Assay Detail
Binding
CHEMBL3372986
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Inhibition of human Weel1 in human NCI-H1299 cells assessed as phosphorylation of Cdk1 after overnight incubation by ELISA PD assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | NCI-H1299 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pyrimidine-based tricyclic molecules as potent and orally efficacious inhibitors of wee1 kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 20 | 6.25 | 7.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3355536 | — | — | 1 | 7.57 |
| CHEMBL3355537 | — | — | 1 | 7.54 |
| CHEMBL3355539 | — | — | 1 | 7.22 |
| CHEMBL3355534 | — | — | 1 | 7.06 |
| CHEMBL3355533 | — | — | 1 | 7.01 |
| CHEMBL3355531 | — | — | 1 | 7.00 |
| CHEMBL3355535 | — | — | 1 | 6.77 |
| CHEMBL3355528 | — | — | 1 | 6.66 |
| CHEMBL3355518 | — | — | 1 | 6.43 |
| CHEMBL3355532 | — | — | 1 | 6.21 |
| CHEMBL3355524 | — | — | 1 | 5.96 |
| CHEMBL3355525 | — | — | 1 | 5.82 |
| CHEMBL3355529 | — | — | 1 | 5.64 |
| CHEMBL3355530 | — | — | 1 | 5.57 |
| CHEMBL3355523 | — | — | 1 | 5.51 |
| CHEMBL3355522 | — | — | 1 | 5.42 |
| CHEMBL3355527 | — | — | 1 | 5.22 |
| CHEMBL3355519 | — | — | 1 | 5.17 |
| CHEMBL3355521 | — | — | 1 | 5.00 |
| CHEMBL3355538 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3355536 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3355537 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3355539 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3355534 | — | EC50 | = | 87.0 | nM | 7.06 |
| CHEMBL3355533 | — | EC50 | = | 98.0 | nM | 7.01 |
| CHEMBL3355531 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3355535 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3355528 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3355518 | — | EC50 | = | 370.0 | nM | 6.43 |
| CHEMBL3355532 | — | EC50 | = | 620.0 | nM | 6.21 |
| CHEMBL3355524 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3355525 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3355529 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3355530 | — | EC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3355523 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL3355522 | — | EC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL3355527 | — | EC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL3355519 | — | EC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL3355521 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3355538 | — | EC50 | < | 13.0 | nM | - |