Assay Detail
Binding
CHEMBL5588779
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 6-His-tagged human Aurora A (126 to 390 residues) expressed in Escherichia coli BL21 (DE3) cells/N-terminal his-tagged/GB-1 fused human TPX2 (7 to 43 residues) expressed in Escherichia coli protein-protein interaction assessed as dissociation constant of compound binding to aurora A in presence of ATP by competitive fluorescence polarization assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Aurora kinase A/Targeting protein for Xklp2 (CHEMBL3883304) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Selective Aurora A-TPX2 Interaction Inhibitors Have <i>In Vivo</i> Efficacy as Targeted Antimitotic Agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 11 | 6.64 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5598235 | — | — | 1 | 7.75 |
| CHEMBL5597404 | — | — | 1 | 7.72 |
| CHEMBL5596916 | — | — | 1 | 7.20 |
| CHEMBL5596260 | — | — | 1 | 7.10 |
| CHEMBL5598288 | — | — | 1 | 7.00 |
| CHEMBL5598166 | — | — | 1 | 6.80 |
| CHEMBL5597168 | — | — | 1 | 6.70 |
| CHEMBL5596300 | — | — | 1 | 6.02 |
| CHEMBL5597558 | — | — | 1 | 5.90 |
| CHEMBL5597299 | — | — | 1 | 4.20 |
| CHEMBL65369 | 3-HYDROXYBENZOIC ACID | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5598235 | — | Kd | = | 18.0 | nM | 7.75 |
| CHEMBL5597404 | — | Kd | = | 19.0 | nM | 7.72 |
| CHEMBL5596916 | — | Kd | = | 63.0 | nM | 7.20 |
| CHEMBL5596260 | — | Kd | = | 79.0 | nM | 7.10 |
| CHEMBL5598288 | — | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL5598166 | — | Kd | = | 158.0 | nM | 6.80 |
| CHEMBL5597168 | — | Kd | = | 200.0 | nM | 6.70 |
| CHEMBL5596300 | — | Kd | = | 955.0 | nM | 6.02 |
| CHEMBL5597558 | — | Kd | = | 1260.0 | nM | 5.90 |
| CHEMBL5597299 | — | Kd | = | 63000.0 | nM | 4.20 |
| CHEMBL65369 | 3-HYDROXYBENZOIC ACID | Kd | = | 1000000.0 | nM | - |