Assay Detail
Binding
CHEMBL5550260
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-tagged recombinant human MKK3 S198E/T193E mutant expressed in baculovirus infected Sf9 insect cells using STK-3-biotin as substrate preincubated for 30 mins followed by substrate/ATP addition measured after 90 mins by TR-FRET assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of pyrazolo[3,4-d]pyrimidines as novel mitogen-activated protein kinase kinase 3 (MKK3) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 5.15 | 5.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545097 | SAPANISERTIB | 2.0 | 1 | 5.96 |
| CHEMBL1241674 | — | — | 1 | 5.82 |
| CHEMBL5570263 | — | — | 1 | 5.34 |
| CHEMBL573578 | — | — | 1 | 5.32 |
| CHEMBL5570047 | — | — | 1 | 5.21 |
| CHEMBL5564326 | — | — | 1 | 5.19 |
| CHEMBL264406 | — | — | 1 | 5.16 |
| CHEMBL5571520 | — | — | 1 | 5.15 |
| CHEMBL5573208 | — | — | 1 | 5.03 |
| CHEMBL5567024 | — | — | 1 | 5.00 |
| CHEMBL5568922 | — | — | 1 | 4.96 |
| CHEMBL5566622 | — | — | 1 | 4.82 |
| CHEMBL5574120 | — | — | 1 | 4.56 |
| CHEMBL1232415 | — | — | 1 | 4.55 |
| CHEMBL5595378 | — | — | 1 | - |
| CHEMBL5569984 | — | — | 1 | - |
| CHEMBL2079165 | — | — | 1 | - |
| CHEMBL5590276 | — | — | 1 | - |
| CHEMBL5565275 | — | — | 1 | - |
| CHEMBL5571929 | — | — | 1 | - |
| CHEMBL5570067 | — | — | 1 | - |
| CHEMBL5563661 | — | — | 1 | - |
| CHEMBL5565866 | — | — | 1 | - |
| CHEMBL2078794 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545097 | SAPANISERTIB | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL1241674 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5570263 | — | Ki | = | 4600.0 | nM | 5.34 |
| CHEMBL573578 | — | Ki | = | 4800.0 | nM | 5.32 |
| CHEMBL5570047 | — | Ki | = | 6200.0 | nM | 5.21 |
| CHEMBL5564326 | — | Ki | = | 6500.0 | nM | 5.19 |
| CHEMBL264406 | — | Ki | = | 7000.0 | nM | 5.16 |
| CHEMBL5571520 | — | Ki | = | 7100.0 | nM | 5.15 |
| CHEMBL5573208 | — | Ki | = | 9300.0 | nM | 5.03 |
| CHEMBL5567024 | — | Ki | = | 9900.0 | nM | 5.00 |
| CHEMBL5568922 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL5566622 | — | Ki | = | 15000.0 | nM | 4.82 |
| CHEMBL5574120 | — | Ki | = | 27500.0 | nM | 4.56 |
| CHEMBL1232415 | — | Ki | = | 27900.0 | nM | 4.55 |
| CHEMBL5595378 | — | Ki | - | — | - | |
| CHEMBL5569984 | — | Ki | - | — | - | |
| CHEMBL2079165 | — | Ki | - | — | - | |
| CHEMBL5590276 | — | Ki | - | — | - | |
| CHEMBL5565275 | — | Ki | - | — | - | |
| CHEMBL5571929 | — | Ki | - | — | - | |
| CHEMBL5570067 | — | Ki | - | — | - | |
| CHEMBL5563661 | — | Ki | - | — | - | |
| CHEMBL5565866 | — | Ki | - | — | - | |
| CHEMBL2078794 | — | Ki | - | — | - |