Assay Detail
Binding
CHEMBL4048003
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG expressed in HEK293 cells assessed as decrease in peak tail current amplitude by path clamp method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Phenotypic Optimization of Urea-Thiophene Carboxamides To Yield Potent, Well Tolerated, and Orally Active Protective Agents against Aminoglycoside-Induced Hearing Loss.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.25 | 5.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4062161 | — | — | 1 | 5.49 |
| CHEMBL4074914 | — | — | 1 | 5.48 |
| CHEMBL4074997 | — | — | 1 | 5.47 |
| CHEMBL4085169 | — | — | 1 | 5.46 |
| CHEMBL4096279 | — | — | 1 | 5.25 |
| CHEMBL4101606 | — | — | 1 | 4.91 |
| CHEMBL4101684 | — | — | 1 | 4.70 |
| CHEMBL4072149 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4062161 | — | IC50 | = | 3260.0 | nM | 5.49 |
| CHEMBL4074914 | — | IC50 | = | 3290.0 | nM | 5.48 |
| CHEMBL4074997 | — | IC50 | = | 3380.0 | nM | 5.47 |
| CHEMBL4085169 | — | IC50 | = | 3510.0 | nM | 5.46 |
| CHEMBL4096279 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL4101606 | — | IC50 | = | 12400.0 | nM | 4.91 |
| CHEMBL4101684 | — | IC50 | = | 20100.0 | nM | 4.70 |
| CHEMBL4072149 | — | IC50 | > | 30000.0 | nM | - |