Assay Detail
Functional
CHEMBL968751
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | CHO-K1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
A new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 6.38 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL473185 | — | — | 1 | 8.15 |
| CHEMBL475245 | — | — | 1 | 7.85 |
| CHEMBL473186 | — | — | 1 | 7.72 |
| CHEMBL472990 | — | — | 1 | 7.52 |
| CHEMBL475407 | — | — | 1 | 7.50 |
| CHEMBL474408 | — | — | 1 | 7.46 |
| CHEMBL2110371 | — | — | 1 | 7.19 |
| CHEMBL474404 | — | — | 1 | 7.12 |
| CHEMBL513994 | PRX-08066 FREE BASE | 2.0 | 1 | 6.57 |
| CHEMBL475406 | — | — | 1 | 6.52 |
| CHEMBL515422 | — | — | 1 | 6.15 |
| CHEMBL514934 | — | — | 1 | 6.08 |
| CHEMBL514453 | — | — | 1 | 6.04 |
| CHEMBL473234 | — | — | 1 | 6.00 |
| CHEMBL514967 | — | — | 1 | 5.96 |
| CHEMBL445809 | — | — | 1 | 5.92 |
| CHEMBL472789 | — | — | 1 | 5.92 |
| CHEMBL472985 | — | — | 1 | 5.77 |
| CHEMBL475778 | — | — | 1 | 5.50 |
| CHEMBL473387 | — | — | 1 | 5.14 |
| CHEMBL472416 | — | — | 1 | 5.00 |
| CHEMBL474839 | — | — | 1 | 4.92 |
| CHEMBL473214 | — | — | 1 | 4.80 |
| CHEMBL474840 | — | — | 1 | - |
| CHEMBL473235 | — | — | 1 | - |
| CHEMBL473775 | — | — | 1 | - |
| CHEMBL473970 | — | — | 1 | - |
| CHEMBL472790 | — | — | 1 | - |
| CHEMBL472791 | — | — | 1 | - |
| CHEMBL472986 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL473185 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL475245 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL473186 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL472990 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL475407 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL474408 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2110371 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL474404 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL513994 | PRX-08066 FREE BASE | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL475406 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL515422 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL514934 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL514453 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL473234 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL514967 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL445809 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL472789 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL472985 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL475778 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL473387 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL472416 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL474839 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL473214 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL473187 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL513993 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL473391 | — | IC50 | > | 2800.0 | nM | - |
| CHEMBL472415 | — | IC50 | > | 2400.0 | nM | - |
| CHEMBL472414 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL515713 | — | IC50 | > | 24000.0 | nM | - |
| CHEMBL472589 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL472986 | — | IC50 | > | 2700.0 | nM | - |
| CHEMBL472791 | — | IC50 | > | 14000.0 | nM | - |
| CHEMBL472790 | — | IC50 | > | 13000.0 | nM | - |
| CHEMBL473970 | — | IC50 | > | 26000.0 | nM | - |
| CHEMBL473775 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL473235 | — | IC50 | > | 23000.0 | nM | - |
| CHEMBL474840 | — | IC50 | > | 26000.0 | nM | - |