Assay Detail
Binding
CHEMBL4355542
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-tagged recombinant human full-length ZAK expressed in baculovirus infected Sf9 insect cells using MBP as substrate after 30 mins by ADP-Glo assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Mitogen-activated protein kinase kinase kinase 20 (CHEMBL3886) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, Synthesis, and Structure-Activity Relationships of 1,2,3-Triazole Benzenesulfonamides as New Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.87 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4524151 | — | — | 1 | 8.72 |
| CHEMBL4542865 | — | — | 1 | 8.68 |
| CHEMBL4526537 | — | — | 1 | 8.64 |
| CHEMBL4574656 | — | — | 1 | 8.52 |
| CHEMBL4579609 | — | — | 1 | 8.48 |
| CHEMBL4446003 | — | — | 1 | 8.42 |
| CHEMBL4450810 | — | — | 1 | 8.40 |
| CHEMBL4468296 | — | — | 1 | 8.38 |
| CHEMBL4454493 | — | — | 1 | 8.36 |
| CHEMBL4448690 | — | — | 1 | 8.35 |
| CHEMBL4457930 | — | — | 1 | 8.24 |
| CHEMBL4449013 | — | — | 1 | 8.16 |
| CHEMBL4559022 | — | — | 1 | 8.05 |
| CHEMBL4096439 | — | — | 1 | 7.83 |
| CHEMBL4476053 | — | — | 1 | 7.61 |
| CHEMBL4473008 | — | — | 1 | 7.54 |
| CHEMBL4457468 | — | — | 1 | 7.33 |
| CHEMBL4532800 | — | — | 1 | 7.28 |
| CHEMBL4523007 | — | — | 1 | 7.26 |
| CHEMBL4452568 | — | — | 1 | 7.20 |
| CHEMBL4444385 | — | — | 1 | 7.07 |
| CHEMBL4582776 | — | — | 1 | 6.38 |
| CHEMBL4459658 | — | — | 1 | 6.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4524151 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4542865 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4526537 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4574656 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4579609 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4446003 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4450810 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4468296 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4454493 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL4448690 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4457930 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL4449013 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL4559022 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL4096439 | — | IC50 | = | 14.7 | nM | 7.83 |
| CHEMBL4476053 | — | IC50 | = | 24.7 | nM | 7.61 |
| CHEMBL4473008 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4457468 | — | IC50 | = | 46.2 | nM | 7.33 |
| CHEMBL4532800 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4523007 | — | IC50 | = | 54.3 | nM | 7.26 |
| CHEMBL4452568 | — | IC50 | = | 63.3 | nM | 7.20 |
| CHEMBL4444385 | — | IC50 | = | 85.7 | nM | 7.07 |
| CHEMBL4582776 | — | IC50 | = | 413.3 | nM | 6.38 |
| CHEMBL4459658 | — | IC50 | = | 983.0 | nM | 6.01 |