Assay Detail
Binding
CHEMBL993738
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of aurora A kinase
50
Total Activities
50
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Discovery and development of aurora kinase inhibitors as anticancer agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 47 | 7.41 | 9.00 |
| Ki | 3 | 8.29 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 9.22 |
| CHEMBL483158 | ALISERTIB | 3.0 | 1 | 9.00 |
| CHEMBL484006 | — | — | 1 | 8.89 |
| CHEMBL484609 | — | — | 1 | 8.80 |
| CHEMBL484951 | — | — | 1 | 8.80 |
| CHEMBL482778 | — | — | 1 | 8.77 |
| CHEMBL381724 | — | — | 1 | 8.52 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 8.52 |
| CHEMBL482779 | — | — | 1 | 8.43 |
| CHEMBL484950 | — | — | 1 | 8.40 |
| CHEMBL482774 | — | — | 1 | 8.40 |
| CHEMBL259084 | MLN-8054 | 1.0 | 1 | 8.40 |
| CHEMBL484007 | — | — | 1 | 8.30 |
| CHEMBL385872 | — | — | 1 | 8.22 |
| CHEMBL385266 | — | — | 1 | 8.05 |
| CHEMBL485337 | — | — | 1 | 7.96 |
| CHEMBL482968 | ENMD-2076 | 2.0 | 1 | 7.85 |
| CHEMBL216053 | — | — | 1 | 7.75 |
| CHEMBL472193 | — | — | 1 | 7.66 |
| CHEMBL427787 | — | — | 1 | 7.62 |
| CHEMBL363160 | PHA-680632 | — | 1 | 7.57 |
| CHEMBL191816 | — | — | 1 | 7.39 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 7.36 |
| CHEMBL472202 | — | — | 1 | 7.28 |
| CHEMBL359482 | — | — | 1 | 7.24 |
| CHEMBL516110 | — | — | 1 | 7.19 |
| CHEMBL214849 | — | — | 1 | 7.06 |
| CHEMBL191402 | — | — | 1 | 7.00 |
| CHEMBL202721 | — | — | 1 | 6.96 |
| CHEMBL192575 | — | — | 1 | 6.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL572878 | TOZASERTIB | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL483158 | ALISERTIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL484006 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL484609 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL484951 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL482778 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL381724 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL495727 | AT-9283 | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL482779 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL484950 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL482774 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL259084 | MLN-8054 | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL484007 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL385872 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL385266 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL485337 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL482968 | ENMD-2076 | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL216053 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL472193 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL427787 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL363160 | PHA-680632 | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL191816 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL482967 | CYC-116 | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL472202 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL359482 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL516110 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL214849 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL191402 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL202721 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL192575 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL190252 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL427170 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL484601 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL215275 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL217804 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL518666 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL384575 | — | IC50 | = | 354.0 | nM | 6.45 |
| CHEMBL214848 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL216769 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL217748 | — | IC50 | = | 452.0 | nM | 6.34 |
| CHEMBL215322 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL461999 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL215152 | DEFOSBARASERTIB | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL459888 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL518981 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL201307 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL485351 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL485186 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL461995 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL513076 | — | IC50 | > | 20000.0 | nM | - |