Assay Detail
Binding
CHEMBL5239394
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant N-terminal GST-tagged human DLK (9 to 111 residues) expressed in Sf21 cells assessed as reduction in substrate phosphorylation using MKK4 and ATP as substrate incubated for 1.5 hrs by HTRF analysis
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| 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 |
|---|---|---|---|
| IC50 | 22 | 7.88 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5272522 | — | — | 1 | 8.70 |
| CHEMBL5286166 | — | — | 1 | 8.70 |
| CHEMBL5283101 | — | — | 1 | 8.52 |
| CHEMBL5281494 | — | — | 1 | 8.52 |
| CHEMBL5288706 | — | — | 1 | 8.52 |
| CHEMBL5268969 | — | — | 1 | 8.40 |
| CHEMBL5271665 | — | — | 1 | 8.40 |
| CHEMBL5271972 | — | — | 1 | 8.40 |
| CHEMBL5270353 | — | — | 1 | 7.92 |
| CHEMBL5276415 | — | — | 1 | 7.89 |
| CHEMBL5268950 | — | — | 1 | 7.89 |
| CHEMBL5276337 | — | — | 1 | 7.89 |
| CHEMBL5277276 | — | — | 1 | 7.85 |
| CHEMBL5284890 | — | — | 1 | 7.77 |
| CHEMBL5278185 | — | — | 1 | 7.62 |
| CHEMBL5269484 | — | — | 1 | 7.55 |
| CHEMBL5278476 | — | — | 1 | 7.33 |
| CHEMBL5273015 | — | — | 1 | 7.28 |
| CHEMBL5284496 | — | — | 1 | 7.28 |
| CHEMBL5269792 | — | — | 1 | 7.21 |
| CHEMBL5277751 | — | — | 1 | 7.11 |
| CHEMBL5281886 | — | — | 1 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5272522 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5286166 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5283101 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5281494 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5288706 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5268969 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5271665 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5271972 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5270353 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5276415 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5268950 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5276337 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5277276 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5284890 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5278185 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5269484 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5278476 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5273015 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5284496 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5269792 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL5277751 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL5281886 | — | IC50 | = | 201.0 | nM | 6.70 |