Assay Detail
Binding
CHEMBL4122825
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG expressed in CHOK1 cells at holding potential of -80 mV after 5 mins by patch clamp assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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
Discovery of a bicyclo[4.3.0]nonane derivative DS88790512 as a potent, selective, and orally bioavailable blocker of transient receptor potential canonical 6 (TRPC6).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 4.88 | 5.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4127190 | — | — | 1 | 5.11 |
| CHEMBL4129456 | — | — | 1 | 5.07 |
| CHEMBL4128079 | — | — | 1 | 4.89 |
| CHEMBL4129002 | — | — | 1 | 4.82 |
| CHEMBL4129805 | — | — | 1 | 4.77 |
| CHEMBL4128782 | — | — | 1 | 4.60 |
| CHEMBL4125756 | — | — | 1 | - |
| CHEMBL4129913 | — | — | 1 | - |
| CHEMBL4126989 | — | — | 1 | - |
| CHEMBL4127992 | — | — | 1 | - |
| CHEMBL4126938 | — | — | 1 | - |
| CHEMBL4126435 | — | — | 1 | - |
| CHEMBL4127600 | — | — | 1 | - |
| CHEMBL4130214 | — | — | 1 | - |
| CHEMBL4126041 | — | — | 1 | - |
| CHEMBL4126528 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4127190 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL4129456 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL4128079 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4129002 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL4129805 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL4128782 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL4125756 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4129913 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4126989 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4127992 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4126938 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4126435 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4127600 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4130214 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4126041 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4126528 | — | IC50 | > | 30000.0 | nM | - |