Assay Detail
Binding
CHEMBL2013813
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CDK1
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Synthesis, SAR and biological evaluation of 1,6-disubstituted-1H-pyrazolo[3,4-d]pyrimidines as dual inhibitors of Aurora kinases and CDK1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.31 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2012408 | — | — | 1 | 8.00 |
| CHEMBL2012409 | — | — | 1 | 8.00 |
| CHEMBL2012403 | — | — | 1 | 7.89 |
| CHEMBL2012399 | — | — | 1 | 7.82 |
| CHEMBL2012398 | — | — | 1 | 7.80 |
| CHEMBL2012400 | — | — | 1 | 7.72 |
| CHEMBL393929 | — | — | 1 | 7.72 |
| CHEMBL2012412 | — | — | 1 | 7.68 |
| CHEMBL2012411 | — | — | 1 | 7.66 |
| CHEMBL2012401 | — | — | 1 | 7.62 |
| CHEMBL2012402 | — | — | 1 | 7.62 |
| CHEMBL2012397 | — | — | 1 | 7.42 |
| CHEMBL2012406 | — | — | 1 | 7.40 |
| CHEMBL2012407 | — | — | 1 | 7.39 |
| CHEMBL2012410 | — | — | 1 | 7.33 |
| CHEMBL2012309 | — | — | 1 | 7.30 |
| CHEMBL2012413 | — | — | 1 | 6.82 |
| CHEMBL2012414 | — | — | 1 | 6.82 |
| CHEMBL2012308 | — | — | 1 | 6.80 |
| CHEMBL2012415 | — | — | 1 | 6.41 |
| CHEMBL2012405 | — | — | 1 | 5.92 |
| CHEMBL2012404 | — | — | 1 | 5.77 |
| CHEMBL259084 | MLN-8054 | 1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2012408 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2012409 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2012403 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2012399 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2012398 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2012400 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL393929 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2012412 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2012411 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2012401 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2012402 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2012397 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL2012406 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2012407 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL2012410 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL2012309 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2012413 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2012414 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2012308 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2012415 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL2012405 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL2012404 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL259084 | MLN-8054 | IC50 | > | 100000.0 | nM | - |