Assay Detail
Binding
CHEMBL1810552
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]AVP from human V1A receptor expressed in CHO cells
31
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimisation of pharmacokinetic properties to afford an orally bioavailable and selective V1A receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 31 | 8.70 | 10.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1807272 | — | — | 1 | 10.43 |
| CHEMBL1807267 | — | — | 1 | 10.40 |
| CHEMBL1807270 | — | — | 1 | 10.02 |
| CHEMBL1807266 | — | — | 1 | 9.74 |
| CHEMBL1807281 | — | — | 2 | 9.68 |
| CHEMBL1774023 | — | — | 1 | 9.63 |
| CHEMBL1807273 | — | — | 1 | 9.62 |
| CHEMBL1807271 | — | — | 1 | 9.60 |
| CHEMBL1807278 | — | — | 2 | 9.43 |
| CHEMBL1807268 | — | — | 1 | 9.28 |
| CHEMBL1807259 | — | — | 1 | 9.26 |
| CHEMBL1807256 | — | — | 1 | 9.21 |
| CHEMBL1807279 | — | — | 2 | 9.17 |
| CHEMBL1807274 | — | — | 1 | 8.95 |
| CHEMBL1807280 | — | — | 1 | 8.75 |
| CHEMBL1807277 | — | — | 2 | 8.68 |
| CHEMBL1807263 | — | — | 1 | 8.52 |
| CHEMBL1807257 | — | — | 1 | 8.33 |
| CHEMBL1807264 | — | — | 1 | 8.15 |
| CHEMBL1807276 | — | — | 1 | 8.15 |
| CHEMBL1807258 | — | — | 1 | 7.96 |
| CHEMBL1807265 | — | — | 1 | 7.73 |
| CHEMBL1807260 | — | — | 1 | 7.56 |
| CHEMBL1807275 | — | — | 1 | 7.55 |
| CHEMBL1807269 | — | — | 1 | 7.20 |
| CHEMBL1807262 | — | — | 1 | 7.05 |
| CHEMBL1807261 | — | — | 1 | 6.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1807272 | — | Ki | = | 0.03715 | nM | 10.43 |
| CHEMBL1807267 | — | Ki | = | 0.03981 | nM | 10.40 |
| CHEMBL1807270 | — | Ki | = | 0.0955 | nM | 10.02 |
| CHEMBL1807266 | — | Ki | = | 0.182 | nM | 9.74 |
| CHEMBL1807281 | — | Ki | = | 0.2089 | nM | 9.68 |
| CHEMBL1774023 | — | Ki | = | 0.2344 | nM | 9.63 |
| CHEMBL1807273 | — | Ki | = | 0.2399 | nM | 9.62 |
| CHEMBL1807271 | — | Ki | = | 0.2512 | nM | 9.60 |
| CHEMBL1807278 | — | Ki | = | 0.3715 | nM | 9.43 |
| CHEMBL1807268 | — | Ki | = | 0.5248 | nM | 9.28 |
| CHEMBL1807259 | — | Ki | = | 0.5495 | nM | 9.26 |
| CHEMBL1807256 | — | Ki | = | 0.6166 | nM | 9.21 |
| CHEMBL1807279 | — | Ki | = | 0.6761 | nM | 9.17 |
| CHEMBL1807274 | — | Ki | = | 1.122 | nM | 8.95 |
| CHEMBL1807280 | — | Ki | = | 1.778 | nM | 8.75 |
| CHEMBL1807277 | — | Ki | = | 2.089 | nM | 8.68 |
| CHEMBL1807277 | — | Ki | = | 2.754 | nM | 8.56 |
| CHEMBL1807263 | — | Ki | = | 3.02 | nM | 8.52 |
| CHEMBL1807279 | — | Ki | = | 4.266 | nM | 8.37 |
| CHEMBL1807257 | — | Ki | = | 4.677 | nM | 8.33 |
| CHEMBL1807264 | — | Ki | = | 7.079 | nM | 8.15 |
| CHEMBL1807276 | — | Ki | = | 7.079 | nM | 8.15 |
| CHEMBL1807281 | — | Ki | = | 9.333 | nM | 8.03 |
| CHEMBL1807258 | — | Ki | = | 10.96 | nM | 7.96 |
| CHEMBL1807278 | — | Ki | = | 14.45 | nM | 7.84 |
| CHEMBL1807265 | — | Ki | = | 18.62 | nM | 7.73 |
| CHEMBL1807260 | — | Ki | = | 27.54 | nM | 7.56 |
| CHEMBL1807275 | — | Ki | = | 28.18 | nM | 7.55 |
| CHEMBL1807269 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL1807262 | — | Ki | = | 89.13 | nM | 7.05 |
| CHEMBL1807261 | — | Ki | = | 169.82 | nM | 6.77 |