMBL5239396
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human DLK expressed in HEK cells assessed as reduction in phospho-c-Jun level preincubated for 45 mins followed by doxycycline stimulation and measured after 24 hrs by MSD ELISA
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK |
| 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 Potent and Selective Dual Leucine Zipper Kinase/Leucine Zipper-Bearing Kinase Inhibitors with Neuroprotective Properties in In Vitro and In Vivo Models of Amyotrophic Lateral Sclerosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 21 | 7.06 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5272522 | — | — | 1 | 8.40 |
| CHEMBL5286166 | — | — | 1 | 8.00 |
| CHEMBL5271665 | — | — | 1 | 7.72 |
| CHEMBL5271972 | — | — | 1 | 7.57 |
| CHEMBL5288706 | — | — | 1 | 7.44 |
| CHEMBL5283101 | — | — | 1 | 7.35 |
| CHEMBL5276415 | — | — | 1 | 7.29 |
| CHEMBL5268969 | — | — | 1 | 7.24 |
| CHEMBL5270353 | — | — | 1 | 7.17 |
| CHEMBL5269792 | — | — | 1 | 7.11 |
| CHEMBL5284890 | — | — | 1 | 7.06 |
| CHEMBL5276337 | — | — | 1 | 6.97 |
| CHEMBL5268950 | — | — | 1 | 6.84 |
| CHEMBL5273015 | — | — | 1 | 6.77 |
| CHEMBL5278185 | — | — | 1 | 6.74 |
| CHEMBL5277276 | — | — | 1 | 6.73 |
| CHEMBL5269484 | — | — | 1 | 6.67 |
| CHEMBL5277751 | — | — | 1 | 6.59 |
| CHEMBL5284496 | — | — | 1 | 6.49 |
| CHEMBL5278476 | — | — | 1 | 6.04 |
| CHEMBL5281886 | — | — | 1 | 5.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5272522 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5286166 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5271665 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5271972 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5288706 | — | EC50 | = | 36.0 | nM | 7.44 |
| CHEMBL5283101 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5276415 | — | EC50 | = | 51.0 | nM | 7.29 |
| CHEMBL5268969 | — | EC50 | = | 58.0 | nM | 7.24 |
| CHEMBL5270353 | — | EC50 | = | 67.0 | nM | 7.17 |
| CHEMBL5269792 | — | EC50 | = | 77.0 | nM | 7.11 |
| CHEMBL5284890 | — | EC50 | = | 88.0 | nM | 7.06 |
| CHEMBL5276337 | — | EC50 | = | 107.0 | nM | 6.97 |
| CHEMBL5268950 | — | EC50 | = | 143.0 | nM | 6.84 |
| CHEMBL5273015 | — | EC50 | = | 171.0 | nM | 6.77 |
| CHEMBL5278185 | — | EC50 | = | 183.0 | nM | 6.74 |
| CHEMBL5277276 | — | EC50 | = | 185.0 | nM | 6.73 |
| CHEMBL5269484 | — | EC50 | = | 212.0 | nM | 6.67 |
| CHEMBL5277751 | — | EC50 | = | 258.0 | nM | 6.59 |
| CHEMBL5284496 | — | EC50 | = | 323.0 | nM | 6.49 |
| CHEMBL5278476 | — | EC50 | = | 902.0 | nM | 6.04 |
| CHEMBL5281886 | — | EC50 | = | 1072.0 | nM | 5.97 |