Assay Detail
Binding
CHEMBL4119867
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to N-terminally GST-tagged wild type human DLK (1 to 520 residues) expressed in sf21 insect cells using N-terminally His-tagged MKK4 K131M as substrate after 60 mins in presence of ATP by TR-FRET assay
28
Total Activities
28
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 12 (CHEMBL1908389) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Selective Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12) with Activity in a Model of Alzheimer's Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 7.91 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3717769 | — | — | 1 | 9.00 |
| CHEMBL3718344 | — | — | 1 | 8.64 |
| CHEMBL4128619 | — | — | 1 | 8.52 |
| CHEMBL4125721 | — | — | 1 | 8.52 |
| CHEMBL4129958 | — | — | 1 | 8.52 |
| CHEMBL3719135 | — | — | 1 | 8.52 |
| CHEMBL3718912 | — | — | 1 | 8.40 |
| CHEMBL3715238 | — | — | 1 | 8.40 |
| CHEMBL4128889 | — | — | 1 | 8.40 |
| CHEMBL4125824 | — | — | 1 | 8.30 |
| CHEMBL3718265 | — | — | 1 | 8.22 |
| CHEMBL3717481 | — | — | 1 | 8.15 |
| CHEMBL3715469 | — | — | 1 | 8.15 |
| CHEMBL3714987 | — | — | 1 | 8.10 |
| CHEMBL4128477 | — | — | 1 | 8.05 |
| CHEMBL3716231 | — | — | 1 | 8.05 |
| CHEMBL3714822 | — | — | 1 | 7.96 |
| CHEMBL3716456 | — | — | 1 | 7.82 |
| CHEMBL3718522 | — | — | 1 | 7.80 |
| CHEMBL4127238 | — | — | 1 | 7.64 |
| CHEMBL3717627 | — | — | 1 | 7.46 |
| CHEMBL4127922 | — | — | 1 | 7.17 |
| CHEMBL4126530 | — | — | 1 | 7.09 |
| CHEMBL3719209 | — | — | 1 | 7.02 |
| CHEMBL3715637 | — | — | 1 | 6.85 |
| CHEMBL3719126 | — | — | 1 | 6.81 |
| CHEMBL3718750 | — | — | 1 | 6.00 |
| CHEMBL3718894 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3717769 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3718344 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL4128619 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4125721 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4129958 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3719135 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3718912 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3715238 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4128889 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4125824 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3718265 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL3717481 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL3715469 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL3714987 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL4128477 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL3716231 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL3714822 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL3716456 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL3718522 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4127238 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL3717627 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL4127922 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL4126530 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL3719209 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL3715637 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL3719126 | — | Ki | = | 154.0 | nM | 6.81 |
| CHEMBL3718750 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL3718894 | — | Ki | > | 1600.0 | nM | - |