Assay Detail
Binding
CHEMBL1069497
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG
8
Total Activities
8
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 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: synthesis, SAR development, and in vivo efficacy in cognition models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.14 | 5.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL597276 | — | — | 1 | 5.66 |
| CHEMBL611369 | — | — | 1 | 5.64 |
| CHEMBL597737 | — | — | 1 | 5.55 |
| CHEMBL597241 | — | — | 1 | 5.48 |
| CHEMBL597440 | — | — | 1 | 5.06 |
| CHEMBL603052 | — | — | 1 | 4.79 |
| CHEMBL598555 | — | — | 1 | 4.56 |
| CHEMBL604798 | — | — | 1 | 4.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL597276 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL611369 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL597737 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL597241 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL597440 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL603052 | — | IC50 | = | 16200.0 | nM | 4.79 |
| CHEMBL598555 | — | IC50 | = | 27700.0 | nM | 4.56 |
| CHEMBL604798 | — | IC50 | = | 40000.0 | nM | 4.40 |