Assay Detail
Toxicity
CHEMBL941016
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of hERG expressed in HEK cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Toxicity |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Kinesin spindle protein (KSP) inhibitors. Part 7: Design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.28 | 6.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL250127 | — | — | 1 | 6.03 |
| CHEMBL429553 | — | — | 1 | 5.70 |
| CHEMBL250532 | — | — | 1 | 5.62 |
| CHEMBL250533 | — | — | 1 | 5.48 |
| CHEMBL401476 | — | — | 1 | 5.34 |
| CHEMBL250126 | — | — | 1 | 5.25 |
| CHEMBL250328 | — | — | 1 | 5.23 |
| CHEMBL398478 | — | — | 1 | 5.21 |
| CHEMBL399378 | — | — | 1 | 5.20 |
| CHEMBL251142 | — | — | 1 | 5.02 |
| CHEMBL250125 | — | — | 1 | 5.00 |
| CHEMBL438876 | — | — | 1 | 4.77 |
| CHEMBL250743 | — | — | 1 | 4.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL250127 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL429553 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL250532 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL250533 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL401476 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL250126 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL250328 | — | IC50 | = | 5940.0 | nM | 5.23 |
| CHEMBL398478 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL399378 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL251142 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL250125 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL438876 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL250743 | — | IC50 | = | 18000.0 | nM | 4.75 |