Assay Detail
Functional
CHEMBL1069496
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human 5HT3 receptor expressed in human skin epithelial cells assessed as stimulation of calcium flux by FLIPR assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Epithelial cell |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
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 | 6.50 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL604798 | — | — | 1 | 8.30 |
| CHEMBL603052 | — | — | 1 | 7.16 |
| CHEMBL597241 | — | — | 1 | 6.32 |
| CHEMBL611369 | — | — | 1 | 6.11 |
| CHEMBL597440 | — | — | 1 | 5.61 |
| CHEMBL598555 | — | — | 1 | 5.48 |
| CHEMBL597276 | — | — | 1 | - |
| CHEMBL597737 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL604798 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL603052 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL597241 | — | IC50 | = | 484.0 | nM | 6.32 |
| CHEMBL611369 | — | IC50 | = | 779.0 | nM | 6.11 |
| CHEMBL597440 | — | IC50 | = | 2480.0 | nM | 5.61 |
| CHEMBL598555 | — | IC50 | = | 3310.0 | nM | 5.48 |
| CHEMBL597276 | — | IC50 | - | — | - | |
| CHEMBL597737 | — | IC50 | > | 7310.0 | nM | - |