Assay Detail
Binding
CHEMBL966955
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal flag-tagged Aurora A expressed in Escherichia coli BL21-DE3 by ELISA
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 48 | 7.34 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL259084 | MLN-8054 | 1.0 | 1 | 9.00 |
| CHEMBL502124 | — | — | 1 | 8.47 |
| CHEMBL508307 | — | — | 1 | 8.37 |
| CHEMBL523991 | — | — | 1 | 8.22 |
| CHEMBL491773 | — | — | 1 | 8.10 |
| CHEMBL522941 | — | — | 1 | 8.05 |
| CHEMBL521949 | — | — | 1 | 8.00 |
| CHEMBL489914 | — | — | 1 | 7.89 |
| CHEMBL523713 | — | — | 1 | 7.85 |
| CHEMBL491774 | — | — | 1 | 7.85 |
| CHEMBL491575 | — | — | 1 | 7.85 |
| CHEMBL492410 | — | — | 1 | 7.75 |
| CHEMBL490711 | — | — | 1 | 7.72 |
| CHEMBL489913 | — | — | 1 | 7.72 |
| CHEMBL491739 | — | — | 1 | 7.70 |
| CHEMBL522476 | — | — | 1 | 7.70 |
| CHEMBL491956 | — | — | 1 | 7.64 |
| CHEMBL522791 | — | — | 1 | 7.60 |
| CHEMBL522598 | — | — | 1 | 7.55 |
| CHEMBL489736 | — | — | 1 | 7.52 |
| CHEMBL492124 | — | — | 1 | 7.47 |
| CHEMBL491574 | — | — | 1 | 7.44 |
| CHEMBL504355 | — | — | 1 | 7.31 |
| CHEMBL490738 | — | — | 1 | 7.30 |
| CHEMBL523463 | — | — | 1 | 7.29 |
| CHEMBL507170 | — | — | 1 | 7.27 |
| CHEMBL490944 | — | — | 1 | 7.23 |
| CHEMBL492409 | — | — | 1 | 7.19 |
| CHEMBL492139 | — | — | 1 | 7.17 |
| CHEMBL491306 | — | — | 1 | 7.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL259084 | MLN-8054 | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL502124 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL508307 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL523991 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL491773 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL522941 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL521949 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL489914 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL523713 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL491774 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL491575 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL492410 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL489913 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL490711 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL522476 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL491739 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL491956 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL522791 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL522598 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL489736 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL492124 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL491574 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL504355 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL490738 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL523463 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL507170 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL490944 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL492409 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL492139 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL491306 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL490712 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL523490 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL491758 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL523818 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL491124 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL492125 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL491975 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL489912 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL491305 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL491759 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL504824 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL489915 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL522644 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL524321 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL491962 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL522599 | — | IC50 | > | 17000.0 | nM | - |
| CHEMBL501636 | — | IC50 | > | 17000.0 | nM | - |
| CHEMBL492108 | — | IC50 | > | 17000.0 | nM | - |