Assay Detail
Functional
CHEMBL1648393
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at recombinant V1b receptor expressed in CHO cells assessed as inhibition of vasopressin-induced calcium release after 10 mins by Fluo4-AM staining
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
The characterization of a novel V1b antagonist lead series.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 33 | 6.41 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1643585 | — | — | 1 | 7.60 |
| CHEMBL572709 | — | — | 1 | 7.36 |
| CHEMBL582857 | NELIVAPTAN | 2.0 | 1 | 7.23 |
| CHEMBL1643587 | — | — | 1 | 7.00 |
| CHEMBL1643588 | — | — | 1 | 7.00 |
| CHEMBL1643586 | — | — | 1 | 7.00 |
| CHEMBL1643595 | — | — | 1 | 7.00 |
| CHEMBL1643612 | — | — | 1 | 6.90 |
| CHEMBL1643584 | — | — | 1 | 6.80 |
| CHEMBL1643596 | — | — | 1 | 6.80 |
| CHEMBL1643610 | — | — | 1 | 6.60 |
| CHEMBL1643589 | — | — | 1 | 6.50 |
| CHEMBL1643598 | — | — | 1 | 6.50 |
| CHEMBL1643590 | — | — | 1 | 6.40 |
| CHEMBL1643608 | — | — | 1 | 6.40 |
| CHEMBL1641623 | — | — | 1 | 6.40 |
| CHEMBL1643597 | — | — | 1 | 6.40 |
| CHEMBL1643592 | — | — | 1 | 6.30 |
| CHEMBL1643603 | — | — | 1 | 6.30 |
| CHEMBL1643593 | — | — | 1 | 6.20 |
| CHEMBL1643611 | — | — | 1 | 6.20 |
| CHEMBL1643609 | — | — | 1 | 6.20 |
| CHEMBL1643600 | — | — | 1 | 6.10 |
| CHEMBL1643594 | — | — | 1 | 6.10 |
| CHEMBL1643602 | — | — | 1 | 6.00 |
| CHEMBL1643605 | — | — | 1 | 5.90 |
| CHEMBL1643606 | — | — | 1 | 5.90 |
| CHEMBL1643604 | — | — | 1 | 5.90 |
| CHEMBL1643613 | — | — | 1 | 5.90 |
| CHEMBL1643599 | — | — | 1 | 5.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1643585 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL572709 | — | Ki | = | 43.65 | nM | 7.36 |
| CHEMBL582857 | NELIVAPTAN | Ki | = | 58.88 | nM | 7.23 |
| CHEMBL1643587 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL1643588 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL1643586 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL1643595 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL1643612 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL1643584 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL1643596 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL1643610 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL1643589 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL1643598 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL1643608 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL1643590 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL1643597 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL1641623 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL1643592 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL1643603 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL1643593 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL1643611 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL1643609 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL1643600 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL1643594 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL1643602 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL1643605 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL1643606 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL1643604 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL1643613 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL1643599 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL1643607 | — | Ki | = | 1995.26 | nM | 5.70 |
| CHEMBL1643591 | — | Ki | = | 2511.89 | nM | 5.60 |
| CHEMBL1643601 | — | Ki | = | 3162.28 | nM | 5.50 |