Assay Detail
Binding
CHEMBL4018867
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Binding affinity to recombinant human N-terminal His6-tagged Wee1 kinase domain (291 to 575 residues) expressed in Escherichia coli BL21 (DE3) by isothermal titration calorimetry
9
Total Activities
9
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 |
Publication
Structural Basis of Wee Kinases Functionality and Inactivation by Diverse Small Molecule Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 9 | 7.16 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49120 | PD-0166285 | 1.0 | 1 | 7.96 |
| CHEMBL1976040 | ADAVOSERTIB | 2.0 | 1 | 7.87 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 7.87 |
| CHEMBL4067978 | — | — | 1 | 7.36 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 7.11 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 7.10 |
| CHEMBL607707 | PELITINIB | 2.0 | 1 | 6.76 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 5.24 |
| CHEMBL217092 | SARACATINIB | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49120 | PD-0166285 | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL1976040 | ADAVOSERTIB | Kd | = | 13.4 | nM | 7.87 |
| CHEMBL564829 | MILCICLIB | Kd | = | 13.6 | nM | 7.87 |
| CHEMBL4067978 | — | Kd | = | 43.7 | nM | 7.36 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 77.5 | nM | 7.11 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 78.7 | nM | 7.10 |
| CHEMBL607707 | PELITINIB | Kd | = | 172.0 | nM | 6.76 |
| CHEMBL5416410 | DASATINIB | Kd | = | 5700.0 | nM | 5.24 |
| CHEMBL217092 | SARACATINIB | Kd | - | — | - |