Assay Detail
Binding
CHEMBL1827221
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Inhibition of Aurora B kinase assessed as reduction in histone H3 phosphorylation in human HCT116 cells
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HCT-116 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 6.86 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1822637 | — | — | 1 | 7.82 |
| CHEMBL1822647 | — | — | 1 | 7.80 |
| CHEMBL1822654 | — | — | 1 | 7.64 |
| CHEMBL1822653 | — | — | 1 | 7.64 |
| CHEMBL1822652 | — | — | 1 | 7.64 |
| CHEMBL1822649 | — | — | 1 | 7.57 |
| CHEMBL1822640 | — | — | 1 | 7.55 |
| CHEMBL1822656 | — | — | 1 | 7.55 |
| CHEMBL1822655 | — | — | 1 | 7.55 |
| CHEMBL1822650 | — | — | 1 | 7.55 |
| CHEMBL1822638 | — | — | 1 | 7.54 |
| CHEMBL1822658 | — | — | 1 | 7.36 |
| CHEMBL1822648 | — | — | 1 | 7.33 |
| CHEMBL1822651 | — | — | 1 | 7.31 |
| CHEMBL1822660 | — | — | 1 | 7.29 |
| CHEMBL1822657 | — | — | 1 | 7.29 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 7.26 |
| CHEMBL1822659 | — | — | 1 | 7.24 |
| CHEMBL1822642 | — | — | 1 | 7.11 |
| CHEMBL1822661 | — | — | 1 | 7.08 |
| CHEMBL1822639 | — | — | 1 | 7.04 |
| CHEMBL1822495 | — | — | 1 | 6.84 |
| CHEMBL1822641 | — | — | 1 | 6.75 |
| CHEMBL1822490 | — | — | 1 | 6.72 |
| CHEMBL1822491 | — | — | 1 | 6.54 |
| CHEMBL1822494 | — | — | 1 | 6.53 |
| CHEMBL1822487 | — | — | 1 | 6.38 |
| CHEMBL1822485 | — | — | 1 | 6.37 |
| CHEMBL1822645 | — | — | 1 | 6.20 |
| CHEMBL1822492 | — | — | 1 | 6.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1822637 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1822647 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1822653 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1822652 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1822654 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1822649 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1822640 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1822656 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1822655 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1822650 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1822638 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1822658 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL1822648 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL1822651 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL1822657 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL1822660 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL572878 | TOZASERTIB | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL1822659 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL1822642 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL1822661 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL1822639 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL1822495 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL1822641 | — | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL1822490 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL1822491 | — | IC50 | = | 288.0 | nM | 6.54 |
| CHEMBL1822494 | — | IC50 | = | 293.0 | nM | 6.53 |
| CHEMBL1822487 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL1822485 | — | IC50 | = | 431.0 | nM | 6.37 |
| CHEMBL1822645 | — | IC50 | = | 637.0 | nM | 6.20 |
| CHEMBL1822492 | — | IC50 | = | 655.0 | nM | 6.18 |
| CHEMBL1822488 | — | IC50 | = | 828.0 | nM | 6.08 |
| CHEMBL1822486 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL1822644 | — | IC50 | = | 1790.0 | nM | 5.75 |
| CHEMBL1822493 | — | IC50 | = | 1830.0 | nM | 5.74 |
| CHEMBL1822643 | — | IC50 | = | 2490.0 | nM | 5.60 |
| CHEMBL1822489 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL1822646 | — | IC50 | = | 15000.0 | nM | 4.82 |