Assay Detail
Binding
CHEMBL4055562
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
16
Total Activities
16
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 20 (CHEMBL3886) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure Based Design of N-(3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.78 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4098896 | — | — | 1 | 8.48 |
| CHEMBL4096439 | — | — | 1 | 8.38 |
| CHEMBL4080860 | — | — | 1 | 8.30 |
| CHEMBL4104859 | — | — | 1 | 8.29 |
| CHEMBL4091071 | — | — | 1 | 8.29 |
| CHEMBL4079935 | — | — | 1 | 8.12 |
| CHEMBL4088739 | — | — | 1 | 8.02 |
| CHEMBL4104171 | — | — | 1 | 7.92 |
| CHEMBL4069195 | — | — | 1 | 7.78 |
| CHEMBL4080626 | — | — | 1 | 7.72 |
| CHEMBL4060505 | — | — | 1 | 7.65 |
| CHEMBL1229517 | VEMURAFENIB | 4.0 | 1 | 7.50 |
| CHEMBL4087178 | — | — | 1 | 7.37 |
| CHEMBL4078038 | — | — | 1 | 6.84 |
| CHEMBL4085336 | — | — | 1 | 6.00 |
| CHEMBL4067092 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4098896 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4096439 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4080860 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4104859 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4091071 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4079935 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL4088739 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL4104171 | — | IC50 | = | 12.1 | nM | 7.92 |
| CHEMBL4069195 | — | IC50 | = | 16.8 | nM | 7.78 |
| CHEMBL4080626 | — | IC50 | = | 19.2 | nM | 7.72 |
| CHEMBL4060505 | — | IC50 | = | 22.6 | nM | 7.65 |
| CHEMBL1229517 | VEMURAFENIB | IC50 | = | 31.4 | nM | 7.50 |
| CHEMBL4087178 | — | IC50 | = | 42.7 | nM | 7.37 |
| CHEMBL4078038 | — | IC50 | = | 143.7 | nM | 6.84 |
| CHEMBL4085336 | — | IC50 | = | 994.1 | nM | 6.00 |
| CHEMBL4067092 | — | IC50 | > | 30000.0 | nM | - |