Assay Detail
Binding
CHEMBL868957
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Inhibition of KSP by ATPase assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Kinesin spindle protein (KSP) inhibitors. Part 3: synthesis and evaluation of phenolic 2,4-diaryl-2,5-dihydropyrroles with reduced hERG binding and employment of a phosphate prodrug strategy for aqueous solubility.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 8.54 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL206115 | — | — | 1 | 9.30 |
| CHEMBL381526 | — | — | 1 | 8.92 |
| CHEMBL262736 | — | — | 1 | 8.89 |
| CHEMBL377596 | — | — | 1 | 8.54 |
| CHEMBL206798 | — | — | 1 | 8.40 |
| CHEMBL206249 | — | — | 1 | 8.26 |
| CHEMBL381533 | — | — | 1 | 8.15 |
| CHEMBL378547 | — | — | 1 | 7.89 |
| CHEMBL439342 | — | — | 1 | - |
| CHEMBL382994 | — | — | 1 | - |
| CHEMBL202734 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL206115 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL381526 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL262736 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL377596 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL206798 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL206249 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL381533 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL378547 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL439342 | — | IC50 | - | — | - | |
| CHEMBL382994 | — | IC50 | - | — | - | |
| CHEMBL202734 | — | IC50 | - | — | - |